International Nonproprietary Name (INN): Atorvastatin
Pharmaceutic group: Hypocholesterolemic
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THERE ARE CONTRAINDICATIONS. CAREFULLY READ THE INSTRUCTIONS FOR USE, OR OBTAIN A SPECIALIST ADVICE
Atorvastatin is an oral drug that lowers the level of cholesterol in the blood. It belongs to a class of drugs referred to as statins, which includes lovastatin (Mevacor), simvastatin, (Zocor), fluvastatin (Lescol), and pravastatin (Pravachol) and rosuvastatin (Crestor). All statins, including atorvastatin, prevent the production of cholesterol in the liver by blocking HMG-CoA reductase, an enzyme that makes cholesterol. Statins reduce total cholesterol as well as LDL cholesterol in blood. LDL cholesterol is believed to be the "bad" cholesterol that is primarily responsible for the development of coronary artery disease. Reducing LDL cholesterol levels retards progression and may even reverse coronary artery disease. Atorvastatin also raises the concentrations of HDL ("good") cholesterol that protects against coronary artery disease and reduces the concentration of triglycerides in the blood. (High blood concentrations of triglycerides also have been associated with coronary artery disease.) The FDA approved atorvastatin in December 1996.
Atorvastatin is used for the treatment of elevated total cholesterol, LDL, and triglycerides and to elevate HDL cholesterol. The effectiveness of atorvastatin in lowering cholesterol is dose-related, meaning that higher doses reduce cholesterol more. Atorvastatin prevents angina, stroke, heart attack, hospitalization for congestive heart failure, and revascularization procedures in individuals with coronary artery disease. Atorvastatin reduces the risk of myocardial infarction (heart attack), stroke, angina and revascularization procedures in adults with multiple risk factors for coronary artery disease. Atorvastatin also prevents heart attacks and strokes in patients with type 2 diabetes with multiple risk factors for coronary artery disease.
DOSING: Atorvastatin is prescribed once daily. The usual starting dose is 10-20 mg per day, and the maximum dose is 80 mg per day. Individuals who need more than a 45% reduction in LDL cholesterol may be started at 40 mg daily. Atorvastatin may be taken with or without food and at any time of day.
DRUG INTERACTIONS: Decreased elimination of atorvastatin could increase levels of atorvastatin in the body and increase the risk of muscle toxicity from atorvastatin. Therefore, atorvastatin should not be combined with drugs that decrease its elimination. Examples of such drugs include erythromycin (E-Mycin), ketoconazole (Nizoral), itraconazole (Sporanox), clarithromycin (Biaxin), telithromycin (Ketek), cyclosporine (Sandimmune), nefazodone (Serzone), and HIV protease inhibitors such as indinavir (Crixivan) and ritonavir (Norvir).
Large quantities of grape fruit juice (>1.2 liters daily) also will increase blood levels of atorvastatin and should not be taken. Amiodarone (Cordarone), verapamil (Calan Verelan, Isoptin), cyclosporine (Sandimmune), niacin (Niacor, Niaspan, Slo-Niacin), gemfibrozil (Lopid) and fenofibrate (Tricor) also may increase the risk of muscle toxicity when combined with atorvastatin.
Atorvastatin increases the effect of warfarin (Coumadin) and the concentration in blood of digoxin (Lanoxin). Patients taking atorvastatin and warfarin or digoxin should be monitored carefully. Cholestyramine (Questran) decreases the absorption of atorvastatin. Atorvastatin should be given at least two hours before and at least four hours after cholestyramine.
PREGNANCY: Atorvastatin should not be taken during pregnancy because the developing fetus requires cholesterol for development, and atorvastatin reduces the production of cholesterol. Atorvastatin should only be administered to women of childbearing age if they are not likely to become pregnant. NURSING MOTHERS: It is not known if atorvastatin is secreted in breast milk. Because of the potential risk of adverse events, breastfeeding mothers should not use atorvastatin.