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Lipid-lowering Agents-Exam 6
Lipid-lowering Agents-Exam 6
6
Pharmacology
Graduate
01/06/2011

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Term
Cholestyramine, Colestipol
Definition
bile acid binding resins
MOA: bind cholesterol-containing bile acids and prevent reabsorption, increase clearance, increased hepatic metabolism of cholesterol to bile acids (regulated by neg feedback), decreased hepatic cholesterol content, upregulation of hepatic LDL receptors
PK: negligible systemic bioavailaility, must be taken with meals to be effective
CI: familial hypercholesterolemia, combo therapy for familial combined hyperlipoproteinemia
AE: GI disturbances (constipation and abdominal discomfort)
DI: may reduce absorption of vitamins and drugs taken at the same time -> patients should take other drugs at least 1 hours before or at least 2 hours after resin
Term
Ezetimibe
Definition
cholesterol absorption inhibitor
MOA: localizes and acts at the brush border of small intestine -> inhibit absorption of cholesterol (decrease delivery of intestinal cholesterol to liver, decrease hepatic cholesterol stores, increase clearance of cholesterol from blood
CI: monotherapy-cholesterol lowering is limited (reduced uptake of dietary cholesterol but upregulates hepatic cholesterol synthesis), combo with HMG CoA reductase inhibitors -> 20% additional decrease (allow reduction of statin dose while achieving cholesterol-lowering goal)
Term
Fenofibrate, Gemfibrozil
Definition
fibrates/cholesterol absorption inhibitor
-ligand for PPAR-alpha
MOA: decrease apoB synthesis, decrease VLDL synthesis, decrease apoC-III synthesis, increase apoA-I and A-II synthesis, increase LPL synthesis, increase catabolism of TRLs -> decrease TG (major effect) and increase HDL
PK (fenofibrate): more potent than gemfibrozil, longer ½ life, renal and fecal excretion
PK (gemfibrozil): well absorbed when taken with meal, shorter ½ life than fenofibrate, most excreted unchanged in urine
CI: dysbetalipoproteinemia, hypertriglyceridemia
AE: GI disturbances, skin rashes, MYOPATHY, arrythmias, fatigue
Contra: renal or hepatic dysfunction
Preexisting gallbladder disease, hypersensitivity
DI: potentiate effects of coumarin and indanedione anticoagulants(reduce anticoagulant doses and monitor prothrombin levels), myalgias and rhabdmyolysis for combo of gemfibrozil and HMG CoA reductase inhibitors
Term
Avostatin, Lovastatin, Simvastatin, Rosuvastatin
Definition
HMG CoA reductase inhibitors
MOA: forms analog of intermediate in conversion of HMG CoA to mevalonic acid, competitively inhibit HMG CoA reductase (rate-limiting and committed step of cholesterol synthesis), hepatic LDL receptors are upregulated -> LDL and IDL clearance increased; inhibition of apoB-100 synthesis, inhibition of TRL synthesis and secretion, improve endothelial function and stabilize atherschlerotic plaque
-atovastatin and simvastatin reduce LDL in homozygous familial hypercholesterolemia
PK: oral bioavail differs between statins; lovastatin and simvastatin admin lactone form (prodrugs); extensive 1st pass metabolism, bound to protein; lovastatin, simvuastatin, atorvastatin -> CYP3A4 (affected by grapefruit juice)
CI: most commonly used drugs for hypercholesterolemia (monotherapy or combo therapy), preservation of bone mineral density, increase osteoblast differentiation and activity
AE: generally well tolerated, hepatotoxicity, myopathy -> rhabdomyolysis and renal failure (risk is increased in combo therapy with fibric acid derivatives and other drugs that inhibit CYP3A4)
Contra: pregnancy, liver disease, major illness or trauma
DI: lovastatin and simvastatin potentiate action of coumarin anticoagulants
Term
Niacin (Nicotinic Acid)
Definition
-vit B3, used in synthesis of NAD and NADP, inhibits adipocyte adenyl cyclase
MOA: decrease TG synthesis, decrease VLDL secretion, decrease apoA-1 clearance, increases LDL, increases VLDL clearance -> decreased TG, decreased LDL, decreased Lp(a), increased HDL (major effect)
PK: rapidly absorbed, sustained-release tablets, distributes throughout body, excreted by kidneys, high doses required for lipid lowering
CI: hypertriglyceridemia w/ elevated LDL-C and low HDL-C; combo therapy w/ resins for familial hypercholesterolemia, any pt whose LDL-C is controlled but HDL-C is low; combo therapy with resin and statin -> reduce LDL-C by 70% or more
AE: CUTANEOUS VASODILATION -> flushing and pruitis (take aspirin prior to reduce rxn), nausea and diarrhea; may precipitate abnormal liver function, hepatoxicity, glucose intolerance, peptic ulcers, gout
Contra: peptic ulcers, glucose intolerance, gout, hepatic function should be monitored
DI: induce hypotension in combo with anti-HTN drugs
Term
Omega-3 Fatty Acid Ethyl Ester
Definition
MOA: adjunct to lipid-lowering diet to reduce TGs in adults with severe hypertriglyceridemia, reduce hepatic TG synthesis and increase plasma lipoprotein lipase activity
Contra: hypersensitivity, fish allergies
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