displayName: DESCRIPTION SECTION
FDA Article Code: 34089-3
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 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 is [1 S -[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 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.
Lovastatin tablets are supplied as 10 mg, 20 mg and 40 mg tablets for oral administration. In addition, each tablet contains the following inactive ingredients: lactose monohydrate, magnesium stearate, microcrystalline cellulose, poloxamer, pregelatinized starch, sodium starch glycolate, butylated hydroxyaniso and talc. Butylated hydroxyanisole (BHA) is added as a preservative.
displayName: CLINICAL PHARMACOLOGY SECTION
FDA Article Code: 34090-1
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.
Lovastatin has been shown to reduce both normal and 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 lovastatin 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 substantially during treatment with lovastatin. Since each LDL particle contains one molecule of apolipoprotein B, and since little apolipoprotein B is found in other lipoproteins, this strongly suggests that lovastatin does not merely cause cholesterol to be lost from LDL, but also reduces the concentration of circulating LDL particles. In addition, lovastatin can produce increases of variable magnitude in HDL-C, and modestly reduces VLDL-C and plasma triglycerides (TG) (see Tables I–III under
). The effects of lovastatin on Lp (a), fibrinogen, and certain other independent biochemical risk markers for coronary heart disease are unknown.
Lovastatin 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
displayName: INDICATIONS & USAGE SECTION
FDA Article Code: 34067-9
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:
(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.
- Myocardial infarction
- Unstable angina
- Coronary revascularization procedures
displayName: CONTRAINDICATIONS SECTION
FDA Article Code: 34070-3
Hypersensitivity to any component of this medication.
Active liver disease or unexplained persistent elevations of serum transaminases (see WARNINGS ).
displayName: ADVERSE REACTIONS SECTION
FDA Article Code: 34084-4
Lovastatin is generally well tolerated; adverse reactions usually have been mild and transient.
displayName: OVERDOSAGE SECTION
FDA Article Code: 34088-5
After oral administration of lovastatin 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 lovastatin can be recommended.
The dialyzability of lovastatin and its metabolites in man is not known at present.
DOSAGE AND ADMINISTRATION
displayName: DOSAGE & ADMINISTRATION SECTION
FDA Article Code: 34068-7
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.
displayName: HOW SUPPLIED SECTION
FDA Article Code: 34069-5
Lovastatin Tablets USP (white to off white round, unscored tablets) containing 10mg of lovastatin and engraved with “CTI; 141″
Repackaged by Aphena Pharma Solutions – TN.
for available configurations.
Bottle of 90 (NDC 42291-375-90)
Lovastatin Tablets USP (white to off white round, unscored tablets) containing 20mg of lovastatin and engraved with “CTI; 142”
Bottle of 90 (NDC 42291-376-90)
Lovastatin Tablets USP (white to off white round, unscored tablets) containing 40mg of lovastatin and engraved with “CTI; 143”
Bottle of 90 (NDC 42291-377-90)
Bottle of 1000 (NDC 42291-377-10)
displayName: STORAGE AND HANDLING SECTION
FDA Article Code: 44425-7
Store at 20º-25º C (68º-77º F). [See USP Controlled Room Temperature.] Lovastatin Tablets must be protected from light and stored in a well-closed, light-resistant container.
Carlsbad Technology, Inc.
Carlsbad, CA 92008
Pulaski, TN 38478
CTI-13 REV B
displayName: SPL UNCLASSIFIED SECTION
FDA Article Code: 42229-5
Please reference the
section listed above for a description of individual tablets or capsules. This drug product has been received by Aphena Pharma – TN in a manufacturer or distributor packaged configuration and repackaged in full compliance with all applicable cGMP regulations. The package configurations available from Aphena are listed below:
Store between 20°-25°C (68°-77°F). See USP Controlled Room Temperature. Dispense in a tight light-resistant container as defined by USP. Keep this and all drugs out of the reach of children.
Cookeville, TN 38506
PRINCIPAL DISPLAY PANEL – 40mg
displayName: PACKAGE LABEL.PRINCIPAL DISPLAY PANEL
FDA Article Code: 51945-4
NDC 43353-763 – Lovastatin 40mg – Rx Only