See also Antihyperlipidemic Agents— HMG-CoA Reductase Inhibitors. Action/Kinetics: Inhibits HMG-CoA reductase enzyme, which reduces cholesterol synthesis. Peak therapeutic response: 4-6 weeks. Approximately 85% absorbed; significant first-pass effect with less than 5% of a PO dose reaching the general circulation. Metabolites excreted in the feces (60%) and urine (13%). Uses: Adjunct to diet for the reduction of elevated total and LDL cholesterol levels in types IIa and IIb hypercho-lesterolemia when the response to diet and other approaches have been inadequate. Prophylaxis of heart attack and decrease in incidence of cardiac death in those with CHD and elevated cholesterol levels. Non-FDA Approved Uses: Heterozygous familial hypercholesterolemia, familial combined hyperlipidemia, diabetic dyslipidemia in non-insulin-dependent diabetes, hyperlipidemia secondary to the nephrotic syndrome, and homozygous familial hy-percholesterolemia in clients with defective LDL receptors. Contraindications: Active liver disease or unexplained persistent increases in liver function tests. Use in pregnancy, during lactation, or in children.
Special Concerns: Use with caution in clients who have a history of liver disease/consume large quantities of alcohol or with drugs that affect steroid levels or activity. Higher plasma levels may be observed in clients with severe renal insufficiency. Safety and efficacy have not been determined in children less than 18 years of age.
Side Effects: Oral: stomatitis. Musculoskeletal: Rhabdomyolysis with renal dysfunction secondary to myo-globinuria, myopathy, arthralgias. GI: N&V, diarrhea, abdominal pain, constipation, flatulence, dyspepsia, pancreatitis, anorexia. Hepatic: Hepatitis (including chronic active hepatitis), cholestatic jaundice, cirrhosis, fatty change in liver, fulminant hepatic necrosis, hepatoma. Neurologic: Dysfunction of certain cranial nerves resulting in alteration of taste, impairment of extraocular movement, and facial paresis. Paresthesia, peripheral neuropathy, peripheral nerve palsy. CNS: Headache, tremor, vertigo, memory loss, anxiety, insomnia, depression. Hypersensitivity Reactions: Although rare, the following symptoms have been noted. ^4n-gioedema, anaphylaxis, lupus ery-thematous-like syndrome, vasculitis, purpura, thrombocytopenia, leuko-penia, hemolytic anemia, polymyal-gia rheumatica, positive ANA, ESR increase, arthritis, arthralgia, asthenia, urticaria, photosensitivity, chills, fever, flushing, malaise, dyspnea, toxic epidermal necrolysis, erythema multiforme (including Stevens-Johnson syndrome). GU: Gynecomastia, loss of libido, erectile dysfunction. Ophthalmologic: Lens opacities, ophthal-moplegia. Hematologic: Transient asymptomatic eosinophilia, anemia, thrombocytopenia, leukopenia. Miscellaneous: Upper respiratory infection, asthenia, alopecia, edema.
Drug Interactions Cyclosporine / T Risk of myopathy or rhabdomyolysis Erythromycin / T Risk of myopathy or rhabdomyolysis
Was this article helpful?