Name: Simvastatin (Zocor)
Class: Blood Lipid-Lowering Agent (HMG CoA Reductase Inhibitor)
Mechanism: Inhib. of HMG CoA reductase ® ¯ cholesterol pool, apoB/E receptor activity, LDL clearance. Large reduction of cholesterol and LDL. Little/no ¯ in TGs, little/no in HDL, no change in VLDL.
Absorption: Dist.: Metabolism.: Excretion, t½:
Toxicity/S.E.s: Common mild GI disturbances. Reversible elevations of liver enzymes in 4-7% (if AST or ALT > 3x normal, discontinue). Possible muscle damage—much more likely w/concurrent cyclosporine, gemfibrozil, niacin, or erythromycin; or if pt has hepatic disease, a severe infxn, or renal insufficiency. Continued use w/myopathy may ® severe myositis, rhabdomyolysis, or acute renal failure. Can shorten sleep period by up to 18%. C/i in kids & preg. E.
Utility: Treat hyperlipidemia IIA/IIB refractory to diet and other drugs. May not be useful for pts. w/homozygous familial hypercholesterolemia.
Special Features: Most effective drug class for lowering LDL. Probably better tolerated than other cholesterol lowering drugs. Synergistic effects w/resins and niacin. If taken once/day, take at night (peak cholesterol synth. occurs between 12:00-3:00 a.m.).