Lovastatin

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[edit] BRAND NAMES

[edit] STRUCTURE

Lovastatin.jpg

[edit] MECHANISM OF ACTION

Lovastatin is an hypolipidemic belonging to the class of drugs called Statins.

Cholesterol is made mainly in the liver. Statins work by blocking a key liver enzyme involved in this process, thereby slowing down the production of cholesterol in the liver. This encourages the liver to take extra cholesterol, LDL cholesterol in particular, out of the bloodstream, by increasing the number of hepatic LDL receptors on the cell-surface and thus, causing the LDL cholesterol level to decrease .

Lovastatin selectively and competitively inhibits the hepatic enzyme hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase. As HMG-CoA reductase is responsible for converting HMG-CoA to mevalonate, this results in a decrease in mevalonate, a precursor of cholesterol. Lovastatin reduces total-cholesterol and LDL-cholesterol, modestly reduces VLDL-cholesterol and plasma triglycerides (TG) and can produce increases of variable magnitude in HDL-cholesterol (good cholesterol).

[edit] INDICATIONS

  • Hyperlipidemia:
    • Patients with primary hypercholesterolemia (Types IIa and IIb) as an adjunct to diet to reduce elevated total-C and LDL-C
    • Adolescent boys and girls who are at least one year post-menarche, 10-17 years of age with Heterozygous Familial Hypercholesterolemia (HeFH) to reduce elevated total-C, LDL-C and ApoB after failing an adequate trial of diet therapy


  • Prevention of Coronary Heart Disease: Cholesterol can cause coronary heart disease by narrowing the coronary arteries. This condition, called atherosclerosis, may lead to angina, a heart attack (myocardial infarction), or a stroke. Lovastatin is indicated to slow the progression of atherosclerosis and to reduce the risk of myocardial infarction, unstable angina, and arterial revascularization procedures (e.g. heart bypass, angioplasty) in patients WITHOUT clinically evident coronary heart disease, but with average to moderately elevated total-C and LDL-C, and below average HDL-C
  • Coronary Heart Disease: Lovastatin is indicated to slow the progression of atherosclerosis in patients WITH coronary heart disease as part of a treatment strategy to lower total-C and LDL-C to target levels

[edit] DOSAGE

Starting and maintenance dosage should be individualized according to baseline LDL-C levels, the goal of therapy, and patient response. After initiation and/or upon titration of Lovastatin, lipid levels should be analyzed after 4 weeks, and dosage adjusted accordingly.

  • Adult recommended starting dose: 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. Patients requiring LDL-C reduction (<20%) may start at 10 mg once daily.
  • 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

[edit] CONTRAINDICATIONS

[edit] WARNINGS AND PRECAUTIONS

  • Skeletal Muscle Effects: Myalgia, myopathy and, rarely, rhabdomyolysis with acute renal failure secondary to myoglobinuria have been reported with HMG-CoA reductase inhibitors, including Lovastatin. These risks can occur at any dose level, but are increased at the highest dose.

Lovastatin should be prescribed with caution in patients with predisposing factors for myopathy (e.g., age ≥ 65 years, inadequately treated hypothyroidism, renal impairment, personal or family history of hereditary muscular disorders, alcohol abuse).

Concomitant use of strong CYP3A4 inhibitors may increase the risk of myopathy. (see Interaction)

Whilst on treatment, patients should be asked to report inexplicable muscle pain, weakness or cramps immediately, particularly if associated with malaise or fever. Creatine Kinase levels should be measured in these patients. Therapy should be discontinued if Creatine Kinase levels are markedly elevated.

  • Liver enzyme abnormalities and monitoring: As with other HMG-CoA reductase inhibitors, persistent elevations in hepatic transaminases can occur. Monitor liver enzymes prior to initiating therapy and repeat it when clinically indicated.

[edit] INTERACTIONS

Drug Interactions Associated with Increased Risk of 
Myopathy/Rhabdomyolysis
Interacting Agents 
Prescribing Recommendations 
Atorvastatin is metabolized by CYP3A4. Strong CYP3A4 inhibitors can raise the plasma levels of lovastatin and may increase the risk of myopathy: Itraconazole, ketoconazole, posaconazole, voriconazole, the macrolide antibiotics erythromycin and clarithromycin, the ketolide antibiotic telithromycin, HIV protease inhibitors, boceprevir, telaprevir, or the antidepressant nefazodone Combination of these drugs with lovastatin is contraindicated
Gemfibrozil Concomitant administration of Lovastatin with Gemfibrozil should be avoided
Other lipid-lowering drugs (other fibrates or ≥1 g/day of niacin) Caution should be used when prescribing other fibrates or lipid-lowering doses (≥1 g/day) of niacin with lovastatin, as these agents can cause myopathy when given alone. The benefit of further alterations in lipid levels by the combined use of lovastatin with other fibrates or niacin should be carefully weighed against the potential risks of these combinations.
Cyclosporine Concomitant administration of Lovastatin with Cyclosporine should be avoided
Patients receiving concomitant medication with Danazol, diltiazem, dronedarone or verapamil with higher doses of lovastatin The dose of lovastatin should not exceed 20 mg daily
Amiodarone The dose of lovastatin should not exceed 40 mg daily
Colchicine The risk of myopathy/rhabdomyolysis is increased with concomitant administration of colchicine. Caution should be exercised
Ranolazine The risk of myopathy/rhabdomyolysis is increased with concomitant administration of Ranolazine. Dose adjustment of Lovastatin may be considered.
Grapefruit juice Avoid grapefruit juice
  • Warfarin and coumarin derivates: Monitor prothrombin times when Lovastatin co-administration is initiated, discontinued, or the dosage changed

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category X (US). Lovastatin should be administered to women of child-bearing potential only when such patients are highly unlikely to conceive and have been informed of the potential hazards. If a woman becomes pregnant while taking Lovastatin, the drug should be discontinued and the patient advised again as to the potential hazards to the fetus.
  • Nursing mothers who require Lovastatin treatment should be advised not to nurse their infants.

[edit] SIDE EFFECTS

Lovastatin is generally well tolerated; adverse reactions usually have been mild and transient and may include nausea, abdominal pain, insomnia, dyspepsia, headache, asthenia, myalgia and transaminases increased.

See also WARNINGS AND PRECAUTIONS section

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

Mevacor_PI (U.S.) Revised: 10/2012

[edit] REFERENCES