It is a competitive inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, the enzyme catalysing the early rate-limiting step in cholesterol biosynthesis. It affects modest reductions in intracellular pools of cholesterol which result is an increased number of LDL-receptors on cell surface, enhanced receptor-mediated catabolism and clearance of circulating low density lipoprotein cholesterol (LDL-C). It also inhibits LDL-C production by inhibiting hepatic synthesis of very low density lipoprotein (VLDL-C), the LDL-C precursor. These effects result in a reduction of total cholesterol (Total-C), LDL-C, VLDL-C, apolipoprotein B and triglycerides, whilst increasing high density liprotein cholesterol (HDL-C) and apoliprotein A.
Atherosclerosis related clinical events as a function of cholesterol level, the presence or absence of coronary heart disease, and other risk factors. Hyperlipidemia, Treatment of patients with primary dysbetalipoproteinemia (Fredrickson Type III).
Initial dose :10 to 20mg or 40mg once daily at bedtime.
Renal/Hepatic function impairment : A starting dose of 10mg/day at bedtime is recommended.
Hypersensitivity, acute liver disease or unexplained, persistent elevations in liver function tests.
Perform liver fuction test before initiating therapy and at 12 weeks thereafter. Monitor patients with renal impairment. May elevate creatine phosphokinase and transaminase levels.Pregnancy, Brest feeding.
Rash , myalgia, headache, non-cardiac chest pain, rarely nausea/vomiting, diarrhoea and fatigue may occur.
Bile acid sequestrants (BAS), Gemfibrozil.
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