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Pharmaco Chapter23

Pharmacology of Cholesterol and Lipoprotein Metabolism

QuestionAnswer
Inhibitors of Cholesterol Synthesis Lovastatin, pravastatin, simvastatin, fluvastatin, atorvastatin, rosuvastatin
Clinical applications of statins Hypercholesterolemia, familial hypercholesterolemia, coronary atherosclerosis
Adverse effects of statins myopathy, rhabdomyolysis, dermatomyositis
Which statins are metabolized by P450 3A4? lovastatin, simvastatin, and atorvastatin
Coadministration of statins with what can induce rhabdomyolysis? gemfibrozil
Coadministration of statins with what can induce myopathy? niacin
Inhibitors of bile acid resorption Cholestyramine, colesevelam, colestipol
Clinical applications cholestyramine, colesevelam, colestipol hypercholesterolemia
Adverse effects cholestyramine, colesevelam, colestipol increase in TG levels, bloating, dyspepsia, bleeding diathesis secondary to vitamin K deficiency
Contraindications cholestyramine, colesevelam, colestipol Hyperlipidemia types III, IV, or V (hypertriglyceridemia)
MOA ezetimibe Decrease cholesterol transport from micelles into the enterocyte by inhibiting uptake through brush border protein NPC1L1
Clinical applications ezetimibe Primary hypercholesterolemia, familial hypercholesterolemia
Combination with what prevents compensatory increase in hepatic cholesterol synthesis? statins
MOA gemfibrozil, fenofibrate Agonists of PPAR-alpha
Clinical applications gemfibrozil, fenofibrate isolated hypertriglyceridemia, hypertriglyceridemia with low HDL, type III dysbetalipoproteinemia
Adverse effects gemfibrozil, fenofibrate elevated LFTs, myopathy when coadministed with statins, arrhythmias, dyspepsia, gallstones
Fenofibrate increases the clearance of what? cyclosporine
MOA niacin reduces free fatty acid release from adipose tissue; increases plasma residence time for apoA1
Clinical applications niacin Isolated low HDL, Low HDL with mildly elevated LDL or triglycerides, familial combined hyperlipidemia
Adverse effects niacin Flushing, pruritus, hyperuricemia and gout, impaired insulin sensitivity (use with caution in diabetics), myopathy
Created by: 7958184
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