Lovastatin

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Induces
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Lovastatin, Mevacor; Bulgaria: Holetar, Lipopres, Medostatin; Cyprus: Lomar, Lovaren, Lovastatin, Medostatin; Czech Republic: Lovastatin, Medostatin; Denmark: Lovastatin; Finland: Lovacol, Lovastatin; Germany: Lovabeta, Lovadura, Lovagamma, Lovahexal, Lovastatin, Mevacor, Mevinacor; Greece: Liferzit, Lipidless, Lostin, Lovatex, Lovatop, Lowlipid, Medovascin, Mevacor, Mevastin, Misodomin, Nabicortin, Terveson, Velkalov, Viking; Hungary: Mevacor, Stoplip; Latvia: Lovasterol; Malta: Medostatin; Poland: Anlostin, Apo-Lova, Holetar, Liprox, Lovastatinum, Lovasterol, Lovastin, Lowastatyna, Mevacor; Portugal: Flozul, Lipdaune, Lipus, Lovastatina, Mevinacor, Mevlor, Tecnolip; Romania: Lovastatin, Lovastatina, Medostatin; Slovakia: Medostatin; Slovenia: Holetar; Spain: Aterkey, Colesvir, Liposcler, Lovastatina, Mevacor, Nergadan, Taucor.

North America

Canada: Lovastatin, Mevacor; USA: Altoprev, Lovastatin, Mevacor.

Latin America

Argentina: Hipovastin; Brazil: Lipoclin, Lovastatina, Mevacor, Mevalip, Reducol; Mexico: Casbame, Dilucid, Liperol, Mevacor.

Drug combinations

Lovastatin and Niacin (Vitamin B~3~)

Chemistry

Lovastatin: C~24~H~36~O~5~. Mw: 404.54. (1) Butanoic acid, 2-methyl-, 1,2,3,7,8,8a-hexahydro-3,7-dimethyl-8-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1-naphthalenyl ester, [1S-[1α(R*),3α,7β,8β(2S*,4S*),8aβ]]-; (2)(S)-2-Methylbutyric acid, 8-ester with (4R,6R)-6-[2-[(1S,2S,6R,8S,8aR)-1,2,6,7,8,8a-hexahydro-8-hydroxy-2,6-dimethyl-1-naphthyl]ethyl]tetrahydro-4-hydroxy-2H-pyran-2-one. CAS-75330-75-5 (1987).

Pharmacologic Category

Antilipemic Agents; HMG-CoA Reductase Inhibitors. (ATC-Code: C10AA02).

Mechanism of action

Acts by competitively inhibiting 3-hydroxyl-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, enzyme which catalyzes rate-limiting step in cholesterol biosynthesis.

Therapeutic use

Adjunct to dietary therapy to decrease elevated serum total and LDL-C concentrations in primary hypercholesterolemia. Primary prevention of coronary artery disease (patients without symptomatic disease with average to moderately elevated total and LDL-C and below average HDL-C). Slow progression of coronary atherosclerosis in coronary heart disease. Adjunct to dietary therapy in adolescent patients (10-17 years of age, females >1 year postmenarche) with heterozygous familial hypercholesterolemia having LDL>189 mg/dL, or LDL>160 mg/dL with positive family history of premature cardiovascular disease, or LDL>160 mg/dL with presence of at least two other CVD risk factors.

Pregnancy and lactiation implications

Cholesterol biosynthesis may be important in fetal development. Contraindicated in pregnancy or while breast-feeding.

Unlabeled use

Contraindications

Hypersensitivity to lovastatin or any component of the formulation. Active liver disease. Unexplained persistent elevations of serum transaminases. Pregnancy. Breast-feeding.

Warnings and precautions

Patients receiving HMG-CoA reductase inhibitors developed rhabdomyolysis with acute renal failure and/or myopathy. Use caution in renal impairment, inadequately treated hypothyroidism, and patients taking other drugs associated with myopathy (e.g. colchicine). Use with caution in hepatic impairment and/or ethanol use. High potential for CYP-mediated interactions. Use with caution in the elderly (predisposed to myopathy). Secondary causes of hyperlipidemia should be ruled out prior to therapy.

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