Term
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Definition
Class: Antilipemic Agent, HMG-CoA Reductase Inhibitor
Indication: Hypercholesterolemia, familial type 3 hyperlipoproteinemia, hypercholesterolemia, hypertriglyceridemia
MOA:
Inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, the rate-limiting enzyme in cholesterol synthesis (reduces the production of mevalonic acid from HMG-CoA); this then results in a compensatory increase in the expression of LDL receptors on hepatocyte membranes and a stimulation of LDL catabolism |
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Term
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Definition
Class: Antiplatelet agent
Indication: Prophylaxis of MI, stroke, vascular deaths in patients with recent MI/stroke, PAD, unstable angina
MOA:
Clopidogrel requires in vivo biotransformation to an active thiol metabolite. The active metabolite irreversibly blocks the P2Y12 component of ADP receptors on the platelet surface, which prevents activation of the GPIIb/IIIa receptor complex, thereby reducing platelet aggregation. Platelets blocked by clopidogrel are affected for the remainder of their lifespan (~7-10 days). |
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Term
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Definition
Class: Atypical antipsychotic
Indication: Schizophrenia, bipolar I disorder, MDD, irritability assoc. w/autistic disorder
MOA:
Aripiprazole is a quinolinone antipsychotic which exhibits high affinity for D2, D3, 5-HT1A, and 5-HT2A receptors; moderate affinity for D4, 5-HT2C, 5-HT7, alpha1 adrenergic, and H1 receptors. It also possesses moderate affinity for the serotonin reuptake transporter; has no affinity for muscarinic (cholinergic) receptors. Aripiprazole functions as a partial agonist at the D2 and 5-HT1A receptors, and as an antagonist at the 5-HT2A receptor. |
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Term
| Advair Diskus (fluticasone/salmeterol) |
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Definition
Class: Inhaled corticosteroid/long-acting beta 2-adrenergic agonist
Indication: Maintenance treatment of asthma & COPD
MOA:
Combination of fluticasone (corticosteroid) and salmeterol (long-acting beta2-agonist) designed to improve pulmonary function and control over what is produced by either agent when used alone. Because fluticasone and salmeterol act locally in the lung, plasma levels do not predict therapeutic effect.
Fluticasone: The mechanism of action for all topical corticosteroids is believed to be a combination of three important properties: Anti-inflammatory activity, immunosuppressive properties, and antiproliferative actions. Fluticasone has extremely potent vasoconstrictive and anti-inflammatory activity.
Salmeterol: Relaxes bronchial smooth muscle by selective action on beta2-receptors with little effect on heart rate |
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Term
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Definition
Class: Atypical antipsychotic
Indication: Bipolar, MDD, schizophrenia
MOA:
Quetiapine is a dibenzothiazepine atypical antipsychotic. It has been proposed that this drug's antipsychotic activity is mediated through a combination of dopamine type 2 (D2) and serotonin type 2 (5-HT2) antagonism. It is an antagonist at multiple neurotransmitter receptors in the brain: Serotonin 5-HT1A and 5-HT2, dopamine D1 and D2, histamine H1, and adrenergic alpha1- and alpha2-receptors; but appears to have no appreciable affinity at cholinergic muscarinic and benzodiazepine receptors. Norquetiapine, an active metabolite, differs from its parent molecule by exhibiting high affinity for muscarinic M1 receptors.
Antagonism at receptors other than dopamine and 5-HT2 with similar receptor affinities may explain some of the other effects of quetiapine. The drug's antagonism of histamine H1-receptors may explain the somnolence observed. The drug's antagonism of adrenergic alpha1-receptors may explain the orthostatic hypotension observed. |
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Term
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Definition
Class: Leukotriene Receptor Antagonist
Indication: asthma, seasonal allergic rhinitis, perennial allergic rhinitis, prevention of exercise-induced bronchoconstriction
MOA:
Selective leukotriene receptor antagonist that inhibits the cysteinyl leukotriene receptor. Cysteinyl leukotrienes and leukotriene receptor occupation have been correlated with the pathophysiology of asthma, including airway edema, smooth muscle contraction, and altered cellular activity associated with the inflammatory process, which contribute to the signs and symptoms of asthma. Cysteinyl leukotrienes are also released from the nasal mucosa following allergen exposure leading to symptoms associated with allergic rhinitis. |
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Term
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Definition
Class: Antilipemic Agent, HMG-CoA Reductase Inhibitor
Indication: Hyperlipidemia, mixed dyslipidemia, hypertriglyceridemia, primary dysbetalipoproteinemia, slowing progression of atherosclerosis, homozygous familial hypercholesterolemia
MOA:
Inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, the rate-limiting enzyme in cholesterol synthesis (reduces the production of mevalonic acid from HMG-CoA); this then results in a compensatory increase in the expression of LDL receptors on hepatocyte membranes and a stimulation of LDL catabolism |
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Term
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Definition
Class: Monoclonal Antibody; Tumor Necrosis Factor (TNF) Blocking Agent
Indication: Ankylosing spondylitis, Crohn's disease, ulcerative colitis, plaque psoriasis, psoriatic/rheumatoid arthritis
MOA:
Adalimumab is a recombinant monoclonal antibody that binds to human tumor necrosis factor alpha (TNF-alpha), thereby interfering with binding to TNFα receptor sites and subsequent cytokine-driven inflammatory processes. Elevated TNF levels in the synovial fluid are involved in the pathologic pain and joint destruction in immune-mediated arthritis. Adalimumab decreases signs and symptoms of psoriatic arthritis, rheumatoid arthritis, and ankylosing spondylitis. It inhibits progression of structural damage of rheumatoid and psoriatic arthritis. Reduces signs and symptoms and maintains clinical remission in Crohn’s disease and ulcerative colitis; reduces epidermal thickness and inflammatory cell infiltration in plaque psoriasis. |
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Term
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Definition
Class: Proton pump inhibitor (PPI)
Indication: Healing of erosive esophagitis, GERD, non-erosive reflux disease (NERD), peptic/gastric ulcers, H. pylori eradication, pathological hypersecretory conditions (Zollinger-Ellison syndrome)
MOA:
Proton pump inhibitor suppresses gastric acid secretion by inhibition of the H+/K+-ATPase in the gastric parietal cell. Esomeprazole is the S-isomer of omeprazole. |
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Term
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Definition
Class: Antidepressant, Serotonin/Norepinephrine reuptake inhibitor (SNRI)
Indication: MDD, diabetic neuropathy, fibromyalgia, GAD, chronic musculoskeletal pain, stress incontinence (unlabeled use)
MOA:
Duloxetine is a potent inhibitor of neuronal serotonin and norepinephrine reuptake and a weak inhibitor of dopamine reuptake. Duloxetine has no significant activity for muscarinic cholinergic, H1-histaminergic, or alpha2-adrenergic receptors. Duloxetine does not possess MAO-inhibitory activity. |
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Term
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Definition
Class: Antirheumatic, Disease Modifying; Tumor Necrosis Factor (TNF) Blocking Agent
Indication: Rheumatoid/psoriatic arthritis, ankylosing spondylitis, plaque psoriasis
MOA:
Etanercept is a recombinant DNA-derived protein composed of tumor necrosis factor receptor (TNFR) linked to the Fc portion of human IgG1. Etanercept binds tumor necrosis factor (TNF) and blocks its interaction with cell surface receptors. TNF plays an important role in the inflammatory processes and the resulting joint pathology of rheumatoid arthritis (RA), polyarticular-course juvenile idiopathic arthritis (JIA), ankylosing spondylitis (AS), and plaque psoriasis. |
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Term
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Definition
Class: Antirheumatic, Disease Modifying; Gastrointestinal Agent, Miscellaneous; Immunosuppressant Agent; Monoclonal Antibody; Tumor Necrosis Factor (TNF) Blocking Agent
Indication: Crohn's disease, ulcerative colitis, psoriatic arthritis (+/- MTX), rheumatoid arthritis (in combo w/MTX), ankylosing spondylitis, plaque psoriasis
MOA:
Infliximab is a chimeric monoclonal antibody that binds to human tumor necrosis factor alpha (TNFα), thereby interfering with endogenous TNFα activity. Elevated TNFα levels have been found in involved tissues/fluids of patients with rheumatoid arthritis, ankylosing spondylitis, psoriatic arthritis, plaque psoriasis, Crohn’s disease and ulcerative colitis. Biological activities of TNFα include the induction of proinflammatory cytokines (interleukins), enhancement of leukocyte migration, activation of neutrophils and eosinophils, and the induction of acute phase reactants and tissue degrading enzymes. Animal models have shown TNFα expression causes polyarthritis, and infliximab can prevent disease as well as allow diseased joints to heal. |
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Term
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Definition
Class: Thiazolidinedione (TZD) - antidiabetic agent
Indication: Type 2 diabetes
MOA:
Thiazolidinedione antidiabetic agent that lowers blood glucose by improving target cell response to insulin, without increasing pancreatic insulin secretion. It has a mechanism of action that is dependent on the presence of insulin for activity. Pioglitazone is a potent and selective agonist for peroxisome proliferator-activated receptor-gamma (PPARgamma). Activation of nuclear PPARgamma receptors influences the production of a number of gene products involved in glucose and lipid metabolism. PPARgamma is abundant in the cells within the renal collecting tubules; fluid retention results from stimulation by thiazolidinediones which increases sodium reabsorption. |
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Term
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Definition
Class: Colony stimulating factor (CSF)
Indication:
To decrease the incidence of infection, by stimulation of granulocyte production, in patients with nonmyeloid malignancies receiving myelosuppressive therapy associated with a significant risk of febrile neutropenia
MOA:
Stimulates the production, maturation, and activation of neutrophils, pegfilgrastim activates neutrophils to increase both their migration and cytotoxicity. Pegfilgrastim has a prolonged duration of effect relative to filgrastim and a reduced renal clearance. |
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Term
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Definition
Class: Antineoplastic Agent, Monoclonal Antibody; Antirheumatic, Miscellaneous; Immunosuppressant Agent; Monoclonal Antibody
Indication: Treatment of CD20-positive non-Hodgkin lymphomas (NHL), low-grade or follicular B-cell NHL, CD20-positive chronic lymphocytic leukemia (CLL) (in combo w/fludarabine and cyclophosphamide), rheumatoid arthritis (in combo w/MTX), granulomatosis with polyangiitis (GPA; Wegner's granulomatosis) (in combo w/glucocorticoids), microscopic polyangiitis (MPA) (in combo w/glucocorticoids)
MOA:
Rituximab is a monoclonal antibody directed against the CD20 antigen on B-lymphocytes. CD20 regulates cell cycle initiation; and, possibly, functions as a calcium channel. Rituximab binds to the antigen on the cell surface, activating complement-dependent B-cell cytotoxicity; and to human Fc receptors, mediating cell killing through an antibody-dependent cellular toxicity. B-cells are believed to play a role in the development and progression of rheumatoid arthritis. Signs and symptoms of RA are reduced by targeting B-cells and the progression of structural damage is delayed. |
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Term
| Zyprexa, Zyprexa Zydis (olanzapine) |
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Definition
Class: Atypical antipsychotic, anti-manic agent
Indication: Schizophrenia, acute mania in bipolar disorder, acute agitation in schizo/bipolar, treatment-resistant depression (+ fluoxetine),
Unlabled uses: delirium, prevention of chemo-associated delayed N/V (in combo w/corticosteroid and serotonin antagonist)
MOA:
Olanzapine is a second generation thienobenzodiazepine antipsychotic which displays potent antagonism of serotonin 5-HT2A and 5-HT2C, dopamine D1-4, histamine H1 and alpha1-adrenergic receptors. Olanzapine shows moderate antagonism of 5-HT3 and muscarinic M1-5 receptors, and weak binding to GABA-A, BZD, and beta-adrenergic receptors. Although the precise mechanism of action in schizophrenia and bipolar disorder is not known, the efficacy of olanzapine is thought to be mediated through combined antagonism of dopamine and serotonin type 2 receptor sites. |
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Term
| Copaxone (glatiramer acetate) |
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Definition
Class: Biological
Indication: Multiple sclerosis (MS)
MOA:
Glatiramer is a mixture of random polymers of four amino acids; L-alanine, L-glutamic acid, L-lysine, and L-tyrosine, the resulting mixture is antigenically similar to myelin basic protein, which is an important component of the myelin sheath of nerves; glatiramer is thought to induce and activate T-lymphocyte suppressor cells specific for a myelin antigen, it is also proposed that glatiramer interferes with the antigen-presenting function of certain immune cells opposing pathogenic T-cell function |
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Term
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Definition
Class: Antidepressant, Selective Serotonin Reuptake Inhibitor (SSRI)
Indication: MDD, GAD, OCD,
Unlabeled: vasomotor symptoms associated w/menopause
MOA:
Escitalopram is the S-enantiomer of the racemic derivative citalopram, which selectively inhibits the reuptake of serotonin with little to no effect on norepinephrine or dopamine reuptake. It has no or very low affinity for 5-HT1-7, alpha- and beta-adrenergic, D1-5, H1-3, M1-5, and benzodiazepine receptors. Escitalopram does not bind to or has low affinity for Na+, K+, Cl-, and Ca++ ion channels. |
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Term
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Definition
Class: Opioid analgesic
Indication: Management of pain
MOA:
Binds to opiate receptors in the CNS, causing inhibition of ascending pain pathways, altering the perception of and response to pain; produces generalized CNS depression |
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Term
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Definition
Class: Colony Stimulating Factor; Erythropoiesis-Stimulating Agent (ESA); Growth Factor; Recombinant Human Erythropoietin
Indication: Anemia of CKD, anemia due to chemotherapy in cancer patients, anemia due to zidovudine in HIV patients, surgery patients with perioperative Hgb outside the 10-13 g/dL range
Unlabeled: synmptomatic anemia associated w/myelodysplastic syndrome
MOA:
Induces erythropoiesis by stimulating the division and differentiation of committed erythroid progenitor cells; induces the release of reticulocytes from the bone marrow into the bloodstream, where they mature to erythrocytes. There is a dose response relationship with this effect. This results in an increase in reticulocyte counts followed by a rise in hematocrit and hemoglobin levels. |
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Term
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Definition
Class: Antineoplastic Agent, Monoclonal Antibody; Vascular Endothelial Growth Factor (VEGF) Inhibitor
Indication: Metastatic colorectal cancer, glioblastoma, non-small cell lung cancer (NSCLC) (nonsquamous cell histology), metastatic renal cell cancer
Unlabeled: Age-related macular degeneration (intravitreal injection), metastatic breast cancer, advanced recurrent ovarian cancer that is platinum-sensitive, soft tissue sarcoma, angiosarcoma
MOA:
Bevacizumab is a recombinant, humanized monoclonal antibody which binds to, and neutralizes, vascular endothelial growth factor (VEGF), preventing its association with endothelial receptors, Flt-1 and KDR. VEGF binding initiates angiogenesis (endothelial proliferation and the formation of new blood vessels). The inhibition of microvascular growth is believed to retard the growth of all tissues (including metastatic tissue). |
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Term
| Atripla (efavirenz/emtricitabine/tenofovir) |
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Definition
Class: Antiretroviral agent
Efavirenz: Reverse Transcriptase Inhibitor (Non-nucleoside) (NNRTI)
Emtricitabine: Reverse Transcriptase Inhibitor (Nucleoside) (NRTI)
Tenofovir: Reverse Transcriptase Inhibitor (Nucleotide) (NtRTI)
Indication: HIV-1 infection
MOA:
Efavirenz:
As a non-nucleoside reverse transcriptase inhibitor, efavirenz has activity against HIV-1 by binding to reverse transcriptase. It consequently blocks the RNA-dependent and DNA-dependent DNA polymerase activities including HIV-1 replication. It does not require intracellular phosphorylation for antiviral activity.
Emtricitabine:
Nucleoside reverse transcriptase inhibitor; emtricitabine is a cytosine analogue which is phosphorylated intracellularly to emtricitabine 5'-triphosphate which interferes with HIV viral RNA dependent DNA polymerase resulting in inhibition of viral replication.
Tenofovir:
Tenofovir disoproxil fumarate (TDF) is an analog of adenosine 5'-monophosphate; it interferes with the HIV viral RNA dependent DNA polymerase resulting in inhibition of viral replication. TDF is first converted intracellularly by hydrolysis to tenofovir and subsequently phosphorylated to the active tenofovir diphosphate; nucleotide reverse transcriptase inhibitor. Tenofovir inhibits replication of HBV by inhibiting HBV polymerase. |
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Term
| Spiriva Handihaler (tiotropium) |
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Definition
Class: Long-acting anticholinergic agent
Indication: COPD (maintenance, treatment, reduction of exacerbations)
MOA:
Competitively and reversibly inhibits the action of acetylcholine at type 3 muscarinic (M3) receptors in bronchial smooth muscle causing bronchodilation |
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Term
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Definition
Class: Dipeptidyl Peptidase IV (DPP-IV) inhibitor - Antidiabetic agent
Indication: Type 2 diabetes
MOA:
Sitagliptin inhibits dipeptidyl peptidase IV (DPP-IV) enzyme resulting in prolonged active incretin levels. Incretin hormones (eg, glucagon-like peptide-1 [GLP-1] and glucose-dependent insulinotropic polypeptide [GIP]) regulate glucose homeostasis by increasing insulin synthesis and release from pancreatic beta cells and decreasing glucagon secretion from pancreatic alpha cells. Decreased glucagon secretion results in decreased hepatic glucose production. Under normal physiologic circumstances, incretin hormones are released by the intestine throughout the day and levels are increased in response to a meal; incretin hormones are rapidly inactivated by the DPP-IV enzyme. |
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Term
| Lantus (insulin glargine) |
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Definition
Class: Long-acting insulin
Indication: Type 1 diabetes, Type 2 diabetes
MOA:
Insulin acts via specific membrane-bound receptors on target tissues to regulate metabolism of carbohydrate, protein, and fats. Target organs for insulin include the liver, skeletal muscle, and adipose tissue.
Within the liver, insulin stimulates hepatic glycogen synthesis. Insulin promotes hepatic synthesis of fatty acids, which are released into the circulation as lipoproteins. Skeletal muscle effects of insulin include increased protein synthesis and increased glycogen synthesis. Within adipose tissue, insulin stimulates the processing of circulating lipoproteins to provide free fatty acids, facilitating triglyceride synthesis and storage by adipocytes; also directly inhibits the hydrolysis of triglycerides. In addition, insulin stimulates the cellular uptake of amino acids and increases cellular permeability to several ions, including potassium, magnesium, and phosphate. By activating sodium-potassium ATPases, insulin promotes the intracellular movement of potassium.
Normally secreted by the pancreas, insulin products are manufactured for pharmacologic use through recombinant DNA technology using either E. coli or Saccharomyces cerevisiae. Insulins are categorized based on the onset, peak, and duration of effect (eg, rapid-, short-, intermediate-, and long-acting insulin). Insulin glargine is a long-acting insulin analog.
Pharmacodynamics/Kinetics:
Note: Rate of absorption, onset, and duration of activity may be affected by site of injection, exercise, presence of lipodystrophy, local blood supply, and/or temperature.
Onset of action: 3-4 hours
Duration: Generally 24 hours or longer; reported range: 10.8 to >24 hours (up to 32 hours documented in some studies)
Absorption: Slow; upon injection into the subcutaneous tissue, microprecipitates form which allow small amounts of insulin glargine to release over time |
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Term
| Truvada (emtricitabine/tenofovir) |
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Definition
Class:
Emtricitabine: Reverse Transcriptase Inhibitor (Nucleoside)(NRTI)
Tenofovir: Reverse Transcriptase Inhibitor (Nucleotide) (NtRTI)
Indication: HIV infection
MOA:
Emtricitabine:
Nucleoside reverse transcriptase inhibitor; emtricitabine is a cytosine analogue which is phosphorylated intracellularly to emtricitabine 5'-triphosphate which interferes with HIV viral RNA dependent DNA polymerase resulting in inhibition of viral replication.
Tenofovir:
Tenofovir disoproxil fumarate (TDF) is an analog of adenosine 5'-monophosphate; it interferes with the HIV viral RNA dependent DNA polymerase resulting in inhibition of viral replication. TDF is first converted intracellularly by hydrolysis to tenofovir and subsequently phosphorylated to the active tenofovir diphosphate; nucleotide reverse transcriptase inhibitor. Tenofovir inhibits replication of HBV by inhibiting HBV polymerase. |
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Term
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Definition
Class: Angiotensin II receptor blocker (ARB)
Indication: Hypertension, heart failure, left ventricular dysfunction after MI
MOA:
Valsartan produces direct antagonism of the angiotensin II (AT2) receptors, unlike the ACE inhibitors. It displaces angiotensin II from the AT1 receptor and produces its blood pressure-lowering effects by antagonizing AT1-induced vasoconstriction, aldosterone release, catecholamine release, arginine vasopressin release, water intake, and hypertrophic responses. This action results in more efficient blockade of the cardiovascular effects of angiotensin II and fewer side effects than the ACE inhibitors. |
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Term
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Definition
Class: Analgesic, Anticonvulsant
Indication: Fibromyalgia, diabetic neuropathic pain, spinal cord injury-associated neuropathic pain, partial-onset seizures (adjunct), postherpetic neuralgia
MOA:
Binds to alpha2-delta subunit of voltage-gated calcium channels within the CNS, inhibiting excitatory neurotransmitter release. Although structurally related to GABA, it does not bind to GABA or benzodiazepine receptors. Exerts antinociceptive and anticonvulsant activity. Decreases symptoms of painful peripheral neuropathies and, as adjunctive therapy in partial seizures, decreases the frequency of seizures. Pregabalin may also affect descending noradrenergic and serotonergic pain transmission pathways from the brainstem to the spinal cord. |
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Term
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Definition
Class: Selective COX-2 inhibitor, NSAID
Indication: Ankylosing spondylitis, Juvenile rheumatoid arthritis, Osteoarthritis, acute pain, Primary dysmenorrhea, Rheumatoid arthritis
MOA:
Inhibits prostaglandin synthesis by decreasing the activity of the enzyme, cyclooxygenase-2 (COX-2), which results in decreased formation of prostaglandin precursors; has antipyretic, analgesic, and anti-inflammatory properties. Celecoxib does not inhibit cyclooxygenase-1 (COX-1) at therapeutic concentrations. |
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Term
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Definition
Class: Angiogenesis Inhibitor; Monoclonal Antibody; Ophthalmic Agent; Vascular Endothelial Growth Factor (VEGF) Inhibitor
Indication: Age-related macular degeneration (AMD), Diabetic macular edema (DME), Macular edema following retinal vein occlusion (RVO)
MOA:
Ranibizumab is a recombinant humanized monoclonal antibody fragment which binds to and inhibits human vascular endothelial growth factor A (VEGF-A). Ranibizumab inhibits VEGF from binding to its receptors and thereby suppressing neovascularization and slowing vision loss. |
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Term
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Definition
Class: Anti-HER2 Antineoplastic Agent, Monoclonal Antibody
Indication: Adjuvant treatment of HER2+ breast & gastric cancers |
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Term
| Diovan HCT (valsartan/hydrochlorothiazide) |
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Definition
Class: Angiotensin II Receptor Blocker (ARB) + Thiazide diuretic
Indication: Hypertension
MOA:
Valsartan produces direct antagonism of the angiotensin II (AT2) receptors, unlike the ACE inhibitors. It displaces angiotensin II from the AT1 receptor and produces its blood pressure-lowering effects by antagonizing AT1-induced vasoconstriction, aldosterone release, catecholamine release, arginine vasopressin release, water intake, and hypertrophic responses. This action results in more efficient blockade of the cardiovascular effects of angiotensin II and fewer side effects than the ACE inhibitors.
Hydrochlorothiazide inhibits sodium reabsorption in the distal tubules causing increased excretion of sodium and water as well as potassium and hydrogen ions. |
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Term
| Avonex (interferon beta-1a) |
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Definition
Class: Interferon
Indication: Multiple sclerosis (MS)
MOA:
Interferon beta differs from naturally occurring human protein by a single amino acid substitution and the lack of carbohydrate side chains; alters the expression and response to surface antigens and can enhance immune cell activities. Properties of interferon beta that modify biologic responses are mediated by cell surface receptor interactions; mechanism in the treatment of MS is unknown. |
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Term
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Definition
Class: Tyrosine Kinase (TK) Inhibitor - Antineoplastic agent
Indication: Gastrointestinal stromal tumors (GIST) kit-positive (CD117), Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML), Ph+ acute lymphoblastic leukemia (ALL), Aggressive systemic mastocytosis (ASM) without/unknown D816V c-Kit mutation, hyperosinophilic syndrome (HES), chronic eosinophilic leukemia (CEL), Myelodysplastic/myeloproliferative disease (MDS/MPD) assoc w/platelet-derived growth factor receptor (PDGFR) gene arrangements
MOA:
Inhibits Bcr-Abl tyrosine kinase, the constitutive abnormal gene product of the Philadelphia chromosome in chronic myeloid leukemia (CML). Inhibition of this enzyme blocks proliferation and induces apoptosis in Bcr-Abl positive cell lines as well as in fresh leukemic cells in Philadelphia chromosome positive CML. Also inhibits tyrosine kinase for platelet-derived growth factor (PDGF), stem cell factor (SCF), c-Kit, and cellular events mediated by PDGF and SCF. |
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Term
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Definition
Class: N-Methyl-D-Aspartate Receptor Antagonist
Indication: Alzheimer's disease
Unlabeled: Mild-to-moderate vascular dementia
MOA:
Glutamate, the primary excitatory amino acid in the CNS, may contribute to the pathogenesis of Alzheimer's disease (AD) by overstimulating various glutamate receptors leading to excitotoxicity and neuronal cell death. Memantine is an uncompetitive antagonist of the N-methyl-D-aspartate (NMDA) type of glutamate receptors, located ubiquitously throughout the brain. Under normal physiologic conditions, the (unstimulated) NMDA receptor ion channel is blocked by magnesium ions, which are displaced after agonist-induced depolarization. Pathologic or excessive receptor activation, as postulated to occur during AD, prevents magnesium from reentering and blocking the channel pore resulting in a chronically open state and excessive calcium influx. Memantine binds to the intra-pore magnesium site, but with longer dwell time, and thus functions as an effective receptor blocker only under conditions of excessive stimulation; memantine does not affect normal neurotransmission. |
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Term
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Definition
Class: Low Molecular Weight Heparin (LMWH)
Indication:
Prophylaxis of deep vein thrombosis (DVT): in obesity, abdominal surgery, hip replacement surgery, knee replacement surgery, patients with severely-restricted mobility during acute illness
Treatment of deep vein thrombosis (DVT): inpatient/outpatient, obesity, pregnant women
ST-elevation MI (STEMI), unstable angina or non-ST-elevation MI (NSTEMI)
Unlabeled: Percutaneous coronary intervention (PCI) adjunct
Unlabeled: bariatric surgery, prevention of recurrent VTE in pregnancy
MOA:
Standard heparin consists of components with molecular weights ranging from 4000-30,000 daltons with a mean of 16,000 daltons. Heparin acts as an anticoagulant by enhancing the inhibition rate of clotting proteases by antithrombin III impairing normal hemostasis and inhibition of factor Xa. Low molecular weight heparins have a small effect on the activated partial thromboplastin time and strongly inhibit factor Xa. Enoxaparin is derived from porcine heparin that undergoes benzylation followed by alkaline depolymerization. The average molecular weight of enoxaparin is 4500 daltons which is distributed as (≤20%) 2000 daltons (≥68%) 2000-8000 daltons, and (≤15%) >8000 daltons. Enoxaparin has a higher ratio of antifactor Xa to antifactor IIa activity than unfractionated heparin. |
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Term
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Definition
Class: Atypical Antipsychotic
Indication: acute bipolar mania, adjunct for bipolar maintenance with lithium or valproate, schizophrenia, acute agitation in schizophrenia
MOA:
Ziprasidone is a benzylisothiazolylpiperazine antipsychotic. The exact mechanism of action is unknown. However, in vitro radioligand studies show that ziprasidone has high affinity for D2, D3, 5-HT2A, 5-HT1A, 5-HT2C, 5-HT1D, and alpha1-adrenergic; moderate affinity for histamine H1 receptors; and no appreciable affinity for alpha2-adrenergic receptors, beta-adrenergic, 5-HT3, 5-HT4, cholinergic, mu, sigma, or benzodiazepine receptors. Ziprasidone functions as an antagonist at the D2, 5-HT2A, and 5-HT1D receptors and as an agonist at the 5-HT1A receptor. Ziprasidone moderately inhibits the reuptake of serotonin and norepinephrine. |
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Term
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Definition
Class: Antilipemic agent
Indication: Hypercholesterolemia (alone or with statin), homozygous sitosterolemia, homozygous familial hypercholesterolemia (+ atorvastatin or simvastatin), mixed hyperlipidemia (+fenobirate)
MOA:
Inhibits absorption of cholesterol at the brush border of the small intestine via the sterol transporter, Niemann-Pick C1-Like1 (NPC1L1). This leads to a decreased delivery of cholesterol to the liver, reduction of hepatic cholesterol stores and an increased clearance of cholesterol from the blood; decreases total C, LDL-cholesterol (LDL-C), ApoB, and triglycerides (TG) while increasing HDL-cholesterol (HDL-C). |
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Term
| Tricor (fenofibrate (48 mg, 145 mg)) |
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Definition
Class: Fibric acid - antilipemic agent
Indication: Hypertriglyceridemia, Hypercholesterolemia, Mixed hyperlipidemia
MOA:
Fenofibric acid, an agonist for the nuclear transcription factor peroxisome proliferator-activated receptor-alpha (PPAR-alpha), downregulates apoprotein C-III (an inhibitor of lipoprotein lipase) and upregulates the synthesis of apolipoprotein A-I, fatty acid transport protein, and lipoprotein lipase resulting in an increase in VLDL catabolism, fatty acid oxidation, and elimination of triglyceride-rich particles; as a result of a decrease in VLDL levels, total plasma triglycerides are reduced by 30% to 60%; modest increase in HDL occurs in some hypertriglyceridemic patients. |
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Term
| Vyvanse (lisdexamfetamine) |
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Definition
Class: CNS stimulant
Indication: Attention Deficit Hyperactivity Disorder (ADHD)
MOA:
Lisdexamfetamine dimesylate is a prodrug that is converted to the active component dextroamphetamine (a noncatecholamine, sympathomimetic amine). Amphetamines are noncatecholamine, sympathomimetic amines that cause release of catecholamines (primarily dopamine and norepinephrine) from their storage sites in the presynaptic nerve terminals. A less significant mechanism may include their ability to block the reuptake of catecholamines by competitive inhibition. |
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Term
| Suboxone (buprenorphine/naloxone) |
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Definition
Class: Opioid partial agonist, opioid analgesic
Indication: Maintenance treatment for opioid dependence
MOA:
Buprenorphine:
Buprenorphine exerts its analgesic effect via high affinity binding to μ opiate receptors in the CNS; displays partial mu agonist and weak kappa antagonist activity
Naloxone:
Pure opioid antagonist that competes and displaces opioids at opioid receptor sites
Absorption: Absorption is variable among patients following sublingual use, but variability within each individual patient is low.
Bioavailability: Potential for greater bioavailability with certain strengths of the sublingual film compared to the same strength of the sublingual tablet. Although pharmacokinetics were similar between the sublingual formulations, bioequivalence is variable. In addition, the sizes and compositions among the sublingual film strengths are different which may result in different systemic exposures.
Half-life: Film: Buprenorphine: 24-42 hours; Naloxone: 2-12 hours |
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Term
| Lidoderm (lidocaine transdermal) |
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Definition
Class: Topical analgesic, local anesthetic
Indication: Relief of allodynia (painful hypersensitivity) and chronic pain in postherpetic neuralgia
MOA:
Blocks both the initiation and conduction of nerve impulses by decreasing the neuronal membrane's permeability to sodium ions, which results in inhibition of depolarization with resultant blockade of conduction |
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Term
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Definition
Class: Colony Stimulating Factor; Erythropoiesis-Stimulating Agent (ESA); Growth Factor; Recombinant Human Erythropoietin
Indication: Anemia of CKD, Anemia due to chemotherapy in cancer patients, Anemia due to zidovudine in HIV patients, surgery patients to maintain perioperative Hgb between 10 and 13 g/dL
MOA:
Induces erythropoiesis by stimulating the division and differentiation of committed erythroid progenitor cells; induces the release of reticulocytes from the bone marrow into the bloodstream, where they mature to erythrocytes. There is a dose response relationship with this effect. This results in an increase in reticulocyte counts followed by a rise in hematocrit and hemoglobin levels. |
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Term
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Definition
Class: Platinum analog, alkylating agent, antineoplastic agent
Indication: Advanced colorectal cancer, stage III colon cancer (adjuvant)
Unlabeled: Esophageal cancer, gastric cancer, hepatobiliary cancer (advanced), non-Hodgkin's lymphoma (refractory), ovarian cancer (advanced, platinum-pretreated), pancreatic cancer (advanced), testicular cancer (refractory)
MOA:
Oxaliplatin, a platinum derivative, is an alkylating agent. Following intracellular hydrolysis, the platinum compound binds to DNA forming cross-links which inhibit DNA replication and transcription, resulting in cell death. Cytotoxicity is cell-cycle nonspecific. |
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Term
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Definition
Class: Antilipemic agent, water-soluble vitamin
Indication: Treatment of dyslipidemias (Fredrickson types IIa and IIb or primary hypercholesterolemia) as mono- or adjunctive therapy; to lower the risk of recurrent MI in patients with a history of MI and hyperlipidemia; to slow progression or promote regression of coronary artery disease; treatment of hypertriglyceridemia in patients at risk of pancreatitis; dietary supplement
MOA:
Component of two coenzymes which is necessary for tissue respiration, lipid metabolism, and glycogenolysis; inhibits the synthesis of very low density lipoproteins (VLDL) and low density lipoproteins (LDL); may also increase the rate of chylomicron triglyceride removal from plasma. |
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Term
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Definition
Class: CNS stimulant
Indication:
Improve wakefulness in patients with excessive daytime sleepiness associated with narcolepsy and shift work sleep disorder (SWSD); adjunctive therapy for obstructive sleep apnea/hypopnea syndrome (OSAHS)
Unlabeled: Attention-deficit hyperactivity disorder (ADHD), treatment of fatigue in MS and other disorders
MOA:
The exact mechanism of action is unclear, it does not appear to alter the release of dopamine or norepinephrine, it may exert its stimulant effects by decreasing GABA-mediated neurotransmission, although this theory has not yet been fully evaluated; several studies also suggest that an intact central alpha-adrenergic system is required for modafinil's activity; the drug increases high-frequency alpha waves while decreasing both delta and theta wave activity, and these effects are consistent with generalized increases in mental alertness |
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Term
| Aranesp (darbopoetin alpha) |
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Definition
Class: Colony Stimulating Factor; Erythropoiesis-Stimulating Agent (ESA); Growth Factor; Recombinant Human Erythropoietin
Indication: Anemia of CKD, anemia due to chemotherapy in cancer patients
Unlabeled: symptomatic anemia associated with MDS
MOA:
Induces erythropoiesis by stimulating the division and differentiation of committed erythroid progenitor cells; induces the release of reticulocytes from the bone marrow into the bloodstream, where they mature to erythrocytes. There is a dose response relationship with this effect. This results in an increase in reticulocyte counts followed by a rise in hematocrit and hemoglobin levels. When administered SubQ or I.V., darbepoetin's half-life is ~3 times that of epoetin alfa concentrations. |
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Term
| Androgel (testosterone gel) |
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Definition
Class: Androgen hormone
Indication: Male hypogonadism (primary or hypogonadotropic)
MOA:
Principal endogenous androgen responsible for promoting the growth and development of the male sex organs and maintaining secondary sex characteristics in androgen-deficient males |
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Term
| Combivent (ipratropium/albuterol) |
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Definition
Class: Anticholinergic agent/beta-2 agonist
Indication:
Treatment of COPD in those patients who are currently on a regular bronchodilator who continue to have bronchospasms and require a second bronchodilator
MOA:
Ipratropium:
Blocks the action of acetylcholine at parasympathetic sites in bronchial smooth muscle causing bronchodilation; local application to nasal mucosa inhibits serous and seromucous gland secretions.
Albuterol:
Relaxes bronchial smooth muscle by action on beta2-receptors with little effect on heart rate |
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Term
| Rebif (interferon beta-1a) |
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Definition
Class: interferon
Indication: Treatment of relapsing forms of multiple sclerosis (MS)
MOA:
Interferon beta differs from naturally occurring human protein by a single amino acid substitution and the lack of carbohydrate side chains; alters the expression and response to surface antigens and can enhance immune cell activities. Properties of interferon beta that modify biologic responses are mediated by cell surface receptor interactions; mechanism in the treatment of MS is unknown. |
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Term
| Vytorin (ezetimibe/simvastatin) |
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Definition
Class: Antilipemic agent/HMG-CoA reductase inhibitor (Statin)
Indication: Homozygous familial hypercholesterolemia: As an adjunct to diet for the reduction of elevated total cholesterol (total-C) and low-density lipoprotein cholesterol (LDL-C) in patients with homozygous familial hypercholesterolemia, as an adjunct to other lipid-lowering treatments (eg, LDL apheresis), or if such treatments are unavailable
Primary hyperlipidemia: As an adjunct to diet for the reduction of elevated total-C, LDL-C, apolipoprotein B (apo B), triglycerides, and non-high-density lipoprotein cholesterol (HDL-C), and to increase HDL-C in patients with primary (heterozygous familial and nonfamilial) hyperlipidemia or mixed hyperlipidemia
Limitations of use: No incremental benefit of ezetimibe/simvastatin on cardiovascular morbidity and mortality over and above that demonstrated for simvastatin has been established. Ezetimibe/simvastatin has not been studied in Fredrickson type I, III, IV, and V dyslipidemias.
MOA: Ezetimibe: Inhibits absorption of cholesterol at the brush border of the small intestine, leading to a decreased delivery of cholesterol to the liver. Ezetimibe inhibits the enzyme Niemann-Pick C1-Like1 (NPC1L1), a sterol transporter.
Simvastatin: A methylated derivative of lovastatin that acts by competitively inhibiting 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, the enzyme that catalyzes the rate-limiting step in cholesterol biosynthesis. |
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Term
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Definition
Class: Nasal corticosteroid
Indication: seasonal and perennial allergic rhinitis, treatment of nasal polyps, rhinosinusitis
MOA:
May depress the formation, release, and activity of endogenous chemical mediators of inflammation (kinins, histamine, liposomal enzymes, prostaglandins). Leukocytes and macrophages may have to be present for the initiation of responses mediated by the above substances. Inhibits the margination and subsequent cell migration to the area of injury, and also reverses the dilatation and increased vessel permeability in the area resulting in decreased access of cells to the sites of injury. |
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Term
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Definition
Class: Phosphodiesterase-5 enzyme (PDE-5) inhibitor
Indication: Erectile dysfunction (Viagra), pulmonary arterial hypertension (PAH) (Revatio)
MOA: Erectile dysfunction: Does not directly cause penile erections, but affects the response to sexual stimulation. The physiologic mechanism of erection of the penis involves release of nitric oxide (NO) in the corpus cavernosum during sexual stimulation. NO then activates the enzyme guanylate cyclase, which results in increased levels of cyclic guanosine monophosphate (cGMP), producing smooth muscle relaxation and inflow of blood to the corpus cavernosum. Sildenafil enhances the effect of NO by inhibiting phosphodiesterase type 5 (PDE-5), which is responsible for degradation of cGMP in the corpus cavernosum; when sexual stimulation causes local release of NO, inhibition of PDE-5 by sildenafil causes increased levels of cGMP in the corpus cavernosum, resulting in smooth muscle relaxation and inflow of blood to the corpus cavernosum; at recommended doses, it has no effect in the absence of sexual stimulation.
Pulmonary arterial hypertension (PAH): Inhibits phosphodiesterase type 5 (PDE-5) in smooth muscle of pulmonary vasculature where PDE-5 is responsible for the degradation of cyclic guanosine monophosphate (cGMP). Increased cGMP concentration results in pulmonary vasculature relaxation; vasodilation in the pulmonary bed and the systemic circulation (to a lesser degree) may occur. |
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Term
| Symbicort (budesonide/formoterol) |
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Definition
Class: Inhaled corticosteroid/long-acting beta2-adrenergic agonist
Indication:
Treatment of asthma in patients ≥12 years of age where combination therapy is indicated; maintenance treatment of airflow obstruction associated with chronic obstructive pulmonary disease (COPD; including chronic bronchitis and emphysema)
MOA:
Formoterol relaxes bronchial smooth muscle by selective action on beta2 receptors with little effect on heart rate. Formoterol has a long-acting effect. Budesonide is a corticosteroid which controls the rate of protein synthesis, depresses the migration of polymorphonuclear leukocytes/fibroblasts, and reverses capillary permeability and lysosomal stabilization at the cellular level to prevent or control inflammation. |
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Term
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Definition
Class: Antimetabolite (anti-folate) Antineoplastic agent
Indication: malignant pleural mesothelioma, non small cell lung cancer (NSCLC)
Unlabeled: bladder cancer, persistent/recurrent cervical cancer, platinum-resistant ovarian cancer, metastatic thymic malignancies
MOA:
Antifolate; disrupts folate-dependent metabolic processes essential for cell replication. Inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), glycinamide ribonucleotide formyltransferase (GARFT), and aminoimidazole carboxamide ribonucleotide formyltransferase (AICARFT), the enzymes involved in folate metabolism and DNA synthesis, resulting in inhibition of purine and thymidine nucleotide and protein synthesis. |
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Term
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Definition
Class: Rapid-acting insulin
Indication: Types 1 and 2 diabetes mellitus
MOA:
Insulin acts via specific membrane-bound receptors on target tissues to regulate metabolism of carbohydrate, protein, and fats. Target organs for insulin include the liver, skeletal muscle, and adipose tissue.
Within the liver, insulin stimulates hepatic glycogen synthesis. Insulin promotes hepatic synthesis of fatty acids, which are released into the circulation as lipoproteins. Skeletal muscle effects of insulin include increased protein synthesis and increased glycogen synthesis. Within adipose tissue, insulin stimulates the processing of circulating lipoproteins to provide free fatty acids, facilitating triglyceride synthesis and storage by adipocytes; it also directly inhibits the hydrolysis of triglycerides. In addition, insulin stimulates the cellular uptake of amino acids and increases cellular permeability to several ions, including potassium, magnesium, and phosphate. By activating sodium-potassium ATPases, insulin promotes the intracellular movement of potassium.
Normally secreted by the pancreas, insulin products are manufactured for pharmacologic use through recombinant DNA technology using either E. coli or Saccharomyces cerevisiae. Insulins are categorized based on the onset, peak, and duration of effect (eg, rapid-, short-, intermediate-, and long-acting insulin). Insulin aspart is a rapid-acting insulin analog.
Pharmacodynamics/Kinetics
Note: Rate of absorption, onset, and duration of activity may be affected by site of injection, exercise, presence of lipodystrophy, local blood supply, and/or temperature.
Onset of action: 0.2-0.3 hours
Peak effect: 1-3 hours
Duration: 3-5 hours
Protein binding: <10%
Half-life elimination: SubQ: 81 minutes
Time to peak, plasma: 40-50 minutes
Excretion: Urine |
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Term
| Lovaza (omega-3 fatty acids) |
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Definition
Class: Omega-3 fatty acids; antilipemic agent
Indication: Hypertriglyceridemia (TG >/= 500 mg/dL)
Unlabeled: treatment of IgA nephropathy
MOA:
Mechanism has not been completely defined. Possible mechanisms include inhibition of acyl CoA:1,2 diacylglycerol acyltransferase, increased hepatic beta-oxidation, a reduction in the hepatic synthesis of triglycerides, or an increase in plasma lipoprotein lipase activity. |
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Term
| Humalog, Humalog Kwikpen (insulin lispro) |
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Definition
Class: Rapid-acting insulin
Indication: Type 1 or 2 diabetes mellitus
MOA:
Insulin acts via specific membrane-bound receptors on target tissues to regulate metabolism of carbohydrate, protein, and fats. Target organs for insulin include the liver, skeletal muscle, and adipose tissue.
Within the liver, insulin stimulates hepatic glycogen synthesis. Insulin promotes hepatic synthesis of fatty acids, which are released into the circulation as lipoproteins. Skeletal muscle effects of insulin include increased protein synthesis and increased glycogen synthesis. Within adipose tissue, insulin stimulates the processing of circulating lipoproteins to provide free fatty acids, facilitating triglyceride synthesis and storage by adipocytes; also directly inhibits the hydrolysis of triglycerides. In addition, insulin stimulates the cellular uptake of amino acids and increases cellular permeability to several ions, including potassium, magnesium, and phosphate. By activating sodium-potassium ATPases, insulin promotes the intracellular movement of potassium.
Normally secreted by the pancreas, insulin products are manufactured for pharmacologic use through recombinant DNA technology using either E. coli or Saccharomyces cerevisiae. Insulins are categorized based on the onset, peak, and duration of effect (eg, rapid-, short-, intermediate-, and long-acting insulin). Insulin lispro is a rapid-acting insulin analog.
Pharmacodynamics/Kinetics
Note: Rate of absorption, onset, and duration of activity may be affected by site of injection, exercise, presence of lipodystrophy, local blood supply, and/or temperature.
Onset of action: 0.25-0.5 hours
Peak effect: 0.5-2.5 hours
Duration: ≤5 hours
Distribution: Vd: 0.26-0.36 L/kg
Bioavailability: 55% to 77%
Half-life elimination:
I.V.: ~0.5-1 hour (dose-dependent)
SubQ: 1 hour
Time to peak, plasma: 0.5-1.5 hours
Excretion: Urine |
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Term
| Adderall (amphetamine/dextroamphetamine mixed salts) |
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Definition
Class: CNS stimulant
Indication: Attention-deficit/hyperactivity disorder (ADHD), Narcolepsy
MOA:
Amphetamines are noncatecholamine, sympathomimetic amines that promote release of catecholamines (primarily dopamine and norepinephrine) from their storage sites in the presynaptic nerve terminals. A less significant mechanism may include their ability to block the reuptake of catecholamines by competitive inhibition. |
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Term
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Definition
Class: Colony Stimulating Factor (CSF)
Indication: Chemo-induced neutropenia, bone marrow transplantation (in pts w/cancer; to shorten the duration of neutropenia and neutropenia-related events), peripheral blood progenitor cell (PBPC) collection, severe chronic neutropenia
MOA:
Stimulates the production, maturation, and activation of neutrophils; filgrastim activates neutrophils to increase both their migration and cytotoxicity. |
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Term
| Flovent HFA (fluticasone HFA) |
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Definition
Class: inhaled corticosteroid
Indication: Asthma (
Maintenance treatment of asthma as prophylactic therapy; also indicated for patients requiring oral corticosteroid therapy for asthma to assist in total discontinuation or reduction of total oral dose)
MOA:
Fluticasone belongs to a group of corticosteroids which utilizes a fluorocarbothioate ester linkage at the 17 carbon position; extremely potent vasoconstrictive and anti-inflammatory activity. The effectiveness of inhaled fluticasone is due to its direct local effect. |
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Term
| Proair HFA, Ventolin HFA (albuterol HFA) |
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Definition
Class: Short-acting Beta2-agonist
Indication: Treatment or prevention of bronchospasm in patients with reversible obstructive airway disease; prevention of exercise-induced bronchospasm
MOA:
Relaxes bronchial smooth muscle by action on beta2-receptors with little effect on heart rate |
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Term
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Definition
Class: Protease inhibitor; antiretroviral agent
Indication: HIV-1 infection
MOA:
Binds to the site of HIV-1 protease activity and inhibits cleavage of viral Gag-Pol polyprotein precursors into individual functional proteins required for infectious HIV. This results in the formation of immature, noninfectious viral particles. |
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Term
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Definition
Class: Proton pump inhibitor (PPI)
Indication: Short-term (4-8 weeks) treatment and maintenance of erosive or ulcerative gastroesophageal reflux disease (GERD); symptomatic GERD; short-term (up to 4 weeks) treatment of duodenal ulcers; long-term treatment of pathological hypersecretory conditions, including Zollinger-Ellison syndrome; H. pylori eradication (in combination therapy)
MOA:
Potent proton pump inhibitor; suppresses gastric acid secretion by inhibiting the parietal cell H+/K+ ATP pump |
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Term
| Concerta (methylphenidate ER) |
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Definition
Class: CNS stimulant
Indication: ADHD, narcolepsy
Unlabeled: depression
MOA:
Mild CNS stimulant; blocks the reuptake of norepinephrine and dopamine into presynaptic neurons; appears to stimulate the cerebral cortex and subcortical structures similar to amphetamines |
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Term
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Definition
Class: Inhaled corticosteroid
Indication: Asthma
MOA:
Controls the rate of protein synthesis, depresses the migration of polymorphonuclear leukocytes and fibroblasts, reverses capillary permeability, and stabilizes lysosomal membranes at the cellular level to prevent or control inflammation |
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Term
| Levemir (insulin detemir) |
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Definition
Class: Intermediate- to long-acting insulin
Indication: Types 1 and 2 diabetes mellitus
MOA:
Insulin acts via specific membrane-bound receptors on target tissues to regulate metabolism of carbohydrate, protein, and fats. Target organs for insulin include the liver, skeletal muscle, and adipose tissue.
Within the liver, insulin stimulates hepatic glycogen synthesis. Insulin promotes hepatic synthesis of fatty acids, which are released into the circulation as lipoproteins. Skeletal muscle effects of insulin include increased protein synthesis and increased glycogen synthesis. Within adipose tissue, insulin stimulates the processing of circulating lipoproteins to provide free fatty acids, facilitating triglyceride synthesis and storage by adipocytes; also directly inhibits the hydrolysis of triglycerides. In addition, insulin stimulates the cellular uptake of amino acids and increases cellular permeability to several ions, including potassium, magnesium, and phosphate. By activating sodium-potassium ATPases, insulin promotes the intracellular movement of potassium.
Normally secreted by the pancreas, insulin products are manufactured for pharmacologic use through recombinant DNA technology using either E. coli or Saccharomyces cerevisiae. Insulins are categorized based on the onset, peak, and duration of effect (eg, rapid-, short-, intermediate-, and long-acting insulin). Insulin detemir is an intermediate- to long-acting insulin analog.
Pharmacodynamics/Kinetics
Note: Rate of absorption, onset, and duration of activity may be affected by site of injection, exercise, presence of lipodystrophy, local blood supply, and/or temperature.
Onset of action: 3-4 hours
Peak effect: 3-9 hours (Plank, 2005)
Duration: Dose dependent: 6-23 hours; Note: Duration is dose-dependent. At lower dosages (0.1-0.2 units/kg), mean duration is variable (5.7-12.1 hours). At 0.4 units/kg, the mean duration was 19.9 hours. At high dosages (≥0.8 units/kg) the duration is longer and less variable (mean of 22-23 hours) (Plank, 2005).
Distribution: Vd: 0.1 L/kg
Protein binding: >98% (albumin)
Bioavailability: 60%
Half-life elimination: 5-7 hours (dose-dependent)
Time to peak, plasma: 6-8 hours
Excretion: Urine |
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Term
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Definition
Class: Protease inhibitor, antiviral agent
Indication: Chronic hepatitis C (CHC) (Treatment of genotype 1 chronic hepatitis C (in combination with peginterferon alfa and ribavirin) in adult patients with compensated liver disease (including cirrhosis) who are treatment naive or who have received previous interferon-based treatment, including null or partial responders, and treatment relapsers)
MOA:
Binds reversibly to nonstructural protein 3 (NS 3) serine protease and inhibits replication of the hepatitis C virus. Considered a direct-acting antiviral treatment for HCV, also called a specifically targeted antiviral therapy for HCV (STAT-C). |
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Term
| Varivax (Varicella virus vaccine live, attenuated) |
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Definition
Class: live vaccine (viral)
Indication: Immunization against varicella in children ≥12 months of age and adults
MOA:
As a live, attenuated vaccine, varicella virus vaccine offers active immunity to disease caused by the varicella-zoster virus
Pharmacodynamics/Kinetics
Onset of action: Seroconversion: ~4-6 weeks
Duration: Antibody titers detectable at 10 years post-vaccination |
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Term
| Prevnar 13 (Pneumococcal 13-valent conjugate vaccine) |
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Definition
Class: Inactivated vaccine (bacterial)
Indication: Immunization of children 6 weeks through 17 years of age against Streptococcus pneumoniae infection caused by serotypes included in the vaccine
Immunization of children 6 weeks through 5 years of age against otitis media caused by Streptococcus pneumoniae serotypes 4, 6B, 9V, 14, 18C, 19F, and 23F
Immunization of adults ≥50 years against pneumococcal pneumonia and invasive disease caused by Streptococcus pneumoniae serotypes included in the vaccine
The Advisory Committee on Immunization Practices (ACIP) recommends routine vaccination for the following (CDC 59[RR-11], 2010):
- All children age 2-59 months
- Children 60-71 months w/underlying medical conditions
- Adults >/= 19 years of age w/underlying conditions
MOA:
Promotes active immunization against invasive disease caused by S. pneumoniae capsular serotypes 1, 3, 4, 5, 6A, 6B, 7F, 9V, 14, 18C, 19A, 19F, and 23F, all which are individually conjugated to CRM197 protein |
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Term
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Definition
Class: Hypnotic
Indication: Insomnia (difficulty of sleep onset and/or sleep maintenance)
MOA:
May interact with GABA-receptor complexes at binding domains located close to or allosterically coupled to benzodiazepine receptors.
Half-life elimination: ~6 hours; Elderly (≥65 years): ~9 hours
Time to peak, plasma: ~1 hour |
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Term
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Definition
Class: Phosphodiesterase-5 (PDE-5)enzyme inhibitor
Indication: benign prostatic hyperplasia (BPH) (Cialis), erectile dysfunction (Cialis), pulmonary arterial hypertension (PAH) to improve exercise ability (Adcirca)
MOA: BPH: Exact mechanism unknown; effects likely due to PDE-5 mediated reduction in smooth muscle and endothelial cell proliferation, decreased nerve activity, and increased smooth muscle relaxation and tissue perfusion of the prostate and bladder
Erectile dysfunction: Does not directly cause penile erections, but affects the response to sexual stimulation. The physiologic mechanism of erection of the penis involves release of nitric oxide (NO) in the corpus cavernosum during sexual stimulation. NO then activates the enzyme guanylate cyclase, which results in increased levels of cyclic guanosine monophosphate (cGMP), producing smooth muscle relaxation and inflow of blood to the corpus cavernosum. Tadalafil enhances the effect of NO by inhibiting phosphodiesterase type 5 (PDE-5), which is responsible for degradation of cGMP in the corpus cavernosum; when sexual stimulation causes local release of NO, inhibition of PDE-5 by tadalafil causes increased levels of cGMP in the corpus cavernosum, resulting in smooth muscle relaxation and inflow of blood to the corpus cavernosum. At recommended doses, it has no effect in the absence of sexual stimulation.
PAH: Inhibits phosphodiesterase type 5 (PDE-5) in smooth muscle of pulmonary vasculature where PDE-5 is responsible for the degradation of cyclic guanosine monophosphate (cGMP). Increased cGMP concentration results in pulmonary vasculature relaxation; vasodilation in the pulmonary bed and the systemic circulation (to a lesser degree) may occur. |
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Term
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Definition
Class: Tetracycline derivative antibiotic
Indication: Extended release (Solodyn®): Only indicated for treatment of inflammatory lesions of non-nodular moderate-to-severe acne
Unlabeled: Rheumatoid arthritis w/low disease activity of short duration, nocardiosis, alternaive treatment for community-acquired MRSA, chronic oral antimicrobial suppression of prosthetic joint injfection
MOA:
Inhibits bacterial protein synthesis by binding with the 30S and possibly the 50S ribosomal subunit(s) of susceptible bacteria; cell wall synthesis is not affected
Rheumatoid arthritis: The mechanism of action of minocycline in rheumatoid arthritis is not completely understood. It is thought to have antimicrobial, anti-inflammatory, immunomodulatory, and chondroprotective effects. More specifically, it is thought to be a potent inhibitor of metalloproteinases, which are active in rheumatoid arthritis joint destruction. |
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Term
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Definition
Class: Integrase inhibitor
Indication: HIV
MOA:
Incorporation of viral DNA into the host cell’s genome is required to produce a self-replicating provirus and propagation of infectious virion particles. The viral cDNA strand produced by reverse transcriptase is subsequently processed and inserted into the human genome by the enzyme HIV-1 integrase (encoded by the pol gene of HIV). Raltegravir inhibits the catalytic activity of integrase, thus preventing integration of the proviral gene into human DNA. |
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Term
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Definition
Class: Fluoroquinolone antibiotic (respiratory)
Indication:Treatment of community-acquired pneumonia, including multidrug resistant strains of S. pneumoniae (MDRSP); nosocomial pneumonia; chronic bronchitis (acute bacterial exacerbation); acute bacterial rhinosinusitis (ABRS); prostatitis (chronic bacterial), urinary tract infection (uncomplicated or complicated); acute pyelonephritis; skin or skin structure infections (uncomplicated or complicated); reduce incidence or disease progression of inhalational anthrax (postexposure); prophylaxis and treatment of plague (pneumonic and septicemic) due to Y. pestis
Unlabeled: Diverticulitis, enterocolitis (Shigella spp), epididymitis (nongonococcal), urethritis (nongonococcal), complicated intra-abdominal infections (in combination with metronidazole), Legionnaires' disease, peritonitis, PID (alternative therapy); traveler’s diarrhea; oral phase treatment of prosthetic joint infection
MOA:
As the S(-) enantiomer of the fluoroquinolone, ofloxacin, levofloxacin, inhibits DNA-gyrase in susceptible organisms thereby inhibits relaxation of supercoiled DNA and promotes breakage of DNA strands. DNA gyrase (topoisomerase II), is an essential bacterial enzyme that maintains the superhelical structure of DNA and is required for DNA replication and transcription, DNA repair, recombination, and transposition. |
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Term
| Janumet (sitagliptin/metformin) |
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Definition
Class: Dipeptidyl peptidase IV (DPP-IV) inhibitor/biguanide - antidiabetic agent
Indication: Type 2 diabetes mellitus
MOA:
Sitagliptin inhibits dipeptidyl peptidase IV (DPP-IV) enzymes resulting in prolonged active incretin levels. Incretin hormones [eg, glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP)] regulate glucose homeostasis by increasing insulin synthesis and release from pancreatic beta cells and decreasing glucagon secretion from pancreatic alpha cells. Decreased glucagon secretion results in decreased hepatic glucose production. Under normal physiologic circumstances, incretin hormones are released by the intestine throughout the day and levels are increased in response to a meal; incretin hormones are rapidly inactivated by DPP-IV enzymes.
Metformin decreases hepatic glucose production, decreasing intestinal absorption of glucose, and improves insulin sensitivity (increases peripheral glucose uptake and utilization). |
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Term
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Definition
Class: Monoclonal antibody (IM inj)
Indication: Preventing Respiratory Syncytial Virus (RSV)
MOA:
Exhibits neutralizing and fusion-inhibitory activity against RSV; these activities inhibit RSV replication in laboratory and clinical studies |
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Term
| Effexor XR (venlafaxine ER) |
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Definition
Class: Serotonin/Norepinephrine Reuptake Inhibitor (SNRI) - Antidepressant
Indication:
Treatment of major depressive disorder, generalized anxiety disorder (GAD), social anxiety disorder (social phobia), panic disorder
Unlabeled: Obsessive-compulsive disorder (OCD); hot flashes; neuropathic pain (including diabetic neuropathy); attention-deficit/hyperactivity disorder (ADHD); post-traumatic stress disorder (PTSD); migraine prophylaxis
MOA:
Venlafaxine and its active metabolite, O-desmethylvenlafaxine (ODV), are potent inhibitors of neuronal serotonin and norepinephrine reuptake and weak inhibitors of dopamine reuptake. Venlafaxine and ODV have no significant activity for muscarinic cholinergic, H1-histaminergic, or alpha2-adrenergic receptors. Venlafaxine and ODV do not possess MAO-inhibitory activity. |
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Term
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Definition
Class: Calcineurin inhibitor - immunosuppressant agent
Indication: Keratoconjunctivitis sicca (AKA xerophthalmia, dry eye syndrome (DES))
MOA:
Ophthalmic: The exact mechanism of action is not known. Cyclosporine emulsion is thought to act as a partial immunomodulator in patients whose tear production is presumed to be suppressed due to ocular inflammation associated with keratoconjunctivitis sicca. When administered systemically, cyclosporine is an immunosuppressive agent. |
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Term
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Definition
Class: Oxazolidinone antibiotic
Indication:
Treatment of vancomycin-resistant Enterococcus faecium (VRE) infections, nosocomial pneumonia caused by Staphylococcus aureus (including MRSA) or Streptococcus pneumoniae (including multidrug-resistant strains [MDRSP]), complicated and uncomplicated skin and skin structure infections (including diabetic foot infections without concomitant osteomyelitis), and community-acquired pneumonia caused by susceptible gram-positive organisms
MOA:
Inhibits bacterial protein synthesis by binding to bacterial 23S ribosomal RNA of the 50S subunit. This prevents the formation of a functional 70S initiation complex that is essential for the bacterial translation process. Linezolid is bacteriostatic against enterococci and staphylococci and bactericidal against most strains of streptococci. |
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Term
| Betaseron (interferon beta-1b) |
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Definition
Class: Interferon
Indication: Treatment of relapsing forms of multiple sclerosis (MS); treatment of first clinical episode with MRI features consistent with MS
MOA:
Interferon beta-1b differs from naturally occurring human protein by a single amino acid substitution and the lack of carbohydrate side chains; mechanism in the treatment of MS is unknown; however, immunomodulatory effects attributed to interferon beta-1b include enhancement of suppressor T cell activity, reduction of proinflammatory cytokines, down-regulation of antigen presentation, and reduced trafficking of lymphocytes into the central nervous system. Improves MRI lesions, decreases relapse rate, and disease severity in patients with secondary progressive MS. |
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Term
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Definition
Class: Selective Estrogen Receptor Modulator (SERM)
Indication: Prevention and treatment of osteoporosis in postmenopausal women; risk reduction for invasive breast cancer in postmenopausal women with osteoporosis and in postmenopausal women with high risk for invasive breast cancer
MOA:
A selective estrogen receptor modulator (SERM), meaning that it affects some of the same receptors that estrogen does, but not all, and in some instances, it antagonizes or blocks estrogen; it acts like estrogen to prevent bone loss and has the potential to block some estrogen effects in the breast and uterine tissues. Raloxifene decreases bone resorption, increasing bone mineral density and decreasing fracture incidence. |
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Term
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Definition
Class: Antineoplastic Agent, Monoclonal Antibody; Epidermal Growth Factor Receptor (EGFR) Inhibitor
Indication: Treatment of KRAS mutation-negative (wild-type), EGFR-expressing metastatic colorectal cancer (in combination with FOLFIRI [irinotecan, fluorouracil, and leucovorin] as first-line treatment, in combination with irinotecan [in patients refractory to irinotecan-based chemotherapy], or as a single agent in patients who have failed oxaliplatin and irinotecan based chemotherapy or who are intolerant to irinotecan); treatment of squamous cell cancer of the head and neck (as a single agent for recurrent or metastatic disease after platinum-based chemotherapy failure; in combination with radiation therapy as initial treatment of locally or regionally advanced disease; in combination with platinum and fluorouracil-based chemotherapy as first-line treatment of locoregional or metastatic disease)
Note: Cetuximab is not indicated for the treatment of KRAS mutation-positive colorectal cancer.
Unlabeled: Treatment of EGFR-expressing advanced nonsmall cell lung cancer (NSCLC); treatment of unresectable squamous cell skin cancer; treatment of neurological symptoms of chordoma
MOA:
Recombinant human/mouse chimeric monoclonal antibody which binds specifically to the epidermal growth factor receptor (EGFR, HER1, c-ErbB-1) and competitively inhibits the binding of epidermal growth factor (EGF) and other ligands. Binding to the EGFR blocks phosphorylation and activation of receptor-associated kinases, resulting in inhibition of cell growth, induction of apoptosis, and decreased matrix metalloproteinase and vascular endothelial growth factor production. EGFR signal transduction results in KRAS wild-type activation; cells with KRAS mutations appear to be unaffected by EGFR inhibition. |
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Term
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Definition
Class: Angiotensin II receptor blocker (ARB)
Indication: Hypertension
MOA:
As a selective and competitive, nonpeptide angiotensin II receptor antagonist, olmesartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II; olmesartan interacts reversibly at the AT1 and AT2 receptors of many tissues and has slow dissociation kinetics; its affinity for the AT1 receptor is 12,500 times greater than the AT2 receptor. Angiotensin II receptor antagonists may induce a more complete inhibition of the renin-angiotensin system than ACE inhibitors, they do not affect the response to bradykinin, and are less likely to be associated with nonrenin-angiotensin effects (eg, cough and angioedema). Olmesartan increases urinary flow rate and, in addition to being natriuretic and kaliuretic, increases excretion of chloride, magnesium, uric acid, calcium, and phosphate. |
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Term
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Definition
Class: Proteasome inhibitor - antineoplastic agent
Indication: Treatment of multiple myeloma; treatment of relapsed or refractory mantle cell lymphoma
Unlabeled: Treatment of relapsed/refractory cutaneous T-Cell lymphomas (mycosis fungoides), relapsed/refractory follicular lymphoma, relapsed/refractory peripheral T-cell lymphoma, systemic light-chain amyloidosis, relapsed/refractory Waldenström’s macroglobulinemia
MOA:
Bortezomib inhibits proteasomes, enzyme complexes which regulate protein homeostasis within the cell. Specifically, it reversibly inhibits chymotrypsin-like activity at the 26S proteasome, leading to activation of signaling cascades, cell-cycle arrest, and apoptosis. |
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Term
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Definition
Class: Bisphosphonate derivative
Indication:
Oncology-related uses: Treatment of hypercalcemia of malignancy (albumin-corrected serum calcium >12 mg/dL); treatment of multiple myeloma; treatment of bone metastases of solid tumors
Nononcology uses: Treatment of Paget’s disease of bone; treatment of osteoporosis in postmenopausal women (to reduce the incidence of fractures or to reduce the incidence of new clinical fractures in patients at high risk, defined as a recent low-trauma hip fracture); prevention of osteoporosis in postmenopausal women, treatment of osteoporosis in men (to increase bone mass); treatment and prevention of glucocorticoid-induced osteoporosis (in patients initiating or continuing prednisone ≥7.5 mg/day [or equivalent] and expected to remain on glucocorticoids for at least 12 months)
Unlabeled: Prevention of bone loss associated with aromatase inhibitor therapy in postmenopausal women with breast cancer; prevention of bone loss associated with androgen deprivation therapy in prostate cancer
MOA:
A bisphosphonate which inhibits bone resorption via actions on osteoclasts or on osteoclast precursors; inhibits osteoclastic activity and skeletal calcium release induced by tumors. Decreases serum calcium and phosphorus, and increases their elimination. In osteoporosis, zoledronic acid inhibits osteoclast-mediated resorption, therefore reducing bone turnover. |
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Term
| Synthroid (levothyroxine) |
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Definition
Class: Thyroid product
Indication: Hypothroidism (thyroid replacement), pituitary TSH suppression
MOA:
Levothyroxine (T4) is a synthetic form of thyroxine, an endogenous hormone secreted by the thyroid gland. T4 is converted to its active metabolite, L-triiodothyronine (T3). Thyroid hormones (T4 and T3) then bind to thyroid receptor proteins in the cell nucleus and exert metabolic effects through control of DNA transcription and protein synthesis; involved in normal metabolism, growth, and development; promotes gluconeogenesis, increases utilization and mobilization of glycogen stores, and stimulates protein synthesis, increases basal metabolic rate |
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Term
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Definition
Class: Anticholinergic agent
Indication:
Treatment of overactive bladder with symptoms of urinary frequency, urgency, or urge incontinence
MOA:
Inhibits muscarinic receptors resulting in decreased urinary bladder contraction, increased residual urine volume, and decreased detrusor muscle pressure. |
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Term
| Xeloda (capecitabine (pro-drug of 5-fluorouracil)) |
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Definition
Class: Antimetabolite (pyrimidine analog) - antineoplastic agent
Indication: Treatment of metastatic colorectal cancer; adjuvant therapy of Dukes' C colon cancer; treatment of metastatic breast cancer
Unlabeled: Treatment of CNS lesions from metastatic breast cancer, esophageal cancer, gastric cancer, hepatobiliary cancers (advanced), neuroendocrine (pancreatic/islet cell) tumors (metastatic or unresectable), ovarian cancer (platinum-refractory), pancreatic cancer (metastatic), unknown primary cancer
MOA:
Capecitabine is a prodrug of fluorouracil. It undergoes hydrolysis in the liver and tissues to form fluorouracil which is the active moiety. Fluorouracil is a fluorinated pyrimidine antimetabolite that inhibits thymidylate synthetase, blocking the methylation of deoxyuridylic acid to thymidylic acid, interfering with DNA, and to a lesser degree, RNA synthesis. Fluorouracil appears to be phase specific for the G1 and S phases of the cell cycle. |
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Term
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Definition
Class: Anticholinergic agent
Indication: Treatment of patients with an overactive bladder with symptoms of urinary frequency, urgency, or urge incontinence
MOA:
Tolterodine is a competitive antagonist of muscarinic receptors. In animal models, tolterodine demonstrates selectivity for urinary bladder receptors over salivary receptors. Urinary bladder contraction is mediated by muscarinic receptors. Tolterodine increases residual urine volume and decreases detrusor muscle pressure. |
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Term
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Definition
Class: Opioid analgesic
Indication: Oral, extended release: Management of moderate-to-severe pain in patients requiring around-the-clock opioid treatment for an extended period of time
MOA:
Oxymorphone hydrochloride is a potent opioid analgesic with uses similar to those of morphine. The drug is a semisynthetic derivative of morphine (phenanthrene derivative) and is closely related to hydromorphone chemically (Dilaudid®). |
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Term
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Definition
Class: Selective T-cell costimulation bocker, antirheumatic, disease modifying
Indication: Treatment of moderately- to severely-active adult rheumatoid arthritis (RA); may be used as monotherapy or in combination with other DMARDs
Treatment of moderately- to severely-active juvenile idiopathic arthritis (JIA); may be used as monotherapy or in combination with methotrexate
Note: Abatacept should not be used in combination with anakinra or TNF-blocking agents
MOA:
Selective costimulation modulator; inhibits T-cell (T-lymphocyte) activation by binding to CD80 and CD86 on antigen presenting cells (APC), thus blocking the required CD28 interaction between APCs and T cells. Activated T lymphocytes are found in the synovium of rheumatoid arthritis patients. |
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Term
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Definition
Class: Protease inhibitor - antiretroviral agent
Indication: HIV
MOA:
Binds to the site of HIV-1 protease activity and inhibits cleavage of viral Gag-Pol polyprotein precursors into individual functional proteins required for infectious HIV. This results in the formation of immature, noninfectious viral particles. |
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Term
| Benicar HCT (olmesartan/hydrochlorothiazide) |
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Definition
Class: Angiotensin II receptor blocker (ARB)/Thiazide diuretic
Indication: hypertension (not recommended for initial treatment)
MOA:
Olmesartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II. Hydrochlorothiazide inhibits sodium reabsorption in the distal tubules causing increased excretion of sodium and water as well as potassium and hydrogen ions. |
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Term
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Definition
Class: Cyclic lipopeptide antibiotic
Indication: Treatment of complicated skin and skin structure infections caused by susceptible aerobic gram-positive organisms; Staphylococcus aureus bacteremia, including right-sided native valve infective endocarditis caused by MSSA or MRSA
Unlabeled: Treatment of severe infections caused by MRSA or VRE; treatment of prosthetic joint infection caused by staphylococci (oxacillin-susceptible or -resistant) or Enterococcus (penicillin-susceptible or -resistant)
MOA:
Daptomycin binds to components of the cell membrane of susceptible organisms and causes rapid depolarization, inhibiting intracellular synthesis of DNA, RNA, and protein. Daptomycin is bactericidal in a concentration-dependent manner. |
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Term
|
Definition
Class: bisphosphonate derivative
Indication: Treatment and prevention of osteoporosis in postmenopausal females
Unlabeled: Hypercalcemia of malignancy; reduce bone pain and skeletal complications from metastatic bone disease due to breast cancer
MOA:
A bisphosphonate which inhibits bone resorption via actions on osteoclasts or on osteoclast precursors; decreases the rate of bone resorption, leading to an indirect increase in bone mineral density. |
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Term
| Sandostatin LAR (octreotide) |
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Definition
Class: Antidiarrheal, somatostatin analog, antidote
Indication: Control of symptoms (diarrhea and flushing) in patients with metastatic carcinoid tumors; treatment of watery diarrhea associated with vasoactive intestinal peptide-secreting tumors (VIPomas); treatment of acromegaly
Unlabeled: Treatment of AIDS-associated diarrhea (including Cryptosporidiosis), chemotherapy-induced diarrhea, graft-versus-host disease (GVHD) associated diarrhea, postgastrectomy dumping syndrome; control of bleeding of esophageal varices; second-line treatment for thymic malignancies; Cushing's syndrome (ectopic); insulinomas; small bowel fistulas; islet cell tumors; Zollinger-Ellison syndrome; congenital hyperinsulinism; hypothalamic obesity; treatment of hypoglycemia secondary to sulfonylurea poisoning; treatment of malignant bowel obstruction
MOA:
Mimics natural somatostatin by inhibiting serotonin release, and the secretion of gastrin, VIP, insulin, glucagon, secretin, motilin, and pancreatic polypeptide. Decreases growth hormone and IGF-1 in acromegaly. Octreotide provides more potent inhibition of growth hormone, glucagon, and insulin as compared to endogenous somatostatin. Also suppresses LH response to GnRH, secretion of thyroid-stimulating hormone and decreases splanchnic blood flow. |
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Term
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Definition
Class: Bisphosphonate derivative
Indication: Treatment of Paget's disease of the bone; treatment and prevention of glucocorticoid-induced osteoporosis; treatment and prevention of osteoporosis in postmenopausal women; treatment of osteoporosis in men
MOA:
A bisphosphonate which inhibits bone resorption via actions on osteoclasts or on osteoclast precursors; decreases the rate of bone resorption, leading to an indirect increase in bone mineral density. In Paget's disease, characterized by disordered resorption and formation of bone, inhibition of resorption leads to an indirect decrease in bone formation; but the newly-formed bone has a more normal architecture. |
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Term
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Definition
Class: Calcimimetic
Indication: Treatment of secondary hyperparathyroidism in patients with chronic kidney disease (CKD) on dialysis; treatment of hypercalcemia in patients with parathyroid carcinoma; treatment of severe hypercalcemia in patients with primary hyperparathyroidism who are unable to undergo parathyroidectomy
MOA:
Increases the sensitivity of the calcium-sensing receptor on the parathyroid gland thereby, concomitantly lowering parathyroid hormone (PTH), serum calcium, and serum phosphorus levels, preventing progressive bone disease and adverse events associated with mineral metabolism disorders. |
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Term
| ASACOL (mesalamine (800 mg, delayed-release tablets)) |
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Definition
Class: 5-aminosalicylic acid derivative
Indication:
Asacol®, Delzicol™, Lialda®, Mezavant®, Pentasa®: Treatment and maintenance of remission of mildly- to moderately-active ulcerative colitis
Asacol® HD: Treatment of moderately-active ulcerative colitis
MOA:
Mesalamine (5-aminosalicylic acid) is the active component of sulfasalazine; the specific mechanism of action of mesalamine is unknown; however, it is thought that it modulates local chemical mediators of the inflammatory response, especially leukotrienes, and is also postulated to be a free radical scavenger or an inhibitor of tumor necrosis factor (TNF); action appears topical rather than systemic |
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Term
| Loestrin 24 FE (norethindrone/ethinyl estradiol) |
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Definition
Class: Contraceptive - estrogen/progestin combination
Indication: Prevention of pregnancy; treatment of acne; moderate-to-severe vasomotor symptoms associated with menopause; prevention of osteoporosis (in women at significant risk only)
Unlabeled: Treatment of hypermenorrhea (menorrhagia); pain associated with endometriosis, dysmenorrhea; dysfunctional uterine bleeding
MOA:
Combination oral contraceptives inhibit ovulation via a negative feedback mechanism on the hypothalamus, which alters the normal pattern of gonadotropin secretion of a follicle-stimulating hormone (FSH) and luteinizing hormone by the anterior pituitary. The follicular phase FSH and midcycle surge of gonadotropins are inhibited. In addition, combination hormonal contraceptives produce alterations in the genital tract, including changes in the cervical mucus, rendering it unfavorable for sperm penetration even if ovulation occurs. Changes in the endometrium may also occur, producing an unfavorable environment for nidation. Combination hormonal contraceptive drugs may alter the tubal transport of the ova through the fallopian tubes. Progestational agents may also alter sperm fertility.
In postmenopausal women, exogenous estrogen is used to replace decreased endogenous production. The addition of progestin reduces the incidence of endometrial hyperplasia and risk of endometrial cancer in women with an intact uterus. |
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Term
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Definition
Class: Antineoplastic Agent, Tyrosine Kinase Inhibitor; Epidermal Growth Factor Receptor (EGFR) Inhibitor
Indication: Nonsmall cell lung cancer (NSCLC): First-line treatment of metastatic NSCLC in patients with known EGFR exon 19 deletions or exon 21 (L858R) substitution mutations; treatment (as monotherapy) of locally-advanced or metastatic NSCLC refractory to at least 1 prior chemotherapy regimen; maintenance treatment of locally-advanced or metastatic NCSLC which has not progressed after 4 cycles of first-line platinum-based chemotherapy
Note: Use in combination with platinum-based chemotherapy is not recommended. First-line treatment in patients with metastatic NSCLC with EGFR mutations other than exon 19 deletion or exon 21 (L858R) substitution has not been evaluated.
Pancreatic cancer (not an approved use in Canada): First-line treatment of locally-advanced, unresectable or metastatic pancreatic cancer (combination with gemcitabine)
MOA:
Reversibly inhibits overall epidermal growth factor receptor (HER1/EGFR) - tyrosine kinase activity. Intracellular phosphorylation is inhibited which prevents further downstream signaling, resulting in cell death. Erlotinib has higher binding affinity for EGFR exon 19 deletion or exon 21 L858R mutations than for the wild type receptor. |
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Term
|
Definition
Class: Thrombin inhibitor - anticoagulant
Indication: Prevention of stroke and systemic embolism in patients with nonvalvular atrial fibrillation
2011 ACCF/AHA/HRS atrial fibrillation guidelines: Not recommended for patients with coexisting prosthetic heart valve or hemodynamically significant valve disease, severe renal failure (Clcr <15 mL/minute), or advanced liver disease (impaired baseline clotting function)
MOA:
Prodrug lacking anticoagulant activity that is converted in vivo to the active dabigatran, a specific, reversible, direct thrombin inhibitor that inhibits both free and fibrin-bound thrombin. Inhibits coagulation by preventing thrombin-mediated effects, including cleavage of fibrinogen to fibrin monomers, activation of factors V, VIII, XI, and XIII, and inhibition of thrombin-induced platelet aggregation. |
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Term
|
Definition
Class: Phosphate binder
Indication: Reduction or control of serum phosphorous in patients with chronic kidney disease on hemodialysis
MOA:
Sevelamer (a polymeric compound) binds phosphate within the intestinal lumen, limiting absorption and decreasing serum phosphate concentrations without altering calcium, aluminum, or bicarbonate concentrations. |
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Term
| Gamunex-C (human immuneglobulin) |
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Definition
Class: Blood product derivative, human immune globulin
Indication: Treatment of primary humoral immunodeficiency syndromes (congenital agammaglobulinemia, severe combined immunodeficiency syndromes [SCIDS], common variable immunodeficiency, X-linked immunodeficiency, Wiskott-Aldrich syndrome) (Bivigam, Carimune NF, Flebogamma DIF, Gammagard Liquid, Gammagard S/D, Gammaked, Gammaplex, Gamunex-C, Hizentra, Octagam, Privigen)
Treatment of acute and chronic immune thrombocytopenia (ITP) (Carimune NF, Gammagard S/D, Gammaked, Gammaplex [chronic only], Gamunex-C, Privigen [chronic only])
Treatment of chronic inflammatory demyelinating polyneuropathy (CIDP) (Gammaked, Gamunex-C)
Treatment of multifocal motor neuropathy (MMN) (Gammagard Liquid)
Prevention of coronary artery aneurysms associated with Kawasaki syndrome (in combination with aspirin) (Gammagard S/D)
Prevention of bacterial infection in patients with hypogammaglobulinemia and/or recurrent bacterial infections with B-cell chronic lymphocytic leukemia (CLL) (Gammagard S/D)
Prevention of serious infection in immunoglobulin deficiency (select agammaglobulinemias) (GamaSTAN S/D)
Provision of passive immunity in the following susceptible individuals (GamaSTAN S/D):
Hepatitis A: Pre-exposure prophylaxis; postexposure: within 14 days and/or prior to manifestation of disease
Measles: For use within 6 days of exposure in an unvaccinated person, who has not previously had measles
Rubella: Postexposure prophylaxis (within 72 hours) to reduce the risk of infection and fetal damage in exposed pregnant women who will not consider therapeutic abortion
Varicella: For immunosuppressed patients when varicella zoster immune globulin is not available
MOA:
Replacement therapy for primary and secondary immunodeficiencies, and IgG antibodies against bacteria, viral, parasitic and mycoplasma antigens; interference with Fc receptors on the cells of the reticuloendothelial system for autoimmune cytopenias and ITP; provides passive immunity by increasing the antibody titer and antigen-antibody reaction potential |
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Term
|
Definition
Class: Serotonin/Norepinephrine Reuptake Inhibitor (SNRI) - antidepressant
Indication: Treatment of major depressive disorder (acute and maintenance)
MOA:
Desvenlafaxine is a potent and selective serotonin and norepinephrine reuptake inhibitor. |
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Term
| Dexilant (dexlansoprazole) |
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Definition
Class: Proton Pump Inhibitor (PPI)
Indication: Short-term (4 weeks) treatment of heartburn associated with nonerosive GERD; short-term (up to 8 weeks) treatment of all grades of erosive esophagitis (EE); to maintain healing of erosive esophagitis and relief of heartburn for up to 6 months
MOA:
Proton pump inhibitor; decreases acid secretion in gastric parietal cells through inhibition of (H+, K+)-ATPase enzyme system, blocking the final step in gastric acid production |
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Term
| Trilipix (fenofibrate (45 mg, 135 mg)) |
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Definition
Class: Fibric acid - antilipemic agent
Indication: Adjunct to dietary therapy for the treatment of severely elevated serum triglyceride levels; adjunct to dietary therapy for the reduction of low density lipoprotein cholesterol (LDL-C), total cholesterol (total-C), triglycerides, and apolipoprotein B (apo B) and to increase high density lipoprotein cholesterol (HDL-C) in patients with primary hypercholesterolemia or mixed dyslipidemia
TriLipix™ is also indicated as adjunct to dietary therapy concomitantly with a statin to reduce triglyceride levels and increase HDL-C levels in patients with mixed dyslipidemia and coronary heart disease (CHD) or at risk for CHD
MOA:
Fenofibric acid, an agonist for the nuclear transcription factor peroxisome proliferator-activated receptor-alpha (PPAR-alpha), downregulates apoprotein C-III (an inhibitor of lipoprotein lipase) and upregulates the synthesis of apolipoprotein A-I, fatty acid transport protein, and lipoprotein lipase resulting in an increase in VLDL catabolism, fatty acid oxidation, and elimination of triglyceride-rich particles; as a result of a decrease in VLDL levels, total plasma triglycerides are reduced by 30% to 60%; modest increased in HDL occurs in some hypertriglyceridemia patients. |
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Term
| Focalin XR (dexmethylphenidate) |
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Definition
Class: CNS stimulant
Indication: Attention-deficit/hyperactivity disorder (ADHD)
MOA:
Dexmethylphenidate is the more active, d-threo-enantiomer, of racemic methylphenidate. It is a CNS stimulant; blocks the reuptake of norepinephrine and dopamine, and increases their release into the extraneuronal space. |
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Term
|
Definition
Class: 5-alpha-reductase inhibitor
Indication: Treatment of symptomatic benign prostatic hyperplasia (BPH) as monotherapy or combination therapy with tamsulosin
Unlabeled: treatment of male pattern baldness
MOA:
Dutasteride is a 4-azo analog of testosterone and is a competitive, selective inhibitor of both reproductive tissues (type 2) and skin and hepatic (type 1) 5α-reductase. This results in inhibition of the conversion of testosterone to dihydrotestosterone and markedly suppresses serum dihydrotestosterone levels. |
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Term
|
Definition
Class: Monoclonal antibody - anti-asthmatic
Indication: Treatment of moderate-to-severe, persistent allergic asthma in patients with a positive skin test or in vitro reactivity to a perennial aeroallergen and not adequately controlled with inhaled corticosteroids
MOA:
Omalizumab is an IgG monoclonal antibody (recombinant DNA derived) which inhibits IgE binding to the high-affinity IgE receptor on mast cells and basophils. By decreasing bound IgE, the activation and release of mediators in the allergic response (early and late phase) is limited. Serum free IgE levels and the number of high-affinity IgE receptors are decreased. Long-term treatment in patients with allergic asthma showed a decrease in asthma exacerbations and corticosteroid usage. |
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Term
|
Definition
Class: Selective Norepinephrine Reuptake Inhibitor (SNRI)
Indication: Treatment of attention deficit/hyperactivity disorder (ADHD)
MOA:
Selectively inhibits the reuptake of norepinephrine (Ki 4.5nM) with little to no activity at the other neuronal reuptake pumps or receptor sites. |
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Term
|
Definition
Class: Glucagon-like Peptide-1 (GLP-1) receptor agonist
Indication: adjunctive treatment of type 2 diabetes mellitus to improve glycemic control
MOA:
Exenatide is an analog of the hormone incretin (glucagon-like peptide 1 or GLP-1) which increases glucose-dependent insulin secretion, decreases inappropriate glucagon secretion, increases B-cell growth/replication, slows gastric emptying, and decreases food intake. Exenatide administration results in decreases in hemoglobin A1c by approximately 0.5% to 1% (immediate release) or 1.5% to 1.9% (extended release). |
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Term
| Pegasys (peginterferon alpha-2a) |
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Definition
Class: Interferon
Indication: Treatment of chronic hepatitis C (CHC), in combination with ribavirin (unless contraindicated or significant intolerance to ribavirin), in patients ≥5 years of age with compensated liver disease and not previously treated with alfa interferons, in patients with histological evidence of cirrhosis (Child-Pugh class A) and compensated liver disease; treatment of adults coinfected with CHC and clinically-stable HIV disease (CD4 count >100 cells/mm3); treatment (monotherapy) of adults with HBeAg-positive and HBeAg-negative chronic hepatitis B with compensated liver disease and evidence of viral replication and liver inflammation
MOA:
Alpha interferons are a family of proteins, produced by nucleated cells that have antiviral, antiproliferative, and immune-regulating activity. There are 16 known subtypes of alpha interferons. Interferons interact with cells through high affinity cell surface receptors. Following activation, multiple effects can be detected including induction of gene transcription. Interferons inhibit cellular growth, alter the state of cellular differentiation, interfere with oncogene expression, alter cell surface antigen expression, increase phagocytic activity of macrophages, and augment cytotoxicity of lymphocytes for target cells. |
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Term
| Gammagard (human immune globulin) |
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Definition
Class: Immune globulin, blood product derivative
Indication: Treatment of primary humoral immunodeficiency syndromes (congenital agammaglobulinemia, severe combined immunodeficiency syndromes [SCIDS], common variable immunodeficiency, X-linked immunodeficiency, Wiskott-Aldrich syndrome) (Bivigam, Carimune NF, Flebogamma DIF, Gammagard Liquid, Gammagard S/D, Gammaked, Gammaplex, Gamunex-C, Hizentra, Octagam, Privigen)
Treatment of acute and chronic immune thrombocytopenia (ITP) (Carimune NF, Gammagard S/D, Gammaked, Gammaplex [chronic only], Gamunex-C, Privigen [chronic only])
Treatment of chronic inflammatory demyelinating polyneuropathy (CIDP) (Gammaked, Gamunex-C)
Treatment of multifocal motor neuropathy (MMN) (Gammagard Liquid)
Prevention of coronary artery aneurysms associated with Kawasaki syndrome (in combination with aspirin) (Gammagard S/D)
Prevention of bacterial infection in patients with hypogammaglobulinemia and/or recurrent bacterial infections with B-cell chronic lymphocytic leukemia (CLL) (Gammagard S/D)
Prevention of serious infection in immunoglobulin deficiency (select agammaglobulinemias) (GamaSTAN S/D)
Provision of passive immunity in the following susceptible individuals (GamaSTAN S/D):
Hepatitis A: Pre-exposure prophylaxis; postexposure: within 14 days and/or prior to manifestation of disease
Measles: For use within 6 days of exposure in an unvaccinated person, who has not previously had measles
Rubella: Postexposure prophylaxis (within 72 hours) to reduce the risk of infection and fetal damage in exposed pregnant women who will not consider therapeutic abortion
Varicella: For immunosuppressed patients when varicella zoster immune globulin is not available
Unlabeled:
Acquired hypogammaglobulinemia secondary to malignancy; Guillain-Barré syndrome; hematopoietic stem cell transplantation (HSCT), to prevent bacterial infections among allogeneic recipients with severe hypogammaglobulinemia (IgG <400 mg/dL) at <100 days post transplant (CDC guidelines); HIV-associated thrombocytopenia; multiple sclerosis (relapsing, remitting when other therapies cannot be used); Lambert-Eaton myasthenic syndrome (LEMS); myasthenia gravis; refractory dermatomyositis/polymyositis
MOA:
Replacement therapy for primary and secondary immunodeficiencies, and IgG antibodies against bacteria, viral, parasitic and mycoplasma antigens; interference with Fc receptors on the cells of the reticuloendothelial system for autoimmune cytopenias and ITP; provides passive immunity by increasing the antibody titer and antigen-antibody reaction potential |
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Term
|
Definition
Class: Calcineurin inhibitor, immunosuppressant
Indication: Prevention of organ rejection in heart (Prograf® only), and kidney or liver (Hecoria™, Prograf®) transplant recipients
Unlabeled: Prevention of organ rejection in lung, small bowel transplant recipients; prevention and treatment of graft-versus-host disease (GVHD) in allogenic hematopoietic stem cell transplantation
MOA:
Suppresses cellular immunity (inhibits T-lymphocyte activation), by binding to an intracellular protein, FKBP-12 and complexes with calcineurin dependent proteins to inhibit calcineurin phosphatase activity |
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Term
|
Definition
Class: Alkylating agent (nitrogen mustard) - antineoplastic agent
Indication: Treatment of chronic lymphocytic leukemia (CLL); treatment of progressed indolent B-cell non-Hodgkin’s lymphoma (NHL)
Unlabeled: Treatment of relapsed or refractory Hodgkin lymphoma; treatment of mantle cell lymphoma; salvage therapy for relapsed multiple myeloma; first-line therapy for follicular lymphoma; treatment of Waldenström’s macroglobulinemia
MOA:
Bendamustine is an alkylating agent (nitrogen mustard derivative) with a benzimidazole ring (purine analog) which demonstrates only partial cross-resistance (in vitro) with other alkylating agents. It leads to cell death via single and double strand DNA cross-linking. Bendamustine is active against quiescent and dividing cells. The primary cytotoxic activity is due to bendamustine (as compared to metabolites). |
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Term
| Risperdal Consta (risperidone) |
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Definition
Class: Atypical antipsychotic, anti-manic agent
Indication:
Oral: Treatment of schizophrenia; treatment of acute mania or mixed episodes associated with bipolar I disorder (as monotherapy in children or adults, or in combination with lithium or valproate in adults); treatment of irritability/aggression associated with autistic disorder
Injection: Treatment of schizophrenia; maintenance treatment of bipolar I disorder in adults as monotherapy or in combination with lithium or valproate
Unlabeled:
Treatment of Tourette's syndrome; psychosis/agitation related to Alzheimer’s dementia; post-traumatic stress disorder (PTSD)
MOA:
Risperidone is a benzisoxazole atypical antipsychotic with mixed serotonin-dopamine antagonist activity that binds to 5-HT2-receptors in the CNS and in the periphery with a very high affinity; binds to dopamine-D2 receptors with less affinity. The binding affinity to the dopamine-D2 receptor is 20 times lower than the 5-HT2 affinity. The addition of serotonin antagonism to dopamine antagonism (classic neuroleptic mechanism) is thought to improve negative symptoms of psychoses and reduce the incidence of extrapyramidal side effects. Alpha1, alpha2 adrenergic, and histaminergic receptors are also antagonized with high affinity. Risperidone has low to moderate affinity for 5-HT1C, 5-HT1D, and 5-HT1A receptors, weak affinity for D1 and no affinity for muscarinics or beta1 and beta2 receptors |
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Term
|
Definition
Class: Anti-gout agent
Indication: Prevention and treatment of acute gout flares; treatment of familial Mediterranean fever (FMF)
Unlabeled: primary biliary cirrhosis, pericarditis
MOA:
Disrupts cytoskeletal functions by inhibiting β-tubulin polymerization into microtubules, preventing activation, degranulation, and migration of neutrophils associated with mediating some gout symptoms. In familial Mediterranean fever, may interfere with intracellular assembly of the inflammasome complex present in neutrophils and monocytes that mediate activation of interleukin-1β. |
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Term
|
Definition
Class: Protease inhibitor, antiretroviral agent
Indication: Treatment of HIV infection; should always be used as part of a multidrug regimen
MOA:
Binds to the site of HIV-1 protease activity and inhibits cleavage of viral Gag-Pol polyprotein precursors into individual functional proteins required for infectious HIV. This results in the formation of immature, noninfectious viral particles |
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Term
| Premarin (conjugated estrogens - equine) |
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Definition
Class: Estrogen derivative
Indication: Treatment of moderate-to-severe vasomotor symptoms associated with menopause; treatment of vulvar and vaginal atrophy due to menopause; hypoestrogenism (due to hypogonadism, castration, or primary ovarian failure); prostatic cancer (palliation); breast cancer (palliation); postmenopausal osteoporosis (prophylaxis); abnormal uterine bleeding
MOA:
Conjugated estrogens contain a mixture of estrone sulfate, equilin sulfate, 17 alpha-dihydroequilin, 17 alpha-estradiol and 17 beta-dihydroequilin. Estrogens are responsible for the development and maintenance of the female reproductive system and secondary sexual characteristics. Estradiol is the principle intracellular human estrogen and is more potent than estrone and estriol at the receptor level; it is the primary estrogen secreted prior to menopause. Following menopause, estrone and estrone sulfate are more highly produced. Estrogens modulate the pituitary secretion of gonadotropins, luteinizing hormone, and follicle-stimulating hormone through a negative feedback system; estrogen replacement reduces elevated levels of these hormones in postmenopausal women. |
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Term
| Nuvaring (etonogestrel/ethinyl estradiol vaginal ring) |
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Definition
Class: Contraceptive - estrogen and progestin combination
Indication: Prevention of pregnancy
Unlabeled: treatment of hypermenorrhea (menorrhagia); pain associated with endometriosis; dysmenorrhea; dysfunctional uterine bleeding
MOA:
Combination hormonal contraceptives inhibit ovulation via a negative feedback mechanism on the hypothalamus, which alters the normal pattern of gonadotropin secretion of a follicle-stimulating hormone (FSH) and luteinizing hormone by the anterior pituitary. The follicular phase FSH and midcycle surge of gonadotropins are inhibited. In addition, combination hormonal contraceptives produce alterations in the genital tract, including changes in the cervical mucus, rendering it unfavorable for sperm penetration even if ovulation occurs. Changes in the endometrium may also occur, producing an unfavorable environment for nidation. Combination hormonal contraceptive drugs may alter the tubal transport of the ova through the fallopian tubes. Progestational agents may also alter sperm fertility. |
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Term
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Definition
Class: Beta-2 agonist
Indication: Treatment or prevention of bronchospasm in children and adults with reversible obstructive airway disease
MOA:
Relaxes bronchial smooth muscle by action on beta2-receptors with little effect on heart rate |
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Term
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Definition
Class: Prostaglandin, anti-glaucoma, ophthalmic agent
Indication: Reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension
MOA:
A selective FP prostanoid receptor agonist which lowers intraocular pressure by increasing trabecular meshwork and outflow |
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Term
| Epzicom (abacavir/lamivudine) |
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Definition
Class: Nucleoside Reverse Transcriptase Inhibitor (NRTI) (combination) - Antiretroviral agent
Indication: Treatment of HIV infections in combination with other antiretroviral agents
MOA:
Nucleoside reverse transcriptase inhibitor combination.
Abacavir is a guanosine analogue which is phosphorylated to carbovir triphosphate which interferes with HIV viral RNA-dependent DNA polymerase resulting in inhibition of viral replication.
Lamivudine is a cytosine analog. After lamivudine is triphosphorylated, the principle mode of action is inhibition of HIV reverse transcription via viral DNA chain termination; inhibits RNA-dependent DNA polymerase activities of reverse transcriptase. |
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Term
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Definition
Class: Selective 5-HT3 (serotonin) receptor antagonist - antiemetic
Indication: Prevention of chemotherapy-associated nausea and vomiting; indicated for prevention of acute (highly-emetogenic therapy) as well as acute and delayed (moderately-emetogenic therapy) nausea and vomiting; prevention of postoperative nausea and vomiting (PONV)
MOA:
Selective 5-HT3 receptor antagonist, blocking serotonin, both on vagal nerve terminals in the periphery and centrally in the chemoreceptor trigger zone |
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Term
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Definition
Class: Opioid analgesic
Indication:
Transdermal patch (eg, Duragesic®): Management of persistent moderate-to-severe chronic pain in opioid-tolerant patients when around-the-clock analgesia is needed for an extended period of time
MOA:
Binds with stereospecific receptors at many sites within the CNS, increases pain threshold, alters pain reception, inhibits ascending pain pathways |
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Term
| ACTOplus met (pioglitazone/metformin) |
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Definition
Class: Thiazolidedinedione (TZD)/Biguanide - antidiabetic agent
Indication: Type 2 diabetes mellitus (Management of type 2 diabetes mellitus (noninsulin dependent, NIDDM) in patients already receiving a thiazolidinedione and metformin or who have inadequate control on either agent)
MOA: Pioglitazone is a thiazolidinedione antidiabetic agent that lowers blood glucose by improving target cell response to insulin, without increasing pancreatic insulin secretion. It has a mechanism of action that is dependent on the presence of insulin for activity.
Metformin decreases hepatic glucose production, decreasing intestinal absorption of glucose, and improves insulin sensitivity (increases peripheral glucose uptake and utilization). |
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Term
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Definition
Class: Antiplatelet agent
Indication: Reduction in the risk of stroke in patients who have had transient ischemia of the brain or ischemic stroke due to thrombosis
Unlabeled: Hemodialysis graft patency; symptomatic carotid artery stenosis (including recent carotid endarterectomy)
MOA:
The antithrombotic action results from additive antiplatelet effects. Dipyridamole inhibits the uptake of adenosine into platelets, endothelial cells, and erythrocytes. Aspirin inhibits platelet aggregation by irreversible inhibition of platelet cyclooxygenase and thus inhibits the generation of thromboxane A2. |
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Term
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Definition
Class: Nucleotide Reverse Transcriptase Inhibitor (NtRTI) - antiretroviral agent
Indication: Management of HIV infections in combination with at least two other antiretroviral agents in patients ≥2 years of age; treatment of chronic hepatitis B virus (HBV) in patients with compensated or decompensated liver disease in patients ≥12 years of age
MOA:
Tenofovir disoproxil fumarate (TDF) is an analog of adenosine 5'-monophosphate; it interferes with the HIV viral RNA dependent DNA polymerase resulting in inhibition of viral replication. TDF is first converted intracellularly by hydrolysis to tenofovir and subsequently phosphorylated to the active tenofovir diphosphate; nucleotide reverse transcriptase inhibitor. Tenofovir inhibits replication of HBV by inhibiting HBV polymerase. |
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Term
| Toprol XL (metoprolol succinate) |
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Definition
Class: Beta-blocker (beta-1-selective); anti-anginal agent
Indication: Treatment of angina pectoris, hypertension, or hemodynamically-stable acute myocardial infarction
Extended release: Treatment of angina pectoris or hypertension; to reduce mortality/hospitalization in patients with heart failure (stable NYHA Class II or III) already receiving ACE inhibitors, diuretics, and/or digoxin
Unlabeled:
Treatment of ventricular arrhythmias, atrial ectopy; migraine prophylaxis, essential tremor; prevention of reinfarction and sudden death after myocardial infarction; prevention and treatment of atrial fibrillation and atrial flutter; multifocal atrial tachycardia; symptomatic treatment of hypertrophic obstructive cardiomyopathy; management of thyrotoxicosis
MOA:
Selective inhibitor of beta1-adrenergic receptors; competitively blocks beta1-receptors, with little or no effect on beta2-receptors at doses <100 mg; does not exhibit any membrane stabilizing or intrinsic sympathomimetic activity |
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Term
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Definition
Class: Parathyroid hormone (PTH) analog
Indication: Treatment of osteoporosis in postmenopausal women at high risk of fracture; treatment of primary or hypogonadal osteoporosis in men at high risk of fracture; treatment of glucocorticoid-induced osteoporosis in men and women at high risk for fracture
MOA:
Teriparatide is a recombinant formulation of endogenous parathyroid hormone (PTH), containing a 34-amino-acid sequence which is identical to the N-terminal portion of this hormone. The pharmacologic activity of teriparatide, which is similar to the physiologic activity of PTH, includes stimulating osteoblast function, increasing gastrointestinal calcium absorption, and increasing renal tubular reabsorption of calcium. Treatment with teriparatide results in increased bone mineral density, bone mass, and strength. In postmenopausal women, teriparatide has been shown to decrease osteoporosis-related fractures. |
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Term
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Definition
Class: Angiotensin II Receptor Blocker (ARB)
Indication: Treatment of hypertension alone or in combination with other antihypertensives; treatment of diabetic nephropathy in patients with type 2 diabetes mellitus (noninsulin dependent, NIDDM) and hypertension
Unlabeled: To slow the rate of progression of aortic-root dilation in pediatric patients with Marfan’s syndrome
MOA:
Irbesartan is an angiotensin receptor antagonist. Angiotensin II acts as a vasoconstrictor. In addition to causing direct vasoconstriction, angiotensin II also stimulates the release of aldosterone. Once aldosterone is released, sodium as well as water are reabsorbed. The end result is an elevation in blood pressure. Irbesartan binds to the AT1 angiotensin II receptor. This binding prevents angiotensin II from binding to the receptor thereby blocking the vasoconstriction and the aldosterone secreting effects of angiotensin II |
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Term
| Mirena (levonorgestrel IUD) |
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Definition
Class: Progestin contraceptive
Indication:
Intrauterine device (IUD): Prevention of pregnancy; treatment of heavy menstrual bleeding in women who also choose to use an IUD for contraception
MOA:
Pregnancy may be prevented through several mechanisms: Thickening of cervical mucus, which inhibits sperm passage through the uterus and sperm survival; inhibition of ovulation, from a negative feedback mechanism on the hypothalamus, leading to reduced secretion of follicle stimulating hormone (FSH) and luteinizing hormone (LH); and inhibition of implantation. Levonorgestrel is not effective once the implantation process has begun. |
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Term
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Definition
Class: Glucagon-Like Peptide-1 (GLP-1) receptor agonist
Indication: Treatment of type 2 diabetes mellitus (noninsulin dependent, NIDDM) to improve glycemic control
MOA:
Liraglutide is a long acting analog of human glucagon-like peptide-1 (GLP-1) (an incretin hormone) which increases glucose-dependent insulin secretion, decreases inappropriate glucagon secretion, increases B-cell growth/replication, slows gastric emptying, and decreases food intake. Liraglutide administration results in decreases in hemoglobin A1c by approximately 1%. |
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Term
| Zosyn (piperacillin/tazobactam) |
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Definition
Class: Penicillin (beta-lactam) antibiotic + beta-lactamase inhibitor
Indication: Treatment of moderate-to-severe infections caused by susceptible organisms, including infections of the lower respiratory tract (community-acquired pneumonia, nosocomial pneumonia); uncomplicated and complicated skin and skin structures (including diabetic foot infections); gynecologic (endometritis, pelvic inflammatory disease); and intra-abdominal infections (appendicitis with rupture/abscess, peritonitis). Tazobactam expands activity of piperacillin to include beta-lactamase producing strains of S. aureus, H. influenzae, E. coli, Bacteroides spp, and other gram-positive and gram-negative aerobic and anaerobic bacteria.
Unlabeled: Treatment of moderate-to-severe infections caused by susceptible organisms, including urinary tract infections, bone and joint infections, septicemia, endocarditis, and cystic fibrosis exacerbations
MOA:
Piperacillin inhibits bacterial cell wall synthesis by binding to one or more of the penicillin-binding proteins (PBPs); which in turn inhibits the final transpeptidation step of peptidoglycan synthesis in bacterial cell walls, thus inhibiting cell wall biosynthesis. Bacteria eventually lyse due to ongoing activity of cell wall autolytic enzymes (autolysins and murein hydrolases) while cell wall assembly is arrested. Piperacillin exhibits time-dependent killing. Tazobactam inhibits many beta-lactamases, including staphylococcal penicillinase and Richmond-Sykes types 2, 3, 4, and 5, including extended spectrum enzymes; it has only limited activity against class 1 beta-lactamases other than class 1C types. |
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Term
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Definition
Class: Acetylcholinesterase inhibitor (central)
Indication: Treatment of mild-to-moderate dementia associated with Alzheimer's disease or Parkinson’s disease
Unlabeled: Severe dementia associated with Alzheimer's disease; Lewy body dementia
MOA:
A deficiency of cortical acetylcholine is thought to account for some of the symptoms of Alzheimer's disease and the dementia of Parkinson's disease; rivastigmine increases acetylcholine in the central nervous system through reversible inhibition of its hydrolysis by cholinesterase |
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Term
| Privigen (human immune globulin) |
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Definition
Class: immune globulin - blood product derivative
Indication: Treatment of primary humoral immunodeficiency syndromes (congenital agammaglobulinemia, severe combined immunodeficiency syndromes [SCIDS], common variable immunodeficiency, X-linked immunodeficiency, Wiskott-Aldrich syndrome) (Bivigam, Carimune NF, Flebogamma DIF, Gammagard Liquid, Gammagard S/D, Gammaked, Gammaplex, Gamunex-C, Hizentra, Octagam, Privigen)
Treatment of acute and chronic immune thrombocytopenia (ITP) (Carimune NF, Gammagard S/D, Gammaked, Gammaplex [chronic only], Gamunex-C, Privigen [chronic only])
Treatment of chronic inflammatory demyelinating polyneuropathy (CIDP) (Gammaked, Gamunex-C)
Treatment of multifocal motor neuropathy (MMN) (Gammagard Liquid)
Prevention of coronary artery aneurysms associated with Kawasaki syndrome (in combination with aspirin) (Gammagard S/D)
Prevention of bacterial infection in patients with hypogammaglobulinemia and/or recurrent bacterial infections with B-cell chronic lymphocytic leukemia (CLL) (Gammagard S/D)
Prevention of serious infection in immunoglobulin deficiency (select agammaglobulinemias) (GamaSTAN S/D)
Provision of passive immunity in the following susceptible individuals (GamaSTAN S/D):
Hepatitis A: Pre-exposure prophylaxis; postexposure: within 14 days and/or prior to manifestation of disease
Measles: For use within 6 days of exposure in an unvaccinated person, who has not previously had measles
Rubella: Postexposure prophylaxis (within 72 hours) to reduce the risk of infection and fetal damage in exposed pregnant women who will not consider therapeutic abortion
Varicella: For immunosuppressed patients when varicella zoster immune globulin is not available
Unlabeled:
Acquired hypogammaglobulinemia secondary to malignancy; Guillain-Barré syndrome; hematopoietic stem cell transplantation (HSCT), to prevent bacterial infections among allogeneic recipients with severe hypogammaglobulinemia (IgG <400 mg/dL) at <100 days post transplant (CDC guidelines); HIV-associated thrombocytopenia; multiple sclerosis (relapsing, remitting when other therapies cannot be used); Lambert-Eaton myasthenic syndrome (LEMS); myasthenia gravis; refractory dermatomyositis/polymyositis
MOA:
Replacement therapy for primary and secondary immunodeficiencies, and IgG antibodies against bacteria, viral, parasitic and mycoplasma antigens; interference with Fc receptors on the cells of the reticuloendothelial system for autoimmune cytopenias and ITP; provides passive immunity by increasing the antibody titer and antigen-antibody reaction potential |
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Term
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Definition
Class: Angiogenesis inhibitor - antineoplastic agent, systemic immunomodulator
Indication:
Mantle cell lymphoma (MCL): Treatment of patients with MCL which has relapsed or progressed after two prior therapies (one of which included bortezomib)
Multiple myeloma: Treatment of multiple myeloma (in combination with dexamethasone) in patients who have received at least one prior therapy
Myelodysplastic syndromes (MDS): Treatment of low- or intermediate-1-risk MDS in patients with deletion 5q (del 5q) cytogenetic abnormality (with or without other cytogenetic abnormalities) with transfusion-dependent anemia
Unlabeled:
Treatment of non-Hodgkin lymphoma (diffuse large B-cell lymphoma); relapsed or refractory chronic lymphocytic leukemia (CLL), systemic light chain amyloidosis; lower-risk myelodysplastic syndrome (MDS) in transfusion-dependent patients without deletion 5q (del 5q); maintenance treatment for multiple myeloma (after response to primary treatment or following autologous stem cell transplant)
MOA:
Immunomodulatory, antiangiogenic, and antineoplastic characteristics via multiple mechanisms. Selectively inhibits secretion of proinflammatory cytokines (potent inhibitor of tumor necrosis factor-alpha secretion); enhances cell-mediated immunity by stimulating proliferation of anti-CD3 stimulated T cells (resulting in increased IL-2 and interferon gamma secretion); inhibits trophic signals to angiogenic factors in cells. Inhibits the growth of myeloma cells by inducing cell cycle arrest and cell death. |
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Term
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Definition
Class: Diagnostic agent
Indication: Radionuclide myocardial perfusion imaging (MPI) in patients unable to undergo adequate exercise stress testing
MOA:
Regadenoson, a low affinity agonist of the A2A adenosine receptor, increases coronary blood flow (CBF) and mimics the increase in CBF caused by exercise. Myocardial uptake of the radiopharmaceutical is proportional to CBF creating the contrast required to identify stenotic coronary arteries. |
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Term
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Definition
Class: Anti-psoriatic agent, interleukin-12 (IL-12) inhibitor, interleukin-23 (IL-23) inhibitor, monoclonal antibody
Indication: Moderate-to-severe plaque psoriasis
MOA:
Ustekinumab is a human monoclonal antibody that binds to and interferes with the proinflammatory cytokines, interleukin (IL)-12 and IL-23. Biological effects of IL-12 and IL-23 include natural killer (NK) cell activation, CD4+ T-cell differentiation and activation. Ustekinumab also interferes with the expression of monocyte chemotactic protein-1 (MCP-1), tumor necrosis factor-alpha (TNF-α), interferon-inducible protein-10 (IP-10), and interleukin-8 (IL-8). Significant clinical improvement in psoriasis patients is seen in association with reduction of these proinflammatory signalers. |
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Term
| Adacel (Tetanus and reduced diphtheria toxoids, acellular pertussis vaccine(Tdap)) |
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Definition
Class: Inactivated (bacterial) vaccine
Indication:
Adacel®, Boostrix® (Tdap): Active booster immunization against diphtheria, tetanus, and pertussis
MOA:
Promotes active immunity to diphtheria, tetanus, and pertussis by inducing production of specific antibodies. |
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Term
| Ortho Tri-Cyclen Lo (norgestimate/ethinyl estradiol) |
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Definition
Class: Estrogen and progestin combination contraceptive
Indication: Prevention of pregnancy, treatment of acne
Unlabeled:
Treatment of hypermenorrhea (menorrhagia); pain associated with endometriosis; dysmenorrhea; dysfunctional uterine bleeding |
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Term
|
Definition
Class: Bile acid sequestrant - antilipemic agent
Indication: Management of elevated LDL in primary hypercholesterolemia (Fredrickson type IIa) when used alone or in combination with an HMG-CoA reductase inhibitor; management of heterozygous familial hypercholesterolemia (heFH) in adolescent patients (males and postmenarcheal females 10-17 years of age) when used alone or in combination with an HMG-CoA reductase inhibitor, in patients who after an adequate trial of dietary therapy have LDL-C ≥190 mg/dL or LDL-C ≥160 mg/dL with positive family history of premature cardiovascular disease (CVD) or with two or more CVD risk factors; improve glycemic control in type 2 diabetes mellitus (noninsulin dependent, NIDDM) in conjunction with diet, exercise, and insulin or oral antidiabetic agents
MOA:
Cholesterol is the major precursor of bile acid. Colesevelam binds with bile acids in the intestine to form an insoluble complex that is eliminated in feces. This increased excretion of bile acids results in an increased oxidation of cholesterol to bile acid and a lowering of the serum cholesterol. |
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Term
|
Definition
Class: Thrombin inhibitor - anticoagulant
Indication: Anticoagulant used in conjunction with aspirin for patients with unstable angina undergoing percutaneous transluminal coronary angioplasty (PTCA) or percutaneous coronary intervention (PCI) with provisional glycoprotein IIb/IIIa inhibitor; anticoagulant used in conjunction with aspirin for patients undergoing PCI with (or at risk of) heparin-induced thrombocytopenia (HIT) / thrombosis syndrome (HITTS)
Unlabeled:
Heparin-induced thrombocytopenia (HIT); ST-elevation myocardial infarction (STEMI) undergoing primary PCI
MOA:
Bivalirudin acts as a specific and reversible direct thrombin inhibitor; it binds to the catalytic and anionic exosite of both circulating and clot-bound thrombin. Catalytic binding site occupation functionally inhibits coagulant effects by preventing thrombin-mediated cleavage of fibrinogen to fibrin monomers, and activation of factors V, VIII, and XIII. Shows linear dose- and concentration-dependent prolongation of ACT, aPTT, PT, and TT. |
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Term
| Gardasil (Quadrivalent human papillomavirus (HPV) types 6, 11, 16, and 18 vaccine) |
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Definition
Class: Inactivated (viral) vaccine
Indication: Females ≥9 years and ≤26 years of age: Prevention of cervical, vulvar, vaginal, and anal cancer caused by HPV types 16 and 18; genital warts caused by HPV types 6 and 11; cervical adenocarcinoma in situ, and vulvar, vaginal, cervical, or anal intraepithelial neoplasia caused by HPV types 6, 11, 16, and 18
Males ≥9 years and ≤26 years of age: Prevention of genital warts caused by human papillomavirus (HPV) types 6 and 11; anal cancer caused by HPV types 16 and 18, and anal intraepithelial neoplasia caused by HPV types 6, 11, 16, and 18
MOA:
Contains inactive human papillomavirus (HPV) proteins HPV 6 L1, HPV 11 L1, HPV 16 L1, and HPV 18 L1 which produce neutralizing antibodies to prevent cervical cancer, cervical adenocarcinoma, cervical, vaginal and vulvar neoplasia, and genital warts caused by HPV. |
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Term
|
Definition
Class: Anti-glaucoma agent, ophthalmic prostaglandin
Indication:
Reduction of intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension; hypotrichosis treatment of the eyelashes
MOA:
As a synthetic analog of prostaglandin with ocular hypotensive activity, bimatoprost decreases intraocular pressure by increasing the outflow of aqueous humor. Bimatoprost may increase the percent and duration of hairs in the growth phase, resulting in eyelash growth. |
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Term
| Pulmozyme (dornase alpha) |
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Definition
Class: Mucolytic agent - enzyme
Indication: Management of cystic fibrosis patients to reduce the frequency of respiratory infections that require parenteral antibiotics in patients with FVC ≥40% of predicted; in conjunction with standard therapies, to improve pulmonary function in patients with cystic fibrosis
Unlabeled:
Infected parapneumonic effusion (following alteplase administration)
MOA:
The hallmark of cystic fibrosis lung disease is the presence of abundant, purulent airway secretions composed primarily of highly polymerized DNA. The principal source of this DNA is the nuclei of degenerating neutrophils, which is present in large concentrations in infected lung secretions. The presence of this DNA produces a viscous mucous that may contribute to the decreased mucociliary transport and persistent infections that are commonly seen in this population. Dornase alfa is a deoxyribonuclease (DNA) enzyme produced by recombinant gene technology. Dornase selectively cleaves DNA, thus reducing mucous viscosity and as a result, airflow in the lung is improved and the risk of bacterial infection may be decreased. |
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Term
|
Definition
Class: Atypical antipsychotic agent
Indication:
Oral: Treatment of schizophrenia; acute treatment of schizoaffective disorder (monotherapy or adjunctive therapy to mood stabilizers and/or antidepressants)
Injection: Treatment of schizophrenia
Unlabeled:
Psychosis/agitation related to Alzheimer's dementia
MOA:
Paliperidone is considered a benzisoxazole atypical antipsychotic as it is the primary active metabolite of risperidone. As with other atypical antipsychotics, its therapeutic efficacy is believed to result from mixed central serotonergic and dopaminergic antagonism. The addition of serotonin antagonism to dopamine antagonism (classic neuroleptic mechanism) is thought to improve negative symptoms of psychoses and reduce the incidence of extrapyramidal side effects. Similar to risperidone, paliperidone demonstrates high affinity to α1, D2, H1, and 5-HT2C receptors, and low affinity for muscarinic and 5-HT1A receptors. In contrast to risperidone, paliperidone displays nearly 10-fold lower affinity for α2 and 5-HT2A receptors, and nearly three- to fivefold less affinity for 5-HT1A and 5-HT1D, respectively. |
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Term
| Reclast (zoledronic acid) |
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Definition
Class: Bisphosphonate derivative
Indication:
Oncology-related uses: Treatment of hypercalcemia of malignancy (albumin-corrected serum calcium >12 mg/dL); treatment of multiple myeloma; treatment of bone metastases of solid tumors
Nononcology uses: Treatment of Paget’s disease of bone; treatment of osteoporosis in postmenopausal women (to reduce the incidence of fractures or to reduce the incidence of new clinical fractures in patients at high risk, defined as a recent low-trauma hip fracture); prevention of osteoporosis in postmenopausal women, treatment of osteoporosis in men (to increase bone mass); treatment and prevention of glucocorticoid-induced osteoporosis (in patients initiating or continuing prednisone ≥7.5 mg/day [or equivalent] and expected to remain on glucocorticoids for at least 12 months)
Unlabeled:
Prevention of bone loss associated with aromatase inhibitor therapy in postmenopausal women with breast cancer; prevention of bone loss associated with androgen deprivation therapy in prostate cancer
MOA:
A bisphosphonate which inhibits bone resorption via actions on osteoclasts or on osteoclast precursors; inhibits osteoclastic activity and skeletal calcium release induced by tumors. Decreases serum calcium and phosphorus, and increases their elimination. In osteoporosis, zoledronic acid inhibits osteoclast-mediated resorption, therefore reducing bone turnover. |
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Term
|
Definition
Class: Alkylating agent (triazene) - antineoplastic agent
Indication: Treatment of newly-diagnosed glioblastoma multiforme (initially in combination with radiotherapy, then as maintenance treatment); treatment of refractory anaplastic astrocytoma
Unlabeled:
Treatment of recurrent glioblastoma multiforme, low-grade astrocytoma, low-grade oligodendroglioma, anaplastic oligodendroglioma, metastatic CNS lesions, refractory primary CNS lymphoma, advanced or metastatic melanoma, cutaneous T-cell lymphomas (mycosis fungoides [MF] and Sézary syndrome [SS]), advanced neuroendocrine tumors (carcinoid or islet cell), Ewing’s sarcoma (recurrent or progressive), soft tissue sarcomas (extremity/retroperitoneal/intra-abdominal or hemangiopericytoma/solitary fibrous tumor), treatment of pediatric neuroblastoma
MOA:
Temozolomide is a prodrug which is rapidly and nonenzymatically converted to the active alkylating metabolite MTIC [(methyl-triazene-1-yl)-imidazole-4-carboxamide]; this conversion is spontaneous, nonenzymatic, and occurs under physiologic conditions in all tissues to which it distributes. The cytotoxic effects of MTIC are manifested through alkylation (methylation) of DNA at the O6, N7 guanine positions which lead to DNA double strand breaks and apoptosis. Non-cell cycle specific. |
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Term
|
Definition
Class: Antibiotic
Indication: Treatment of travelers' diarrhea caused by noninvasive strains of E. coli; reduction in the risk of overt hepatic encephalopathy (HE) recurrence
Unlabeled: Treatment of hepatic encephalopathy; alternative treatment for Clostridium difficile-associated diarrhea (CDAD)
MOA:
Rifaximin inhibits bacterial RNA synthesis by binding to bacterial DNA-dependent RNA polymerase. |
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Term
| NovoSeven RT (recombinant coagulation factor VIIa (rFVIIa)) |
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Definition
Class: Antihemophilic agent
Indication: Treatment of bleeding episodes and prevention of bleeding in surgical interventions in patients with either hemophilia A or B with inhibitors to factor VIII or factor IX, acquired hemophilia, or congenital factor VII deficiency
Unlabeled:
Warfarin-related intracerebral hemorrhage; treatment of refractory bleeding after cardiac surgery in nonhemophiliac patients |
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Term
|
Definition
Class: Beta blocker (beta-1 selective)
Indication: Treatment of hypertension, alone or in combination with other agents
Unlabeled: Heart failure
MOA:
Highly-selective inhibitor of beta1-adrenergic receptors; at doses ≤10 mg nebivolol preferentially blocks beta1-receptors. Nebivolol, unlike other beta-blockers, also produces an endothelium-derived nitric oxide-dependent vasodilation resulting in a reduction of systemic vascular resistance. |
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Term
| Lialda (mesalamine 1.2 gram delayed-release tabs) |
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Definition
Class: 5-aminosalicylic acid derivative
Indication:
Oral:
Asacol®, Delzicol™, Lialda®, Mezavant®, Pentasa®: Treatment and maintenance of remission of mildly- to moderately-active ulcerative colitis
Apriso™: Maintenance of remission of ulcerative colitis
Asacol® HD: Treatment of moderately-active ulcerative colitis
Rectal: Treatment of active mild-to-moderate distal ulcerative colitis, proctosigmoiditis, or proctitis
MOA:
Mesalamine (5-aminosalicylic acid) is the active component of sulfasalazine; the specific mechanism of action of mesalamine is unknown; however, it is thought that it modulates local chemical mediators of the inflammatory response, especially leukotrienes, and is also postulated to be a free radical scavenger or an inhibitor of tumor necrosis factor (TNF); action appears topical rather than systemic |
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Term
|
Definition
Class: Sphingosine 1-phosphate (S1P) receptor modulator
Indication: Treatment of relapsing forms of multiple sclerosis (MS) to reduce the frequency of clinical exacerbations and delay disability progression
MOA:
Fingolimod-phosphate, active metabolite of fingolimod, binds to sphingosine 1-phosphate receptors 1, 3, 4, and 5. The amount of lymphocytes available to the central nervous system are decreased which reduces central inflammation. |
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Term
| Pneumovax 23 (Pneumococcal vaccine (each of 23 polysaccharide isolates)) |
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Definition
Class: Inactivated (bacterial) vaccine
Indication:
Immunization against pneumococcal disease caused by serotypes included in the vaccine. Routine vaccination is recommended for persons ≥50 years of age and persons ≥2 years in certain situations.
The Advisory Committee on Immunization Practices (ACIP) recommends routine vaccination for patients with the following underlying medical conditions (CDC, 59[34], 2010; CDC, 59[11], 2010; CDC, 2012):
Children ≥2 years of age and adults 19-64 years with functional or anatomic asplenia, including sickle cell disease or other hemoglobinopathies, congenital or acquired asplenia, splenic dysfunction, or splenectomy
Immunocompetent children ≥2 years of age with chronic heart disease (particularly cyanotic congenital heart disease and heart failure), chronic lung disease (including asthma if treated with high dose corticosteroids), diabetes, cerebrospinal fluid leaks, or cochlear implants
Immunocompetent adults 19-64 years with chronic heart disease (including heart failure and cardiomyopathies; excluding hypertension), chronic lung disease (including COPD, emphysema, and asthma), diabetes, cerebrospinal fluid leaks, cochlear implants, alcoholism, chronic liver disease, cirrhosis, and cigarette smokers
Immunocompromised children ≥2 years of age and adults 19-64 years with congenital or acquired immunodeficiency (includes B or T cell deficiency, compliment deficiencies and phagocytic disorders; excludes chronic granulomatous disease), HIV infection, chronic renal failure, nephrotic syndrome, leukemia, lymphoma, Hodgkin disease, generalized malignancies, solid organ transplant, multiple myeloma, or other diseases requiring immunosuppressive drugs (including long-term systemic corticosteroids and radiation therapy)
All adults ≥65 years of age
MOA:
Although there are more than 80 known pneumococcal capsular types, pneumococcal disease is mainly caused by only a few types of pneumococci. Pneumococcal vaccine contains capsular polysaccharides of 23 pneumococcal types of Streptococcal pneumoniae which represent at least 85% to 90% of pneumococcal disease isolates in the United States. The 23 capsular pneumococcal vaccine contains purified capsular polysaccharides of pneumococcal types 1, 2, 3, 4, 5, 6B, 7F, 8, 9N, 9V, 10A, 11A, 12F, 14, 15B, 17F, 18C, 19F, 19A, 20, 22F, 23F, and 33F. |
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Term
| Kaletra (lopinavir/ritonavir) |
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Definition
Class: Protease inhibitor combination - antiretroviral agent
Indication: Treatment of HIV infection in combination with other antiretroviral agents
MOA:
A coformulation of lopinavir and ritonavir. The lopinavir component binds to the site of HIV-1 protease activity and inhibits the cleavage of viral Gag-Pol polyprotein precursors into individual functional proteins required for infectious HIV. This results in the formation of immature, noninfectious viral particles. The ritonavir component inhibits the CYP3A metabolism of lopinavir, allowing increased plasma levels of lopinavir. |
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Term
| Zostavax (Varicella zoster vaccine, live, attenuated) |
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Definition
Class: Live (viral) vaccine
Indication: Prevention of herpes zoster (shingles) in patients ≥50 years of age
The Advisory Committee on Immunization Practices (ACIP) recommends routine vaccination of all patients ≥60 years of age, including patients who report a previous episode of zoster; patients with chronic medical conditions (eg, chronic renal failure, diabetes mellitus, rheumatoid arthritis, chronic pulmonary disease) unless those conditions are contraindications; and residents of nursing homes and other long-term care facilities without contraindications (CDC, 2008).
Although not specifically recommended for their profession, healthcare providers within the recommended age group should also receive the zoster vaccine (CDC, 2013)
MOA:
As a live, attenuated vaccine (Oka/Merck strain of varicella-zoster virus), zoster virus vaccine stimulates active immunity to disease caused by the varicella-zoster virus. Administration has been demonstrated to protect against the development of herpes zoster, with the highest efficacy in patients 60-69 years of age. It may also reduce the severity of complications, including postherpetic neuralgia, in patients who develop zoster following vaccination. |
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Term
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Definition
Class: Taxane antineoplastic agent (antimicrotubule)
Indication:
Taxotere: Treatment of breast cancer (locally-advanced/metastatic) after prior chemotherapy failure, or adjuvant treatment of operable node-positive); locally-advanced or metastatic nonsmall cell lung cancer (NSCLC); hormone refractory, metastatic prostate cancer; advanced gastric adenocarcinoma; locally-advanced squamous cell head and neck cancer
Unlabeled: Treatment of bladder cancer (metastatic), ovarian cancer, cervical cancer (recurrent), esophageal cancer, small cell lung cancer (relapsed), soft tissue sarcoma, Ewing’s sarcoma, osteosarcoma, and unknown-primary adenocarcinoma
MOA:
Docetaxel promotes the assembly of microtubules from tubulin dimers, and inhibits the depolymerization of tubulin which stabilizes microtubules in the cell. This results in inhibition of DNA, RNA, and protein synthesis. Most activity occurs during the M phase of the cell cycle. |
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Term
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Definition
Class: Selective adhesion-molecule inhibitor - gastrointestinal agent; monoclonal antibody
Indication: Monotherapy for the treatment of relapsing forms of multiple sclerosis; treatment of moderately- to severely-active Crohn’s disease
MOA:
Natalizumab is a monoclonal antibody against the alpha-4 subunit of integrin molecules. These molecules are important to adhesion and migration of cells from the vasculature into inflamed tissue. Natalizumab blocks integrin association with vascular receptors, limiting adhesion and transmigration of leukocytes. Efficacy in specific disorders may be related to reduction in specific inflammatory cell populations in target tissues. In multiple sclerosis, efficacy may be related to blockade of T-lymphocyte migration into the central nervous system; treatment results in a decreased frequency of relapse. In Crohn’s disease, natalizumab decreases inflammation by binding to alpha-4 integrin, blocking adhesion and migration of leukocytes in the gut. |
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Term
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Definition
Class: Acetylcholinesterase inhibitor (central)
Indication: Treatment of mild, moderate, or severe dementia of the Alzheimer's type
Unlabeled: behavioral syndromes in dementia; mild-to-moderate dementia associated with Parkinson's disease; Lewy body dementia
MOA:
Alzheimer's disease is characterized by cholinergic deficiency in the cortex and basal forebrain, which contributes to cognitive deficits. Donepezil reversibly and noncompetitively inhibits centrally-active acetylcholinesterase, the enzyme responsible for hydrolysis of acetylcholine. This appears to result in increased concentrations of acetylcholine available for synaptic transmission in the central nervous system. |
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Term
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Definition
Class: Smoking cessation aid - partial nicotine agonist
Indication: Smoking cessation
MOA:
Partial neuronal α4 β2 nicotinic receptor agonist; prevents nicotine stimulation of mesolimbic dopamine system associated with nicotine addiction. Also binds to 5-HT3 receptor (significance not determined) with moderate affinity. Varenicline stimulates dopamine activity but to a much smaller degree than nicotine does, resulting in decreased craving and withdrawal symptoms. |
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Term
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Definition
Class: Bone-modifying agent; monoclonal antibody
Indication:
Osteoporosis/bone loss (Prolia): Treatment of osteoporosis in postmenopausal women at high risk of fracture; treatment of osteoporosis (to increase bone mass) in men at high risk of fracture; treatment of bone loss in men receiving androgen-deprivation therapy (ADT) for nonmetastatic prostate cancer; treatment of bone loss in women receiving aromatase inhibitor (AI) therapy for breast cancer
Tumors (Xgeva): Prevention of skeletal-related events (eg, fracture, spinal cord compression, bone pain requiring surgery/radiation therapy) in patients with bone metastases from solid tumors; treatment of giant cell tumor of the bone in adults and skeletally mature adolescents that is unresectable or where surgical resection is likely to result in severe morbidity
Unlabeled:
Treatment of bone destruction caused by rheumatoid arthritis
MOA:
Denosumab is a monoclonal antibody with affinity for nuclear factor-kappa ligand (RANKL). Osteoblasts secrete RANKL; RANKL activates osteoclast precursors and subsequent osteolysis which promotes release of bone-derived growth factors, such as insulin-like growth factor-1 (IGF1) and transforming growth factor-beta (TGF-beta), and increases serum calcium levels. Denosumab binds to RANKL, blocks the interaction between RANKL and RANK (a receptor located on osteoclast surfaces), and prevents osteoclast formation, leading to decreased bone resorption and increased bone mass in osteoporosis. In solid tumors with bony metastases, RANKL inhibition decreases osteoclastic activity leading to decreased skeletal related events and tumor-induced bone destruction. In giant cell tumors of the bone (which express RANK and RANKL), denosumab inhibits tumor growth by preventing RANKL from activating its receptor (RANK) on the osteoclast surface, osteoclast precursors, and osteoclast-like giant cells. |
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Term
| Nutropin AQ (somatotropin) |
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Definition
Class: Growth Hormone (GH)
Indication: Children:
Treatment of growth failure due to inadequate endogenous growth hormone secretion (Genotropin®, Humatrope®, Norditropin®, Nutropin®, Nutropin AQ®, Omnitrope®, Saizen®, Tev-Tropin®)
Treatment of short stature associated with Turner syndrome (Genotropin®, Humatrope®, Norditropin®, Nutropin®, Nutropin AQ®, Omnitrope®)
Treatment of Prader-Willi syndrome (Genotropin®, Omnitrope®)
Treatment of growth failure associated with chronic renal insufficiency (CRI) up until the time of renal transplantation (Nutropin®, Nutropin AQ®)
Treatment of growth failure in children born small for gestational age who fail to manifest catch-up growth by 2 years of age (Genotropin®, Omnitrope®) or by 2-4 years of age (Humatrope®, Norditropin®)
Treatment of idiopathic short stature (nongrowth hormone-deficient short stature) defined by height standard deviation score (SDS) ≤-2.25 and growth rate not likely to attain normal adult height (Genotropin®, Humatrope®, Nutropin®, Nutropin AQ®, Omnitrope®)
Treatment of short stature or growth failure associated with short stature homeobox gene (SHOX) deficiency (Humatrope®)
Treatment of short stature associated with Noonan syndrome (Norditropin®)
Adults:
HIV patients with wasting or cachexia with concomitant antiviral therapy (Serostim®)
Replacement of endogenous growth hormone in patients with adult growth hormone deficiency who meet both of the following criteria (Genotropin®, Humatrope®, Norditropin®, Nutropin®, Nutropin AQ®, Omnitrope®, Saizen®):
Biochemical diagnosis of adult growth hormone deficiency by means of a subnormal response to a standard growth hormone stimulation test (peak growth hormone ≤5 mcg/L). Confirmatory testing may not be required in patients with congenital/genetic growth hormone deficiency or multiple pituitary hormone deficiencies due to organic diseases.
and
Adult-onset: Patients who have adult growth hormone deficiency whether alone or with multiple hormone deficiencies (hypopituitarism) as a result of pituitary disease, hypothalamic disease, surgery, radiation therapy, or trauma
or
Childhood-onset: Patients who were growth hormone deficient during childhood, confirmed as an adult before replacement therapy is initiated
Treatment of short-bowel syndrome (Zorbtive®)
Unlabeled:
Pediatric HIV patients with wasting/cachexia (Serostim®); HIV-associated adipose redistribution syndrome (HARS) (Serostim®)
MOA:
Somatropin is a purified polypeptide hormones of recombinant DNA origin; somatropin contains the identical sequence of amino acids found in human growth hormone; human growth hormone assists growth of linear bone, skeletal muscle, and organs by stimulating chondrocyte proliferation and differentiation, lipolysis, protein synthesis, and hepatic glucose output; stimulates erythropoietin which increases red blood cell mass; exerts both insulin-like and diabetogenic effects; enhances the transmucosal transport of water, electrolytes, and nutrients across the gut |
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Term
| Flonase (fluticasone nasal spray) |
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Definition
Class: Intranasal corticosteroid
Indication:
Flonase®: Management of seasonal and perennial allergic rhinitis and nonallergic rhinitis
MOA:
Fluticasone belongs to a group of corticosteroids which utilizes a fluorocarbothioate ester linkage at the 17 carbon position; extremely potent vasoconstrictive and anti-inflammatory activity |
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Term
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Definition
Class: Respiratory fluoroquinolone - antibiotic
Indication:
Treatment of mild-to-moderate community-acquired pneumonia, including multidrug-resistant Streptococcus pneumoniae (MDRSP); acute bacterial exacerbation of chronic bronchitis; acute bacterial rhinosinusitis (ABRS); complicated and uncomplicated skin and skin structure infections; complicated intra-abdominal infections
Unlabeled:
Treatment of Legionella pneumonia; treatment of mild-to-moderate community-acquired pneumonia (CAP), including multidrug-resistant Streptococcus pneumoniae (MDRSP) in adolescents with skeletal maturity; tuberculosis (second-line therapy)
MOA:
Moxifloxacin is a DNA gyrase inhibitor, and also inhibits topoisomerase IV. DNA gyrase (topoisomerase II) is an essential bacterial enzyme that maintains the superhelical structure of DNA. DNA gyrase is required for DNA replication and transcription, DNA repair, recombination, and transposition; inhibition is bactericidal. |
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Term
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Definition
Class: Antineoplastic agent; monoclonal antibody
Indication: Treatment of unresectable or metastatic melanoma
MOA:
Ipilimumab is a recombinant human IgG1 immunoglobulin monoclonal antibody which binds to the cytotoxic T-lymphocyte associated antigen 4 (CTLA-4). CTLA-4 is a down-regulator of T-cell activation pathways. Blocking CTLA-4 allows for enhanced T-cell activation and proliferation. In melanoma, ipilimumab may indirectly mediate T-cell immune responses against tumors. |
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Term
| Exforge (amlodipine/valsartan) |
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Definition
Class: Calcium channel blocker (dihydropyridine)/Angiotensin II receptor blocker (ARB)
Indication: treatment of hypertension
MOA: Amlodipine inhibits calcium ion from entering the “slow channels” or select voltage-sensitive areas of vascular smooth muscle and myocardium during depolarization, producing a relaxation of coronary vascular smooth muscle and coronary vasodilation; increases myocardial oxygen delivery in patients with vasospastic angina. Amlodipine directly acts on vascular smooth muscle to produce peripheral arterial vasodilation reducing peripheral vascular resistance and blood pressure.
Valsartan produces direct antagonism of the angiotensin II (AT2) receptors, unlike the ACE inhibitors. It displaces angiotensin II from the AT1 receptor and produces its blood pressure-lowering effects by antagonizing AT1-induced vasoconstriction, aldosterone release, catecholamine release, arginine vasopressin release, water intake, and hypertrophic responses. This action results in more efficient blockade of the cardiovascular effects of angiotensin II and fewer side effects than the ACE inhibitors. |
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Term
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Definition
Class: Dipeptidyl Peptidase IV (DPP-IV) Inhibitor - Antidiabetic Agent
Indication: Treatment of type 2 diabetes mellitus (noninsulin dependent, NIDDM) as an adjunct to diet and exercise as monotherapy or in combination therapy with other antidiabetic agents to improve glycemic control
MOA:
Saxagliptin inhibits dipeptidyl peptidase IV (DPP-IV) enzyme resulting in prolonged active incretin levels. Incretin hormones (eg, glucagon-like peptide-1 [GLP-1] and glucose-dependent insulinotropic polypeptide [GIP]) regulate glucose homeostasis by increasing insulin synthesis and release from pancreatic beta cells and decreasing glucagon secretion from pancreatic alpha cells. Decreased glucagon secretion results in decreased hepatic glucose production. Under normal physiologic circumstances, incretin hormones are released by the intestine throughout the day and levels are increased in response to a meal; incretin hormones are rapidly inactivated by the DPP-IV enzyme |
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Term
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Definition
Class: Taxane antineoplastic agent - antimicrotubular
Indication: Treatment of refractory (metastatic) or relapsed (within 6 months of adjuvant therapy) breast cancer; first-line treatment of locally advanced or metastatic nonsmall cell lung cancer (NSCLC) (in combination with carboplatin) in patients ineligible for curative surgery or radiation therapy
Unlabeled: Treatment of recurrent or persistent ovarian, fallopian tube, or primary peritoneal cancers; metastatic pancreatic cancer
MOA:
Albumin-bound paclitaxel nanoparticle formulation; paclitaxel promotes microtubule assembly by enhancing the action of tubulin dimers, stabilizing existing microtubules, and inhibiting their disassembly, interfering with the late G2 mitotic phase, and inhibiting cell replication. May also distort mitotic spindles, resulting in the breakage of chromosomes. Paclitaxel may also suppress cell proliferation and modulate immune response. |
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Term
| Vicodin, Lorcet, Lortab, Maxidone, Norco, Xodol, Zamicet, Zydone (hydrocodone/acetaminophen) |
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Definition
Class: Analgesic combination (opioid)
Indication: Relief of moderate-to-severe pain
MOA:
Hydrocodone, as with other opioid analgesics, blocks pain perception in the cerebral cortex by binding to specific receptor molecules (opiate receptors) within the neuronal membranes of synapses. This binding results in a decreased synaptic chemical transmission throughout the CNS thus inhibiting the flow of pain sensations into the higher centers. Mu and kappa are the two subtypes of the opiate receptor which hydrocodone binds to cause analgesia.
Acetaminophen inhibits the synthesis of prostaglandins in the CNS and peripherally blocks pain impulse generation; produces antipyresis from inhibition of hypothalamic heat-regulating center. |
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Term
| Synvisc-One (hylan G-F 20; hyaluronic acid) |
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Definition
Class: Antirheumatic, ophthalmic agent, skin and mucus membrane agent
Indication: Intra-articular injection: Treatment of pain in osteoarthritis in knee in patients who have failed nonpharmacologic treatment and simple analgesics (Euflexxa®, Hyalgan®, OrthoVisc®, Supartz®, Synvisc®, Synvisc-One®)
MOA:
Sodium hyaluronate is a biological polysaccharide which is distributed widely in the extracellular matrix of connective tissue in man (vitreous and aqueous humor of the eye, synovial fluid, skin, and umbilical cord). Sodium hyaluronate and its derivatives form a viscoelastic solution in water (at physiological pH and ionic strength) which makes it suitable for aqueous and vitreous humor in ophthalmic surgery, and functions as a tissue and/or joint lubricant which plays an important role in modulating the interactions between adjacent tissues. Intradermal injection may decrease the depth of facial wrinkles. In the topical management of wounds and ulcers, sodium hyaluronate protects the skin against friction and abrasion. |
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Term
| Wellbutrin XL (bupropion XL) |
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Definition
Class: Dopamine reuptake inhibitor - antidepressant; smoking cessation aid
Indication: Treatment of major depressive disorder, including seasonal affective disorder (SAD); adjunct in smoking cessation (Buproban®, Zyban®)
Unlabeled: Attention-deficit/hyperactivity disorder (ADHD); depression associated with bipolar disorder
MOA:
Aminoketone antidepressant structurally different from all other marketed antidepressants; like other antidepressants the mechanism of bupropion's activity is not fully understood. Bupropion is a relatively weak inhibitor of the neuronal uptake of norepinephrine and dopamine, and does not inhibit monoamine oxidase or the reuptake of serotonin. Metabolite inhibits the reuptake of norepinephrine. The primary mechanism of action is thought to be dopaminergic and/or noradrenergic. |
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Term
| Qvar (beclomethasone HFA) |
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Definition
Class: Inhaled corticosteroid
Indication: Maintenance and prophylactic treatment of asthma; includes those who require corticosteroids and those who may benefit from a dose reduction/elimination of systemically-administered corticosteroids. Not for relief of acute bronchospasm.
MOA:
Controls the rate of protein synthesis; depresses the migration of polymorphonuclear leukocytes, fibroblasts; reverses capillary permeability and lysosomal stabilization at the cellular level to prevent or control inflammation |
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Term
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Definition
Class: Antimigraine Agent; Serotonin 5-HT1B, 1D Receptor Agonist
Indication: Acute treatment of migraine with or without aura
MOA:
Selective agonist for serotonin (5-HT1B and 5-HT1D receptors) in cranial arteries; causes vasoconstriction and reduces sterile inflammation associated with antidromic neuronal transmission correlating with relief of migraine |
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Term
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Definition
Class: Vitamin D analog
Indication:
I.V.: Prevention and treatment of secondary hyperparathyroidism associated with stage 5 chronic kidney disease (CKD)
Oral: Prevention and treatment of secondary hyperparathyroidism associated with stage 3 and 4 CKD and stage 5 CKD patients on hemodialysis or peritoneal dialysis
MOA:
Decreased renal conversion of vitamin D to its primary active metabolite (1,25-hydroxyvitamin D) in chronic renal failure leads to reduced activation of vitamin D receptor (VDR), which subsequently removes inhibitory suppression of parathyroid hormone (PTH) release; increased serum PTH (secondary hyperparathyroidism) reduces calcium excretion and enhances bone resorption. Paricalcitol is a synthetic vitamin D analog which binds to and activates the VDR in kidney, parathyroid gland, intestine and bone, thus reducing PTH levels and improving calcium and phosphate homeostasis. |
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Term
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Definition
Class: Taxane Antineoplastic Agent - Antimicrotubular
Indication:
Taxotere: Treatment of breast cancer (locally-advanced/metastatic) after prior chemotherapy failure, or adjuvant treatment of operable node-positive); locally-advanced or metastatic nonsmall cell lung cancer (NSCLC); hormone refractory, metastatic prostate cancer; advanced gastric adenocarcinoma; locally-advanced squamous cell head and neck cancer
MOA:
Docetaxel promotes the assembly of microtubules from tubulin dimers, and inhibits the depolymerization of tubulin which stabilizes microtubules in the cell. This results in inhibition of DNA, RNA, and protein synthesis. Most activity occurs during the M phase of the cell cycle. |
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Term
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Definition
Class: glycopeptide antibiotic
Indication:
I.V.: Treatment of patients with infections caused by staphylococcal species and streptococcal species
Oral: Treatment of C. difficile-associated diarrhea and treatment of enterocolitis caused by Staphylococcus aureus (including methicillin-resistant strains)
Unlabeled: Bacterial endophthalmitis; treatment of infections caused by gram-positive organisms in patients who have serious allergies to beta-lactam agents; treatment of beta-lactam resistant gram-positive infections; surgical prophylaxis; treatment of prosthetic joint infection; group B streptococcus maternal use for neonatal prophylaxis
MOA:
Inhibits bacterial cell wall synthesis by blocking glycopeptide polymerization through binding tightly to D-alanyl-D-alanine portion of cell wall precursor |
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Term
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Definition
Class: Anticonvulsant
Indication:
Immediate release: Adjunctive therapy in the treatment of generalized seizures of Lennox-Gastaut syndrome, primary generalized tonic-clonic seizures, and partial seizures; conversion to monotherapy in patients with partial seizures who are receiving treatment with a single antiepileptic drug (AED) (specifically carbamazepine, phenytoin, phenobarbital, primidone, or valproic acid); maintenance treatment of bipolar I disorder
Extended release: Adjunctive therapy for primary generalized tonic-clonic seizures and partial seizures (with or without secondary generalization); conversion to monotherapy in patients with partial seizures who are receiving treatment with a single antiepileptic drug AED
MOA:
A triazine derivative which inhibits release of glutamate (an excitatory amino acid) and inhibits voltage-sensitive sodium channels, which stabilizes neuronal membranes. Lamotrigine has weak inhibitory effect on the 5-HT3 receptor; in vitro inhibits dihydrofolate reductase. |
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Term
| Menactra (Neisseria meningitidis polysaccharides 4mcg each of Group A, C, Y, and W-135, vaccine) |
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Definition
Class: Inactivated (bacterial) vaccine
Indication: Provide active immunization of children and adults against invasive meningococcal disease caused by N. meningitidis serogroups A, C, Y, and W-135.
The Advisory Committee on Immunization Practices (ACIP) (CDC, 62[2], 2013):
ACIP recommends routine vaccination of the following:
- Children and adolescents 11-18 years of age
- Persons ≥2 months of age who are at increased risk of meningococcal disease
- Persons (in all recommended age groups) at increased risk who are part of outbreaks caused by vaccine preventable serogroups
Those at increased risk of meningococcal disease include the following:
- Persons ≥2 months of age with medical conditions such as anatomical or functional asplenia or persistent compliment component deficiencies (eg, C5-C9, properdin, factor H, or factor D)
- Persons ≥9 months of age that travel to or reside in countries where meningococcal disease is hyperendemic or epidemic, especially if contact with the local population will be prolonged
- Unvaccinated or incompletely vaccinated first year college students living in residence halls
- Military recruits
- Microbiologists with occupational exposure
MOA:
Induces immunity against meningococcal disease via the formation of bactericidal antibodies directed toward the polysaccharide capsular components of Neisseria meningitidis serogroups A, C, Y and W-135. |
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Term
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Definition
Class: DNA Methylation inhibitor -Antineoplastic agent
Indication: Treatment of myelodysplastic syndrome (MDS)
Unlabeled: treatment of acute myelogenous leukemia (AML)
MOA:
Antineoplastic effects may be a result of azacitidine's ability to promote hypomethylation of DNA leading to direct toxicity of abnormal hematopoietic cells in the bone marrow. |
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Term
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Definition
Class: Antiviral agent
Indication: Treatment of cytomegalovirus (CMV) retinitis in patients with acquired immunodeficiency syndrome (AIDS); prevention of CMV disease in high-risk patients (donor CMV positive/recipient CMV negative) undergoing kidney, heart, or kidney/pancreas transplantation
MOA:
Valganciclovir is rapidly converted to ganciclovir in the body. The bioavailability of ganciclovir from valganciclovir is increased 10-fold compared to oral ganciclovir. A dose of 900 mg achieved systemic exposure of ganciclovir comparable to that achieved with the recommended doses of intravenous ganciclovir of 5 mg/kg. Ganciclovir is phosphorylated to a substrate which competitively inhibits the binding of deoxyguanosine triphosphate to DNA polymerase resulting in inhibition of viral DNA synthesis. |
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Term
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Definition
Class: Radiological/contrast media (nonionic, low osmolality) - iodinated contrast media
Indication:
Intrathecal: Myelography; contrast enhancement for computerized tomography
Intravascular: Angiocardiography, aortography, digital subtraction angiography, peripheral arteriography, excretory urography; contrast enhancement for computed tomographic imaging
Oral/body cavity: Arthrography, GI tract examination, hysterosalpingography, pancreatography, cholangiopancreatography, herniography, cystourethrography; enhanced computed tomography of the abdomen
MOA:
Opacification of vessels and anatomical structures in the path of flow of the contrast media which allows for radiographic visualization |
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Term
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Definition
Class: Antianginal agent - cardiovascular agent
Indication: Treatment of chronic angina
MOA:
Ranolazine exerts antianginal and anti-ischemic effects without changing hemodynamic parameters (heart rate or blood pressure). At therapeutic levels, ranolazine inhibits the late phase of the inward sodium channel (late INa) in ischemic cardiac myocytes during cardiac repolarization reducing intracellular sodium concentrations and thereby reducing calcium influx via Na+-Ca2+ exchange. Decreased intracellular calcium reduces ventricular tension and myocardial oxygen consumption. It is thought that ranolazine produces myocardial relaxation and reduces anginal symptoms through this mechanism although this is uncertain. At higher concentrations, ranolazine inhibits the rapid delayed rectifier potassium current (IKr) thus prolonging the ventricular action potential duration and subsequent prolongation of the QT interval. |
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