OralHyperlipidaemias, Primary prophylaxis of coronary artery diseaseAdult: 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: 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.
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| CrCl (mL/min) |
Dosage |
| <30 |
Use w/ caution in doses >20 mg/day. |
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Should be taken with food.
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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.
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History of liver disease; patients at risk of myopathy;. alcoholism; inadequately controlled hypothyroidism. Severe renal impairment.
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GI disturbances, headache, dizziness, insomnia, myopathy or rhabdomyolysis (dose related), myalgia, arthralgia, wt gain, blurred vision, rash, asymptomatic hepatic aminotransferase elevation.
Potentially Fatal: Severe rhabdomyolysis w/ acute renal failure. Hepatitis, pancreatitis. Rare: Stevens-Johnson syndrome, anaphylaxis, toxic epidermal necrolysis.
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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.
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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.
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Reduced serum levels w/ St John's wort. Increased serum level w/ grapefruit juice, avoid concurrent intake of >1 quart/day.
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May alter thyroid function tests.
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Description:
Mechanism of Action: Lovastatin reduces cholesterol by competitively inhibiting HMG-CoA reductase, the rate-limiting step in cholesterol biosynthesis.
Pharmacokinetics:
Absorption: 30% absorbed from the GI tract. Time to peak plasma concentration: W/in 2-4 hr.
Distribution: <5% reach the circulation. Plasma protein binding: >95%.
Metabolism: Extensively hepatic via hydrolysis; converted to active β-hydroxyacid form.
Excretion: Via faeces (approx 85%); via urine (approx 10%). Elimination half-life: 1-2 hr.
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Anon. Lovastatin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 24/10/2013. Buckingham R (ed). Lovastatin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 24/10/2013. FDA Drug Safety Communication: Interactions Between Certain HIV or Hepatitis C Drugs and Cholesterol-Lowering Statin Drugs Can Increase The Risk of Muscle Injury. U.S. FDA. https://www.fda.gov/. Accessed 24/10/2013. Lovastatin Tablet (Actavis Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 24/10/2013. McEvoy GK, Snow EK, Miller J et al (eds). Lovastatin. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 24/10/2013. Statins and HIV or Hepatitis C Drugs: Drug Safety Communication - Interaction Increases Risk of Muscle Injury. U.S. FDA. https://www.fda.gov/. Accessed 31/10/2013.
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