MEVACOR- lovastatin tablet
Merck Sharp & Dohme Corp.
DESCRIPTION
MEVACOR� (Lovastatin) is a cholesterol lowering agent isolated from a strain of Aspergillus terreus. After oral ingestion, lovastatin, which is an inactive lactone, is hydrolyzed to the corresponding ??hydroxyacid form. This is a principal metabolite and an inhibitor of 3?hydroxy-3?methylglutaryl-coenzyme A (HMG?CoA) reductase. This enzyme catalyzes the conversion of HMG?CoA to mevalonate, which is an early and rate limiting step in the biosynthesis of cholesterol.
Lovastatin is [1S -[1?(R *),3?,7?,8?(2S *,4S *), 8a?]]-1,2,3,7, 8,8a?hexahydro-3,7?dimethyl-8-[2?(tetrahydro-4-hydroxy-6-oxo-2H -pyran-2?yl)ethyl]-1-naphthalenyl 2-methylbutanoate. The empirical formula of lovastatin is C24 H36 O5 and its molecular weight is 404.55
Lovastatin is a white, nonhygroscopic crystalline powder that is insoluble in water and sparingly soluble in ethanol, methanol, and acetonitrile.
Tablets MEVACOR are supplied as 20 mg and 40 mg tablets for oral administration. In addition to the active ingredient lovastatin, each tablet contains the following inactive ingredients: cellulose, lactose, magnesium stearate, and starch. Butylated hydroxyanisole (BHA) is added as a preservative. Tablets MEVACOR 20 mg also contain FD&C Blue 2 aluminum lake. Tablets MEVACOR 40 mg also contain D&C Yellow 10 aluminum lake and FD&C Blue 2 aluminum lake.
CLINICAL PHARMACOLOGY
The involvement of low-density lipoprotein cholesterol (LDL?C) in atherogenesis has been well-documented in clinical and pathological studies, as well as in many animal experiments. Epidemiological and clinical studies have established that high LDL?C and low high-density lipoprotein cholesterol (HDL?C) are both associated with coronary heart disease. However, the risk of developing coronary heart disease is continuous and graded over the range of cholesterol levels and many coronary events do occur in patients with total cholesterol (total?C) and LDL?C in the lower end of this range.
MEVACOR has been shown to reduce elevated LDL?C concentrations. LDL is formed from very low-density lipoprotein (VLDL) and is catabolized predominantly by the high affinity LDL receptor. The mechanism of the LDL-lowering effect of MEVACOR may involve both reduction of VLDL?C concentration, and induction of the LDL receptor, leading to reduced production and/or increased catabolism of LDL?C. Apolipoprotein B also falls during treatment with MEVACOR.
MEVACOR is a specific inhibitor of HMG?CoA reductase, the enzyme which catalyzes the conversion of HMG?CoA to mevalonate. The conversion of HMG?CoA to mevalonate is an early step in the biosynthetic pathway for cholesterol.
INDICATIONS AND USAGE
Therapy with MEVACOR should be a component of multiple risk factor intervention in those individuals with dyslipidemia at risk for atherosclerotic vascular disease. MEVACOR should be used in addition to a diet restricted in saturated fat and cholesterol as part of a treatment strategy to lower total?C and LDL?C to target levels when the response to diet and other nonpharmacological measures alone has been inadequate to reduce risk.
Primary Prevention of Coronary Heart Disease
In individuals without symptomatic cardiovascular disease, average to moderately elevated total?C and LDL?C, and below average HDL?C, MEVACOR is indicated to reduce the risk of:
- Myocardial infarction
- Unstable angina- Coronary revascularization procedures
Hypercholesterolemia
Therapy with lipid-altering agents should be a component of multiple risk factor intervention in those individuals at significantly increased risk for atherosclerotic vascular disease due to hypercholesterolemia. MEVACOR is indicated as an adjunct to diet for the reduction of elevated total?C and LDL?C levels in patients with primary hypercholesterolemia (Types IIa and IIb 2), when the response to diet restricted in saturated fat and cholesterol and to other nonpharmacological measures alone has been inadequate