Brands, Medical Use, Clinical Data
- Antineoplastic Agents
- Anticholesteremic Agents
- HMG-CoA Reductase Inhibitors
Brands / Synonyms
6 alpha-Methylcompactin; Advicor; Altocor; Altoprev; Artein; Belvas; Cholestra; Closterol; Colevix; Compactin; Hipolip; Hipovastin; Lestatin; Lipdip; Lipivas; Lipofren; Lovalip; Lovalord; Lovastatin [Usan:Ban:Inn]; Lovastatina [Spanish]; Lovastatine [French]; Lovastatinum [Latin]; Lovasterol; Lovastin; Lozutin; Mevacor; Mevastatin; Mevinacor; Mevinolin; Mevlor; Monacolin K; Nergadan; Paschol; Pravastatin; Rodatin; Rovacor; Sivlor; Taucor; Tecnolip; Teroltrat
For management as an adjunct to diet to reduce elevated total-C, LDL-C, apo B, and TG levels in patients with primary hypercholesterolemia and mixed dyslipidemia; For primary prevention of coronary heart disease
Lovastatin, an antilipemic agent produced by fermentation of Aspergillus terreus, is the first of a class of lipid-lowering agents known as the HMG-CoA reductase inhibitors. Lovastatin is used to treat hypercholesterolemia, to slow coronary atherosclerosis, and to prevent myocardial infarction and stroke. Lovastatin, like simvastin and unlike pravastatin, is a prodrug, concentrating active drug in the liver during first-pass circulation.
Mechanism of Action
Lovastatin is a lactone that is readily hydrolyzed in vivo to the corresponding b-hydroxyacid, a potent inhibitor of HMG-CoA reductase, the enzyme that 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.
LD50>1000 mg/kg (orally in mice)
Biotrnasformation / Drug Metabolism
Hypersensitivity to any component of this medication.
Active liver disease or unexplained persistent elevations of serum
Pregnancy and Lactation: 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
Lovastatin is metabolized by CYP3A4 but has no CYP3A4 inhibitory activity;
therefore it is not expected to affect the plasma concentrations of other
drugs metabolized by CYP3A4. Potent inhibitors of CYP3A4 (below) increase
the risk of myopathy by reducing the elimination of lovastatin.
HIV protease inhibitors
Large quantities of grapefruit juice (>1 quart daily)
Interactions with lipid-lowering drugs that can cause myopathy when given
The risk of myopathy is also increased by the following lipid-lowering drugs
that are not potent CYP3A4 inhibitors, but which can cause myopathy when given
See WARNINGS, Myopathy/Rhabdomyolysis.
Niacin (nicotinic acid) (=1 g/day)
Other drug interactions
Danazol: The risk of myopathy/rhabdomyolysis is increased by concomitant
administration of danazol particularly with higher doses of lovastatin (see
Amiodarone or Verapamil: The risk of myopathy/rhabdomyolysis is increased when
either amiodarone or verapamil is used concomitantly with a closely related
member of the HMG-CoA reductase inhibitor class (see WARNINGS, Myopathy/Rhabdomyolysis).
Coumarin Anticoagulants: In a small clinical trial in which lovastatin was administered
to warfarin treated patients, no effect on prothrombin time was detected. However,
another HMG-CoA reductase inhibitor has been found to produce a less than two-second
increase in prothrombin time in healthy volunteers receiving low doses of warfarin.
Also, bleeding and/or increased prothrombin time have been reported in a few patients
taking coumarin anticoagulants concomitantly with lovastatin. It is recommended that in
patients taking anticoagulants, prothrombin time be determined before starting lovastatin
and frequently enough during early therapy to insure that no significant alteration of
prothrombin time occurs.
Once a stable prothrombin time has been documented, prothrombin times can be monitored
at the intervals usually recommended for patients on coumarin anticoagulants. If the
dose of lovastatin is changed, the same procedure should be repeated. Lovastatin therapy
has not been associated with bleeding or with changes in prothrombin time in patients not
Propranolol: In normal volunteers, there was no clinically significant pharmacokinetic or
pharmacodynamic interaction with concomitant administration of single doses of lovastatin
Digoxin: In patients with hypercholesterolemia, concomitant administration of lovastatin
and digoxin resulted in no effect on digoxin plasma concentrations.
Oral Hypoglycemic Agents: In pharmacokinetic studies of MEVACOR in hypercholesterolemic
noninsulin dependent diabetic patients, there was no drug interaction with glipizide or