Classification Antihyperlipidemic agent

See also Antihyperlipidemic Agents—HMG-CoA Reductase Inhibitors.

Action/Kinetics: Competitively inhibits HMG-CoA reductase enzyme, which reduces cholesterol synthesis. Drug increases survival in heart transplant recipients. Rapidly absorbed from the GI tract. Peak plasma levels: 1-1.5 hr. Significant firstpass extraction and metabolism in the liver, which is the site of action of the drug; thus, plasma levels may not correlate well with lipid-lower-ing effectiveness. t1/2, elimination: 77 hr. Metabolized in the liver; approximately 20% of a PO dose is excreted through the urine and 70% in the feces.

Uses: Adjunct to diet for reducing elevated total and LDL cholesterol levels in clients with primary hyper-cholesterolemia (type IIa and IIb) when the response to a diet with restricted saturated fat and cholesterol has not been effective. Reduce the risk of heart attack and slow progression of coronary atherosclerosis in those with hypercholesterolemia and heart disease. Non-FDA Approved Uses: To lower cholesterol levels in those with heterozygous familial hypercholesterolemia, familial combined hyperlipidemia, diabetic dyslipidemia in non-insulin-dependent diabetics, hypercholesterolemia secondary to nephrotic syndrome, homozygous familial hypercholes-terolemia in those not completely devoid of LDL receptors but who have a decreased level of LDL receptor activity.

Contraindications: To treat hyper-cholesterolemia due to hyperalpha-proteinemia. Active liver disease; unexplained, persistent elevations in liver function tests. Use during pregnancy and lactation and in children less than 18 years of age. Special Concerns: Use with caution in clients with a history of liver disease, renal insufficiency, or heavy alcohol use.

Side Effects: Musculoskeletal: Rhab-domyolysis with renal dysfunction secondary to myoglobinuria, myalgia, myopathy, arthralgias, localized pain. CNS: CNS vascular lesions characterized by perivascular hemorrhage, edema, and mononuclear cell infiltration of perivascular spaces; headache, dizziness, psychic disturbances. Dizziness, vertigo, memory loss, anxiety, insomnia, depression. GI: N&V, diarrhea, abdominal pain, cramps, constipation, flatulence, heartburn, anorexia. Hepatic: Hepatitis (including chronic active hepatitis), fatty change in liver, cirrhosis, fulminant hepatic necrosis, hepatoma, pancreatitis, cholestatic jaundice. GU: Gynecomastia, erectile dysfunction, loss of libido. Ophthalmic: Progression of cataracts, lens opacities, ophthalmo-plegia. Hypersensitivity reaction: Vasculitis, purpura, polymyalgia rheumatica, angioedema, lupus ery-thematosus-like syndrome, throm-bocytopenia, hemolytic anemia, leu-kopenia, positive ANA, arthritis, ar-thralgia, urticaria, asthenia, ESR increase, fever, chills, photosensitivity, malaise, dyspnea, toxic epidermal ne crolysis, Stevens-Johnson syndrome.

Dermatologic: Alopecia, pruritus, skin nodules, discoloration of skin, dryness of skin and mucous membranes, changes in hair and nails. Neurologic: Dysfunction of certain cranial nerves resulting in alteration of taste, impairment of extraocular movement, and facial paresis; pares-thesia, peripheral neuropathy, tremor, vertigo, memory loss peripheral nerve palsy. Respiratory: Common cold, rhinitis, cough. Hematologic: Anemia, transient asymptomatic eosin-ophilia, thrombocytopenia, leukope-nia. Miscellaneous: Rash, pruritus, cardiac chest pain, fatigue, influenza.

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