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Drug Catalog - Product Detail

LOVASTATIN, USP TB 40MG 500

NDC Mfr Size Str Form
45963-0635-04 ACTAVIS 500 40MG TABLET
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Description
DESCRIPTION Lovastatin, USP 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 β-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, USP is [1S-[1α( R * ),3α,7β,8β(2 S * ,4 S * ), 8aβ]]-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 molecular formula of lovastatin is C 24 H 36 O 5 and its molecular weight is 404.55. Its structural formula is: Lovastatin, USP is a white, nonhygroscopic crystalline powder that is insoluble in water and sparingly soluble in ethanol, methanol, and acetonitrile. Each tablet for oral administration, contains 10 mg, 20 mg, or 40 mg of lovastatin, USP. In addition, each tablet contains the following inactive ingredients: lactose monohydrate, magnesium stearate, microcrystalline cellulose, and pregelatinized starch (corn). Butylated hydroxyanisole is added as a preservative. The 20 mg tablet also contains D&C Red #30 aluminum lake. The 40 mg tablet also contains D&C Yellow #10 HT aluminum lake. a643ae4b-figure-01
How Supplied
HOW SUPPLIED Lovastatin Tablets, USP are available as follows: 10 mg — Each white, round, flat faced beveled edge tablet debossed with on one side and 633 on the other side contains 10 mg of lovastatin, USP. Tablets are supplied in bottles of 60 (NDC 45963-633-01) and 500 (NDC 45963-633-04). 20 mg — Each pink, round, flat faced beveled edge tablet debossed with on one side and 634 on the other side contains 20 mg of lovastatin, USP. Tablets are supplied in bottles of 60 (NDC 45963-634-01) and 500 (NDC 45963-634-04). 40 mg — Each yellow, round, flat faced beveled edge tablet debossed with on one side and 635 on the other side contains 40 mg of lovastatin, USP. Tablets are supplied in bottles of 60 (NDC 45963-635-01) and 500 (NDC 45963-635-04). Dispense in a tight, light-resistant container as defined in the USP. Store between 5° to 25°C (41° to 77°F). Protect from light and store in a well-closed, light-resistant container. Manufactured by: Actavis Elizabeth LLC Elizabeth, NJ 07207 USA Distributed by: Actavis Pharma, Inc. Parsippany, NJ 07054 USA 40-9186 Rev. A 6/2020 a643ae4b-figure-03 a643ae4b-figure-04 a643ae4b-figure-05
Indications & Usage
INDICATIONS AND USAGE Therapy with lovastatin should be a component of multiple risk factor intervention in those individuals with dyslipidemia at risk for atherosclerotic vascular disease. Lovastatin 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, lovastatin is indicated to reduce the risk of: - Myocardial infarction - Unstable angina - Coronary revascularization procedures (See CLINICAL PHARMACOLOGY, Clinical Studies .) Coronary Heart Disease Lovastatin is indicated to slow the progression of coronary atherosclerosis in patients with coronary heart disease as part of a treatment strategy to lower total-C and LDL-C to target levels. 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. Lovastatin 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 IIb2), when the response to diet restricted in saturated fat and cholesterol and to other nonpharmacological measures alone has been inadequate. 2 Classification of Hyperlipoproteinemias Lipid Lipoproteins Elevations Type elevated major minor I chylomicrons TG ↑→C IIa LDL C — IIb LDL, VLDL C TG III (rare) IDL C/TG — IV VLDL TG ↑→C V (rare) chylomicrons, VLDL TG ↑→C IDL = intermediate-density lipoprotein. Adolescent Patients with Heterozygous Familial Hypercholesterolemia Lovastatin is indicated as an adjunct to diet to reduce total-C, LDL-C and apolipoprotein B levels in adolescent boys and girls who are at least one year post-menarche, 10 to 17 years of age, with heFH if after an adequate trial of diet therapy the following findings are present: LDL-C remains greater than 189 mg/dL or LDL-C remains greater than 160 mg/dL and: there is a positive family history of premature cardiovascular disease or two or more other CVD risk factors are present in the adolescent patient General Recommendations Prior to initiating therapy with lovastatin, secondary causes for hypercholesterolemia (e.g., poorly controlled diabetes mellitus, hypothyroidism, nephrotic syndrome, dysproteinemias, obstructive liver disease, other drug therapy, alcoholism) should be excluded, and a lipid profile performed to measure total-C, HDL-C, and TG. For patients with TG less than 400 mg/dL (less than 4.5 mmol/L), LDL-C can be estimated using the following equation: LDL-C = total-C – [0.2 × (TG) + HDL-C] For TG levels greater than 400 mg/dL (greater than 4.5 mmol/L), this equation is less accurate and LDL-C concentrations should be determined by ultracentrifugation. In hypertriglyceridemic patients, LDL-C may be low or normal despite elevated total-C. In such cases, lovastatin is not indicated. The National Cholesterol Education Program (NCEP) Treatment Guidelines are summarized below: NCEP Treatment Guidelines: LDL-C Goals and Cutpoints for Therapeutic Lifestyle Changes and Drug Therapy in Different Risk Categories Risk Category LDL Goal Initiate Therapeutic Lifestyle Changes Consider Drug Therapy (mg/dL) (mg/dL) (mg/dL) LDL Level at Which to LDL Level at Which to CHD † or CHD risk equivalents <100 ≥100 ≥130 (10-year risk >20%) (100-129: drug optional) †† 2 + Risk factors <130 ≥ 130 10-year risk 10 to 20%: ≥130 (10 year risk ≤20%) 10-year risk <10%: ≥160 0 to 1 Risk factor ††† <160 ≥ 160 ≥ 190 (160 to 189: LDL-lowering drug optional) † CHD, coronary heart disease †† Some authorities recommend use of LDL-lowering drugs in this category if an LDL-C level of <100 mg/dL cannot be achieved by therapeutic lifestyle changes. Others prefer use of drugs that primarily modify triglycerides and HDL-C, e.g., nicotinic acid or fibrate. Clinical judgment also may call for deferring drug therapy in this subcategory. ††† Almost all people with 0 to 1 risk factor have a 10-year risk <10%; thus, 10-year risk assessment in people with 0 to 1 risk factor is not necessary. After the LDL-C goal has been achieved, if the TG is still greater than or equal to 200 mg/dL, non-HDL-C (total-C minus HDL-C) becomes a secondary target of therapy. Non-HDL-C goals are set 30 mg/dL higher than LDL-C goals for each risk category. At the time of hospitalization for an acute coronary event, consideration can be given to initiating drug therapy at discharge if the LDL-C is greater than or equal to 130 mg/dL (see NCEP Guidelines above). Since the goal of treatment is to lower LDL-C, the NCEP recommends that LDL-C levels be used to initiate and assess treatment response. Only if LDL-C levels are not available, should the total-C be used to monitor therapy. Although lovastatin may be useful to reduce elevated LDL-C levels in patients with combined hypercholesterolemia and hypertriglyceridemia where hypercholesterolemia is the major abnormality (Type IIb hyperlipoproteinemia), it has not been studied in conditions where the major abnormality is elevation of chylomicrons, VLDL or IDL (i.e., hyperlipoproteinemia types I, III, IV, or V). 2 The NCEP classification of cholesterol levels in pediatric patients with a familial history of hypercholesterolemia or premature cardiovascular disease is summarized below: Category Total-C (mg/dL) LDL-C (mg/dL) Acceptable <170 <110 Borderline 170 to 199 110 to 129 High ≥200 ≥130 Children treated with lovastatin in adolescence should be re-evaluated in adulthood and appropriate changes made to their cholesterol-lowering regimen to achieve adult goals for LDL-C.
Dosage and Administration
DOSAGE AND ADMINISTRATION The patient should be placed on a standard cholesterol-lowering diet before receiving lovastatin and should continue on this diet during treatment with lovastatin (see NCEP Treatment Guidelines for details on dietary therapy). Lovastatin should be given with meals. Adult Patients The usual recommended starting dose is 20 mg once a day given with the evening meal. The recommended dosing range of lovastatin is 10 to 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 (see NCEP Guidelines and CLINICAL PHARMACOLOGY ). Patients requiring reductions in LDL-C of 20% or more to achieve their goal (see INDICATIONS AND USAGE ) should be started on 20 mg/day of lovastatin. A starting dose of 10 mg of lovastatin may be considered for patients requiring smaller reductions. Adjustments should be made at intervals of 4 weeks or more. The 10 mg dosage is provided for information purposes only. Although lovastatin tablets 10 mg are available in the marketplace, lovastatin is no longer marketed in the 10 mg strength. Cholesterol levels should be monitored periodically and consideration should be given to reducing the dosage of lovastatin if cholesterol levels fall significantly below the targeted range. Dosage in Patients taking Danazol, Diltiazem, Dronedarone or Verapamil In patients taking danazol, diltiazem, dronedarone or verapamil concomitantly with lovastatin, therapy should begin with 10 mg of lovastatin and should not exceed 20 mg/day (see CLINICAL PHARMACOLOGY, Pharmacokinetics , WARNINGS, Myopathy/Rhabdomyolysis , PRECAUTIONS, Drug Interactions, Other Drug Interactions ). Dosage in Patients taking Amiodarone In patients taking amiodarone concomitantly with lovastatin, the dose should not exceed 40 mg/day (see WARNINGS, Myopathy/Rhabdomyolysis and PRECAUTIONS, Drug Interactions, Other Drug Interactions ). Adolescent Patients (10 to 17 years of age) with Heterozygous Familial Hypercholesterolemia The recommended dosing range of lovastatin is 10 to 40 mg/day; the maximum recommended dose is 40 mg/day. Doses should be individualized according to the recommended goal of therapy (see NCEP Pediatric Panel Guidelines4, CLINICAL PHARMACOLOGY , and INDICATIONS AND USAGE ). Patients requiring reductions in LDL-C of 20% or more to achieve their goal should be started on 20 mg/day of lovastatin. A starting dose of 10 mg of lovastatin may be considered for patients requiring smaller reductions. Adjustments should be made at intervals of 4 weeks or more. 4 National Cholesterol Education Program (NCEP): Highlights of the Report of the Expert Panel on Blood Cholesterol Levels in Children and Adolescents. Pediatrics . 89(3):495-501. 1992 Concomitant Lipid-Lowering Therapy Lovastatin is effective alone or when used concomitantly with bile-acid sequestrants (see WARNINGS, Myopathy/Rhabdomyolysis and PRECAUTIONS, Drug Interactions ). Dosage in Patients with Renal Insufficiency In patients with severe renal insufficiency (creatinine clearance less than 30 mL/min), dosage increases above 20 mg/day should be carefully considered and, if deemed necessary, implemented cautiously (see CLINICAL PHARMACOLOGY and WARNINGS, Myopathy/Rhabdomyolysis ).