See also Antihyperlipidemic Agents—HMG-CoA Reductase Inhibitors.
Action/Kinetics: It specifically inhibits HMG—coenzyme A reductase enzyme, which reduces cholesterol synthesis. Approximately 35% of a dose is absorbed. Extensive firstpass effect—less than 5% reaches the general circulation. Absorption is decreased by about one-third if the drug is given on an empty stomach rather than with food. Onset: within 2 weeks using multiple doses. Time to peak plasma levels: 2—4 hr. Time to peak effect: 4—6 weeks using multiple doses. Duration: 4—6 weeks after termination of therapy. Over 95% is bound to plasma proteins. Metabolized in the liver (its main site of action) to active metabolites. Over 80% of a PO dose is ex creted in the feces, via the bile, and approximately 10% is excreted through the urine.
Uses: As an adjunct to diet in primary hypercholesterolemia (types IIa and IIb) in clients with a significant risk of CAD and who have not responded to diet or other measures. May also be useful in clients with combined hypercholesterolemia and hypertriglyceridemia. To slow the progression of coronary atherosclerosis in clients with CAD in order to lower total and LDL cholesterol levels. Non-FDA Approved Uses: Diabetic dyslipidemia, nephrotic hyperlipide-mia, familial dysbetalipoproteine-mia, and familial combined hyper-lipidemia.
Contraindications: During pregnancy and lactation, active liver disease, persistent unexplained elevations of serum transaminases. Use in children less than 18 years of age. Special Concerns: Use with caution in clients who have a history of liver disease or who are known heavy consumers of alcohol. Carefully monitor clients with impaired renal function.
Side Effects: GI: Flatus (most common), abdominal pain, cramps, diarrhea, constipation, dyspepsia, N&V, heartburn, anorexia, stomatitis, acid regurgitation, dry mouth. CNS: Headache, dizziness, tremor, vertigo, memory loss, paresthesia, anxiety, depression, insomnia. Musculoskel-etal: Myalgia, muscle cramps, localized pain, arthralgia, myopathy, rhab-domyolysis with renal dysfunction secondary to myoglobinuria. Hyper-sensitivity reaction: Vasculitis, purpura, polymyalgia rheumatica, an-gioedema, lupus erythematosus-like syndrome, thrombocytopenia, hemolytic anemia, leukopenia, eosinophil-ia, positive ANA, arthritis, arthralgia, urticaria, asthenia, ESR increase, fever, chills, flushing, photosensitivity, malaise, dyspnea, toxic epidermal necrolysis, anaphylaxis, erythema multiforme including Stevens-Johnson syndrome. Dermatologic: Alopecia, pruritus, rash, skin changes, including nodules, discoloration, dryness, changes to hair and nails. Hepatic: Hepatitis (including chronic active hepatitis), cholestatic jaundice, fatty change in liver, cirrhosis, fulminant hepatic necrosis, hepatoma, pancreatitis. GU: Gynecomastia, loss of libido, erectile dysfunction. Ophthalmic: Blurred vision, progression of cataracts, lens opacities, ophthalmo-plegia. Hematologic: Anemia, leuko-penia, transient asymptomatic eo-sinophilia, thrombocytopenia. Miscellaneous: Cardiac chest pain, dysgeusia, edema, alteration of taste, impairment of extraocular movement, facial paresis, peripheral neuropathy, peripheral nerve palsy. Drug Interactions Cyclosporine / T Risk of rhabdom-yolysis or severe myopathy
Erythromycin / T Risk of rhabdom-yolysis or severe myopathy How Supplied: Tablet: 10 mg, 20 mg, 40 mg
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