Simvastatin

Trade Names:
Zocor
- Tablets 5 mg
- Tablets 10 mg
- Tablets 20 mg
- Tablets 40 mg
- Tablets 80 mg

Pharmacology

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Increases rate at which body removes cholesterol from blood and reduces production of cholesterol by inhibiting enzyme that catalyzes early rate-limiting step in cholesterol synthesis.

Pharmacokinetics

Absorption

Simvastatin T _max is 4 h and 85% of an oral dose is absorbed.

Distribution

Simvastatin is approximately 95% bound to plasma proteins.

Metabolism

Simvastatin undergoes extensive first-pass metabolism in the liver, its primary site of action.

Elimination

Thirteen percent of the drug is excreted in urine; 60% in feces.

Indications and Usage

Use lipid-altering agents in addition to a diet restricted in saturated fat and cholesterol.

For the reduction of the risk of total mortality by reducing coronary heart disease (CHD) deaths; reduction of the risk of nonfatal MI and stroke; reduction of the need for coronary and noncoronary revascularization procedures in patients at high risk of coronary events from existing CHD, diabetes, peripheral vessel disease, history of stroke, or other cerebrovascular disease.

For the reduction of elevated total cholesterol, LDL-cholesterol, apolipoprotein B (apo B) and triglyceride levels, and the increase of HDL-cholesterol in patients with primary hypercholesterolemia and mixed dyslipidemia (Fredrickson types IIa and IIb); treatment of patients with hypertriglyceridemia (Fredrickson type IV hyperlipemia); treatment of patients with primary dysbetalipoproteinemia (Fredrickson type III hyperlipidemia); the reduction of total cholesterol and LDL-cholesterol in patients with homozygous familial hypercholesterolemia as an adjunct to other lipid-lowering treatments or if such treatments are unavailable.

If after an adequate trial of diet therapy, LDL-cholesterol remains at 190 mg/dL or more, or LDL-cholesterol remains at 160 mg/dL or more and there is a positive family history of premature CV disease or 2 or more other CV disease risk factors are present, in adolescent boys and girls at least 1 yr postmenarche, 10 to 17 yr of age, with heterozygous familial hypercholesterolemia as an adjunct to diet to reduce total cholesterol, LDL-cholesterol, and apo B levels.

Contraindications

Active liver disease or unexplained persistent elevations of liver function values; pregnancy; lactation; hypersensitivity to any component.

Dosage and Administration

PO Start with 20 to 40 mg once daily in the evening. For patients at high risk for a CHD event, start with 40 mg/day. Perform lipid determinations after 4 wk of therapy and periodically thereafter.

PO Start with 40 mg/day in the evening or 80 mg/day in 3 divided doses of 20 mg, 20 mg, and an evening dose of 40 mg.

PO Start with 10 mg/day in the evening. Make dose adjustments at intervals of 4 wk or more (max, 40 mg/day).

PO Do not exceed 10 mg/day.

PO Start with 5 mg/day (max, 10 mg/day).

PO Do not exceed 20 mg/day.

PO Dosage adjustment should not be necessary in mild to moderate renal function impairment. Start with 5 mg/day in patients with severe renal function impairment and monitor closely.

Storage/Stability

Store at 41° to 86°F.

Drug Interactions

Risk of myopathy or rhabdomyolysis may be increased.

Anticoagulant effect of warfarin may be increased.

Simvastatin plasma levels may be reduced, decreasing the efficacy.

Simvastatin peak plasma levels may be decreased. The clinical importance of this interaction has not been determined.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Headache (4%); asthenia (2%).

GI

Constipation, diarrhea, flatulence (2%); dyspepsia, nausea (1%).

Musculoskeletal

Myalgia (1%); myopathy/rhabdomyolysis (less than 0.1%).

Respiratory

Upper respiratory tract infection (2%).

Miscellaneous

Abdominal pain (3%).

Precautions

Pregnancy

Category X .

Lactation

Undetermined.

Children

Safety and efficacy not established in children younger than 10 yr of age with heterozygous familial hypercholesterolemia

Hepatic Function

Use drug with caution in patients who consume substantial quantities of alcohol or who have history of liver disease. Marked, persistent increases in serum transaminases have occurred.

Skeletal muscle effects

Rhabdomyolysis with renal function impairment secondary to myoglobinuria has occurred in this class of drugs. Consider myopathy in any patient with diffuse myalgias, muscle tenderness or weakness, or marked CPK elevation.

Patient Information

• Caution patient that this medication must not be taken during pregnancy or when pregnancy is possible. Advise patient to use reliable form of birth control while taking this drug.
• Advise patient to control weight and to adhere to prescribed dietary regimen.
• Advise patient that exercise and diets that reduce intake of cholesterol and saturated fats are helpful.
• Instruct patient to report the following symptoms to health care provider: any unexplained muscle pain, tenderness, or weakness, especially if accompanied by fever or malaise; yellowing of skin or eyes.
• Tell patient to avoid alcoholic beverages.

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