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| PHARMACOLOGY 0586 - Exam 1 |
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Definition
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ALPRAZOLAM (Xanax) |
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Definition
| Benzodiazepine … acts as agonist at Benzodiazepine receptor, a subunit of the GABA-A receptor, opens the channel … used for anti-anxiety, produces sedation, induces sleep at high levels, anesthetic at high doses, anticonvulsant, muscle relaxant … side FX include respiratory depression, drowsiness, abuse potential, abuse potential, tolerance may develop as well as dependence/withdrawal, and overdose potential ... Alprazolam undergoes rapid oral absorption, no active metabolites, medium-short halflife T1/2 = 12-15 hours |
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CHLORDIAZEPOXIDE (Librium) |
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| Benzodiazepine … acts as agonist at Benzodiazepine receptor, a subunit of the GABA-A receptor, opens the channel … used for anti-anxiety, produces sedation, induces sleep at high levels, anesthetic at high doses, anticonvulsant, muscle relaxant … Chlordiazepoxide sometimes used during ethanol withdrawal ... side FX include respiratory depression, drowsiness, abuse potential, abuse potential, tolerance may develop as well as dependence/withdrawal, and overdose potential ... Chlordiazepoxide produces active metabolites, T1/2 halflife = 15-40 hours |
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LORAZEPAM (Ativan) |
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| Benzodiazepine … acts as agonist at Benzodiazepine receptor, a subunit of the GABA-A receptor, opens the channel … used for anti-anxiety, produces sedation, induces sleep at high levels, anesthetic at high doses, anticonvulsant, muscle relaxant … side FX include respiratory depression, drowsiness, abuse potential, abuse potential, tolerance may develop as well as dependence/withdrawal, and overdose potential ... Lorazepam does not require active metabolites, medium-short T1/2 halflife = 10-20 hours |
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MIDAZOLAM (Versed) |
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Definition
| Benzodiazepine … acts as agonist at Benzodiazepine receptor, a subunit of the GABA-A receptor, opens the channel … used for anti-anxiety, produces sedation, induces sleep at high levels, anesthetic at high doses, anticonvulsant, muscle relaxant … when Midazolam is used in surgical anesthesia (one common use), the problem of respiratory depression can be significant ... other side FX drowsiness, abuse potential, tolerance may develop as well as dependence/withdrawal, and overdose potential |
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| Benzodiazepine … acts as agonist at Benzodiazepine receptor, a subunit of the GABA-A receptor, opens the channel … used for anti-anxiety, produces sedation, induces sleep at high levels, anesthetic at high doses, anticonvulsant, muscle relaxant … side FX include respiratory depression, drowsiness, abuse potential, tolerance may develop as well as dependence/withdrawal, overdose potential ... Oxazepam does not produce active metabolites, and has an intermediate duration of action (t1/2 = 10-20hrs |
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TEMAZEPAM (Restoril) |
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Definition
| Benzodiazepine … acts as agonist at Benzodiazepine receptor, a subunit of the GABA-A receptor, opens the channel … used for anti-anxiety, produces sedation, induces sleep at high levels, anesthetic at high doses, anticonvulsant, muscle relaxant … side FX include respiratory depression, drowsiness, abuse potential, abuse potential, tolerance may develop as well as dependence/withdrawal, and overdose potential ... Temazepam exhibits slow oral absorption, t1/2 halflife = 10-20 hours |
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TRIAZOLAM (Halcion) |
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Definition
| Benzodiazepine … acts as agonist at Benzodiazepine receptor, a subunit of the GABA-A receptor, opens the channel … used for anti-anxiety, produces sedation, induces sleep at high levels, anesthetic at high doses, anticonvulsant, muscle relaxant … "rebound anxiety" is especially problematic with this short-acting (t1/2 = 2-3hrs) benzodiazepine that can lead to vicious cycles of drug use and dependence ... other side FX include respiratory depression, drowsiness, abuse potential, tolerance may develop ... Triazolam does not require active metabolites, it exhibits rapid absorption, rapid onset of action, short duration of action |
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FLUMAZENIL (Romazicon) |
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Definition
| Benzodiazepine ANTAGONIST … reverses the sedative actions of benzodiazepines in sedative overdose … Flumazenil also administered post-op to surgical patients to wake them up after using anesthetics, administered by IV injection … acts rapidly with short duration of action B6 |
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BUTALBITAL (Fiorinal) |
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Definition
| Barbiturate … binds to Barbituate receptor subunit on GABA-A receptors, increases the duration of chloride channel opening … dose-dependant depressant effects on CNS, anti-anxiety, may see amnesia or hypnosis, coma, or respiratory depression, used in anesthesia ... Barbiturates in general are not used as much these days because of side FX and overdose potential |
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PENTOBARBITAL (Nembutal) |
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Definition
| Barbiturate … binds to Barbituate receptor subunit on GABA-A receptors, increases the duration of chloride channel opening … dose-dependant depressant effects on CNS, anti-anxiety, may see amnesia or hypnosis, coma, or respiratory depression, used in anesthesia ... Barbiturates in general are not used as much these days because of side FX and overdose potential |
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Definition
| Barbiturate … binds to Barbituate receptor subunit on GABA-A receptors, increases the duration of chloride channel opening … dose-dependant depressant effects on CNS, anti-anxiety, may see amnesia or hypnosis, coma, or respiratory depression, used in anesthesia ... Barbiturates in general are not used as much these days because of side FX and overdose potential ... Phenobarbital is a long-acting barbituate used as an anticonvulsant |
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Definition
| Barbiturate … binds to Barbituate receptor subunit on GABA-A receptors, increases the duration of chloride channel opening … dose-dependant depressant effects on CNS, anti-anxiety, may see amnesia or hypnosis, coma, or respiratory depression, used in anesthesia ... Barbiturates in general are not used as much these days because of side FX and overdose potential ... Thiopental is an ultra short-acting used in anesthesia |
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BACLOFEN (Lioresal) |
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Definition
Baclofen is an analog of GABA that acts as an agonist at certain types of GABA receptors; centrally-acting muscle relaxant
Used in treating spasticity resulting from multiple sclerosis, spinal cord injuries, etc.
Main adverse side FX involve CNS depression (sedation, drowsiness, ataxia, muscle weakness) or euphoria or hallucinations |
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CYCLOBENZAPRINE (Flexeril) |
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Definition
| Cyclobenzaprene is structurally related to the tricyclic antidepressants ... acts at the brainstem to inhibit both gamma and alpha motor systems ... used in treating muscle spasms of local origin (strains, pulls) ... main side FX are CNS depression (sedation, drowsiness, loss of coordination) |
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DIAZEPAM (Valium) |
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Definition
| Muscle Relaxant, centrally-acting … diazepam is the gold standard prototype drug used for muscle spasticity (e.g. back spasms), also anxiolytic, anticonvulsant ... agonist at GABA benzodiazepine receptors, produces graded dose-dependent CNS depression ... diazepam is one of the longest-acting benzodiazepines (t1/2 = 20-70hrs), so can be prone to "hangover effect" if discontinued abruptly |
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METAXALONE (Skelaxin) |
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Definition
| Muscle Relaxant, centrally-acting … used for muscle spasticity (e.g. back spasms), diazepam is the gold standard for this … Metaxalone is getting more and more popular |
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TIZANIDINE (Zanaflex) |
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Definition
| Muscle Relaxant, centrally-acting … used for muscle spasticity (e.g. back spasms) Tizanidine acts as an Alpha-2 adrenergic receptor agonist, much like Clonidine ... can cause hypotension; very sedating |
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Definition
| Non-barbiturate, Non-benzodiazepine Anxiolytic & Sedative Hypnotic … as a hypnotic, alcohols decrease sleep latency (less time to fall asleep) but they also decrease quality of sleep (fewer and smaller REM sleep cycles), newer drugs are better at this than alcohol |
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BUSPIRONE (Buspar) |
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| Non-barbiturate, Non-benzodiazepine Anxiolytic & Sedative Hypnotic … this drug is distinct from barbituates and benzodiazepines in its chemical structure, but it shares a mechanism of action that is very similar to benzodiazepines … Buspirone is used as sedative-hypnotic for sleep disorders ... Buspirone is one of the newer anti-anxiety drugs, causing far less psychomotor impairment ... Buspirone has a slow onset of action and relieves anxiety without marked sedative or hypnotic or euphoric effects, thus lower abuse potential ... Buspirone patients exhibit no rebound anxiety or withdrawal symptoms ... but some side effects such as non-specific chest pain, tachycardia, palpitations, dizziness, nervousness, tinnitus, GI distress may occur |
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ESZOPICLONE (Lunesta) |
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Definition
| Non-barbiturate, Non-benzodiazepine Anxiolytic & Sedative Hypnotic … Eszoplicone is one of the newer hypnotics on the market ... this drug is distinct from barbituates and benzodiazepines in its chemical structure, but it shares a mechanism of action that is very similar to benzodiazepines … Eszopiclone doesn't have as much of an anti-anxiety effect ... additive side FX with CNS depressants |
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GAMMAHYDROXYBUTYRATE (GHB) |
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Definition
| Non-barbiturate, Non-benzodiazepine Anxiolytic & Sedative Hypnotic … this drug is distinct from barbituates and benzodiazepines in its chemical structure, but it shares a mechanism of action that is very similar to benzodiazepines … GHB commonly referred to as the "date rape drug" ... does not exhibit much of an anti-anxiety effect |
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Definition
| Melatonin is a hormone produced by the pineal gland, available as an o-t-c sleep aid for several years ... melatonin is NOT a barbiturate and NOT a benzodiazepine, although its MofA does share similarities (note that Ramelteon is related, acts as agonist at melatonin receptors) … melatonin receptors are thought to be involved in maintaining circadian rhythms underlying the sleep-wake cycle; melatonin advances the phase of sleep if taken a couple hours before sleep ... few side FX observed |
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RAMELTEON (Rozerem) |
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Definition
| Non-barbiturate, Non-benzodiazepine Anxiolytic & Sedative Hypnotic … Ramelteon is a Melatonin receptor agonist ... this drug is distinct from barbituates and benzodiazepines in its chemical structure, but it shares a mechanism of action that is very similar to benzodiazepines … Ramelteon used specifically for pt's having trouble falling asleep, it reduces sleep latency (less time to fall asleep) with no effects on quality of sleep and no rebound insomnia |
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ZOLPIDEM (Ambien) |
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Definition
| Non-barbiturate, Non-benzodiazepine Anxiolytic & Sedative Hypnotic … Zolpidem is one of the newer hympnotics and is absorbed rapidly into the bloodstream ... this drug is distinct from barbituates and benzodiazepines in its chemical structure, but it shares a mechanism of action that is very similar to benzodiazepines … additive side FX with CNS depressants |
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ZALEPLON (Sonata) |
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Definition
| Non-barbiturate, Non-benzodiazepine Anxiolytic & Sedative Hypnotic … Zaleplon is one of the newer hypnotics and is absorbed rapidly in the bloodstream ... this drug is distinct from barbituates and benzodiazepines in its chemical structure, but it shares a mechanism of action that is very similar to benzodiazepines … additive side FX with CNS depressants |
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DISULFIRAM (Antibuse) |
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Definition
| Alcoholism Treatment Drug … inhibits aldehyde dehydrogenase, and so acetaldehyde accumulates = patient gets really sick, creates disincentive to drink … disulfiram can be hepatotoxic, which limits its use; also adherence to medication is low, evidence suggests low effectiveness b/c this |
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ACAMPROSATE (Campral) |
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Definition
| Alcoholism Treatment Drug … can decrease craving for alcohol, help maintain abstinence in recovering alcoholics … MofA may involve GABA and/or glutamate receptors ... a newer drug with less potential for hepatotoxicity, so often used in patients with liver problems; naltrexone and acomprosate together may be more effective than either drug alone … main side FX are GI diarrhea, anxiety, insomnia and depression |
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NALTREXONE (ReVIA) |
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Definition
| Alcoholism Treatment Drug … long-acting opioid antagonist, reported to reduce alcohol cravings in alcohoolics … but has significant tendency to cause hepatotoxicity, the combination of naltrexone plus disulfiram should be avoided for this reason |
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Chloride Channel Complex |
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Definition
| with Benzodiazepine receptor, Barbiturate receptor, GABA-A receptor … benzodiazepines and barbiturates facilitate or enhance the effects of the inhibitory neurotransmitter GABA … GABA causes the chloride channel to open, and the subsequent influx of (Cl-) into the cell hyperpolarizes the membrane and decreases neuronal firing |
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PREDNISONE (Deltasone) |
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| Corticosteroid, Immunosuppressive … inhibit phospholipase A2, inhibits COX-2, cause vasoconstriction, inhibit complement activity, reduce cytokine production, reduce antibody production, reduce antigen response, affects concentration and dsitribution of peripheral leukocytes (increases PMNs, but decreases T/B lymphocytes)... side FX unusual with short-term use, but long-term use w/ risk of iatrogenic Cushing's syndrome ... also risk of GI ulcers, increased infections, obesity, glucose intolerance |
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METHYLPREDNISOLONE (Medrol) |
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Definition
| Corticosteroid, Immunosuppressive … inhibit phospholipase A2, inhibits COX-2, cause vasoconstriction, inhibit complement activity, reduce cytokine production, reduce antibody production, reduce antigen response, affects concentration and dsitribution of peripheral leukocytes (increases PMNs, but decreases T/B lymphocytes) ... side FX unusual with short-term use, but long-term use w/ risk of iatrogenic Cushing's syndrome ... also risk of GI ulcers, increased infections, obesity, glucose intolerance |
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AZATHIOPRINE (Imuran) |
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Definition
| Azathioprine is an immunosuppressive, used to treat severe progressive RA in adults; also for kidney transplant rejection ... MofA is not well known, suppresses both B and T cells ... main side FX are GI nausea/vomiting, leukopenia/thrombocytopenia, fetal harm, carcinogenic, and constant risk of serious infections |
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METHOTREXATE (Rheumatrex) |
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Definition
| Antiproliferative Agent (T and B cells), Cytotoxic … *important drug* … methotrexate used in treatment of adult rheumatoid arthritis and juvenile RA (drug of choice) also some anti-cancer … inhibits dihyrdofolic acid reductase enzyme, affecting DNA synthesis and repair and cellular replication ... major side FX are GI in the short-term (nausea, malaise, chills, ulcers, leukopenia) as well as hepatotoxicity and nephrotoxicity with long-term use, obstructive pulmonary disease occasionally |
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CYCLOPHOSPHAMIDE (Cytoxan) |
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| Cyclophosphamide = nitrogen mustard ... potent anti-inflammatory and immunosuppressive effects as a result of direct cytotoxicity on (T and B lymphocytes); it can inhibit established immune responses ... only used for severe rheumatologic conditions (Wgener's, severe RA, systemic lupus) or for malignant disease (lymphomas, multiple myelomas, breast/ovarian cancer) ... cyclophosphamide is an "alkylating agent" that requires metabolic activation by cytochrome P450s; inhibits nucleotide synthesis ... with significant immunosuppression, sometimes fatal infections may develop ... other side FX are GI, blood toxicity, genitourinal, frequent alopecia |
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CYCLOSPORINE (Sandimmune) |
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| Immunosuppressant, T cell suppressant … inhibits Signal 1 (calineurin phosphatases), which inhibits release of IL-2 and activation of T cells … structurally, it's a cyclic peptide; gets metabolized by P-450 3A enzymes in the liver … side FX include GI ulcers and CV hypertension and may cause fetal harm; but main side FX is renal/nephrotoxicity, interstitial fibrosis ... Cyclosporine mainly used for allogenic transplants (prevent rejection) of kidney and liver and heart, taken w/ corticosteroids; also used for severe, active rheumatoid arthritis; also used for psoriasis |
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MYCOPHENOLATE MOFETIL (Cellcept) |
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Definition
| an Immunosuppressant (T cell suppressant) Mycophenolate Mofetil is used along with cyclosporine and corticosteroids in the prophylaxis of organ rejection in patients receiving renal, hepatic or cardiac transplants ... how? mycophenolate hydrolyzed to form MPA, a potent inhibitor of IMP dehydrogenase, inhibiting the DNA synthesis of guanosine, affects cell cycle (S phase); inhibits Signal 3; inhibits proliferative response of T/B lymphocytes, also suppresses antibody formation ... side FX include GI upset, leukopenia, infections |
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MUROMONAB-CD3 (Orthoclone OKT3) |
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Definition
| an Immunosuppressant (T cell suppressant) used to minimize allograft rejection of kidney/liver/pancreas/heart transplants ... a murine monoclonal antibody (IgG) that blocks function of TCR(CD3) of human T lymphocytes; blocks Signal 1 in T cells; CD3+ T cells are removed from circulation within minutes after IV administration of Muromonab-CD3 … side FX if patient has hypersentivity to murine products (raised in mice) |
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LYMPHOCYTE IMMUNE GLOBULIN (Atgam) |
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| Immunosuppressant, T cell suppressant … obtained from horses immunized with human thymus lymphocytes; selectively reduces number of T cells in blood, as well as spleen and lymph nodes … Lymphocyte Immune Globulin used in renal transplant allograft rejection ... watch for equine hypersensitivity, avoid in pregnancy, side FX of leukopenia, infections, |
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DACLIZUMAB (Zenepax) |
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Definition
Immunosuppressant (T cell suppressant)
Daclizumab is used as part of immunospressive regimen (w/ cyclosporine and corticosteroids) in minimizing allograft rejection in renal and cardiac transplants ... humanized IgG1 monoclonal antibody that binds IL-2, blocks Signal 3, inhibits IL-2-mediated activation of T lymphocytes ... side FX mostly GI disorders of constipation or nausea or diarrhea, others minor |
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RH0 IMMUNE GLOBULIN (RhoGam) |
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| Antibody Immunosuppressive … used to prevent Rho hemolytic disease of the newborn, where a pregnant Rho(-) woman generates a response against a Rho(+) fetus ... so in order to suppress that immune response, we take human plasma obtained from donors immunized with high levels of Rho antibodies, then give it to the mother (within 72 hours after birth) to prevent hypersensitivity reaction |
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IMMUNE GLOBULIN (Gamimune) |
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| Replacement Therapy (immuno) agent … antibody preparation, with a broad spectrum of IgG antibodies, prepared from donors; affects Signal 1, like most antibodies … Immune Globulin most frequently used as replacement therapy for hypogammaglobulinemia; also used for prevention of acute infection in HIV kids; treat thrombocytopenic purpura and systemic/local infections in bone marrow transplant patients, Guillain-Barre syndrome (autoimmune disease) ... side FX include history of allergic response and possibility of blood-borne pathogens (human IV plasma) |
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INTERFERON BETA-1b (Betaseron) |
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Definition
| Immunomodulator … interferons are a family of naturally occurring proteins/glycoproteins; binding of IFN-beta to receptor initiates complex cascade, producing biologically active products; has antiproliferative and immunoregulatory activities … IFN-beta used in ambulatory patients with relapse-remitting MS multiple sclerosis attacks ... serious side FX include depression and suicidal ideation |
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INTERFERON GAMMA (Actimmune) |
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| Interferon-gamma fights infections ... highly purified protein has potent phagocyte-activating effects including generation of toxic oxygen metabolites within phagocytes capable of intracellular killing microbugs ... used to reduce frequency/severity of infection in CGD ... adverse reactions to interferon-gamma use are typically "flu-like" (fever, headache, chills, fatigue) |
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| What are the four different kinds of drug allergy (hypersensitivity type reactions)? |
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Definition
| Type I = anaphylactic; immediate hypersensitivity … mediated by IgE; lymphocyte becomes sensitized upon re-exposure, the drug becomes cross-linked, and antibodies generated; IgE is fixed to tissue mast cells and basophils … antagonists include prednisone, epi ___ Type II = cytotoxic ... involves IgG/IgM, targets cells in circulatory system ... treat with drug abstinence and immunosuppressive corticosteroids ____ Type III = serum sickness (Arthus) reactions ... involves IgM/IgG, not IgE, which generate drug-antibody complexes, deposit in blood vessel walls, activate complement, PMNs can aggregate and invade, hemorrage, lesions ... treat with drug abstince and immunosuppressive corticosteroids ____ Type IV = cell-mediated (delayed) ... mediated by sensitized T lymphocytes and macrophages (so no PMNs), see inflammatory reaction, contact dermatitis ... treat with drug abstinence, administer corticosteroids |
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Definition
| Antiarthritic, NSAID … irreversibly inhibits platelet COX, antiinflammatory and antiplatelet effects … asprin used to prevent ischemic attacks, for unstable angina, for coronary thrombosis w/ MI, antiarthritic … main side FX are GI upset, ulcers, hepatotoxicity, asthma, rashes; contraindicated with hemophiliacs |
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CELECOXIB (Celebrex) |
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Definition
| Antiarthritic, NSAID … selective COX-2 inhibitor … shown to have no impact on platelet aggregation; associated with fewer ulcers; but may cause of renal toxicities and less cardioprotective effect (association with CV thrombosis resulted in withdrawal from the market) |
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ETODOLAC (Lodine) |
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Definition
| Antiarthritic, NSAID … nonselective COX inhibitor, antiinflammatory with an intermediate halflife |
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IBUPROFEN (Advil, Motrin) |
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Definition
| Antiarthritic, NSAID … phenylpropionic acid derivative with analgesic but no antiinflammatory effects … ibuprofen used in dustus arteriosus and osteoarthritis; rare hematologic effects include agranulocytosis and aplastic anemia |
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INDOMETHACIN (Indocin) |
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Definition
| Antiarthritic, NSAID … indole derivative, a nonselective COX inhibitor … was particularly popular for gout and ankylosing spondylitis, and to accelerate closure of patent ductus arteriosus … side FX of GI upset, headache, dizziness, confusion and depression |
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KETOROLAC (Toradol) |
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Definition
| Antiarthritic, NSAID … systemically used as an analgesic not as an antiinflammatory, ketorolac has been used successfully to replace morphine; most often given intramuscularly or IV |
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NAPROXEN (Aleve, Anaprox) |
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Definition
| Antiarthritic, NSAID … naphthylpropionic acid derivative … naproxen is effective for the usual rheumatological indications and is available in a slow-release formulation … side FX of upper GI bleeding in low occurrence, rare pneumonitis; common NSAID-associated adverse effects |
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TOLMETIN (Tolectin) |
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Definition
| Antiarthritic, NSAID … nonselective COX inhibitor, with a short halflife (1-2 hours) and is not often used; efficacy and toxicity profiles are similar to those of other NSAIDs; except its ineffective with gout, and may cause thrombocytopenic purpura |
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HYDROXYCHLOROQUINE SULFATE (Plaquenil) |
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Definition
| Hydroxychloroquine is a Disease Modifying Anti-Rheumatic Drugs (DMARDs), second most commonly used DMARD ... used as second-line treatment for patients with mild/moderate RA who are refractory to NSAID therapy; also anti-lupus; also anti-malarial … inexpensive drug, but needs to accumulate for 3-6 months before benefits, commonly used with methotrexate ... precise MofA unknown ... side FX are infrequent, but most serious is retinal toxicity w/ possibility of blindness, other side FX mild GI or dermatologic |
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METHOTREXATE (Rheumatrex) |
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Definition
| Disease Modifying Anti-Rheumatic Drugs (DMARDs), NON-BIOLOGICAL … currently favored by most rheumatologists because of rapid response (1-2 months), high response rate, and sustained efficacy … indicated for treatment of severe RA, unresponsive to NSAID therapy ... may need folic acid/folate supplements ... most common and effective DMARD combination in the US is methotrexate w/ hydroxychloroquine and sulfasalazine |
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SULFASALZINE (Azulfidine) |
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Definition
| Disease Modifying Anti-Rheumatic Drugs (DMARDs), NON-BIOLOGICAL … split in colon by intestinal bacteria ... sulfasalzine effective in long-term management of severe RA, an efficacy similar to gold and penicillamine; used in conjunction with methotrexate and hydroxychloroquine; inhibit macrophage phagocytosis, inhibit lysosomal enzyme release ... slow/fast metabolizers issue = more side FX in slow metabolizers, as drug accumulates |
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LEFLUNOMIDE (Arava) |
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Definition
| Disease Modifying Anti-Rheumatic Drugs (DMARDs), NON-BIOLOGICAL …. Pyrimidine synthesis inhibitor with antiproliferative activity and antiinflammatory effect … inhibits T cell proliferation and production of autoantibodies by B cells … leflunomide is as effective as methotrexate in treating rheumatoid arthritis, including inhibition of bony damage ... main side FX of GI diarrhea, elevation of liver enzymes, increased blood pressure, weight gain, dermatologic alopecia, contraindicated in pregnancy |
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PENICILLAMINE (Cuprimine, Depen) |
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Definition
| Disease Modifying Anti-Rheumatic Drugs (DMARDs), NON-BIOLOGICAL … lowers IgM rheumatoid factor; depresses T cell but not B cell activity … exact MofA is unknown … Penicillamine used for severe RA unresponsive to methotrexate, gold and hydroxychloroquine; Wilson's Disease ... high incidence of adverse reactions, some of which are potentially fatal; hypersensitivity, GI pain and upset, renal proteinuria and/or hematuria may progress to nephrotic syndrome, fatalities reported as a result of thrombocytopenia, agranulocytosis, aplastic anemia and sideroblastic anemia |
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AUROTHIOGLUCOSE (Solganal) |
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Definition
| Disease Modifying Anti-Rheumatic Drugs (DMARDs), Gold compound (50% gold) … gold compounds suppress but do not cure arthritis … Aurothioglucose decrease concentration of rheumatoid factor and IgG, decrease synovial inflammation, retard bone/cartilage destruction, inhibit phagocytosis and lysosomal enzyme release of macrophages ... therapeutic FX slowly (3-6 months), used for methotrexate intolerance in early RA and juvenile RA ... side FX are mainly GI (diarrhea) or dermatologic (dermatitis) |
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GOLD SODIUM THIOMALATE (Myochrysine) |
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Definition
| Disease Modifying Anti-Rheumatic Drugs (DMARDs), Gold compound (50% gold) … gold compounds suppress but do not cure arthritis … Gold Sodium Thiomalate decrease concentration of rheumatoid factor and IgG, decrease synovial inflammation, retard bone/cartilage destruction, inhibit phagocytosis and lysosomal enzyme release of macrophages ... therapeutic FX slowly (3-6 months), used for methotrexate intolerance in early RA and juvenile RA ... side FX are mainly GI (diarrhea) or dermatologic (dermatitis) |
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AURANOFIN (Ridaura) |
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Definition
| Disease Modifying Anti-Rheumatic Drugs (DMARDs), Gold compound (29% gold) … gold compounds suppress but do not cure arthritis … Auranofin decrease concentration of rheumatoid factor and IgG, decrease synovial inflammation, retard bone/cartilage destruction, inhibit phagocytosis and lysosomal enzyme release of macrophages ... therapeutic FX slowly (3-6 months), used for methotrexate intolerance in adults with active RA ... Auranofin causes fewer side FX; mainly GI (diarrhea) or dermatologic (dermatitis) |
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ETANERCEPT (Enbrel) |
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Definition
| Disease Modifying Anti-Rheumatic Drugs (DMARDs), BIOLOGIC … anticytokine agent, etanercept is a dimeric fusion protein that links to human TNF-alpha receptor, rendering TNF cytokines inactive ... etanercept used in combination with methotrexate for decreasing TNF reduces signs and symptoms of moderate-severe active RA, also for juvenile RA ... risk of serious infections and sepsis (TB, fungals), may result in fatalities |
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INFLIXIMAB (Remicade) |
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Definition
| Disease Modifying Anti-Rheumatic Drugs (DMARDs), BIOLOGIC … anticytokine agent, infliximab is a chimeric IgG1 monoclonal antibody prep (human-murine); infliximab more specific to TNF-alpha than TNF-beta … infliximab reduces infiltration of inflammatory cells and TNF-alpha production in inflamed areas ... infliximab used in combination with methotrexate for reducing signs and symptoms of moderate-severe active RA, and for Crohn's disease |
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INFLIXIMAB and ETANERCEPT immunoglobulin binding complex |
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CHLORPROMAZINE (Throrazine) |
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Definition
| Antipsychotic, Phenothiazine … *the prototype antipsychotic* … drug used in the treatment of schizophrenia, alleviation of psychotic symptoms ... decreased interest in environment, some sedative effect early in therapy, some antiemetic with some control of nausea/vomiting, some poikilothermic effects loss of body temp control, anticholinergic effects like dry mouth and constipation, some antihistaminic action ... all antipsychotics have cardiovascular effects (postural hypotension, tachycardia) that can prevent their use, some sexual dysfunction in males, weight gain is common ... Chlorpromazine is unpleasant to take, produces dysphoria; idiosyncratic and allergic reactions can be serious ... neurological side effects (extrapyramidal motor symptoms) may be severe including (1) acute distonia, bizarre muscle spasms; (2) akathisia, motor restlessness; (3) Parkinsonism, tremor and muscular rigidity; (4) neuroleptic malignant syndrome of severe muscle rigidity, hyperthermia, stupor; (5) tardive dyskinesia, involuntary movements of lip/jaw/tongue ... MofA of these drugs is not well understood, but may involve inhibition of dopamine receptors |
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Term
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FLUPHENAZINE (Prolixin, Prolixin Decanoate) |
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Definition
| Antipsychotic, Phenothiazine … drug used in the treatment of schizophrenia, alleviation of psychotic symptoms; fluphenazine is more potent and less sedating than chlorpromazine, but increased extrapyramidal motor problems ... decreased interest in environment, some sedative effect early in therapy, some antiemetic with some control of nausea/vomiting, some poikilothermic effects loss of body temp control, anticholinergic effects like dry mouth and constipation, some antihistaminic action ... all antipsychotics have cardiovascular effects (postural hypotension, tachycardia) that can prevent their use, some sexual dysfunction in males, weight gain is common ... Fluphenazine is unpleasant to take, produces dysphoria; idiosyncratic and allergic reactions can be serious; its chemical structure means that long-acting forms (decanoate and enanthate) can be given by depot injection every 3-4 weeks ... neurological side effects (extrapyramidal motor symptoms) may be severe including (1) acute distonia, bizarre muscle spasms; (2) akathisia, motor restlessness; (3) Parkinsonism, tremor and muscular rigidity; (4) neuroleptic malignant syndrome of severe muscle rigidity, hyperthermia, stupor; (5) tardive dyskinesia, involuntary movements of lip/jaw/tongue ... MofA of these drugs is not well understood, but may involve inhibition of dopamine receptors |
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Term
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PROCHLORPERAZINE (Compazine) |
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Definition
| Antipsychotic drug similar to trifluoperazine but is commonly used as an antiemetic ... alleviation of psychotic symptoms; more potent and less sedating than chlorpromazine, but increased extrapyramidal motor problems ... otherwise, actions and uses and toxicities characteristic of first-generation antipsychotics (chlorpromazine being the prototype) |
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Term
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TRIFLUOPERAZINE (Stelazine, Suprazine) |
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Definition
| Antipsychotic, Phenothiazine … drug used in the treatment of schizophrenia, alleviation of psychotic symptoms ... trifluoperazine is more potent and less sedating than chlorpromazine, but increased extrapyramidal motor problems ... decreased interest in environment, some sedative effect early in therapy, some antiemetic with some control of nausea/vomiting (common use), some poikilothermic effects loss of body temp control, anticholinergic effects like dry mouth and constipation, some antihistaminic action ... all antipsychotics have cardiovascular effects (postural hypotension, tachycardia) that can prevent their use, some sexual dysfunction in males, weight gain is common ... Trifluoperazine is unpleasant to take, produces dysphoria; idiosyncratic and allergic reactions can be serious ... neurological side effects (extrapyramidal motor symptoms) may be severe including (1) acute distonia, bizarre muscle spasms; (2) akathisia, motor restlessness; (3) Parkinsonism, tremor and muscular rigidity; (4) neuroleptic malignant syndrome of severe muscle rigidity, hyperthermia, stupor; (5) tardive dyskinesia, involuntary movements of lip/jaw/tongue ... MofA of these drugs is not well understood, but may involve inhibition of dopamine receptors |
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Term
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HALOPERIDOL (Haldol, Haldol Decanoate) |
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Definition
| Antipsychotic, Phenothiazine … drug used in the treatment of schizophrenia, alleviation of psychotic symptoms; **most widely used** of the 1st generation drugs ... Haloperidol has less anticholinergic activity and is less sedating than chlorpromazine, but increased extrapyramidal motor problems ... decreased interest in environment, some sedative effect early in therapy, some antiemetic with some control of nausea/vomiting (common use), some poikilothermic effects loss of body temp control, anticholinergic effects like dry mouth and constipation, some antihistaminic action ... all antipsychotics have cardiovascular effects (postural hypotension, tachycardia) that can prevent their use, some sexual dysfunction in males, weight gain is common ... Haloperidol is unpleasant to take, produces dysphoria; idiosyncratic and allergic reactions can be serious ... its structure means that it is available in long-acting form (haldol decanoate) ... neurological side effects (extrapyramidal motor symptoms) may be severe including (1) acute distonia, bizarre muscle spasms; (2) akathisia, motor restlessness; (3) Parkinsonism, tremor and muscular rigidity; (4) neuroleptic malignant syndrome of severe muscle rigidity, hyperthermia, stupor; (5) tardive dyskinesia, involuntary movements of lip/jaw/tongue ... MofA of these drugs is not well understood, but may involve inhibition of dopamine receptors |
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Term
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CLOZAPINE (Clozaril) |
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Definition
| Antipsychotic, "Second Generation" or "Atypical" … a "rich man's drug for a poor man's disease"; generally regarded as the most efficacious antipsychotic, may preferentially block mesolimbic dopamine receptors (D4), also blocks 5-HT2, also anticholinergic … demonstrates very few extrapyramidal motor problems, unlike other antipsychotics ... also targets "negative symptoms" of schizophrenia, such as social withdrawal ... Clozapine has potential for causing granulocytopenia, agranulocytosis (towards anemia), and seizures, so close monitoring of bloodwork is necessary, an expensive drug ... causes weight gain and hyperglycemia similar to Type II diabetes (this can be transformative!) |
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Term
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OLANZAPINE (Zyprexa) |
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Definition
| Antipsychotic, "Second Generation" or "Atypical" … alleviation of psychotic symptoms, may preferentially block mesolimbic dopamine receptors (D4), also blocks 5-HT2, also anticholinergic … an analog of clozapine that is generally safer in terms of blood toxicity (granulocytopenia), but may be more likely to cause extrapyramidal motor FX (acute distonia, tardive dyskinesia), although still far less likely than older generation antipsychotics ... Olanzapine also targets "negative symptoms" of schizophrenia, such as social withdrawal ... causes weight gain and hyperglycemia similar to Type II diabetes (this can be transformative!) |
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Term
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RISPERIDONE (Risperdal) |
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Definition
| Antipsychotic, "Second Generation" or "Atypical" … newer drug approved in the 1990s, now one of the most widely used, available in a depot formulation for injection every 2-4 weeks ... alleviation of psychotic symptoms; blocks both dopamine and serotonin receptors … an analog of clozapine that is generally safer in terms of blood toxicity (granulocytopenia), but may be more likely to cause extrapyramidal motor FX (acute distonia, tardive dyskinesia), although still far less likely than older generation antipsychotics ... also targets "negative symptoms" of schizophrenia, such as social withdrawal ... Risperidone causes weight gain and hyperglycemia similar to Type II diabetes (this can be transformative!) |
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Term
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ARIPIPRAZOLE (Abilify) |
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Definition
| Antipsychotic, "Second Generation" or "Atypical" … *Abilify!* … approved in 2003 for mania and refractory depression, when patient is not responding to drugs … novel MofA = acts as a partial agonist/antagonist at D2 and 5-HT1a receptors … effective against positive and negative symptoms of schizophrenia, also approved for mania ... aripiprazole may be less effective than clozapine or other 2nd generation antipsychotics, but it has less tendency for weight gain and hyperglycemia (Type II diabetes) |
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Term
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QUETIAPINE (Seroquel) |
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Definition
| Antipsychotic, "Second Generation" or "Atypical" newer drug approved in late 1990s for alleviation of psychotic symptoms … similar to clozapine, preferentially blocks mesolimbic dopamine receptors (D4), and also 5-HT2 receptors, also strong anticholinergic ... Quetiapine effective against both positive and negative symptoms of schizophrenia; very low tendency to cause extrapyramidal side effects; does not seem to cause blood toxicity (no agranulocytosis) ... drug is fairly expensive, and may be less efficacious than other 2nd generation antipsychotics, but comes with fewer metabolic complications (less weight gain) |
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Term
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ZIPRASIDONE (Geodon) |
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Definition
| Antipsychotic, "Second Generation" or "Atypical" newer drug approved in late 1990s for alleviation of psychotic symptoms … similar to clozapine, preferentially blocks mesolimbic dopamine receptors (D4), and also 5-HT2 receptors, also strong anticholinergic ... Ziprasidone effective against both positive and negative symptoms of schizophrenia; very low tendency to cause extrapyramidal side effects; does not seem to cause blood toxicity (no agranulocytosis) ... drug is fairly expensive, and may be less efficacious than other 2nd generation antipsychotics, but comes with fewer metabolic complications (less weight gain) |
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Term
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Postsynatptic dopamine blockade |
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Definition
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Term
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LYSERGIC and DIETHYLAMIDE (LSD) |
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Definition
| Hallucinogen, Indole … LSD is extremely potent, typical dose is 25-500micro-g's; can be formulated into papers or oral sugar tablets, may interfere with serotonin receptors … sympathomimetic FX include pupil dilation, increased BP, tachycardia, piloerection, hyperflexia, tremors, increase in body temp; other somatic FX include dizziness, weakness, paresthesias, nausea; subjective psychic changes may include anxiety, euphoria, giddiness, emotional lability; hallucinogenic FX develop more slowly, visual disturbances, depersonalized "out of body" experience, difficulty differentiating reality, panic, psychosis ... the drug itself is not all that toxic, it's behavior; signs of a "bad trip" are similar, panic, fear, anxiety; tolerance does develop ... controversial use in treatment of alcoholism and drug addiction |
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Term
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PSILOCYBIN and PSILOCIN |
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Definition
| Hallucinogen, Indole … hallucinogenic mushrooms … sympathomimetic FX include pupil dilation, increased BP, tachycardia, piloerection, hyperflexia, tremors, increase in body temp; other somatic FX include dizziness, weakness, paresthesias (tingling/burning), nausea; subjective psychic changes may include anxiety, euphoria, giddiness, emotional lability; hallucinogenic FX develop more slowly, visual disturbances, depersonalized "out of body" experience, difficulty differentiating reality, panic, psychosis ... the drug itself is not all that toxic, it's behavior; signs of a "bad trip" are similar, panic, fear, anxiety; tolerance does develop |
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Term
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Definition
| Hallucinogen, Indole … found in mushrooms, and in the skin of some amphibians, hence the urban legend of 'toad licking' … sympathomimetic FX include pupil dilation, increased BP, tachycardia, piloerection, hyperflexia, tremors, increase in body temp; other somatic FX include dizziness, weakness, paresthesias, nausea; subjective psychic changes may include anxiety, euphoria, giddiness, emotional lability; hallucinogenic FX develop more slowly, visual disturbances, depersonalized "out of body" experience, difficulty differentiating reality, panic, psychosis ... the drug itself is not all that toxic, it's behavior; signs of a "bad trip" are similar, panic, fear, anxiety; tolerance does develop |
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Term
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Definition
| Hallucinogen, Indole … a powerful hallucinogen found in the roots of an Agrican shrub (Tabernanthe iboga) … sympathomimetic FX include pupil dilation, increased BP, tachycardia, piloerection, hyperflexia, tremors, increase in body temp; other somatic FX include dizziness, weakness, paresthesias, nausea; subjective psychic changes may include anxiety, euphoria, giddiness, emotional lability; hallucinogenic FX develop more slowly, visual disturbances, depersonalized "out of body" experience, difficulty differentiating reality, panic, psychosis ... the drug itself is not all that toxic, it's behavior; signs of a "bad trip" are similar, panic, fear, anxiety; tolerance does develop ... controversial use in treatment of alcoholism and drug addiction |
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Term
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Definition
| Hallucinogen, Phenylethylamine (~Amphetamine) … Mescaline found in the buttons of the peyote cactus, produces effects similar to LSD but the somatic autonomic changes (dizziness, tingling, nausea) are more pronounced … sympathomimetic FX include pupil dilation, increased BP, tachycardia, piloerection, hyperflexia, tremors, increase in body temp; other somatic FX include dizziness, weakness, paresthesias, nausea; subjective psychic changes may include anxiety, euphoria, giddiness, emotional lability; hallucinogenic FX develop more slowly, visual disturbances, depersonalized "out of body" experience, difficulty differentiating reality, panic, psychosis ... the drug itself is not all that toxic, it's behavior; signs of a "bad trip" are similar, panic, fear, anxiety; tolerance does develop |
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Term
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METHYLENEDIOXYMETHAMPHETAMINE (MDMA; Ecstasy) |
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Definition
| Hallucinogen, Phenylethylamine (~Amphetamine) … MDMA is somewhere between a stimulant and a hallucinogenic, now one of the more common hallucinogens ... sympathomimetic FX include pupil dilation, increased BP, tachycardia, piloerection, hyperflexia, tremors, increase in body temp; other somatic FX include dizziness, weakness, paresthesias, nausea; subjective psychic changes may include anxiety, euphoria, giddiness, emotional lability; hallucinogenic FX develop more slowly, visual disturbances, depersonalized "out of body" experience, difficulty differentiating reality, panic, psychosis ... the drug itself is not all that toxic, it's behavior; signs of a "bad trip" are similar, panic, fear, anxiety; tolerance does develop |
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Term
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CANNABIS (MARIJUANA) |
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Definition
| Cannabinoid … delta9-tetrahydro-cannabinol is the psychoactive ingredient, and it affects the brain by activating specific cannabinoid receptors … endogenous brain lipids (2-AG) are CB1 ligands, they are rapidly synthesized in response to depolarization/Ca2+ influx ... cannabinoids travel backwards from postsynaptic neurons to presynaptic neurons, suppressing neurotransmitter release ... cannabinoids may affect memory, cognition and pain perception; relaxation, giddiness, confusion, cognitive impairment, psychomotor slowing, increase in appetite, tachycardia, reddening of eyes, decreased intraocular pressure, inhibition of vomiting reflex, sometimes paranoia, hallucinations, psychosis ... used medically to prevent nausea/vomiting, prevent wasting away of AIDS pateints, treat glaucoma and asthma ... cannabis side FX include immunosuppression, decreased libido, teratogenic effects, lung damage, "Amotivational Syndrome" |
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Term
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Definition
| Salvia plant grows wild all over North America; active agent is salvinorin A, a kappa opioid agonist and D2 dopaminergic … hallucinogenic activities are qualitatively different from classic hallucinogens like LSD; usually taken by smoking |
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Term
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Definition
| Kratom is a plant indigenous to regions of Thailand, where it has been used as a stimulant and a pain reliever; reported to have opiod-like effects … chemically different from morphine, but some mu-opioid agonist activity … touted as legal opioid, possible control of withdrawal, physical responses vary |
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Term
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Definition
| Ketamine, Special K, Angel dust is a really nasty drug characterized by aggression, dulled pain, mania, slurred speech, stupor, increases in BP, vertical nystagmus (involuntary rapid eye movment), psychotic reactions ... the veterinary anesthetic, easy to synthesize; the human anesthetic, harder to synthesize |
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Term
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OXYTOCIN (Pitocin, Syntocinon) |
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Definition
| Oxytocic drug used to induce labor (go-to drug) … MofA involves oxytocin receptors in the myometrium and endometrium leading to increased intracellular Ca2+, producing contraction ... Oxytocin also helps to control some of the postpartum uterine hemorraging (as a result of constriction) ... side FX of decreased BP, increased HR (reflex response), arrhythmias, major risk of sustained uterine contractions that can harm fetus |
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Term
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Prostaglandins, PGE2 - DINOPROSTONE (Prepidil, Cervidil, Prostin E2) |
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Definition
| Oxytocics, Drugs that stimulate uterine activity … used to induce labor; also important for softening and dilating the cervix (aka "cervical ripening") … similar MofA to oxytocin, binds to prostaglandin receptors, increase Ca2+ that produce contractions ... can be given IV or vaginal insert ... side FX include same risk of overstimulating uterine contraction, and causing fetal harm; also some GI upset |
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Term
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Prostaglandins, 15-METHYL PGF 2-ALPHA - CARBOPROST TROMETHAMINE (Hemabate) |
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Definition
| Oxytocics, Drugs that stimulate uterine activity … Carboprost can be used to control postpartum bleeding, but its main use is to induce abortion in the second trimester … side FX of some GI upset |
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Term
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Prostaglandins, PGE1 ANALOG - MISOPROSTOL (Cytotec) |
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Definition
| Oxytocics, Drugs that stimulate uterine activity … Misoprostol can be used with antiprogestin Mifepristone RU486 for early termination of pregnancy (up to 49 days from last menstrual period) … side FX of some GI upset |
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Term
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Ergot Alkaloids, ERGONOVINE MALEATE (Ergotrate) |
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Definition
| Oxytocics, Drugs that stimulate uterine activity … Ergonovine Maleate induces intense contractions of the uterus, used to be used for childbirth, but not anymore (stillbirths); now used to treat postpartum or postabortion hemorrhage … side FX of hypertension, GI nausea/vomiting/diarrhea, also possibility of Gangrene in fingers and toes |
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Term
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Ergot Alkaloids, METHYLERGONOVINE MALEATE (Methergine) |
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Definition
| Oxytocics, Drugs that stimulate uterine activity … Methylergonovine Maleate induces intense contractions of the uterus, used to be used for childbirth, but not anymore (stillbirths); now used to treat postpartum or postabortion hemorrhage … side FX of hypertension (methylergonovine is better at this), GI nausea/vomiting/diarrhea, also possibility of Gangrene in fingers and toes |
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Term
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MIFEPRISTONE - RU486 (Mifeprex) |
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Definition
| Oxytocics, Drugs that stimulate uterine activity … the "abortion drug", Mifepristone is an antiprogestin or progesterone receptor antagonist that can terminate pregnancy early on (up to 49 days from the last menstrual period) … mifepristone is administered (600mg orally) followed two days later by misoprostol (400micro-g orally) ... main side FX is bleeding and cramping |
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Term
TERBUTALINE SULFATE (Brethine) |
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Definition
| Tocolytic Agents, Drugs that inhibit uterine activity … used to delay premature labor (before 37th week of gestation), buys time at least temporarily (for 48 hours) so mother can relocate to special facility … terbutaline is a beta-2 adrenergic agonist of uterine smooth muscle, increase in cAMP may decrease contractions ... side FX can cause fetal and maternal tachycardia (due to a reflex response to lowered diastolic pressure), edema (risk increases with corticosteroid use), and can cause hyperglycemia so be careful with diabetics |
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Term
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MAGNESIUM SULFATE |
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Definition
| Tocolytic Agents, Drugs that inhibit uterine activity … Magnesium sulfate delays the onset of labor, buys time for mother to relocate; alternative option to terbutaline … inhibits calcium channels … main side FX are due to magnesium intoxication (flushing, sweating, hypotension, CNS depression) |
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Term
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Prostaglandin-Synthetase Inhibitor, INDOMETHACIN (Indocin) |
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Definition
| Tocolytic Agents, Drugs that inhibit uterine activity … used in prevention of labor, buys time for mother to relocate; can also be used to treat painful menstrual cramps associated with primary dysmenorrhea … Indomethacin inhibits production of prostaglandins (F2-alpha and E2) which are important for cervical ripening and myometrial contraction |
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Term
| What are the most common drug interactions with sedative hypnotics? |
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Definition
| The most common drug interactions with sedative hypnotics (benzodiazepines, barbituates, etc.) are with other CNS depressants, especially alcohol. Less obvious drug interactions are with antihistamines, antihypertensive agents, and trycyclic antidepressants (?) |
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Term
| What is the pyramid approach in selecting medication treatment for Rheumatoid Arthritis (RA)? |
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Definition
For mild cases of RA, go for Hydroxychloroquine (DMARD)
For moderate cases of RA, remember to "SHMILE" and look to Sulfazalazine, Hydroxychloroquine, Methotrexate, Infliximab, Leflunomide, Etanercept
For severe cases of RA, go for Methotrexate; or go for Azathioprine, Gold, Penicillamine, Cyclosporine |
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Term
| What drugs would you give to a schizophrenic patient on antipsychotics who demonstrates neuroleptic malignant syndrome (NMS) with severe muscular rigidity, stupor and hyperthermia? |
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Definition
| There is massive release of Ca2+ from the sarcoplasmic reticulum in NMS. So giving Dantrolene (inhibits the release of Ca2+) or Bromocryptine (a dopamine agonist) may help. |
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Term
| What is the major advantage of using the benzodiazepines instead of barbiturates? |
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Definition
| Look at the dose-response curves. Benzodiazepines like diazepam are not likely to cause fatalities, even at doses 100 times higher than the normal sedative dose. This is not the case for barbiturates (or alcohol) |
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Term
| In what psychomotor systems do benzodiazepines exert their therapeutic effects - and whare are their effects? |
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Definition
Benzos act in the limbic system to relieve anxiety (anixolytic).
Benzos act on the reticular activating system to decrease levels of arousal and wakefulness (sedative-hypnotic).
Benzos act in the cerebral cortex to inhibit the spread and propagation of seizure activity (anticonvulsant).
Benzos modify internuncial polysynaptic reflexes in the brainstem and spinal cord to cause the relaxation of skeletal muscle (muscle relaxant). |
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Term
| What is the effect of benzodiazepines on sleep? |
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Definition
Benzos decrease sleep latency (time it takes to fall asleep) with some decrease in the duration of REM sleep (aka quality sleep) although this reduction in REM sleep is not as problematic as with barbiturates and alcohol.
There may be a rebound increase in REM sleep after stopping drug abruptly (REM rebound).
Also, note that a shorter-acting drug such as triazolam might be best for an individual who has trouble falling asleep, whereas a longer-acting drug such as flurazepam might be better for someone who has trouble staying asleep. But longer-acting drugs tend to have "hangover effect", while shorter-acting drugs tend to cause "rebound anxiety". |
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Term
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Definition
| A compelling need to be in motion; manifests as fidgeting or pacing; and is often mistaken for psychotic agitation. This akathisia is a possible neurological side FX observed with use of antipsychotics. |
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Term
| What drug might improve condition of someone suffering from acute dystonia (muscle spasms, grimacing) as a result of antipsychotic Rx? |
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Definition
| A centrally-acting anticholinergic drug (such as trihexiphenydyl or ARTANE) may help in this scenario. |
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Term
| Why does clozapine not produce extrapyramidal side FX like the older antipsychotics do? |
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Definition
| The current hypothesis is that schizophrenia symptoms result from an excess of dopamine activity in the frontal cortex and limbic system. But there are different subtypes of dopamine receptors. Clozapine acts as an antagonist at D4 receptors mainly in limbic and mesocortical areas, also has a high affinity for 5-HT2 receptors. This contrasts with older antipsychotics that act as antagonists at D2 receptors found in limbic, mesocortical AND extrapyramidal areas. Clozapine seems to block the actions of dopamine and serotonin in mesolimbic and mesocortical areas, but not in the striatum or tuberoinfundibular system. |
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Term
| How are Parkinsonism and choreiform movements like Tardive Dyskinesia related? |
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Definition
| Parkinson's Disease results from a chronic deficiency of dopaminergic activity relative to cholinergic activity (remember the see-saw model). Tardive Dyskinesia is the opposite situation. The body responds to low levels of DA and compensates with a massive production of DA receptors, which leads to excessive dopaminergic activity as a result. This is called "denervation supersensitivity". So the opposite condition can arise from the same observed levels of DA. Both are pathological conditions invovling dopamine, but they differ in terms of which side the see-saw eventually tips to. |
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Term
| What are the four major categories of inflammatory mediators? |
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Definition
| Eicosanoids (signalling lipid molecules, local hormones, e.g. prostaglandins); cytokines (signalling protein molecules, e.g. IL-1, TNF-alpha); enzymes (lysosomal); & oxygen free radical species |
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Term
| Are DMARDs such as Hydroxychloroquine and Leflunomide considered to be first-line drugs in the treatment of arthritis? |
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Definition
| No. The therapy of arthritic diseases involves a number of agents including NSAIDs and corticosteroids (first-line) for antiinflammatory symptomatic relief, followed by so called slow-acting (SAARDs) or disease-modifying antirheumatic drugs (DMARDs) such as gold compounds and penicillamine. Due to their toxicity, SAARDs and DMARDs are reserved for progressive diseases unresponsive to more conservative therapy. |
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Term
| What are Signal 1 and Signal 3 in the context of immunomodulation? |
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Definition
| Recalling the interaction between antigen-presenting cells (APCs) and T cells, remember that there needs to be certain actions before a T cell is "activated." As it turns out, Signal 1 and Signal 2 are sufficient for lymphocyte proliferation and cytokine production (mainly B cells); but a third Signal 3 is required to generate cytotoxic effects (from T cells). This is why so many of the T/B cell antiproliferative drugs can work by inhibiting Signal 1 or Signal 3. |
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Term
| What drugs would be used in the treatment of alcohol withdrawal syndrome and why? |
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Definition
| The main objective in treating alcohol withdrawal is to prevent seizures, delirium and arrhythmias. Benzodiazepines such as diazepam, lorazepam, and oxazepam suppress withdrawal symptoms. Lorazepam and oxazepam may be the preferred drug in patients with impaired hepatic function. |
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Term
| Should Indomethacin be used in the treatment of juvenile rheumatoid arthritis JRA? |
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Definition
No.
potential for serious adverse side FX in children under 14 with this NSAID |
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Term
| Should corticosteroids be used in children with juvenile rheumatoid arthritis JRA? |
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Definition
NO.
Potential adverse reactions of giving corticosteroids to kids - growth retardation and problems associated with withdrawal. |
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Term
| As a review, what do anticholinergics do? |
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Definition
Anticholinergic drugs (like atropine) inhibit parasympathetic nerve impulses by selectively blocking the activity of Ach on its receptors.
Anticholinergics can be grouped into three categories - antimuscarinics, ganglionic blockers, and neuromuscular blockers.
Anticholinergics increase heart rate, increase body temp, dilate the pupils, decreased bowel movement, retention of fluids.
They can be used to treat GI disorders, vertigo, asthma and other respiratory disorders. |
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