Names and pronunciation
(a-tore′va-stat-in) Lipitor
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Drug reference
(a-tore′va-stat-in) Lipitor
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Func. class.: Antilipidemic
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Chem. class.: HMG-CoA reductase inhibitor (statin)
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Do not confuse: atorvastatin/atomoxetine Lipitor/Loniten/ZyrTEC
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ACTION: Inhibits HMG-CoA reductase enzyme, which reduces cholesterol synthe- sis; high doses lead to plaque regression
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USES: As adjunct for primary hypercho- lesterolemia (types Ia, Ib), elevated triglyceride levels, prevention of CV disease A by reduction of heart risk in those with mildly elevated cholesterol, heterozygous familial hypercholesterolemia in pediatric patients , intensive lipid-lowering after an ACS event, non-cardioembolic stroke/TIA, to reduce total/LDL cholesterol in homozy- gous familial hypercholesterolemia
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CONTRAINDICATIONS: Preg- nancy, breastfeeding, hypersensitivity, active hepatic disease Precautions: Previous hepatic disease, alcoholism, severe acute infections, trauma, severe metabolic disorders, electrolyte imbalance
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SIDE EFFECTS CNS: Headache, asthenia, insomnia EENT: Lens opacities GI: Abdominal cramps, constipation, diarrhea, flatus, heartburn, dyspepsia, liver dysfunction, pancreatitis, nausea, increased serum transaminase GU: Impotence, UTI INTEG: Rash MISC: Hypersensitivity; gynecomastia (child) MS: Arthralgia, myalgia, rhabdomyolysis, myositis RESP: Pharyngitis, sinusitis
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INTERACTIONS Increase: rhabdomyolysis—azole antifun- gals, cycloSPORINE, erythromycin, niacin, gemfibrozil, clofibrate, amiodarone, bocepre- vir, nelfinavir, lopinavir/ritonavir, macrolides, tacrolimus, telaprevim; use lower dose Increase: serum level of digoxin Increase: toxicity, decreased metabolism of HMG-CoA: colchicine, diltiazem, fibric acid derivatives, protease inhibitors Increase: levels of oral contraceptives Increase: levels of atorvastatin, myopa- thy—CYP3A4 inhibitors Increase: effects of warfarin Decrease: atorvastatin levels—colesti- pol, antacids, cholestyramine Drug/Herb Decrease: effect—St. John’s wort Drug/Food • Possible toxicity when used with grapefruit juice (large amounts); oat bran may reduce effectiveness Drug/Lab Test Increase: ALT, AST, CK
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DOSAGE AND ROUTES • Adult: PO 10-20 mg/day, usual range 10- 80 mg/day, dosage adjustments may be made in 2- to 4-wk intervals, max 80 mg/day; pa- tients who require >45% reduction in LDL may be started at 40 mg/day; concurrent use with clarithromycin, itraconazole, saquina- vir/ritonavir, derunavir, fosamprenivir, fosamprenavir/ritonavir max 20 mg/day • Child 10-17 yr: PO 10 mg daily, adjust q4wk, max 20 mg/day
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Available forms: Tablets 10, 20, 40, 80 mg
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Administer: • Total daily dose at any time of day without regard to meals • Store in cool environment in tight container protected from light
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Assess: • Hypercholesterolemia: diet, obtain diet history including fat, cholesterol in diet; cholesterol triglyceride levels periodically during treatment; check lipid panel 6-12 wk after changing dose • Hepatic studies q1-2mo, at initiation, 6, 12 wk after initiation or change in dose, periodically thereafter; AST, ALT, LFTs may be increased • Bowel status: constipation, stool soft- eners may be needed; if severe, add fiber, water to diet • Rhabdomyolysis: for muscle pain, tenderness, obtain CPK baseline; if markedly increased, product may need to be discontinued; many drug interac- tions may increase possibility for rhab- domyolysis • Pregnancy/breastfeeding: do not breastfeed or use in pregnancy
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Evaluate: • Therapeutic response: decrease in LDL, total cholesterol, triglycerides, CAD; increase in HDL:LDL ratio
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • That compliance is needed for positive results to occur, not to skip or double doses • That blood work and eye exam will be necessary during treatment • To report blurred vision, severe GI symptoms, headache, muscle pain, and weakness; to avoid alcohol • That previously prescribed regimen will continue: low-cholesterol diet, exer- cise program, smoking cessation • Pregnancy/breastfeeding: identify if pregnancy is planned or suspected, or if breastfeeding
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PHARMACOKINETICS Peak 1-2 hr, metabolized in liver, highly protein-bound, excreted primarily in urine, half-life 14 hr, protein binding 98%
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• Adult: PO 10-20 mg/day, usual range 10- 80 mg/day, dosage adjustments may be made in 2- to 4-wk intervals, max 80 mg/day; pa- tients who require >45% reduction in LDL may be started at 40 mg/day; concurrent use with clarithromycin, itraconazole, saquina- vir/ritonavir, derunavir, fosamprenivir, fosamprenavir/ritonavir max 20 mg/day
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