Lovastatin
(British Approved Name, US Adopted Name, rINN)
Drug Nomenclature
International Nonproprietary Names (INNs) in main languages (French, Latin, Russian, and Spanish):
Pharmacopoeias. In Europe and US.
European Pharmacopoeia, 6th ed., 2008 and Supplements 6.1 and 6.2 (Lovastatin). A white or almost white crystalline powder. Practically insoluble in water; sparingly soluble in dehydrated alcohol; soluble in acetone. Store under nitrogen at a temperature of 2° to 8°.
The United States Pharmacopeia 31, 2008, and Supplements 1 and 2 (Lovastatin). A white to off-white crystalline powder. Insoluble in water; sparingly soluble in alcohol; practically insoluble in petroleum spirit; freely soluble in chloroform; soluble in acetone, in acetonitrile, and in methyl alcohol. Store under nitrogen in airtight containers at a temperature not exceeding 8°.
Adverse Effects and Precautions
As for Simvastatin.
Incidence of adverse effects. Adverse effects led to withdrawal of lovastatin in 21 of 745 patients receiving the drug for about 5 years. They included asymptomatic elevation of hepatic aminotransferases in 10 patients, gastrointestinal symptoms in 3, rash in 2, myopathy in 2, myalgia in 1, arthralgia in 1, insomnia in 1, and weight gain in 1.
Interactions
As for Simvastatin.
For specific dosage reductions in patients taking lovastatin with interacting drugs, see Uses and Administration, below.
Pharmacokinetics
Lovastatin is absorbed from the gastrointestinal tract and must be hydrolysed to its active p-hydroxyacid form. Three other metabolites have also been isolated. Lovastatin is a substrate for the cytochrome P450 isoenzyme CYP3A4 and undergoes extensive first-pass metabolism in the liver, its primary site of action; less than 5% of an oral dose has been reported to reach the circulation. Peak plasma concentrations occur within 2 to 4 hours, and steady-state concentrations are achieved after 2 to 3 days with daily dosage. Both lovastatin and its p-hydroxyacid metabolite are more than 95% bound to plasma proteins. Lovastatin is mainly excreted in the bile as metabolites; about 85% of a dose has been recovered from the faeces and about 10% from the urine. The half-life of the active metabolite is 1 to 2 hours.
Uses and Administration
Lovastatin, a 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor (a statin), is a lipid regulating drug with actions on plasma lipids similar to those of simvastatin.
Lovastatin is used to reduce cholesterol in the treatment of hyperlipidaemias, particularly in type IIa and IIb hyperlipoproteinaemias. It is also given for cardiovascular risk reduction in both primary and secondary prevention of ischaemic heart disease. Lovastatin is given in an initial oral dose of 10 to 20 mg daily in the evening with food, increased, if necessary, at intervals of 4 weeks or more to 80 mg daily as a single dose or in 2 divided doses. Lower doses of lovastatin should be used in patients at risk of myopathy, including patients with severe renal impairment (see below) and those taking drugs that interact with lovastatin; an initial dose of 10 mg daily is recommended in patients taking ciclosporin or danazol, and the daily dose should not exceed 20 mg in patients taking ciclosporin, danazol, fibric acid derivatives, or nicotinic acid, or 40 mg in those taking amiodarone or verapamil.
For the use of lovastatin in children, see below.
Administration in children. Lovastatin reduces plasma-cholesterol concentrations in children and adolescents with heterozygous familial hypercholesterolaemia and has been given safely for up to 48 weeks in boys, and up to 24 weeks in girls. In the USA it is licensed in children aged 10 to 17 years and is given orally in an initial dose of 10 to 20 mg once daily, increased at intervals of 4 weeks or more, if necessary, to a maximum dose of 40 mg once daily.
Administration in renal impairment. Patients with renal impairment may be at increased risk of myopathy and US licensed product information states that doses of lovastatin above 20 mg daily should be used cautiously in patients with a creatinine clearance below 30 mL/minute.
Adrenoleucodystrophy. A preliminary study has shown that lovastatin may be useful in the treatment of adrenoleucodystrophy (see under Lorenzo’s Oil). Lovastatin reduced the plasma levels of very-long-chain fatty acids which are known to be elevated in patients with this rare metabolic disorder.
Preparations
The United States Pharmacopeia 31, 2008, and Supplements 1 and 2: Lovastatin Tablets.
Single-ingredient Preparations
The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed
Argentina: Hipovastin; Loriter¤; Mevlor; Sivlor; Austria: Mevacor; Brazil: Lovasc¤; Lovast; Lovaton; Lovax; Mevacor; Minor; Neolipid; Reducol; Canada: Mevacor; Chile: Colevix¤; Hiposterol; Lispor; Lovacol; Mevacor; Nij-Terol¤; Sanelor; Czech Republic: Holetar; Lovacard; Medostatin; Mevacor; Denmark: Lipivas¤; Lovacodan; Mevacor; Finland: Lovacol; Mevacor; Germany: Lova; Lovabeta; Lovadura; Lovagamma; Lovahexal; Mevinacor; Greece: Aurostatin; B-Lovatin¤; Cecural; Ilopar; Liferzit; Lipidless; Lovadrug; Lovapen; Lovasten; Lovatex; Lovatop; Lowlipid; Medovascin; Mevacor; Mevastin; Mevinol¤; Misodomin; Nabicortin; Terveson; Velkalov; Viking; Hong Kong: Ellanco; Lofacol; Lomar; Medostatin; Mevacor; Hungary: Mevacor; India: Lovacard; Pro-HDL; Rovacor; Israel: Lovalip¤; Malaysia: Lestric; Lostatin; Lovastin; Medostatin; Mevacor¤; Mexico: Casbame; Dilucid; Liperol; Mevacor; Norway: Mevacor; Portugal: Lipdaune; Lipus; Mevinacor; Mevlor; Tecnolip; Russia: Cardiostatin (Кардиостатин); Holetar (Холетар); Lovasterol (Ловастерол); Medostatin (Медостатин); Rovacor (Ровакор); Singapore: Elstatin; Lostatin; Medostatin; Rovacor; Spain: Aterkey; Colesvir; Lipofren¤; Liposcler; Mevacor; Mevasterol; Nergadan; Taucor; United States: Altoprev; Mevacor; Venezuela: Dislipin; Levistan; Lostatin; Lovanil; Lovas; Mevacor
Multi-ingredient Preparations
United States: Advicor
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