Simvastatin

DEA Class; Rx

Common Brand Names; Zocor, FloLipid

Indicated for the treatment of hypercholesterolemia, including hyperlipidemia, hyperlipoproteinemia, or hypertriglyceridemia, as an adjunct to dietary control; and for reduction in cardiovascular mortality, including myocardial infarction prophylaxis and stroke prophylaxis.

Hypersensitivity to simvastatin

Active liver disease or unexplained transaminase elevation

Strong CYP3A4 inhibitors (eg, itraconazole, ketoconazole, erythromycin, clarithromycin, posaconazole, voriconazole, HIV protease inhibitors, cobicistat, nefazodone), gemfibrozil, cyclosporine, and danazol

• CPK elevation (>3x ULN) (5%)
• Constipation (2%)
• Upper respiratory infection (9%)
• Flatulence (1-2%)
• Transaminases increased (>3x ULN) (1%)
• Headache (3-7%)
• Myalgia (5%)
• Eczema (5%)
• Vertigo (5%)
• Abdominal pain (7%)
• Myalgia
• Myopathy
• Arthralgia
• Arthritis
• Eosinophilia
• Chills
• Angioedema
• Rhabdomyolysis
• Abdominal pain

Rule out secondary causes of hyperlipidemia prior to initiating therapy

Nonserious and reversible cognitive side effects may occur

Increased blood sugar and glycosylated hemoglobin (HbA1c) levels reported with statin intake

Heavy alcohol use, history of liver disease, renal failure

Monitor LFTs before initiating treatment and thereafter when clinically indicated; reports of fatal and nonfatal hepatic failure in patients taking statins

Discontinue if markedly elevated CPK levels occur or myopathy is diagnosed or suspected

Increases in HbA1c and fasting serum glucose levels reported with simvastatin

Severe electrolyte, endocrine, or metabolic disorders

Grapefruit juice increases simvastatin systemic exposure; avoid large quantities of grapefruit juice (ie, ≥1 quart/day)

Discontinue therapy when pregnancy recognized; alternatively, consider ongoing therapeutic needs of individual patient

Therapy decreases synthesis of cholesterol and possibly other biologically active substances derived from cholesterol; therefore, this drug may cause fetal harm when administered to pregnant patients based on mechanism of action; in addition, treatment of hyperlipidemia is not generally necessary during pregnancy

There is no information about presence of this drug in human or animal milk, effects on breastfed infant or on milk production; however, it has been shown that another drug in this class passes into human milk; statins, including this drug, decrease cholesterol synthesis and possibly synthesis of other biologically active substances derived from cholesterol and may cause harm to breastfed infant