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CARDIOVASCULAR SYSTEM › LIPID MODIFYING AGENTS › LIPID MODIFYING AGENTS, PLAIN › HMG CoA reductase inhibitors
lovastatin
C10AA02
Forms & Strengths
- Tablets: 10 mg, 20 mg, 40 mg
Adult Dosing
- Initial: 20 mg orally once daily with the evening meal
- Range: 10 mg to 80 mg daily administered as a single dose or in divided doses
- Adjust dose at intervals of 4 weeks or more
Pediatric Dosing
- Children 10-17 years (heterozygous familial hypercholesterolemia): Initial 10 mg once daily with evening meal
- Range: 10 mg to 40 mg daily
Indications
- Adjunct to diet to reduce elevated total-C, LDL-C, apoB, and TG levels, and to increase HDL-C in patients with primary hypercholesterolemia and mixed dyslipidemia
- Slow progression of coronary atherosclerosis in patients with coronary heart disease
Mechanism of Action
- Competitive inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase
- Prevents conversion of HMG-CoA to mevalonate, an early and rate-limiting step in cholesterol biosynthesis
- Upregulates hepatic LDL receptors, increasing clearance of LDL from plasma
Contraindications
- Active liver disease or unexplained persistent elevations of serum transaminases
- Concomitant use of strong CYP3A4 inhibitors (e.g., itraconazole, ketoconazole, posaconazole, voriconazole, HIV protease inhibitors, boceprevir, telaprevir, erythromycin, clarithromycin, telithromycin, nefazodone)
- Pregnancy and lactation
Adverse Reactions
- Myopathy, rhabdomyolysis
- Increased serum transaminases
- Headache, dizziness
- Constipation, dyspepsia, abdominal pain, nausea
- Nasopharyngitis, myalgia
Drug Interactions
- Strong CYP3A4 inhibitors (increase lovastatin exposure and myopathy risk)
- Cyclosporine, danazol, gemfibrozil, niacin (increase risk of myopathy and rhabdomyolysis)
- Coumarin anticoagulants (may enhance anticoagulant effect)
- Grapefruit juice (increases plasma concentrations of lovastatin)
Curated Content: Needs Vetting Before Put to Clinical Use