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Hyperlipidemics
USMLE Step 1
Drug | MOA & ADRs |
---|---|
Type 1: Familial Lipoprotein Lipase Deficiency | deficiency of 1) lipoprotein lipase, 2) abnml lipoprotein lipase, 3) apo-C2 defects leading to increases in chylomicrons, TGs; autosomal recessive; not atherogenic, so tx is to lower fat intake |
Type 2A: Familial Hypercholesterolemia | defect of the LDL receptor, causing elevations in LDL & cholesterol; autosomal dominant; very atherogenic |
Type 2B: Familial hypercholesterolemia | mutant apolipoprotein B100, resulting in increased levels of LDL, VLDL, cholesterol & TGs; autosomal dominant; very atherogenic |
Type 3: Familial dysbetalipoproteinemia | mutant apo E, resulting in increased cholesterol & TGs, as well as 'floating LDLs'; very atherogenic |
Type 4: Familial Hypertriglyceridemia | due 2 overprod of VLDL in assoc w/ glucose intolerance & hyperinsulinemia (increase VLDL & TGs); autosomal dominant; mildly atherogenic; increases one risk of pancreatitis; most common inherited hyperlipidemia |
Type 5: Familial Hyperlipoproteinemia | similar to Type 1 defect in LPL or apo C2, causing increased levels of VLDL, chylomicrons & TGs; mildly atherogenic; increases one's risk for pancreatitis |
Niacin | MOA:decreases hepatic intake of released FAs,- lipolysis in fat cells,increases HDL,decreases LDL, increasing efficacy of resins(bile acid?),decreased TGs,increased chylomicron & VLDL clearance from bld,4 type 2B;ADRs:severe cutaneous flushing & pruriti |
Clofibrate | MOA:fibric acid increases lipoprotein lipase activity 2 decrease chylomicron & VLDL levels,tx 4 hyperlipidemia types 3 & 4,increase several apoprotein receptor recognition sites 2 increase lipoprotein uptake by liver;ADR:gallstones,dysrhythmias,malignancy |
Fenofibrate | MOA: fibric acid agent increases lipoprotein lipase activity 2 decrease chylomicron & VLDL levels, tx 4 hyperlipidemia, increase several apoprotein receptor recognition sites 2 increase lipoprotein uptake by liver; ADRs: gallstones,dysrhythmias,malignancy |
Gemfibrozil | MOA: fibric acid agent increases lipoprotein lipase activity 2 decrease chylomicron & VLDL levels, tx 4 hyperlipidemia, increase several apoprotein receptor recognition sites 2 increase lipoprotein uptake by liver; ADRs: gallstones,dysrhythmias,malignancy |
Colestipol | MOA:bile acid sequestrant binds cholesterol in gut,increased liver cholesterol syn that increases liver serum LDL intake & decreases plasma LDL,used in types 2 A & B;ADRs:major contraindication is hypertriglyceridemia,- absorption of many drugs |
Colesevelam | MOA: bile acid sequestrant binds cholesterol in the gut, increased liver cholesterol syn that increases liver serum LDL intake & decreases plasma LDL; ADRs: major contraindication is hypertriglyceridemia |
Atorvastatin | MOA: HMG-CoA reductase - (statin), decrease rate-limiting step of cholesterol syn, esp in hepatocytes, decrease pool of intracell cholesterol cause increased uptake of serum LDL = less cholesterol in bld; ADRs: hepatotoxic, myopathy esp w/ niacin |
Fluvastatin | MOA: HMG-CoA reductase - (statin), decrease rate-limiting step of cholesterol syn, esp in hepatocytes, decrease pool of intracell cholesterol cause increased uptake of serum LDL = less cholesterol in bld; ADRs: hepatotoxic, myopathy esp w/ niacin |
Pravastatin | MOA: HMG-CoA reductase - (statin), decrease rate-limiting step of cholesterol syn, esp in hepatocytes, decrease pool of intracell cholesterol cause increased uptake of serum LDL = less cholesterol in bld; ADRs: hepatotoxic, myopathy esp w/ niacin |
Rosuvastatin | MOA: HMG-CoA reductase - (statin), decrease rate-limiting step of cholesterol syn, esp in hepatocytes, decrease pool of intracell cholesterol cause increased uptake of serum LDL = less cholesterol in bld; ADRs: hepatotoxic, myopathy esp w/ niacin |
Simvastatin | MOA: HMG-CoA reductase - (statin), decrease rate-limiting step of cholesterol syn, esp in hepatocytes, decrease pool of intracell cholesterol cause increased uptake of serum LDL = less cholesterol in bld; ADRs: hepatotoxic, myopathy esp w/ niacin |
Cholestyramine | MOA:bile acid sequestrant binds cholesterol in gut,increased liver cholesterol syn that increases liver serum LDL intake & decreases plasma LDL,used 4 types 2A & B;ADRs: major contraindication is hypertriglyceridemia & - many drug absorption |
Lovastatin | MOA:HMG-CoA reductase -,decrease rate-limiting step of cholesterol syn,esp in hepatocytes,decrease pool of intracell cholesterol=increased uptake of serum LDL=less cholesterol in bld,4 types 2A & B;ADRs:hepatotoxic,myopathy esp w/ niacin,contra in pregger |
Diet | MOA: most important factor in improving all types of hyperlipidemia, the ONLY option for Type 1 |