ZOCOR

Zocor Generic Name & Formulations

Legal Class

General Description

Simvastatin 10mg, 20mg, 40mg; tabs.

Pharmacological Class

HMG-CoA reductase inhibitor.

How Supplied

Tabs—30, 90

Manufacturer

Organon & Co.

Generic Availability

YES

Mechanism of Action

Simvastatin inhibits 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, thus preventing the conversion of HMG-CoA to mevalonate, an early and rate limiting step in the biosynthetic pathway for cholesterol.

Zocor Indications

Indications

In adults with established coronary heart disease (CHD), cerebrovascular disease, peripheral vascular disease, and/or diabetes, who are at high risk of CHD events: to reduce the risk of total mortality by reducing risk of CHD death, non-fatal MI and stroke, and the need for coronary and non-coronary revascularization procedures. Adjunct to diet to reduce LDL-C: in adults with primary hyperlipidemia; in adults and pediatric patients with heterozygous familial hypercholesterolemia (HeFH). Adjunct to other LDL-C-lowering therapies to reduce LDL-C in adults with homozygous hypercholesterolemia (HoFH). Adjunct to diet in adults with primary dysbetalipoproteinemia or hypertriglyceridemia.

Zocor Dosage and Administration

Adult

≥18yrs: 20–40mg once daily in the PM; monitor lipids after 4 weeks and adjust dose if needed. Max 40mg/day. Concomitant lomitapide: reduce simvastatin dose by 50%; max 20mg/day (or 40mg/day for those previously taken 80mg/day chronically). Concomitant verapamil, diltiazem, dronedarone: max simvastatin 10mg/day. Concomitant amiodarone, amlodipine, ranolazine: max simvastatin 20mg/day. Severe renal impairment (CrCl 15–29mL/min): initially 5mg/day, monitor closely; use another simvastatin product to initiate dosing (as Zocor 5mg and 80mg are no longer marketed). Restrict 80mg/day dose to chronic users (≥12mos) without evidence of muscle toxicity. For patients that require a high-intensity statin or are unable to achieve their LDL-C goal using simvastatin 40mg; switch to alternative LDL-C lowering regimen. See full labeling.

Children

<10yrs: not established. 10–17yrs: 10–40mg once daily in the PM; monitor lipids after 4 weeks and adjust dose if needed. Max 40mg/day.

Zocor Contraindications

Contraindications

Concomitant strong CYP3A4 inhibitors (eg, itraconazole, ketoconazole, posaconazole, voriconazole, HIV protease inhibitors, boceprevir, telaprevir, erythromycin, clarithromycin, telithromycin, nefazodone), gemfibrozil, cyclosporine, danazol. Active liver disease. Decompensated cirrhosis.

Zocor Boxed Warnings

Not Applicable

Zocor Warnings/Precautions

Warnings/Precautions

Increased risk of myopathy/rhabdomyolysis with simvastatin 80mg doses including predisposing factors (eg, age ≥65yrs, uncontrolled hypothyroidism, renal impairment). Discontinue if markedly elevated CPK levels occur or myopathy diagnosed or suspected. Temporarily withhold if acute or serious condition predisposing to the development of renal failure secondary to rhabdomyolysis occurs. Discontinue if immune-mediated necrotizing myopathy is suspected. Monitor liver function prior to initiation and repeat as clinically indicated. Discontinue promptly if serious liver injury with clinical symptoms and/or hyperbilirubinemia or jaundice occurs. History of liver disease. Substantial alcohol consumption. Severe renal impairment. Chinese patients (may be at higher risk for myopathy): monitor. Elderly. Pregnancy: discontinue therapy if occurs. Nursing mothers: not recommended.

Zocor Pharmacokinetics

Distribution

Plasma protein bound: ~95%.

Metabolism

Hepatic (CYP3A4).

Elimination

Fecal (60%), renal (13%).

Zocor Interactions

Interactions

See Contraindications. Avoid concomitant grapefruit juice. Reduce max simvastatin dose if amiodarone, dronedarone, verapamil, diltiazem, amlodipine, ranolazine must be used. Concomitant lipid-modifying doses (≥1g/day) of niacin: not recommended in Chinese patients. Increased rhabdomyolysis with concomitant daptomycin; suspend simvastatin temporarily. Caution with other fibrates, lomitapide, colchicine. Monitor digoxin, oral anticoagulants.

Zocor Adverse Reactions

Adverse Reactions

Upper respiratory infection, headache, abdominal pain, constipation, nausea, elevated serum transaminases, myopathy, rhabdomyolysis; increased HbA1c and fasting serum glucose, rare: cognitive impairment, non-fatal hepatic failure.

Zocor Clinical Trials

See Literature

Zocor Note