Lovastatin

Indications
 Oral
Hyperlipidaemias, Primary prophylaxis of coronary artery disease
Adult: Initially, 10-20 mg daily at night; may be increased at 4-wk intervals as necessary. Max: 80 mg/day (immediate-release); 60 mg/day (extended-release).
Child: Adjunct to diet in adolescent patients with heterozygous familial hypercholesterolaemia with LDL >189 mg/dl, or LDL >160 mg/dl with positive family history of premature CVD, or LDL >160 mg/dl in the presence of at least 2 other CVD risk factors: 10-17 yr: Immediate-release tablet: LDL reduction <20%: Initially, 10 mg/day. ≥20%: Initially, 20 mg/day. Usual range: 10-40 mg daily, then adjust dose at 4-wk intervals. Doses to be taken at night.
CrCl (ml/min)Dosage Recommendation
<30Doses >20 mg/day should be used with caution.
Contraindications
 Active liver disease; unexplained persistently elevated serum transaminases. Pregnancy and lactation.
Warnings / Precautions
 Renal impairment; inadequately controlled hypothyroidism; history of liver disease; alcoholism; patients at risk of rhabdomyolysis. Elderly. Monitor LFTs.
Adverse Reactions
 Increased creatine phosphokinase; flatulence, nausea, dyspepsia, constipation or diarrhoea, abdominal pain; muscle cramps, myalgia, weakness; blurred vision; headache, dizziness; rash.
Potentially Fatal: Rhabdomyolysis and acute renal failure.
Drug Interactions
 Reduced absorption with cholestyramine, isradipine. May increase warfarin effect.
Potentially Fatal: Increased risk of myopathy and rhabdomyolysis with amiodarone, azole antifungals, fibrates, colchicine, ciclosporin, danazol, macrolides, nefazodone, niacin (high doses), protease inhibitors, verapamil. Increased levels/effects with diclofenac, doxycycline, imatinib, isoniazid, nicardipine, propofol, quinidine, diltiazem.
See Below for More lovastatin Drug Interactions
Lab Interactions
 May alter thyroid function tests.
Food Interactions
 Bioavailability of extended-release tablet reduced by food; bioavailability of immediate-release tablet increased by food. Serum levels increased with grapefruit juice; avoid concurrent intake of >1 quart/day. Serum levels reduced with St John's wort.
Mechanism of Actions
 Lovastatin reduces cholesterol synthesis by inhibiting the rate-limiting step catalysed by HMG-CoA reductase.
Absorption: 30% absorbed from the GI tract; peak plasma concentrations after 2-4 hr (oral).
Distribution: <5% reach the circulation. Protein-binding: >95%.
Metabolism: Extensively hepatic via hydrolysis; converted to active β-hydroxyacid form.
Excretion: Via faeces (85%); via urine (10%); 1-2 hr (elimination half-life).
Administration
 Should be taken with food.
Storage Conditions
 Oral: Immediate-release tablet: Store at 5-30°C (41-86°F). Extended-release tablet: Store at 20-25°C (68-77°F).
ATC Classification
 C10AA02 - lovastatin ; Belongs to the class of HMG CoA reductase inhibitors. Used in the treatment of hyperlipidemia.
Storage
 Oral: Immediate-release tablet: Store at 5-30°C (41-86°F). Extended-release tablet: Store at 20-25°C (68-77°F).
Available As
  • Lovastatin 10 mg
  • Lovastatin 20 mg

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