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20 Cards in this Set

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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

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

Whats the first-line therapy for hyperlipidemia?

.

Name some statins?

Atrovastatin, lovastatin, fluvastatin, simvastatin

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.

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.

Who have the longest half life in statins?

Atrovastatins

Adverse effect of statins?

Rash, GI disturbances, hepatotoxicity, myopathy, risk high especially with fibrates, Cyp450 3A4 interactions, cant be used in pregnancy.

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.

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)

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)

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.

What are the uses of ezetimibe ?

-hypercholesterolemia. (More effective when combined with statins.

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)

What are the uses of niacin

Hypertriglyceridemia, mixed elevation of LDL and TG (combined with statins) [start low dose and gradually increase]

What are the adverse effects of niacin?

Flushing, nausea n abdominal discomfort, hyperuricemia, hepatotoxicity [not well-tolerated]

Name some fibrates?

Gemfibrozil, fenofibrate, clofibrate)

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

What are the uses of fibrates?

Hypertriglyceridemia, mixed elevation of LDL and TG (w statins)

What are the adverse effects of fibrates?

Nausea, rashes, cholesterol gallstones, myopathy