Atorvastatin Calcium Than 98% Bound to Plasma Proteins

2006 - Nurses Drug Database -

Atorvastatin calcium (ah-TORE-vah-stah-tin) Classification: Antihyperlipidemic, HMG-CoA reductase inhibitor Pregnancy Category: X (Rx) Lipitor

See also Antihyperlipidemic Agents—HMG-CoA Reductase Inhibitors. Action/Kinetics: Undergoes first-pass metabolism by CYP3A4 enzymes to active metabolites. t½: 14 hr. Plasma levels are not affected by renal disease but they are markedly increased with chronic alco- holic liver disease. Metabolized in the liver to active metabolites. Decreases in LDL cholesterol range from 35–40% (10 mg/day) to 50–60% (80 mg/day). Less than 2% excreted in the urine. Greater than 98% bound to plasma proteins. Uses: (1) Adjunct to diet to decrease elevated total and LDL cholesterol, apo-B, and triglyceride levels and to increase HDL cholesterol in primary hypercholesterolemia (including heterozygous familial and nonfamilial) and mixed dyslipidemia (including Frederickson type IIa and IIb). (2) Adjunct to other lipid- lowering treatments to reduce total and LDL cholesterol in homozygous familial hypercholesterolemia. (3) Primary dysbetalipoproteinemia (Frederickson type III) in those not responding adequately to diet. (4) Adjunct to diet to treat elevated serum triglyceride levels (Frederickson type IV). (5) Adjunct to diet to reduce total and LDL cholesterol and apo-B levels in boys and postmenarchal girls 10–17 years of age with heterozygous familial hypercholesterolemia; used after a trial of diet therapy if the following are present: (a) LDL cholesterol remains 190 mg/dL or higher or (b) LDL remains 160 mg/dL or higher AND there is a positive family history of premature CV disease or two or more other CVD risk factors are present. (6) Prophylaxis of CV disease by reducing the risk of MI, revascularization, and angina in adults without clinically evident coronary heart disease but with multiple risk factors (e.g., diabetes, smoking, normal to mildly elevated cholesterol levels) for it. Contraindications: Active liver disease or unexplained persistently high LFTs. Use with grapefruit juice. Pregnancy, lactation. Special Concerns: Safety and efficacy have not been determined in children less than 18 years of age. Side Effects: See also Antihyperlipidemic Agents—HMG-CoA Reductase Inhibitors. GI: Altered LFTs (usually within the first 3 months of therapy), flatulence, dyspepsia. CNS: Headache, paresthesia, asthenia, insomnia. Musculoskeletal: Myalgia, leg pain, back pain, arthritis, arthralgia. Respiratory: Sinusitis, bronchitis, pharyngitis, rhinitis. Miscellaneous: Infection, rash, pruritus, allergy, influenza, accidental trauma, peripheral edema, chest pain, alopecia. Laboratory Test Considerations: CPK (due to myalgia). Drug Interactions: Additional Interactions: • Antacids / Atorvastatin plasma levels

• Clarithromycin / Atorvastatin plasma levels; possibility of severe myopathy or rhabdomyolysis • Colestipol / Atorvastatin plasma levels

• Digoxin / Digoxin levels after 80 mg atorvastatin R/T digoxin absorption

• Diltiazem / Plasma atorvastatin levels risk of myopathy

• Erythromycin / Atorvastatin plasma levels; possibility of severe myopathy or rhabdomyolysis

• Nefazodone / RIsk of myopathy

• Oral contraceptives / Plasma levels of norethindrone and ethinyl estradiol

• Protease inhibitors (e.g., nelfinavir, ritonavir) / Atorvastatin levels risk of myopathy

• Verapamil Risk of myopathy

How Supplied: Tablets: 10 mg, 20 mg, 40 mg, 80 mg

Dosage • Tablets • Hypercholesterolemia (heterozygous familial and non-familial) and mixed dyslipidemia (Fredrieksen type IIa and IIb). Initial: 10–20 mg once daily (40 mg/day for those who require more than a 45% reduction in LDL cholesterol); then, a dose range of 10–80 mg once daily may be used. Individualize therapy according to goal of therapy and response. • Homozygous familial hypercholesterolemia. 10–80 mg/day. Used as an adjunct to other lipid-lowering treatments. • Heterozygous familial hypercholesterolemia in children 10–17 years of age. Initial: 10 mg/day; then, individualize dosage to a maximum of 20 mg/day. Adjust dosage at 4–week or more intervals. • Prophylaxis of CV disease. Adults: 10 mg/day.

Nursing Considerations Administration/Storage: 1. Give as a single dose at any time of the day, with or without food. 2. Determine lipid levels within 2–4 weeks; adjust dosage accordingly. 3. For an additive effect, may be used in combination with a bile acid binding resin. Do not use atorvastatin with fibrates. Assessment: 1. Document indications for therapy, onset and duration of disease, and other agents and mea- sures trialed. 2. Obtain baseline cholesterol profile and LFTs. Monitor LFTs at 6 and 12 weeks after starting therapy and with any dosage change, then semiannually thereafter. If ALT or AST exceed 3 times the normal level, reduce dose or withdraw drug. Assess need for liver biopsy if eleva- tions remain after stopping drug therapy. 3. Review dietary habits, weight, and exercise patterns; identify life-style changes needed. Client/Family Teaching: 1. These drugs help to lower blood cholesterol and fat levels, which have been proven to pro- mote CAD. 2. Take drug at the same time each day with or without food; avoid alcohol. 3. Continue dietary restrictions of saturated fat and cholesterol, regular exercise and weight loss in the overall goal of lowering cholesterol levels. See dietician for additional dietary recom- mendations. 4. Report immediately any unexplained muscle pain, weakness, or tenderness, especially if ac- companied by fever or malaise. 5. Use UV protection (i.e., sunglasses, sunscreens, clothing/hat) to prevent photosensitivity. Avoid prolonged exposure to direct or artificial sunlight. 6. Practice reliable birth control; may cause fetal damage. 7. Report for lab studies to evaluate effectiveness and need for dosage adjustments.

Outcomes/Evaluate: Reduction in total and LDL cholesterol levels