Lovastatin

A to Z Drug Facts

 Actions Increases rate at which body removes cholesterol from blood and reduces production of cholesterol in body by inhibiting enzyme that catalyzes early rate-limiting step in cholesterol synthesis; increases HDL; reduces LDL, VLDL, and triglycerides.

 Indications Reduction of elevated cholesterol and LDL cholesterol levels in patients with primary hypercholesterolemia (types IIa and IIb); slow progression of coronary atherosclerosis in patients with coronary heart disease; reduce risk of MI, unstable angina, and coronary revascularization procedures; as an adjunct to diet to reduce total and LDL cholesterol and apolipoprotein B levels in adolescent boys and girls (who are at least 1 yr postmenarche), 10 to 17 yr, with heterozygous familial hypercholesterolemia (immediate release only).

Treatment of diabetic dyslipidemia, nephrotic hyperlipidemia, familial dysbetalipoproteinemia, familial combined hyperlipidemia.

 Contraindications Active liver disease or unexplained persistent elevations of LFTs; pregnancy; lactation.

 Route/Dosage

ADULTS: PO 20 to 80 mg/day in single or divided doses with meals.

Heterozygous Familial Hypercholesterolemia: Adolescents (10 to 17 yr): PO Immediate release: 10 to 40 mg/day (max, 40 mg/day).

 Interactions

Azole antifungal agents (eg, itraconazole), cyclosporine, danazol, gemfibrozil, grapefruit juice, macrolide antibiotics (eg, erythromycin), niacin, verapamil: Severe myopathy or rhabdomyolysis may occur with coadministration. Isradipine: May increase the clearance of lovastatin and its metabolites by increasing hepatic blood flow. Warfarin: Enhanced anticoagulant effect.

 Lab Test Interferences None well documented.

 Adverse Reactions

CNS: Headache; dizziness; paresthesia; insomnia. DERMATOLOGIC: Rash; pruritus. EENT: Blurred vision; dysfunction of certain cranial nerves (including alteration of taste, impairment of extraocular movement, facial paresis). GI: Nausea; vomiting; diarrhea; abdominal pain; constipation; flatulence; heartburn; dyspepsia; pancreatitis. HEPATIC: Hepatitis; cholestatic jaundice; fatty change in liver; cirrhosis; fulminant hepatic necrosis; hepatoma. OTHER: Myalgia; muscle cramps; myopathy; rhabdomyolysis with increased CPK; arthralgias; hypersensitivity syndrome (eg, anaphylaxis, angioedema, lupus erythematosus-like syndrome, polymyalgia rheumatica, vasculitis, purpura, thrombocytopenia, leukopenia, hemolytic anemia, arthritis, arthralgia, urticaria, fever, chills, dyspnea, toxic epidermal necrolysis, erythema multiforme.)

 Precautions

Pregnancy: Category X. Lactation: Undetermined. CHILDREN: Safety and efficacy not established in children under 18 yr. Adults above 70 yr: The AUC of lovastatin is increased. Liver dysfunction: Use with caution in patients who consume substantial quantities of alcohol or those with liver disease. Marked, persistent increases in serum transaminases have occurred during therapy. Ophthalmologic effects: There was a high prevalence of baseline lenticular opacities during the early trials of lovastatin. Skeletal muscle effects: Rhabdomyolysis with renal dysfunction secondary to myoglobinuria has been reported, mostly in those taking lovastatin concomitantly with cyclosporine, erythromycin, gemfibrozil, or nicotinic acid. Immunosuppressants may increase active lovastatin metabolites, which are associated with myopathy, myalgia, and muscle weakness associated with markedly increased CPK levels.

 Administration/Storage

• Administer with meals. If given as a single dose, administer with evening meal.
• Store at room temperature in tightly closed, light-resistant container.

 Assessment/Interventions

• Obtain patient history, including drug history and any known allergies. Note hepatic impairment, alcohol consumption, and other medications that may increase risk of myopathy.
• Ensure that blood cholesterol and triglyceride levels are assessed before beginning therapy and repeated periodically during treatment.
• Place patient on standard cholesterol-lowering diet before beginning therapy and continue diet during treatment.
• Ensure that LFTs are performed q 4 to 6 wk during first 3 mo of therapy, q 6 to 8 wk during next 18 mo, and q 6 mo thereafter.
• If elevated serum transaminase levels develop during treatment, repeat tests more frequently.
• If transaminase levels rise to 3 times upper limit of normal and are persistent, notify health care provider. Drug may be discontinued.
• If muscle tenderness or weakness develops during therapy, monitor CPK levels. Notify health care provider if CPK levels are markedly increased or if symptoms continue.

 Patient/Family Education

• Caution patient that this medication must not be taken during pregnancy or when pregnancy is possible. Advise patient to use reliable form of birth control while taking this drug.
• Advise patient to take medication with evening meal if possible.
• Explain importance of adhering to low-cholesterol, low-fat diet during treatment. Suggest consultation with nutritionist as needed.
• Instruct patient to report the following symptoms to health care provider: unexplained muscle pain, tenderness, or weakness, especially if accompanied by fever or malaise.
• Caution patient to avoid or decrease alcohol intake.
• Advise patient not to take any additional medications or supplementation without approval by health care provider.
• Emphasize importance of returning for follow-up liver function and blood cholesterol tests as instructed.
• Explain that this treatment must be continued over years.

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Copyright © 2003 Facts and Comparisons
David S. Tatro
A to Z Drug Facts