Lovastatin Tablet USP, Revision H

/Lovastatin Tablet USP, Revision H
Lovastatin Tablet USP, Revision H2018-09-06T09:12:40+00:00

Prescription Drug Name:

Lovastatin Tablet USP, Revision H

ID:

c195fb1e-6c9a-4471-9b95-5aa70a9bb5d1

Code:

34391-3

DESCRIPTION


id: 27426ce6-1a75-4dee-9928-43f31e653ca4
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 to the active ingredient lovastatin, 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.

CLINICAL PHARMACOLOGY


id: b87d6ae5-7e7b-4261-91bf-7c9c60006466
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 during treatment with lovastatin. 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


id: 5b66dfb7-a6a4-4e3d-947c-28567dd99092
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.

CONTRAINDICATIONS


id: 4f63b369-21d1-4f7d-94eb-0c7d09972db3
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 ). Concomitant administration with strong CYP3A4 inhibitors (e.g., itraconazole, ketoconazole, posaconazole, voriconazole, HIV protease inhibitors, boceprevir, telaprevir, erythromycin, clarithromycin, telithromycin ,nefazodone, and cobicistat-containing products) (see WARNINGS,
Myopathy/Rhabdomyolysis)
.

ADVERSE REACTIONS


id: 5a0bfd4c-7042-485e-b432-f7c045809191
displayName: ADVERSE REACTIONS SECTION
FDA Article Code: 34084-4

____________________________________ 3 Manson, J.M., Freyssinges, C., Ducrocq, M.B., Stephenson, W.P., Postmarketing Surveillance of Lovastatin and Simvastatin Exposure During Pregnancy.
Reproductive Toxicology. 10(6):439-446. 1996.

OVERDOSAGE


id: d25c9b91-dfc8-44ca-998a-c972a5378fe7
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 to 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


id: 7f726df1-5603-4e4d-ae44-43979bda79b9
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.

Dosage in Patients taking Danazol, Diltiazem, Dronedarone, or Verapamil


id: 03ee24e4-0404-4663-9059-cc023c7c640a
displayName: SPL UNCLASSIFIED SECTION
FDA Article Code: 42229-5

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 ).

HOW SUPPLIED


id: efe39b16-e327-4b8b-9ed6-f96ff9a500fa
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 —-Bottle of 60 (NDC 61442-141-60), Bottle of 90 (NDC 61442-141-90), Bottle of 100 (NDC 61442-141-01), Bottle of 500 (NDC 61442-141-05), Bottle of 1,000 (NDC 61442-141-10) Lovastatin Tablets USP (white to off white round, unscored tablets) containing 20mg of lovastatin and engraved with “CTI” 142 —- Bottle of 60 (NDC 61442-142-60), Bottle of 90 (NDC 61442-142-90), Bottle of 100 (NDC 61442-142-01), Bottle of 500 (NDC 61442-142-05), Bottle of 1,000 (NDC 61442-142-10) Lovastatin Tablets USP (white to off white round, unscored tablets) containing 40mg of lovastatin and engraved with “CTI” 143 —- Bottle of 60 (NDC 61442-143-60), Bottle of 90 (NDC 61442-143-90), Bottle of 100 (NDC 61442-143-01), Bottle of 500 (NDC 61442-143-05), Bottle of 1,000 (NDC 61442-143-10) ____________________________________ 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.