Lovastatin

Indications

Lovastatin is used for: Coronary Artery Disease, Hyperlipidaemias

Adult Dose

Oral Hyperlipidaemias; Primary prophylaxis of coronary artery disease Adult: Initially, 10-20 mg/day in the evening, may increase at intervals of at least 4 wk to max 80 mg/day as a single or in 2 divided doses.

Child Dose

Oral Hyperlipidaemias; Primary prophylaxis of coronary artery disease Child: As an adjunct w/ heterozygous familial hypercholesterolaemia: 10-17 yr Initially, 10-20 mg once daily, may increase at intervals of 4 wk to max 40 mg once daily.

Renal Dose

Renal impairment: CrCl (ml/min) Dosage Recommendation <30 Use w/ caution in doses >20 mg/day.

Administration

Should be taken with food.

Contra Indications

Active liver disease or unexplained persistent elevated serum transaminases. Concomitant use w/ CYP3A4 inhibitors (e.g. nefazodone, erythromycin, boceprevir, clarithromycin, telithromycin, HIV protease inhibitors, itraconazole, ketoconazole, posaconazole, telaprevir), gemfibrozil, ciclosporin. Pregnancy and lactation.

Precautions

History of liver disease; patients at risk of myopathy; alcoholism; inadequately controlled hypothyroidism. Severe renal impairment. Monitoring Parameters Monitor creatine kinase (CK) periodically and LFT. Discontinue if there is significant or persistent increase in CK levels, serum aminotransferase levels or evidence of myopathy. Lactation: Contraindicated; unsafe

Pregnancy-Lactation

Pregnancy category: X Lactation: Contraindicated; unsafe

Interactions

Increased risk of myopathy/rhabdomyolysis w/ amiodarone, colchicine, ranolazine, danazol, diltiazem and verapamil. May increase anticoagulant effect of warfarin. Potentially Fatal: Increased risk of myopathy and rhabdomyolysis w/ concomitant CYP3A4 inhibitors (e.g. nefazodone, erythromycin, boceprevir, clarithromycin, telithromycin, HIV protease inhibitors, itraconazole, ketoconazole, posaconazole, telaprevir), gemfibrozil, ciclosporin.

Adverse Effects

Side effects of Lovastatin : >10% CPK elevation (11%) 1-10% Flatulence (4-5%), Abdominal pain (2-3%), Constipation (2-3%), Diarrhea (2-3%), Myalgia (2-3%), Nausea (2-3%), Dyspepsia (1-2%), Weakness (1-2%), Blurred vision (0.8-1%), Rash (0.8-1%), Muscle cramps (0.6-1%), Dizziness (0.5-1%) <1% Dermatomyositis, Increased LFTs, Hepatotoxicity, Myopathy, Rhabdomyolysis Potentially Fatal: Rhabdomyolysis and acute renal failure.

Mechanism of Action

Lovastatin reduces cholesterol by competitively inhibiting HMG-CoA reductase, the rate-limiting step cholesterol biosynthesis.