Names and pronunciation
(sim-va-sta′tin) FloLipid, Zocor
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Drug reference
(sim-va-sta′tin) FloLipid, Zocor
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Func. class.: Antilipemic
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Chem. class.: HMG-CoA reductase inhibitor
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Do not confuse: Zocor/Cozaar/Zoloft
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ACTION: Inhibits HMG-CoA reductase enzyme, which reduces cholesterol synthesis
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USES: As an adjunct for primary hyper- cholesterolemia (types IIa, IIb), isolated hypertriglyceridemia (Fredrickson type IV), and type III hyperlipoproteinemia, CAD, heterozygous familial hypercholes- terolemia; MI/stroke prophylaxis
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CONTRAINDICATIONS: Preg- nancy, breastfeeding, hypersensitivity, active hepatic disease Precautions: Past hepatic disease, alco- holism, severe acute infections, trauma, severe metabolic disorders, electrolyte imbalances, Chinese patients
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SIDE EFFECTS CNS: Headache, cognitive impairment GI: Nausea, constipation, diarrhea, dys- pepsia, flatus, abdominal pain, liver dys- function, pancreatitis, hyperglycemia INTEG: Rash, pruritus MS: Muscle cramps, myalgia, myositis, rhabdomyolysis, myopathy RESP: Upper respiratory tract infection
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INTERACTIONS • Do not use with cycloSPORINE, gemfi- brozil Increase: effects of warfarin Increase: rhabdomyolysis, myalgia; do not use concurrently—CYP3A4 inhibitors, niacin, erythromycin, clofibrate, clarithro- mycin, ketoconazole, itraconazole, protease inhibitors, macrolide antibiotics, danazol, delavirdine, nefazodone, verapamil, diltiaZEM, amiodarone, azole antifungals, telithromycin, voriconazole Increase: simvastatin effect—ATP1B1 inhibitors Increase: serum level of digoxin Drug/Herb Increase: effect—red yeast rice, kava, eucalyptus Decrease: effect—St. John’s wort Drug/Food Increase: simvastatin level—grapefruit juice (large amounts) Drug/Lab Test Increase: CK, LFTs, HbA1c
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DOSAGE AND ROUTES Hyperlipidemia Adult: PO 10-20 mg daily in the evening (range 5-40 mg) Atheroclerosis (unlabeled) • Adult: PO 20-40 mg/day in PM ini- tially; usual range 5-40 mg/day in PM, max 40 mg/day for most patients, max 80 mg/day for patients taking 80 mg/day chronically without myopathy; dosage adjustments may be made in ≥4-wk in- tervals; those taking verapamil and amio- darone max 20 mg/day; max <80 mg for Chinese patients taking lipid-modifying niacin doses Heterozygous familial hypercholester- olemia • Child/adolescent ≥10 yr including girls ≥1 yr postmenarche: PO 10 mg in PM, range 10-40 mg/day Renal dose • Adult: PO 5 mg/day in the evening (severe renal disease)
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Available forms: Tabs 5, 10, 20, 40, 80 mg
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Administer: • Discontinuing use before surgery is rec- ommended in renal failure; restart afterward • Avoid grapefruit juice • Total daily dose in evening • Store in cool environment in tight con- tainer protected from light
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Assess: • Diet history: fat consumption; baseline and lipid profile: LDL, HDL, TG, choles- terol • Hepatic studies at baseline, if clinically indicated; AST, ALT may increase • Rhabdomyolysis: muscle tenderness, increased CPK levels (10 × ULN); therapy should be discontinued, more likely in those receiving >80 mg/day, first year of treatment, those ≥65 yr, females • Chinese patients: avoid high doses (80 mg) if taking niacin >1 g/day due to increased risk of myopathies • Renal studies in patients with compro- mised renal systems: BUN, I&O ratio, creatinine • Pregnancy/breastfeeding: do not use in pregnancy, breastfeeding
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Evaluate: • Therapeutic response: decrease in LDL, total cholesterol, triglycerides; in- crease in HDL; slowing CAD
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • That blood work, follow-up exams will be necessary during treatment • To report severe GI symptoms, headache • That previously prescribed regimen will continue: low-cholesterol diet, exer- cise program, smoking cessation • To take in evening, avoid using grape- fruit juice • To report muscle pain, weakness, ab- dominal pain, dark urine; yellowing of skin, eyes; memory loss • This product may affect blood sugar levels in diabetes • That compliance is needed for positive results, not to skip or double doses • To notify prescriber if pregnancy is suspected or planned; not to breast- feed
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PHARMACOKINETICS Metabolized in liver (active metabolites); >98% protein bound; excreted primarily in bile, feces (60%), kidneys (15%); peak 1-2 hr; half-life 3 hr
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• Child/adolescent ≥10 yr including girls ≥1 yr postmenarche: PO 10 mg in PM, range 10-40 mg/day Renal dose
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