Classification Antihyperlipidemic agentHMGCoA reductase inhibitors

See also Antihyperlipidemic Agents—HMG-CoA Reductase Inhibitors.

Action/Kinetics: Competitive inhibitor of HMG-CoA reductase leading to inhibition of cholesterol synthesis and decrease in plasma cholesterol levels. Peak plasma levels: 2.5 hr.

tV2, terminal: 2-3 hr. Food does not affect blood levels. Metabolized in liver and excreted through urine and feces.

■ Uses: Adjunct to diet to reduce elevated total and LDL cholesterol in clients with primary hypercholesterolemia and mixed dyslipidemia when response to diet or other non-pharma-cologic approaches have not been adequate.

Contraindications: Use in active liver disease or unexplained elevation of serum transaminases. Pregnancy, lactation.

Special Concerns: Use in women of child-bearing age only when pregnancy is unlikely and they have been informed of potential risks. Drug has not been evaluated in rare homozygous familial hypercholes-terolemia. Due to interference with cholesterol synthesis and lower cholesterol levels, may be blunting of adrenal or gonadal steroid hormone production. Use with caution in renal or hepatic insufficiency. Safety and efficacy have not been determined in children.

Side Effects: See also HMG-CoA Reductase Inhibitors. Musculoskeletal: Rarely, rhabdomyolysis with acute renal failure secondary to myoglobi-nemia.

Drug Interactions: T Risk of myopa-thy when used with azole antifun-gals, cyclosporine, and erythromy-cin.

How Supplied: Tablets: 0.2 mg, 0.3 mg


Hypercholesterolemia. Adults: 0.3 mg once daily in evening. Recommended starting dose in those with significant renal impairment (CCR less than 60 mL/min/1.73 m2) is 0.2 mg once daily in evening.

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