Lovastatin

Mechanism :

Lovastatin is a synthetic lipid-lowering agent. Lovastatin is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase. This enzyme catalyzes the conversion of HMG-CoA to mevalonate, an early and rate-limiting step in cholesterol biosynthesis.

Indication :

• Dyslipidemia who are at risk for atherosclerotic vascular disease
• Heterozygous familial hypercholesterolemia.

Contraindications :

Hypersensitivity to any component of this medication. Active liver disease or unexplained persistent elevations of serum transaminases exceeding 3 times the upper limit of normal. It is to be used with caution in children.

Dosing :

Adverse Effect :

Myopathy, muscle cramps, paraesthesia, myositis, alopecia, pancreatitis, hepatitis, cholestatic jaundice, anorexia, flatulence, abdominal pain, myalgia, nausea, dyspepsia, weakness, constipation, vomiting, blurred vision, rash, dizziness, pruritus, peripheral neuropathy, impotence, hyperglycemia and hypoglycemia, increase in serum transaminase levels.

Interaction :

Concomitant Therapy with Other Lipid Metabolism Regulators: Combined drug therapy should be approached with caution as information from controlled studies is limited.
Bile Acid Sequestrants: Patients with Mild to Moderate Hypercholesterolemia: LDL-C reduction was greater when lovastatin and colestipol were coadministered than when either drug was administered alone.
Patients with Severe Hypercholesterolemia: LDL-C reduction was similar.
Fibric Acid Derivatives (Gemfibrozil, Fenofibrate, Bezafibrate) and Niacin (Nicotinic Acid): The risk of myopathy during treatment with other drugs in this class is increased with concurrent administration.
Digoxin: Coadministration of multiple doses increased steady-state plasma digoxin concentrations.
Oral Contraceptives: Coadministration with an oral contraceptive, increased plasma concentrations (AUC levels) of norethindrone and ethinyl estradiol.
Cimetidine: The triglyceride-lowering effect was reduced.
Erythromycin: Plasma concentrations increased approximately with coadministration of erythromycin, a known inhibitor of cytochrome P450 3A4.
Other Concomitant Therapy: Caution should be exercised with concomitant use of immunosuppressive agents and azole antifungals.
Drug/Laboratory Test Interactions: May elevate serum transaminase and creatinine phosphokinase levels (from skeletal muscle).

Hepatic Dose :