Classifications: antilipemic; hmg-coa reductase inhibitor (statin); Therapeutic: antihyperlipemic; statin
Pregnancy Category: X
5 mg, 10 mg, 20 mg, 40 mg, 80 mg tablets
Inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase; similar in action to lovastatin but more potent.
HMG-CoA reductase inhibitors increase HDL cholesterol, and decrease LDL cholesterol, and total cholesterol synthesis.
Effectiveness indicated by decreased serum triglycerides, decreased LDL, cholesterol, and modest increases in HDL cholesterol.
Hypercholesterolemia (alone or in combination with bile acid sequestrants), familial hypercholesterolemia. Reduces risk
of coronary death and nonfatal MI.
Hypersensitivity to simvastatin; active liver disease, hepatic encephalopathy, hepatitis, jaundice, rhabdomyolysis; cholestasis;
pregnancy (category X), children <10 y, lactation.
Homozygous familial hypercholesterolemia, history of liver disease, alcoholics; renal disease, renal impairment; seizure
Route & Dosage
Adult: PO 540 mg q.d. (max: 80 mg q.d.). Patients taking danazol or cyclosporine should not exceed 10 mg q.d.
- Adjust dosage usually at 4-wk intervals.
- Give in the evening.
- Store at 15°30° C (59°86° F).
Adverse Effects (≥1%)CV:
Dizziness, headache, vertigo, asthenia, fatigue
Nausea, diarrhea, vomiting, abdominal pain, constipation
, flatulence, heartburn, transient elevations in liver transaminases,
transient elevations in CPK. Body as a Whole: Fatigue
May increase PT when administered with warfarin; cyclosporine, gemfibrozil, fenofibrate, clofibrate,
antilipemic doses of niacin, fluconazole, itraconazole, ketoconazole, miconazole, nefazodone, nelfinavir, ritonavir, saquinavir, sildenafil, tacrolimus, clarithromycin, erythromycin, telithromycin
may increase serum
levels and increase risk of myopathy, rhabdomyolysis and acute kidney failure. Food: Grapefruit juice
(>1 qt/d) may increase risk of myopathy, rhabdomyolysis. Herbal: Peppermint oil
may increase plasma
concentrations. St. John's wort
may decrease efficacy
Rapidly from GI tract. Onset:
2 wk. Peak:
46 wk. Distribution:
95% protein bound; achieves high liver concentrations; crosses placenta. Metabolism:
Extensive first-pass metabolism
in liver to its active metabolite
13% in urine, 60% in bile and feces.
Assessment & Drug Effects
- Lab tests: Obtain baseline and periodic (q6mo) liver function during the first year and yearly thereafter. Monitor cholesterol
levels throughout therapy.
- Monitor coagulation studies with patients receiving concurrent warfarin therapy. PT may be prolonged.
- Assess for and report unexplained muscle pain. Determine CPK level at onset of muscle pain.
Patient & Family Education
- Report unexplained muscle pain, tenderness, or weakness, especially if accompanied by malaise or fever, to physician.
- Report signs of bleeding to physician promptly when taking concurrent warfarin.
- Moderate intake of grapefruit juice while taking this medication.