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20 Cards in this Set
- Front
- Back
Classification of hyperlipidemic drug? |
1)Drug for hypercholesteremia: HMG reductase inhibitors, bile acid sequestrants, cholesterol absorption inhibitors. 2) lower TG and raise HDL: fibrates, niacin |
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Specify the classification more: |
HMG reductase inhibitors (atrovastatin, fluvastatin, lovastaton, pravastatin, rosuvastatin simvastatin) bile acid sequestrants( colesevelam, colestipol, cholestyramine) cholesterol absorption (ezetimibe) fibrates (fenofibrates, gemfibrozil) niacin |
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Whats the first-line therapy for hyperlipidemia? |
. |
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Name some statins? |
Atrovastatin, lovastatin, fluvastatin, simvastatin |
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MOA of statins? |
-Inhibit the hepatic HMG coA reductase > inhibits synthesis of cholesterol which causes hepatocytes to synthesize more LDL receptors> hepatocytes remove more LDL from the blood. [Most effective for LDL] - decrease production of apolipoprotein B-100 > decrease production of VLDL. -decrease plaque cholesterol content and inflammation at plaque site. |
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What are the uses of statins? |
-Hypercholesterolemia [atrovastatin is the most efficacious] -coronary heart disease (reduse mortality rate in patients with Ischaemic HD) -patients with TG higher than 250 mg/dl and with reduced HDL levels. |
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Who have the longest half life in statins? |
Atrovastatins |
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Adverse effect of statins? |
Rash, GI disturbances, hepatotoxicity, myopathy, risk high especially with fibrates, Cyp450 3A4 interactions, cant be used in pregnancy. |
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Bile acid resisns (cholestyramine and colestipol) MOA? |
They bind to bile acid in the intestinal lumen and inhibit its reabsorption > increase LDL receptors by liver cells to capture more cholesterol and synthesise bile acids. |
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What are the uses of of bile acid binding resins? |
-hypercholesterolemia (lower LDL) -usually uses adjuncts to statins -can be used to relieve pruritis in patients with cholestasis - severe digitalis toxicity (available in powder form, must be taken with meals) |
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What are the side effects of bile acid resisns? |
GI discomfort, impair absorption of vitamins (A,D,E and K), they bind to drugs like digoxin, warfarin, tetracycline, thyroxine) |
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MOA of ezetimibe? |
Inhibits intestinal absorption of dietary and biliary cholesterol in small intestine> decreased delivery of intestinal cholesterol into liver> decreased hepatic cholesterol stores and increased clearance from the blood. |
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What are the uses of ezetimibe ? |
-hypercholesterolemia. (More effective when combined with statins. |
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MOA of niacin |
(Decreases HDL catabolic rate) -inhibit VLDL secretion into the blood> preventing production of LDL. - increases clearance of VLDL via lipoprotein lipase pathway. - inhibits FA release from adipose tissue by inhibiting intracellular lipase system. - decreases HDL catabolic rate. (Inhibit lipoprotien lipase > decrease production of VLDL) |
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What are the uses of niacin |
Hypertriglyceridemia, mixed elevation of LDL and TG (combined with statins) [start low dose and gradually increase] |
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What are the adverse effects of niacin? |
Flushing, nausea n abdominal discomfort, hyperuricemia, hepatotoxicity [not well-tolerated] |
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Name some fibrates? |
Gemfibrozil, fenofibrate, clofibrate) |
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Whats the MOA of fibrates? |
Activation of peroxisome proliferator-activated receptor alpha (PPAR-alpha) > increase activity of endothelial lipoprotein lipase, increase FA oxidation in hepatocytes, decrease secretion of VLDL by liver, decrease HDL by increasing apo AI and Apo AII |
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What are the uses of fibrates? |
Hypertriglyceridemia, mixed elevation of LDL and TG (w statins) |
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What are the adverse effects of fibrates? |
Nausea, rashes, cholesterol gallstones, myopathy |