Simvastatin
Simvastatin (Zocor)
Simvastatin
( sim-vah- STAH-tin)
Pregnancy Category: X Zocor (Rx)

Classification: Antihyperlipidemic

See Also: See also Antihyperlipidemic Agents HMG-CoA Reductase Inhibitors .

Action/Kinetics: Does not reduce basal plasma cortisol or testosterone levels or impair renal reserve. 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. Significantly bound to plasma proteins. t 1/2: 3 hr. Metabolites excreted in the feces (60%) and urine (13%).

Uses: Adjunct to diet to reduce elevated total and LDL cholesterol, apoprotein B, and triglyceride levels in hypercholesterolemia and mixed dyslipidemia (types IIa and IIb) when the response to diet and other approaches has been inadequate. To increase HDL cholesterol in primary hypercholesterolemia and mixed dyslipidemias. Treatment of isolated hypertriglyceridemia (Frederickson IV) and hyperlipoproteinemia (type III). In coronary heart disease and hypercholesterolemia to reduce risk of total mortality by reducing coronary death; to reduce the risk of non-fatal MI; to reduce the risk for undergoing myocardial revascularization procedures; to reduce the risk of stroke or TIAs. Investigational: Heterozygous familial hypercholesterolemia, familial combined hyperlipidemia, diabetic dyslipidemia in non-insulin-dependent diabetes, hyperlipidemia secondary to the nephrotic syndrome, and homozygous familial hypercholesterolemia in clients with defective LDL receptors.

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 hepatic and severe renal insufficiency. Safety and efficacy have not been determined in children less than 18 years of age.

Side Effects: Musculoskeletal: Rhabdomyolysis with renal dysfunction secondary to myoglobinuria, myopathy, arthralgias. GI: N&V;, diarrhea, abdominal pain, constipation, flatulence, dyspepsia, pancreatitis, anorexia, stomatitis. 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. Angioedema, anaphylaxis lupus erythematous-like syndrome, vasculitis, purpura, thrombocytopenia, leukopenia, hemolytic anemia polymyalgia 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, ophthalmoplegia. Hematologic: Transient asymptomatic eosinophilia, anemia, thrombocytopenia, leukopenia. Miscellaneous: URI, asthenia, alopecia, edema.

Laboratory Test Alterations: CPK, AST, ALT.

Additional Drug Interactions: Chronic use of grapefruit juice simvastatin plasma levels due to liver metabolism

How Supplied: Tablet: 5 mg, 10 mg, 20 mg, 40 mg, 80 mg

Dosage
?Tablets
Adults, initially: 5-10 mg once daily in the evening; maintenance: 5-40 mg/day as a single dose in the evening. Consider a starting dose of 5 mg/day for clients on immunosuppressives or those with LDL less than 190 mg/dL and 10 mg/day for clients with LDL greater than 190 mg/dL. For geriatric clients, the starting dose should be 5 mg/day with maximum LDL reductions seen with 20 mg or less daily.