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69 Cards in this Set
- Front
- Back
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Aspirin |
NSAID, Anticoagulant -Mechanism: irreversible acetylation of COX, has high first pass effect. Antipyretic and anangleic dose (0.625g/single dose, every 4-6 hours). Anti-inflammatory (3.6-4.5 g/day). Anti-coagulant, has anti-platelet activity, doesn't effect endothelial cells (81 - 325 mg/day). -Uses: Mild pain, antipyertic for infections (but not children with viral infections- Reyes Syndome). High does anti-inflammatory for OA and RA. Low dose for transient ischemic attacks, unstable angina, thrombosis with MI, prevention of arterial thrombosis. - Adverse effects: GI irritation, GI ulcers, fecal bleeding, high doses could cause Salicylism (vomit, tinnitus, vertigo) |
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Celecoxib |
Mechanism: selective COX2 inhibition Uses: OA and RA relief, reduce polyps in FAP Adverse effects: edema, prevent from giving to patients with aspirin induced asthma and women in late pregnancy Drug interactions: may reduce ACE inhibitor effect and 2C9 inhibitors. |
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Ibuprofen |
NSAID |
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Ketoprofen |
NSAID |
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Indomethacin |
NSAID |
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Nabumetone |
NSAID |
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Ketorolac |
NSAID |
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Naproxen
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NSAID |
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Adverse effects from NSAIDs (Except Aspirin) |
- All carry warnings for risk of cardiovascular events, are contraindicated from patients following coronary bypass (reduce beneficial prostocylin) |
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Acetaminophen |
Not NSAID - Analgesic and antipyretic but not anti-inflammatory, no antiplatelet activity - Adverse effects: few -Uses: moderate pain, children with viral infection |
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Gold |
Disease modifying anti-rheumatic drug Aurothiomalate, aurothioglucose (i.m), auronofin (thioglucose derivative, oral) -Mechanism: decrease function of inflammatory cells (Progression and symptoms) Uses: Ra, takes 1-4 months Adverse effects: dermatitis, eosinophilia, thrombocytopenia, leukopenia, pancytopenia |
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Methotrexate |
Disease Modifying antirheumatic drug Folic acid analog -Mechanism: inhibit thymidylate synthetase, decrease neutrophil movement and macrophage function -Uses: RA patients at lose doses -Adverse effects: nausae, mucosal ulcers, hepatotoxicity, contraindicated from pregnant women |
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Infliximab |
Anti-TNFa drug disease modifying antirheumatic drug biologic, 2 approved for RA -given i.v. with methotrexate -Adverse effects: RTI, nausea, headache, sinusitis, rash cough, can lead to human antibody against TNF |
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Etanercept |
Anti-TNFa drug approved for RA -administed s.c. 25 mg/biweekly, recombinant fusion protein, binds TNFa molecules Adverse effects: local pain and swelling |
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Phenylephrine |
Decongestant
-Postsynaptic alpha receptor antagonist, constricts blood vessels in nasal mucosea , releives nasal congestion -Mechanism: decrease volume in nasal mucosa, reduces hyperemia, edema and nasal congestion, promote sinus drainage -adverse effects: hypertension, cardiac arrhythmia headache, insomnia |
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Oxymetazoline and Xylometazoline |
Decongestants Topical sprays, longer acting then phenylephrnie -Mechanism: decrease volume in nasal mucosa, reduces hyperemia, edema and nasal congestion, promote sinus drainage-adverse effects: hypertension, cardiac arrhythmia headache, insomnia |
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Pseudoephedrine |
Decongestant available as single ingredient or part of OTC cold remedy - Mechanism: inhibits catecholamine storage, short-term catecholamine release from synaptic terminal, decongest nasal mucosa -Adverse effects: hypertension, tacchyarythmia, insomnia, restlessness |
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Beclomethasone, Flucticasone (Flonase), Budesonide, Flunisolide, Memetasone |
Corticosteroids Nasal spray desirable treatment for allergic rhinitis (anti-inflammatory without systemic adverse effects) Uses: decrease late phase symptoms, effective in seasonal and perennial allergies Mechanism: decrease number of inflammatory cells Systemic: not commonly used due to adverse effects (growth impairment), only used for severe allergic rhinitis for short term therapy. Prednisolone |
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Prednisolone |
Corticosteroid Systemicly used for short term treatment of severe allergic rhinitis |
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Cromolyn and Nedocromil |
mast-cell stabilizers |
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Immunotherapy |
allergy shots, desesitize the immune system, get immunotolerance, IgG instead of IgE, takes 6 months to a year, last resort |
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Leukotriene Antagonists |
Anti-allergenic compound |
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Diphenhydramine (Benadryl), Cyclizine, Meclizine, Chlorpheniramine |
H1 blocker 1st Generation Mechanism: Cross B.B.B. inhibiting histamine receptors, signal from vestibular nucleas to tvomitting centers in medulla also inhibited -Uses: sedative anti-nausea, anti-cholinergic , alpha-adrenoceptor blocker, reduce itching, allergic reactions, rhinitis - Shoudn't take with MAO or anti-depressants, can alter metabolism of certain drugs, inhibit CYP450 in liver |
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Fexofenadine (Allegra), Loratadine (Claritin), Centrizine (Zyrtec), Acrivastine, Azelastine, Levocabastine |
H1 blocker 2nd generation Don't cross B.B.B., useful in casual allergies, includes other nasal sprays and eyedrops - Watery or itchy eyes |
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Heparin (Unfractionated) |
Anticoagulant negatively charged sulfate mucopolysaccharide found in seceratory granules of mast cells -Unfractionated (5-30 kD) --Mechanism: Binds to antithrombin III to create a complex with greater affinity to clotting factors Thrombin, Xa, IXa, VIIa; results in prolongation of aPTT,, i.v. or s.c. --Uses: prevent and treatment of deep vein thrombosis, prevent propagation of pulmonary embolism, after an acute MI, unstable angina, catheters --Adverse effects: Bleeding, HIT-1, long term osteoporosis, excessive anticoagulant action (tx with discontinuing drug and protamine sulfate) |
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Heparin (LMWH) |
1-5 kD -- Less anti-thrombin activity, equal factor Xa activity, more favorable benefit/risk ration, good bioavailability. s.c. Enoxaparin, Dalteparin, Tinzaparin --Uses: prevent deep vein thrombosis, enoxapain and dalteparin used in treatment of acute coronary syndromes --Adverse effects: caution with patients with renal insufficiency |
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Fondaparinux |
Selective Xa inhibitor |
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Lepirudin and Bivalirudin |
Direct Thrombin Inhibitors Used in patients with HIT Bivalirudin used in percutaneous coronary angioplasty and unstable angina - adverse effect: bleeding |
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Warfarin |
Delayed acting oral anticoagulant -Mechanism: prevent recycling of reduced vitamin K, 8-12 hours delay,36 hours half life , highly bound to albumin -Uses: with heparin for prevention and treatment of thrombosis, pulmonary and systemic embolism after MI or atrial fibrillation - Adverse effects: crosses placenta and can cause hemmorhagic fever or birth defect in fetus, cutaneous necrosis - Increase effects: ethanol, broad spectrum antibiotics, anabolic steroids - Decrease effects: Vitamin K |
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Streptokinase |
Fibrolytic Drug - Lyse already existing fibrous clots from streptococci -Mechanism: combines with plasminogen, catalyzes plasminogen to plasmin and hydrolyze fibrin plugs -Uses: acute pulmonary embolism ,deep vein thrombosis, acute MI, arterial thrombosis -Adverse effects: hypersensitivity, bleeding disorders, systemic fibrinolysis doesn't work well after 4 hours of MI, continue Treatment for 1-3 days |
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Urokinase |
Fibrinolytic drug originally from human urin, not antigenic -Mechanism: plasminogen activator, degrades fibrin and fibrinogen - Uses: severe pulmonary emboli, deep vein thrombosis - Adverse effects: bleeding |
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Alteplase (human), Reteplase (engineered, longer half life), tenecteplase, anisetreplase |
t-PA, a serine protease -Mechanism: Fibrin selective, only lyse fibrin bound to plasminogen in thrombus or hemostatic plug -Uses: treat MI, pulmonary and arterial embolisms, most effective if given within 4 hours -Adverse effects: bleeding, cerebral hemorrhages (not given to patient with recent hemorrhagic strokes) |
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Ticlopidine |
Inhibitor of ADP receptor can induce thrombocytopenia, must monitor blood count - used in secondary prevention of thrombotic stoke in patients intolerant of aspirin and in combination with aspirin to prevent stent thrombosis |
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Clopidogrel |
ADP receptor inhibitor les adverse effects then ticlopidine, GI disturbances can occur - used in prevention in patients with recent MI, stroke, or vasculature disease, also used in patients after coronary bypass |
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Dipyridamole |
Phosphodiesterase inhibitor inhibit cAMp breakdown has Vasodilator activity usually given with warfarin or aspirin Use: prevent thrombosis in prosthetic heart valves Adverse effects: bleeding |
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Abciximab |
GPII/IIIa antibody platelet inhibitor, blocks binding to fibrinogen humanized monoclonal Ab against IIb/IIIA complex administered parenterally -Adverse effects: bleeding if used with thrombolytics |
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Eptifibatide and Tirofiban |
GPIIb/IIIa antibody platelet inhibitor, blocks binding to fibrinogen fibrinogen analogs- reversibly inhibit fibrinogen to receptor administered parenterally cause bleeding if administered with thrombolytics |
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Nifedepine, Amlodipine, Nicardipine (Antiangina) |
Calcium Channel Antagonists Dihydropyridines, vascular selective - Mechanism: decrease afterload, decrease myocardial oxygen demand, increase coronary blood flow by dilating arteries - Uses: variant angina (dilating cornary arteries reducing vasospasm), angina of effort (reduce afterload), reduce oxygen demand -Adverse effects: hypotension, peripheral edema, flushing, reflex tachycardia |
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Verapamil (Antiangina) |
Calcium Channel Antagonists Nonselective Reduce heart work by reducing calcium current -Mechanism: decrease contractility, arteriolar vasodilator, dilates coronary vessels, ventricular wall stress declines, oxygen demand reduces - Uses: angina of effort and variant angina , advantageous in angina with atrial fibrillation, tacchycardia, or flutter -Adverse effects: Constipation, peripheral edema, hypotension, bradycardia, heart failure |
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Diltiazem (Antiangina) |
Calcium channel antagonists nonselective, vasodilates coronary vessel without as much negative inotropic effect -Mechanism: similar to verapamil -Adverse effects: bradycardia, hypotension, similar to verapamil but will not cause as much reflex tachycardia as dihydropyridines Used: angina of effort and variant angina |
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Nitroglycerin Isosorbide dinitrate Amyl Nitrite (antiangina) |
N :given sublingually, low oral bioavailability, if long duration transdermal Isosorbide dinitrate: sublingually, oral pre available Amyl Nitrite: inhalant - Mechanism: Increase coronary blood flow, first decrease preload by dilating veins (decrease diastolic wall tension), then decrease afterload (vasodilator); inhibits platelet aggregation, cornonary spasm and restenosis, increase myocardial oxygen supply/demand ration - Uses: all forms of angina, decrease infact size and post MI mortality when used with ACE inhibitor -Adverse effects: tolerance due to depletion of sulfhydryl groups, hypotension, tachycardia, decrease diastolic coronary perfusion, headaches, toxic with sildenafil (Viagra, increase cGMP) |
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Propanolol, Nadolol, Carveilol (Nonselective) Metoprolol, Atenolol (B1) Pindolol (non), Acebutolol (B1)- Agonists (Antiangina) |
Beta-blockers -Mechanism: decrease HR, contractility, and BP, reduce myocardial oxygen demand at rest and during exercise -Uses: stable angina, angina with recent history of MI - Adverse effects: bradycardia, fatigue, nightmares, increase triglycerides and decrease HDL, increase end-diastolic volume and increase ejection times (not used in variant angina, would cause constriction) B1 selective won't make asthma or diabetes worse Partial agonists have less negative inotropic and chronotropic effects and longer half life (bind to site not normal to agonists, smaller response) |
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Thiazide |
Diuretic -Mechanism: first decrease extracellular volume and cardiac output, hypotensive effects maintained during long term therapy because of reduced vascular resistance while CO returns to normal, but extracellular volume remains the same -Uses: if mono best used with potassium sparing drugs (amiloride or spironolactone), can decrease BP with 12.5 mg/day, shouldnt exceed 25 mg/day, best in elderly ptients with low renin levels -Adverse effects: hypokalemia, hyperlipidemia, weakness, fatigue, increase VLDL and LDL |
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Propanolol (Antihypertension) |
Beta-receptor blockers Nonselective -mechanism: decrease HR, CO and over time TPR, inhibit stimulation of renin-angiiotensis system, most effective with high plasma renin levels, high lipid solubility, crosses B.B.B., nightmares - Adverse effects: too much blocking can lead to too much slowing of the hear, Fatigue, must consider asthma, diabetic and patients with vascular insufficiency; doesn't cause postural hypotension, reflex tachycardia or salt and water retention. -Uses: mild hypertension in patient with high renin levels,after Mi to reduce work of heart, young hypertensives with rapid heart rate, used with thiazides, never used alone, less effective in african americans |
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Metoprolol, Atenolol |
B1 selective, less chance causing problems with diabetics, and asthmatic patients |
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Nadolol, Cartelol |
nonselective B-blocker |
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Acebutolol (B1), Penbutolol (nonselective), Pindolol (nonselective) |
Partial B receptor blocker agonists, reduce maximum response; do not cause as much adverse effects or rise in triglycerides |
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Prazosin |
alpha-adrenoceptor blocker -Mechanism: works peripherally to reduce arterial pressure dilating vessels and increasing capacitance; affects A1, work more in upright position, always with other drugs - Uses: hypertension in any degree, hypertensiives with prostatism -Adverse effects: postural hypotension, salth and water retention, reflex from dilating peripherals, positive ANF test |
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Alpha-methyldopa |
Centrally acting sympatholytic, acts in brain Mech: activate A2 receptors, increase uptake of norepinephrine , lower BP -Tocixity: sedation, mental lassitude, lack of concentration, don't use with antidepressant -Use: moderate hypertension with thiazide, pregnancy induced hypertension,Cant be stopped abruptly |
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Clonidine |
Centrally acting sympatholytic, act on brain increase A2 activation, decrease BP Toxicity: dry mouth, sedation, withdraw may be life threatening , don't use with ntidepressant, can't be stopped abruptly use: hypertension with thiazide diuretic |
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Hydralazine |
Vasodilator Mech: cause direct relaxtion of arteriolar smooth muscle, postural hypotension does occur, increase No or potassium release to hyperpolartize the cell, vasodilation associated with reflex stimulation of Symp nervous systemresulting in nicrease HR and Contractility, increase plasma renin levels and fluid retention -Adverse effects: headache, nausea, flushing, hypotension, palpitation, tachycardia, dizziness, angina pectoris, postural hypotension, LUPUS - USes: as 3rd drug in moderate hypertension , pregnancy induced hypertension |
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Minoxidil |
Rogain, Vasodilator -Mech: arterial vasodilator, increase NO release, hyperpolarize vascular smooth muscle, increase blood flow to skin - adverse effects: headache, nausae, dizziness, angina pectoris, postural hypotension, palpitations, Hypertrichosis is used for extended perios of time - Uses: 3rd drug in severe hypertension |
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Sodium Nitroprusside |
Vasodilator, interact with RBC to release NO from CN, dilates arterioles and venules, i.v. only, peak within 2 minutes - adverse effects: cyanide poisoning, excessive vasodilation -uses: hypertensive emergencies |
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Nicardipine, nifedipine, nimodipine |
dihydropyridine vascular selective, no effect on heart -used alone to treat moderate hypertension with asthma, renal problems, hyperlipidemia, and patients with angina adverse effects: headache, dizziness, peripherl edema, excessive hypotension -cause relflex tachycardia |
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Verapamil and Diltiazem |
Calcium channel blocker --used alone to treat moderate hypertension with asthma, renal problems, hyperlipidemia, and patients with angina -adverse effects: headache, dizziness, peripherl edema, excessive hypotension, verapamil: constipation, verapamil and diltiazem can cause bradycardia |
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Captopril, Enalapril, Lisinopril |
ACE inhibitors Mechanism: reduce amount of angiotensis II produced therefore reduce resistance and wsalt and water retention, inhibit bradykinin breakdown and potentiate its hyptotensive effect, cause arteriolar dilation and increase compliance in large arteries -Uses: good in heart failure patients because they can reduce afterload while CO and SV increase. Can decrease thickness in left ventricle. hypertension with high renin levels, CHF, acute MI with left ventricle dysfunction -Adverse effects: DRY COUGH, angioedema in the face, no change in lipoprotein or cholesterol levels, not to be taken with potassium sparing drugs, never to be taken by pregnant women (neonatal morbidity) or people with renal stenosis. |
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Losartan |
Angiotensin II receptor antagonist No dry cough from increase bradykinin,, mostly effect A1 receptor on vascular tissue, undergoes substantial 1st pass metabolism -adverse effects: not to be taken with protein sparing drug, by pregnant women or patient with renal stenosis, angioedema in the face, no change in lipoprotein or cholesterol levels - uses: mild to severe hypertension, hypertension with CHF |
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Alpha-1 Receptor |
Agonist Potency: NA>A>>ISo selective agonist: Phenylephrine Selective antagonist: Prazosin - cause vasoconstriction, relaxation of GI smooth muscle, salivary secretion, glycogenolysis; blockers cause vasodilation |
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Alpha-2 Receptor |
Agonist Potency: A>NA>>ISO selective agionist: Clonidine selective antagonist: Idozoxan (cocaine) - inhibition of transmitter release (norepinephrine); platlet aggregation, insulin release, vasculat smooth muscle contraction, blocker increase transmitter release |
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Beta-1 receptor |
Agonist Potency: ISO>NA>A selective antagonist: Atenolol, Metoprolol -increase cardiac rate and force; blockers decrease cardiac rate and heart rate |
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Beta-2 receptor |
Agonist Potency: ISO>A>NA Selective agonist: sulbutamol - broncodilation, vasodilation; blockers cause bronchoconstriction and vasoconstriction |
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Beta-3 receptor
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muscle relaxation, bladder can swell when activated |
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Hemicholinium, vesamicol |
Block ACh synthesis, H- block choline coming into vessel, formation V- block transport of synaptic vessel, transport |
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Pilocarpine, Cevimeline |
Cholinergic Agents Pilocarpine: works on muscarinic receptors, contriction of pupils for glaucoma Cevimeline- works on muscarinic receptors, increase salivation and lacrimal secretion, use for Sjorgrens syndrome |
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Timolol, Pilocarpine |
Drugs in eye Timolol- B-antagonist, eye drops, may cause bradycardia, bronchoconstriction Pilocarpine- muscarinic agonist, eye drops |
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Botilinium |
Inhibit ACH release causes respiratory paralysis, difficultyl swallowing, blurred vision, dry mouth -uses: blephrospasm, urinary incontinence, sialorrhoea, hyerhidrosis, wrinkles, headaches |
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Neostigmine |
ACH esterase inhibitor works on NMJ reverse competitive neuromuscular block i.v. only increase ACh in synapse treat myasthenia gravis |
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Varenicline |
ANS transsmission agonist work on CNS autonomic ganglia, stimulates nicotine receptors, used for nicotine addiction |
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Pancuroniumm |
ANS transmission antagonists work on NMJ, transmission block, muscle relaxants for anesthesia |
