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13 Cards in this Set
- Front
- Back
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-statins, in general
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hyperlipidemia tx
fluvastatin - complete GI absorption best given at night absorption enhanced with food high 1st pass hepatic metabolism mostly excreted into bile structural analogs of HMG-CoA, inhibit HMG-CoA reductase to reduce hepatic formation of cholesterol, increase LDL receptors in hepatocytes to lower plasma LDL decrease plasma TGs and increase HDL cholesterol reversal of endothelial dysfxn - improved vasodilatory responses to NO decreased inflammation decreased coagulation improved plaque stability decreases LDL, decr TGs, increases HDL Tx lower plasma LDL, alone or in combo w/ resins, niacin, or ezetimide 1st line therapy for elevated LDL reduce mortality form MI and CVD in pts at high risk Side effects: contraindicated in pregnancy! hepatic tox - elevations in serum aminotransaminase atorvastatin, lovastatin, simvastatin - CYP3A4 fluvastatin, rosuvastatin - CYP2C9 fluvastatin, rosuvastatin - CYP2C9 pravastatin - not metabolized by P450 increases creatine kinase activity - indicates rhabdomyolysis gemfibrazole - may enhance the myopathic effect, may increase concentration amiodorone + simvastatin also --> increased rhabdomyolysis |
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fluvastatin
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GI absorption nearly complete
CYP2C9 metabolism - ketoconazole, metronidazole, sulfinpyrazone, amiodarone, cimetidine |
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atorvastatin
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CYP3A4
macrolides, cyclosporine, ketoconazole, fibrates, grapefruit juice, barbiturates, phenytoin, rifampin |
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pravastatin
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not metabolized by P450
favored in combo w/ other drugs |
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rosuvastatin
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CYP2C9 metabolism - ketoconazole, metronidazole, sulfinpyrazone, amiodarone, cimetidine
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simvastatin
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CYP3A4
macrolides, cyclosporine, ketoconazole, fibrates, grapefruit juice, barbiturates, phenytoin, rifampin when combined with amiodorone, --> increased rhabdomyolysis |
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lovastatin
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CYP3A4
macrolides, cyclosporine, ketoconazole, fibrates, grapefruit juice, barbiturates, phenytoin, rifampin |
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simcor
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niacin + simvastatin
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vytorin
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ezetimibe + simvastatin
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nicotinic acid, vitamin B3
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water soluble vitamin, converted to amide, incroporated into NAD, excreted in urine
lg doses improve every lipid parameter dcrease lipase activity in adipose tissues reduce FFA flux to the liver decrease hepatic synthseis of TGs and VLDL lower plasma LDL and TGs decreases LDL, decreases TGs, increases HDL Tx: drug of choice for pts with elevated LDL and lowered HDL most effective drug for elevating HDL side effects: cutaneous flushing, add aspirin |
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gemfibrozil, fenofibrate
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fibric acid derivatives
ligands for PPAR-alpha in hepatocytes activation of hepatic PPAR-alpha decreases plasma TGs, VLDL, and LDL, and increases plasma HDL decreases TGs, LDL, increases HDL Tx: hypertriglyceridemia and dysbetalipoproteinemia Side effects: rare skin rashses, GI, myopathy, arrhythmias, hypokalemai, increases aminotransferases or alk phos decreases WBC or Hct potentiate anticoagsinanedione and coumarin rarely rhabdomyolysis avoid in pts w/ hepatic or renal dyxfxn modest increase in risk for cholesterol gallstones risk of myopathy increases in combo with statins |
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colestipol, cholestyramine, colesevalam
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bile acid binding resins
large cationic exchange resins, insoluble in water bind bile acids and increase excretion 7alpha-hydroxylase up-regulated (synths bile acids from cholesterol), increased bild acid synthessis --> reduced hepatic cholesterol --> increased LDL receptors enhances removal of LDL from circulatio decreases plasma LDL Tx: primary hypercholesterolemia might --> increased VLDL, add niacin or fibrate may be used for tx digoxin toxicity 2nd line agents after statins Side effects: no systemic effects - not absorbed possibly decrease absorption of fat-solubel vitamins additive effect in combo with statins bloating and constipation - increase fiber may impair absorption of certain drugs - digoxin, thizides, tetracycline, fluvastatin, thyroxine, or aspirin |
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ezetimibe
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intestinal sterol absorption inhibitor
inhibits intestinal absoprtion of cholesterol and phytosterols reduces plasma LDL effective when there is no dietary cholesterol b/c inhibits absorption of cholesterol excreted in bile tx primary hypercholesterolemia low incidence of reversible hepatic impairment single daily dose reduces LDL by 18% |
