(Reduce the amount of LDL cholesterol in blood)
Chemical Name of Lovastatin: [1 S -[1(alpha)( R *),3(alpha),7(beta),8(beta)(2 S *,4 S *),8a(beta)]]-1,2,3, 7,8,8a-hexahydro-3,7-dimethyl-8-[2-(tetrahydro-4-hydroxy-6-oxo-2 H -pyran-2-yl)ethyl]-1-naphthalenyl 2-methylbutanoate
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 (beta)-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 an HMG CoA reductase inhibitor. Lovastatin blocks the production of cholesterol (a type of fat) in the body.
Lovastatin is used to reduce the amounts of LDL (bad) cholesterol and total cholesterol in the blood. These actions are important in the prevention of heart disease and hardening of the arteries, which can lead to heart attack, stroke, and peripheral vascular disease .
Lovastatin may also be used for purposes other than those listed in this medication guide.
Lovastatin is [1 S -[1(alpha)( R *),3(alpha),7(beta),8(beta)(2 S *,4 S *),8a(beta)]]-1,2,3, 7,8,8a-hexahydro-3,7-dimethyl-8-[2-(tetrahydro-4-hydroxy-6-oxo-2 H -pyran-2-yl)ethyl]-1-naphthalenyl 2-methylbutanoate. The empirical formula of lovastatin is C 24 H 36 O 5 and its molecular weight is 404.55. Its structural formula is:
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 10 mg, 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 10 mg also contain red ferric oxide and yellow ferric oxide. Tablets MEVACOR 20 mg also contain FD&C Blue 2. Tablets MEVACOR 40 mg also contain D&C Yellow 10 and FD&C Blue 2.
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After oral administration of MEVACOR to mice the median lethal dose observed was >15 g/m 2 .
Five healthy human volunteers have received up to 200 mg of lovastatin as a single dose without clinically significant adverse experiences. A few cases of accidental overdosage have been reported; no patients had any specific symptoms, and all patients recovered without sequelae. The maximum dose taken was 5-6 g.
Until further experience is obtained, no specific treatment of overdosage with MEVACOR can be recommended.
The dialyzability of lovastatin and its metabolites in man is not known at present.
DOSAGE AND ADMINISTRATION
The patient should be placed on a standard cholesterol-lowering diet before receiving MEVACOR and should continue on this diet during treatment with MEVACOR (see NCEP Treatment Guidelines for details on dietary therapy). MEVACOR should be given with meals.
The usual recommended starting dose is 20 mg once a day given with the evening meal. The recommended dosing range is 10-80 mg/day in single or two divided doses; the maximum recommended dose is 80 mg/day. Doses should be individualized according to the recommended goal of therapy. Patients requiring reductions in LDL-C of 20% or more to achieve their goal should be started on 20 mg/day of MEVACOR. A starting dose of 10 mg may be considered for patients requiring smaller reductions. Adjustments should be made at intervals of 4 weeks or more.
Cholesterol levels should be monitored periodically and consideration should be given to reducing the dosage of MEVACOR if cholesterol levels fall significantly below the targeted range.
Dosage in Patients taking Cyclosporine or Danazole
In patients taking cyclosporine or danazol concomitantly with lovastatin, therapy should begin with 10 mg of MEVACOR and should not exceed 20 mg/day.
Dosage in Patients taking Amiodarone or Verapamil
In patients taking amiodarone or verapamil concomitantly with MEVACOR, the dose should not exceed 40 mg/day
Adolescent Patients (10-17 years of age) with Heterozygous Familial Hypercholesterolemia
The recommended dosing range is 10-40 mg/day; the maximum recommended dose is 40 mg/day. Doses should be individualized according to the recommended goal of therapy. Patients requiring reductions in LDL-C of 20% or more to achieve their goal should be started on 20 mg/day of MEVACOR. A starting dose of 10 mg may be considered for patients requiring smaller reductions. Adjustments should be made at intervals of 4 weeks or more.