LOVASTATIN tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

LOVASTATIN (UNII: 9LHU78OQFD) (LOVASTATIN - UNII:9LHU78OQFD)

Available from:

PD-Rx Pharmaceuticals, Inc.

INN (International Name):

LOVASTATIN

Composition:

LOVASTATIN 40 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

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. 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 .) 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. Therapy with lipid-altering agents should be a component of multiple risk factor intervention in those individuals at significantly increased risk for artherosclerotic 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 IIb 2 ), when the response to diet restricted in saturated fat and cholesterol and to other nonpharmacological measures alone has been inadequate. 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 >189 mg/dL or - LDL-C remains >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 - there is a positive family history of premature cardiovascular disease or - two or more other CVD risk factors are present in the adolescent patient 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 (<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 >400 mg/dL (>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: † 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 0-1 risk factor have a 10-year risk <10%; thus, 10-year risk assessment in people with 0-1 risk factor is not necessary. After the LDL-C goal has been achieved, if the TG is still ≥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 ≥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). *** The NCEP classification of cholesterol levels in pediatric patients with a familial history of hypercholesterolemia or premature cardiovascular disease is summarized below: 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. 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) . Pregnancy and lactation. ( see PRECAUTIONS, Pregnancy and Nursing Mothers).    Atherosclerosis is a chronic process and the discontinuation of lipid-lowering drugs during pregnancy should have little impact on the outcome of long-term therapy of primary hypercholesterolemia. Moreover, cholesterol and other products of the cholesterol biosynthesis pathway are essential components for fetal development, including synthesis of steroids and cell membranes. Because of the ability of inhibitors of HMG-CoA reductase such as lovastatin to decrease the synthesis of cholesterol and possibly other products of the cholesterol biosynthesis pathway, lovastatin is contraindicated during pregnancy and in nursing mothers. Lovastatin should be administered to women of childbearing age only when such patients are highly unlikely to conceive. If the patient becomes pregnant while taking this drug, lovastatin should be discontinued immediately and the patient should be apprised of the potential hazard to the fetus (see PRECAUTIONS, Pregnancy ).

Product summary:

Lovastatin Tablets USP (white to off white round, unscored tablets) containing 40mg of lovastatin and engraved with “CTI 143” Bottle of 14...............................................................................................(NDC 43063-548-14) Bottle of 30...............................................................................................(NDC 43063-548-30) Bottle of 90...............................................................................................(NDC 43063-548-90) Bottle of 180.............................................................................................(NDC 43063-548-93) Bottle of 1000...........................................................................................(NDC 43063-548-95) 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. Store at 20º to 25º C (68º to 77º F). [See USP Controlled Room Temperature.] Lovastatin Tablets must be protected from light and stored in a well-closed, light-resistant container.

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

LOVASTATIN- LOVASTATIN TABLET
PD-RX PHARMACEUTICALS, INC.
----------
LOVASTATIN TABLET USP
RX ONLY
DESCRIPTION
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
H
O
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 hydroxyanisole and talc. Butylated hydroxyanisole (BHA) is
added as a
preservative.
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
24
36
5
patients with total cholesterol (total-C) and LDL-C in the