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Lovastatin is recommended in Primary Prevention of Coronary Heart Disease, Coronary Heart Disease, Hypercholesterolemia, Adolescent Patients with Heterozygous Familial Hypercholesterolemia
Lovastatin reduces cholesterol by competitively inhibiting HMG-CoA reductase, the rate-limiting step in cholesterol biosynthesis.
Lovastatin is structurally similar to the HMG, a substituent of the endogenous substrate of HMG-CoA reductase. Lovastatin is a prodrug that is activated in vivo via hydrolysis of the lactone ring to form the β-hydroxyacid. The hydrolyzed lactone ring mimics the tetrahedral intermediate produced by the reductase allowing the agent to bind to HMG-CoA reductase with 20,000 times greater affinity than its natural substrate. The bicyclic portion of lovastatin binds to the coenzyme A portion of the active site.
The patient should be placed on a standard cholesterol-lowering diet before receiving Lovastatin and should continue on this diet during treatment with Lovastatin . Lovastatin should be given with meals.
Adult Patients: The usual recommended starting dose is 20 mg once a day given with the evening meal. The recommended dosing range of Lovastatin is 10-80 mg/day in single or two divided doses; the maximum recommended dose is 80 mg/day. Doses should be individualized according to the recommended goal of therapy. Patients requiring reductions in LDLC of 20% or more to achieve their goal should be started on 20 mg/day of Lovastatin . A starting dose of 10 mg of Lovastatin may be considered for patients requiring smaller reductions. Adjustments should be made at intervals of 4 weeks or more. The 10 mg dosage is provided for information purposes only. Although Lovastatin tablets 10 mg are available in the marketplace, Lovastatin is no longer marketed in the 10 mg strength.
Cholesterol levels should be monitored periodically and consideration should be given to reducing the dosage of Lovastatin if cholesterol levels fall significantly below the targeted range.
Dosage in Patients taking Danazol, Diltiazem, Dronedarone or Verapamil: In patients taking danazol, diltiazem, dronedarone or verapamil concomitantly with Lovastatin , therapy should begin with 10 mg of Lovastatin and should not exceed 20 mg/day
Dosage in Patients taking Amiodarone: In patients taking amiodarone concomitantly with Lovastatin , the dose should not exceed 40 mg/day
Adolescent Patients (10-17 years of age) with Heterozygous Familial Hypercholesterolemia: The recommended dosing range of Lovastatin is 10-40 mg/day; the maximum recommended dose is 40 mg/day. Doses should be individualized according to the recommended goal of therapy. Patients requiring reductions in LDL-C of 20% or more to achieve their goal should be started on 20 mg/day of Lovastatin . A starting dose of 10 mg of Lovastatin may be considered for patients requiring smaller reductions. Adjustments should be made at intervals of 4 weeks or more.
Concomitant Lipid-Lowering Therapy: Lovastatin is effective alone or when used concomitantly with bile-acid sequestrants
Increased risk of myopathy/ rhabdomyolysis with amiodarone, colchicine, ranolazine, danazol, diltiazem and verapamil. May increase anticoagulant effect of warfarin.
Active liver disease or unexplained persistent elevated serum transaminases. Concomitant use with CYP3A4 inhibitors (e.g. nefazodone, erythromycin, boceprevir, clarithromycin, telithromycin, HIV protease inhibitors, itraconazole, ketoconazole, posaconazole, telaprevir), gemfibrozil, ciclosporin. Pregnancy and lactation.
GI disturbances, headache, dizziness, insomnia, myopathy or rhabdomyolysis (dose related), myalgia, arthralgia, wt gain, blurred vision, rash, asymptomatic hepatic aminotransferase elevation.
Pregnancy Category X. Studies in animals or human beings have demonstrated foetal abnormalities or there is evidence of foetal risk based on human experience or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.
Store between 20-25° C.
Lovastatin 20mg, 40mg