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Rogers Test 1
Drugs on Dr. Rogers Med Chem Exam 1
| Drug Class | Representatives | Beneficial Effects | Adverse Effects | Adverse drug Interactions |
|---|---|---|---|---|
| Statins | Simvastatin, Atorvastatin | antidyslipidemic effects including reduction of plasta LDL and trigs, increase in HDL and apoA-1 levels | Hepatotoxicity, myopaty | Myopathy intensified by fibrates, macrolide antibiotics, some calcium blockers |
| Fibrates | Clofibrate (Atromid-S), gemfibrozil (Lopid) | variable decreases in levels of triglycerids, VLDL, and LDL, increases in HDL | GI distress, flu-like syndrome | increased myopathies with statis, potentiation of hemorrhagic effects of oral anticoagulants |
| Niacin | Nicotinic Acid | decreased LDL, LP(a) and TG increased HDL, inhibition of hormone sensitive lipase in adipose tissue, decreased FA synthesis in liver, Decreased synthesis of HDL receptors in liver | Skin flushing, promotion of peptic ulcer (contraindicated) hepatotoxicity may be severe enough to d/c niacin therapy, cardiac arrhythmias (a-fib) | (blank) |
| Cholesterol absorption inhibitors | ezetimibe (zetia) | moderate reductions of LDL and increases in HDL. Enhancement of lipid altering effects of statins | Back Pain, possibility of increasing hepatotoxicity of statins (contraindicated in patients with hepatic insufficiency) | (blank) |
| Cholesteryl ester transfer protein (CETP) inhibitors | Torcetrapib | Increases in HDL and reductions in LDL - designed for administration with statins | No clear - ongoing clinical trialsq | (blank) |
| Heparin | Heparin, LMWH | inhibiion of fibrin clot formation, decreased risk of thrombosis | bleeding (hemorrhage), HIT | Increased hemorrhagic effects of oral anticoagulants, antiplatelet drugs, and thrombolytic drugs |
| Oral Anticoagulants | Warfarin | inhibition of fibrin clot formation, decreased risk of thrombosis | Hemorrhage | Increased Bleeding (drugs that displace warfarin from plasma protein sites, inhibit warfarin metabolism, decreased clotting factor synthesis, inhibit platelet aggregation, lyse thrombin clots, inhibit fibrin formation, or decrease availability of Vit K) |
| Factor Xa inhibitors | Fondaparinux (arixtra), idraparinux | activation of antithrombin retards thrombus formation and decreases the risk of thrombosis | hemorrhage | (blank) |
| Thrombin inhibitors | Ximelagatran, melagatra, hirudin, argatroban | Direct inhibition of thrombin decreases the risk of thrombosis | Hemorrhage | (blank) |
| Aspirin | ASA | Inhibition of platelet aggregation, Decreased risk of thrombosis | GI upset, ulceration; Hemorrhage | Increased risk of hemorrhage with reteplase, warfarin, eptifibitide, and heparin |
| Glycoprotein IIb/IIIa inhibitors | abciximab (reopro), eptifibatide (Intergrilin), tirofiban (aggrastat), lamifiban, fadafiban | inhibition of platelet aggregation, decreased risk of thrombosis | Bleeding, thrombocytopenia | increased risk of hemorrhage with reteplase, ticlopidine, heparin, warfarin |
| Purinergic receptor antagonists | Ticlopidine (ticlid), Clopidogrel (plavix) | Inhibition of platelet aggregation, decreased risk of thrombosis | Neutropenia, Thrombocytopenia, GI distress | Increased risk of hemorrhage with reteplase, warfarin abciximab, aspirin |
| Thrombolytics | Anistreplase (eminase), tPA, reteplase (Retavase) | regression and dissolution of preformed thrombi, decreased risk of thrombotic ischemia | hemorrhage | increased risk of hemorrhage with heparin and oral anticoagulants |
| Nitrates | nitroglyerin (nitro-BID), isosorbide dinitrate (isordil) | Dilation of large coronary arteries, decreased pressure loading (total peripheral vascular resistance), decreased volume loading (ventricular diastolic volume) | Reflex increase in sympathetic drive (Tachycardia, increased renin production), tolerance, HA, postural hypotension | pronounced hypotension and increased risk of coronary ischemia with sildenafil (viagra) |
| Beta Blockers | Propranolol (Inderal), atenolol (Tenormin), metoprolol (Lopressor) | Bradycardia, mild cardiodepression | Potential for coronary vasoconstricion, bronchoconstriction, and increased diastolic ventricular volume | Severe bradycardia, AV block, and marked cardiodepression with calcium channel blockers |
| Calcium Channel blockers (CCB's) | amlodipine (Norvasc), nifedipine (procardia), diltiazem (cardizem), verapamil (Isoptin) | Dilation of coronary arteries and arterioles, bradycardia, decreased pressure loading, mild cardiodepression | potential for coronary steal, variable reflex tachycardia | severe bradycardia, AV block, and cardiodepression with beta blockers |
| Alternative coronary vasodilators | Nicorandil | binds and opens ATP-dependent potassium channels in coronary vascular smooth muscle resulting in cellulat hyperpolarization and restricting calcium influx causing muscle relaxation and artery dilation delivering more blood and oxygen to the muscle | (blank) | (blank) |
| Reducer of O2 demand | Ivabridine | Binds and inhibits Na channels in sinoatrial nodal cells that carry the pacemaker current (if), slowing heart rate and thus reducing o2 demand | (blank) | (blank) |
| Enhancer of contraction efficiency | Ranolizine, Trimetazidine, | inhibit FA beta oxidation in mitochondria of cardia muscle cells, causing promotion of blucose oxidation. Increased the efficiency of contraction as measure by the number of moles ATP produced per mole of o2 consumed by the muscle | (blank) | (blank) |
| Drug-eluting stents | paclitaxel (taxol), Sirolimus (rapamycin) | inhibit restenosis after implating stents - retards overgrowth by surrounding smooth muscle and endothelia | Paclitaxel - inhibits microtubules to prevent proliferation | Sirolimus - binds to FKBP12 intracellularly to inhibit a kinase involved in cell cycle progression, mammalian target of rapamycin (mTOR) interrupting cell division |