Term
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Definition
MOA: irreversible inhibitor of platelet aggregation (covalent modifier of P2Y12 ADP receptor)
INDICATION: secondary prevention of MI, stroke, peripheral vascular disease; coronary artery stents; coronary artery bypass grafting
PHARM EFFECTS: inhibits sustained platelet aggregation (transient aggregation can still occur)
NOTES: elective procedures should be deferred until pt has completed appropriate course of clopidogrel therapy (12 mo after drug-eluting stent implantation or 1 mo for bare-metal stent) |
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Term
| dipyridamole (Persantine) |
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Definition
MOA: inhibitor of phosphodiesterase (an enzyme which degrades cAMP; high [cAMP] leads to a decrease in platelet aggregation)
INDICATION: ADJUNCT -- used with warfarin in prosthetic heart valve replacement; used with ASA to reduce stroke risk
PHARM EFFECTS: increase in [cAMP] leading to decrease in platelet aggregation
ADVERSE EFECTS: gingival bleeding |
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Term
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Definition
MOA: irreversible nonselective inhibitor of COX, thereby inhibiting thromboxane A2 (TXA2) formation which is a potent inducer of platelet aggregation
INDICATION: prevention of arterial thrombosis (stroke, MI, TIA)
PHARM EFFECTS: reduction in clotting inducer TXA2
ADVERSE EFECTS: gastric ulcer
NOTES: 4-10 days to recover platelet aggregation following ASA discontinuation |
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Term
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Definition
MOA: inhibitor of vit K epoxide reductase (vit K is a cofactor for synthesis of many clotting factors)
ADVERSE EFECTS: too much: bleeding; too little: angina, blood clots
CONTRAINDICATIONS: extensive drug interactions-
NOTES: pt must avoid vit K in diet (primarily leafy greens); INR every 2 weeks
no need to abruptly discontinue warfarin prior to common dental procedures; risk of life-threatening bleeding < risk of thrombembolic event
aim for INR < 3.0
40 h half-life
can be reversed with vit K in case of emergency |
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Term
heparin
enoxaparin (Lovenox) |
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Definition
MOA: binds to and activates antithrombin III which itself covalently binds to serine protease and prevents it from participating in coagulation cascade --> inactivates thrombin, factors IXa, Xa, Xia, XIIa
INDICATION: "used by patients at home as a 'bridge to warfarin'"
PHARM EFFECTS: efficient inactivation of Xa as well as thrombin, Ixa, Xia, & XIIa
NOTES: AT III inhibits clotting; heparin binds ATIII and speeds up the anti-clotting reaction 1000x |
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Term
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Definition
MOA: direct thrombin inhibitor
INDICATION: reduces risk for stroke in pts w/ atrial fibrillation
NOTES: unlike warfarin, there is no reversal agent due to its MOA. 14 h half-life compared to warfarin's 40 h half-life; therefore, a missed dose is more serious |
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Term
atorvastatin (Lipitor)
"statin" |
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Definition
MOA: competitively inhibits HMG-CoA reductase
INDICATION: hyperlipidemia
PHARM EFFECTS: inc in synthesis of hepatic LDL receptors; inc in hepatic uptake of LDL and ID
ADVERSE EFECTS: rhadbomyolysis leading to kidney failure; constipation, diarrhea, stomach pain, nausea
CONTRAINDICATIONS: EtOH increases active level of drug --> rhabdomyolysis; erythromycin, itraconazole, ketoconazole all contraindicated with lovastatin (Mevacor) especially, but w/ all statins as well --> rhabdomyolysis |
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Term
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Definition
MOA: selectively inhibits cholesterol uptake through a brush border protein (NPC1L1)
INDICATION: hyperlipidemia
PHARM EFFECTS: dec cholesterold absorption by 50%; dec LDL concentration in the plasma; dec cholesterol content of chylomicrons
ADVERSE EFECTS: abdominal pain, diarrhea
CONTRAINDICATIONS: hepatic impairment |
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Term
fenofibrate (TriCor)
gemfibrozil (Lopid) |
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Definition
MOA: PPARa agonist (binds to PPARa, a transcription factor controlling expression of lipid-metabolizing enzymes)
INDICATION: hyperlipidemia
PHARM EFFECTS: inc muscle expression of lipoprotein lipase, inc uptake of TG-containing lipoproteins; inc HDL; dec TGs
CONTRAINDICATIONS: warfarin (fibric acid derivatives displace warfarin from its albumin binding site) |
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Term
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Definition
MOA: inhibition of acyl-CoA acyltransferase, inc mitochondrial & peroxisomal b-oxidation in liver, dec lipogenesis in liver, and inc plasma lipoprotein lipase activity
INDICATION: hyperlipidemia |
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Term
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Definition
MOA: non-absorbed polymer which sequesters bile acids in the intestines so that they are not reabsorbed
INDICATION: hyperlipidemia, ADJUNCT w/ statins
PHARM EFFECTS: inc conversion of cholesterol to bile acids; inc clearance of plasma LDL-cholesterol
Boys and postmenarchal girls, 10 to 17 years of age, with heterozygous familial hypercholesterolemia
Adjunct with statins |
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Term
albuterol (Proventil)
salmeterol |
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Definition
MOA: B2 adrenergic receptor agonist;
acts via G-protein-coupled receptor, ultimately leading to an efflux of Ca++ from intracellular compartment --> dec myosin light chain relaxation --> bronchodilation
INDICATION:
SHORT-ACTING - albuterol --> used for acute bronchospasm relief;
LONG-ACTING salmeterol --> used as a controller for asthma (long-term control of bronchospasm)
PHARM EFFECTS: dec inflammatory cytokine production, dec in responsiveness of airway to inflammatory mediators, dec plasma exudation
ADVERSE EFECTS: w/ long-term use, inc asthma exacerbations, loss of bronchoprotection |
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Term
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Definition
PHARM EFFECTS: dec accumulation of macrophages and leukocytes; dec phagocytosis; dec lysosomal enzyme release; dec release of chemical mediators of inflammation
ADVERSE EFECTS: oropharyngeal candidiasis, dysphonia, leads to decreased adherence and quality of life |
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Term
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Definition
MOA: inhibition of phosphodiesterase; direct histone deacetylase activation
INDICATION: asthma
PHARM EFFECTS: bronchodilation; anti-inflammatory effects --> dec mediator release from inflammatory cells, dec allergen response
ADVERSE EFECTS: nausea, vomiting, headache, insomnia; overdose: persistent vomiting, cardiac arrythmias, & intractable seizures which can be lethal |
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Term
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Definition
MOA: competitive antagonist of cysteinyl leukotriene receptor
INDICATION: asthma & seasonal allergy rhinitis
CONTRAINDICATIONS: ASA & NSAIDs |
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Term
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Definition
MOA: inhibits 5-lipoxygenase
INDICATION: prophylaxis & chronic treatment of asthma
ADVERSE EFECTS: can cause liver problems --> must monitor liver enzymes during therapy |
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Term
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Definition
MOA: anti-IgE monoclonal antibody
ADVERSE EFECTS: nasopharyngitis, upper respiratory infection, headache; rare anaphylaxis reaction
"mab" Monoclonal AntiBody |
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Term
ipratropium (Atrovent)
tiotropium (Spiriva) |
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Definition
MOA: competitive antagonism of acetylcholine at M3 receptors in the lung
ADVERSE EFECTS: dry mouth, altered taste & coughing after administration |
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Term
| Diuretic potency greatest to least |
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Definition
| loop (furosemide), thiazide, potassium sparing (spironolactone) |
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Term
| Spironolactone (Aldactone) |
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Definition
aldosterone antagonist and potassium sparing diuretic
-It prevents the nuclear translocation of the mineralocorticoid receptor.
-Indications
Hypertension
Edema states
Heart failure
Hepatic cirrhosis
Congestive Heart Failure
Hypokalemia
Male to female gender transformation
- decrease anti hypertension with NSAIDs
Spirono"lactate" = lactate, man boobs, gender transformation |
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Term
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Definition
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Term
| Hydrochlorothiazide (HCTZ) |
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Definition
Mechanism: Binds to the Na+Cl- cotransporter in the distal tubule and inhibits turnover
MOA: binds to the NaCl cotransporter in the distal tubule and inhibits turnover
INDICATION: HTN, edema (CHF, hepatic cirrhosis, renal dysfunction, corticosteroid therapy)
PHARM EFFECTS: dec in NaCl reabsorption, inc absorption of Ca++
ADVERSE EFECTS: hypokalemia, hyponatremia, gout, dry mouth, lichenoid rxns, orhtostatic hypotension
CONTRAINDICATIONS: NSAIDs -- dec anti-HTN effect
opiates -- inc orthostatic hypotension |
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Term
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Definition
MOA: inhibition of NaCl reabsorption in loop of Henle by binding to Cl- site of cotransporter
INDICATION: HTN, heart failure, acute pulmonary edema, hyperkalemia, hypercalcemia, edema states
PHARM EFFECTS: reduces extracellular fluid volume and BP with a greater magnitude than with thiazides
ADVERSE EFECTS: same as those for thiazides with respect to hypokalemia and hyponatremia
CONTRAINDICATIONS: NSAIDs -- dec anti-HTN effect |
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Term
| Diuretics main dental concerns: |
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Definition
| Dry Mouth, lichenoid rxs, orthostatic hypotension |
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Term
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Definition
MOA: binds & activates guanylyl cyclase in endothelial cells
greatly decreases preload
INDICATION: acute chest pain
PHARM EFFECTS: relaxation of vascular smooth muscle leading to vasodilation and dec BP
ADVERSE EFECTS: headache, orthostatic hypotension, stroke, dizziness, reflex tachycardia,
CONTRAINDICATIONS: opiates -- inc effects of NO |
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Term
| Which Ca channel blocker that can be used with beta blockers? |
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Definition
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Term
| Which Ca channel blockers are contraindicated with beta blockers? |
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Definition
verapamil (Calan)
dilitazem (Cardizem) |
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Term
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Definition
Positive ionotrope
effects contractility
Inhibition of the sodium-potassium ATPase
in available sodium
↓ the rate of calcium-sodium exchange
More calcium is available for contraction of cardiac muscle
↑ force of contraction
↓ rate of contraction
Heart pumps more efficiently
metabolized by gut bacteria, can have a problem if pt is on antibiotics leading to digoxin toxicity --
Signs of toxicity
Excessive salivation
Headache
Fatigue and drowsiness
Abdominal pain
Visual disturbances Yellow or green haze around objects |
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Term
| Most common heart rhythm disturbance |
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Definition
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Term
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Definition
MOA: alteration of the lipid membrane in which channels are receptors are located
PHARM EFFECTS: lengthens refractory period by inhibiting K+ channels, blocks Na+ & Ca++ channels, antagonizes a & b adrenergic receptors |
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Term
| Dental Management Precautions with hypertension |
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Definition
Avoid the use of epinephrine-impregnated gingival retraction cord
Avoid the use of vasoconstrictors for direct hemostasis to control local bleeding
Avoid stimulating the gag reflex in patients with a history of hypertension |
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Term
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Definition
Thiazide diuretics
β blockers |
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Term
Amlodipine (Norvasc)/ Ramipril (Altace)
Why is this an efficacious therapeutic combination? |
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Definition
Baroreceptor reflexes
↑sympathetic outflow
Tachycardia
Increased contractility
Vasoconstriction
Renal perfusion reflexes
↑Renin release
you are able to block the compensatory changes associated with the baroreceptor reflex, so when rein increases you inhibit that Angiotensin/Aldosterone cycle. |
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Term
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Definition
MOA: binds AP-1 or NK-kB intraceullar transcription factors to inhibit their pro-inflammatory action; inc expression of glucocorticoid-induced leucine zipper proteins; chromatin remodeling
INDICATION: chronic inflammatory and immune diseases (see list at right)
PHARM EFFECTS: inhibition of accumulation of macrophages and leukocytes, phagocytosis, lysosomal enzyme release, and release of chemical mediators of inflammation
NOTES: withdrawal syndrome (requires 3 day tapering period for all courses of therapy) --> joint pain, muscle pain, fatigue, fever, nausea & vomiting may cause acute adrenal crisis (low endogenous cortisol) with chronic therapy -- low BP, dehydration, confusion, tachypnea, sweating, shock, coma, seizures, delays wound healing |
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Term
| prednisone adverse effects |
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Definition
Dermatologic:
impaired and delayed wound healing
Thin fragile skin
Neurologic:
Convulsions
Vertigo
Headache
Endocrine:
Development of Cushing's state
Secondary adrenocortical and pituitary unresponsiveness
Diabetes
Fluid and Electrolyte:
Sodium and fluid retention
CHF, HTN and potassium loss
Musculoskeletal:
Loss of muscle mass
Osteoporosis
Compression fractures
GI:
Peptic ulcer
Pancreatitis
Ulcerative esophagitis |
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Term
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Definition
MOA: folate analog which inhibits endogenous folate synthesis --> apoptosis of CD4 & CD8 T cells
INDICATION: rheumatoid arthritis, psoriasis, graft vs. host disease, severe asthma
PHARM EFFECTS: anti-inflammatory effects
ADVERSE EFECTS: leukopenia
NOTES: once-per-week dosing |
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Term
| mycophenolate mofetil (CellCept) |
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Definition
MOA: inhibitor of inosine monophosphate dehydrogenase (rate limiting enzyme in biosynthesis of guanosine)
INDICATION: not listed, but presumably the same as methotrexate's?
PHARM EFFECTS: induces activated T cell apoptosis, dec lymphocyte activation and activity, dec expression of adhesion molecules, dec production of NO by neutrophils
ADVERSE EFECTS: mout ulceration, gingival hyperplasia, gingivitis, dry mouth, dysphagia |
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Term
cyclosporine
tacrolimus (Prograf) |
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Definition
MOA: inhibits synthesis of IL-2 (responsible for activation and proliferation of activated lymphocytes) in activated T cells
INDICATION: immunosuppressant for graft survival, topical for oral lichen planus, psoriasis, rheumatoid arthritis, chronic dry eyes
ADVERSE EFECTS: renal toxicity, HTN, hyperlipidemia, neurotoxicity, gingival hyperplasia |
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Term
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Definition
MOA: inverse agonist which stiblizes the inactive conformation of H1 histamine receptor; some are competitive inhibitors of H2 histamine receptor
INDICATION: DENTISTRY: conscious sedation, pre-med for general anesthesia, reduction of post-op nausea, allergic lesions of oral mucosa; OTHER: nasal allergies, symptomatic relief of common cold, motion sickness, sedation
PHARM EFFECTS: H1 blockage: anti-inflammatory effects; H2 blockage: anti-emetic effects (e.g. Phenergan)
ADVERSE EFECTS: CNS depression --> drowsiness, lethargy, dec motor coordination; anti-muscarinic effects --> dry mouth, constipation, blurred vision |
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Term
| 1st GENERATION antihistamines |
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Definition
diphenhydramine (Benadryl)
chlorpheniramine (Chlor-Trimeton)
meclizine (Antivert)
for vertigo
promethazine (Phenergan)
for nausea & vomiting |
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Term
| 2nd GENERATION antihistamines (less CNS depression than what is seen in 1st generation) |
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Definition
loratadine (Claritin)
fexofenadine (Allegra)
cetirizine (Zyrtec) |
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Term
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Definition
MOA: binds to and inactivates TNFa (cytokine which enables normal inflammatory and immune responses)
INDICATION: autoimmune diseases: rheumatoid arthritis, ulcerative colitis, Crohn's disease, psoriasis
PHARM EFFECTS: immunosuppression
ADVERSE EFECTS: inc susceptibility to opportunistic infections, inc risk for TB, invasive fungal infections, sepsis, CNS demyelination |
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Term
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Definition
MOA: IL-2 receptor antagonist
INDICATION: autoimmune diseases: rheumatoid arthritis, ulcerative colitis, Crohn's disease, psoriasis
PHARM EFFECTS: inhibits IL-2 activation of lymphocytes
ADVERSE EFECTS: inc susceptibility to opportunistic infections |
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Term
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Definition
MOA: arrests mitosis in metaphase by binding to microtubular protein and preventing spindle formation, inhibits neutrophil migration and phagocytic activity in inflamed joints, inhibits inflammatory response by inhibiting neutrophil activation
INDICATION: gout
PHARM EFFECTS: dec trafficking of phagocytosed particles to lysosomes, dec release of chemotactic factors, dec motility and adhesion of neutrophils, phosphorylation of neutrophil proteins
ADVERSE EFECTS: neutropenia, diarrhea
NOTES: to treat gout, red meat is eliminated from the diet, and NSAIDs + colchicine for first 4-6 months to prevent acute episodes during beignning of chronic therapy |
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Term
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Definition
MOA: non-competitive inhibitor of xanthene oxidase
INDICATION: chronic gout
PHARM EFFECTS: dec biosynthesis of uric acid |
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Term
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Definition
MOA: inhibits the basolateral anion exchanger of
PHARM EFFECTS: dec [urate] in plasma
ADVERSE EFECTS: may develop urate stones in kidney or ureter, gingival soreness, nausea+vomiting, dizziness |
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Term
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Definition
MOA: soluble TNF receptor dimer-Fc fusion protein
Rheumatoid arthritis |
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Term
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Definition
MOA: monoclonal antibodies consisting of the ligand binding portion of the TNFa receptor
Rheumatoid arthritis |
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Term
| Proposed Roles for Tumor Necrosis Factor in Rheumatoid Arthritis |
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Definition
Cytokine
Central to many aspects of the inflammatory response
Stimulates macrophages to secrete phagocytic compounds
Stimulates production of acute phase proteins |
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Term
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Definition
Drug Therapy:
Acetaminophen
NSAIDS
Duloxetine (Cymbalta)-approved indication
Glucosamine/Condroitin sulfates
Intra-articular hyaluronic acid injections
Joint replacement surgery |
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