simvastatin

simvastatin /sim·va·stat·in/ (sim´vah-stat″in) an antihyperlipidemic agent that acts by inhibiting cholesterol synthesis, used in the treatment of hypercholesterolemia and other forms of dyslipidemia and to lower the risks associated with atherosclerosis and coronary heart disease.

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sim·va·stat·in (smv-sttn)

n.

A statin drug derived from the mold Aspergillus terreus, used to treat hyperlipidemia.

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simvastatin, (sim´vstat´n),

n brand name: Zocor;
drug class: cholesterol-lowering agent;
action: inhibits 3hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase enzyme, which reduces cholesterol synthesis;
use: as an adjunct in primary hypercholesterolemia types IIa and IIb.

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simvastatin

Simvador (UK), Zocor

Pharmacologic class: HMG-CoA reductase inhibitor

Therapeutic class: Antihyperlipidemic

Pregnancy risk category X

Action

Inhibits hepatic enzyme HMG-CoA reductase, interrupting cholesterol synthesis and low-density lipoprotein (LDL) consumption. Net effect is total cholesterol and serum triglyceride reductions.

Availability

Tablets: 5 mg, 10 mg, 20 mg, 40 mg, 80 mg

⊘Indications and dosages

➣ Coronary artery disease; hyperlipidemia

Adults: 20 to 40 mg P.O. daily in evening, adjusted q 4 weeks based on response. Range is 5 to 80 mg/day.

➣ Hypercholesterolemia

Adults: Initially, 40 mg P.O. daily at bedtime. Alternatively, 80 mg daily divided as 20 mg in morning, 20 mg in afternoon, and 40 mg at bedtime.

Children and adolescents ages 10 to 17: Initially, 10 mg P.O. daily in evening. Range is 10 to 40 mg daily, adjusted at intervals of 4 weeks or longer.

Dosage adjustment

• Severe renal impairment
• Concurrent use of amiodarone, fibrates, niacin, or verapamil
• Elderly patients

Contraindications

• Hypersensitivity to drug or its components
• Active hepatic disease or unexplained persistent serum transaminase elevations
• Pregnancy or breastfeeding

Precautions

Use cautiously in:
• renal impairment; severe acute infection; hypotension; severe metabolic, endocrine, or electrolyte problems; uncontrolled seizures; visual disturbances; myopathy; major surgery; trauma; alcoholism
• history of hepatic disease
• concurrent use of amiodarone, clarithromycin, cyclosporine, digoxin, erythromycin, gemfibrozil and other fibrates, itraconazole, ketoconazole, nefazodone, nicotinic acid, protease inhibitors, verapamil, or warfarin
• cross-sensitivity to other drugs that can affect steroid levels
• females of childbearing age
• children younger than age 18 (safety not established).

Administration

• Check liver function tests before starting therapy.
• Give with evening meal. Don't give with large amounts of grapefruit juice.

Route	Onset	Peak	Duration
P.O.	Unknown	Unknown	Unknown

Adverse reactions

CNS: headache, asthenia

GI: nausea, vomiting, diarrhea, constipation, abdominal pain or cramps, flatulence, dyspepsia

Musculoskeletal: myalgia, rhabdomyolysis

Respiratory: upper respiratory infection

Interactions

Drug-drug. Amiodarone, verapamil: increased risk of severe myopathy or rhabdomyolysis

Digoxin: increased digoxin blood level and possible toxicity

Other lipid-lowering drugs (such as fibrates, gemfibrozil, nicotinic acid): myopathy

Potent CYP3A4 inhibitors (clarithromycin, cyclosporine, erythromycin, itraconazole, ketoconazole, nefazodone, protease inhibitors): increased risk of severe myopathy or rhabdomyolysis

Propranolol: decreased bioavailability of both drugs

Warfarin: increased anticoagulant effects

Drug-diagnostic tests. Alanine aminotransferase, aspartate aminotransferase: increased levels

Drug-food. Grapefruit juice (more than 1 qt daily): increased drug blood level, greater risk of adverse reactions

Drug-herbs. Red yeast rice: increased risk of adverse reactions

Drug-behaviors. Alcohol use: increased risk of hepatotoxicity

Patient monitoring

☞ Watch closely for myositis and other adverse musculoskeletal reactions. Know that drug may cause rhabdomyolysis.
• Monitor liver function tests, CBC, and lipid levels.
• In patients receiving warfarin concurrently, closely monitor prothrombin time and International Normalized Ratio.

Patient teaching

• Advise patient to take with evening meal, but not with large amounts of grapefruit juice.
• Tell patient drug may take up to 4 weeks to be effective.
☞ Caution patient to stop taking drug and contact prescriber if she suspects she is pregnant.
☞ Teach patient to recognize and report signs and symptoms of myopathy or hepatic disorders.
• Instruct patient to avoid alcohol and red yeast rice.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, herbs, and behaviors mentioned above.

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simvastatin

Zocor^® Therapeutics A lipid-lowering HMG-CoA reductase inhibitor used in hypercholesterolemia, to improve lipid profiles and ↓ mortality from CAD, DM, TIAs, stroke Adverse effects Constipation, flatulence, dyspepsia, abdominal pain, myalgia, muscle weakness. See Cholesterol-lowering drugs, Gemfibrozil, HMG-CoA reductase inhibitors, Hypercholesterolemia, Statin.