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Lipitor. Rol (total-C), LDL-cholesterol (LDL-C), and apolipoprotein B (apo B) promote human atherosclerosis and are risk factors for developing cardiovascular disease, while increased levels of HDL-C are associated with a decreased cardiovascular risk. In animal models, LIPITOR lowers plasma cholesterol and lipoprotein levels by inhibiting HMG-CoA reductase and cholesterol synthesis in the liver and by increasing the number of hepatic LDL receptors on the cell-surface to enhance uptake and catabolism of LDL; LIPITOR also reduces LDL production and the number of LDL particles. LIPITOR reduces LDL-C in some patients with homozygous familial hypercholesterolemia (FH), a population that rarely responds to other lipid-lowering medication(s). A variety of clinical studies have demonstrated that elevated levels of total-C, LDL-C, and apo B (a membrane complex for LDL-C) promote human atherosclerosis. Similarly, decreased levels of HDL-C (and its transport complex, apo A) are associated with the develo lipitor

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Pment of atherosclerosis. Epidemiologic investigations have established that cardiovascular morbidity and mortality vary directly with the level of total-C and LDL-C, and inversely with the level of HDL-C. LIPITOR reduces total-C, LDL-C, and apo B in patients with homozygous and heterozygous FH, nonfamilial forms of hypercholesterolemia, and mixed dyslipidemia. LIPITOR also reduces VLDL-C and TG and produces variable increases in HDL-C and apolipoprotein A-1. LIPITOR reduces total-C, LDL-C, VLDL-C, apo B, TG, and non- HDL-C, and increases HDL-C in patients with isolated hypertriglyceridemia. LIPITOR reduces intermediate density lipoprotein cholesterol (IDL-C) in patients with dysbetalipoproteinemia. Like LDL, cholesterol-enriched triglyceride-rich lipoproteins, including VLDL, intermediate density lipoprotein (IDL), and remnants, can also promote atherosclerosis. Elevated plasma triglycerides are frequently found in a triad with low HDL-C levels and small LDL particles, as well as in a lipitor

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lipitor be based on therapeutic response (see DOSAGE AND ADMINISTRATION). Pharmacokinetics and Drug Metabolism. Absorption: Atorvastatin is rapidly absorbed after oral administration; maximum plasma concentrations occur within 1 to 2 hours. Extent of absorption increases in proportion to atorvastatin dose. The absolute bioavailability of atorvastatin (parent drug) is approximately 14% and the systemic availability of HMG-CoA reductase inhibitory activity is approximately 30%. The low systemic availability is attributed to presystemic clearance in gastrointestinal mucosa and or hepatic first-pass metabolism. Although food decreases the rate and extent of drug absorp lipitor.

lipitor Tion by approximately 25% and 9% lipitor, respectively lipitor, as assessed by Cmax and AUC lipitor, LDL-C reduction is similar whether atorvastatin is given with or without food. Plasma atorvastatin concentrations are lower (approximately 30% for Cmax and AUC) following evening drug administration compared with morning. However lipitor, LDL-C reduction is the same regardless of the time of day of drug administration (see DOSAGE AND ADMINISTRATION). Distribution: Mean volume of distribution of atorvastatin is approximately 381 liters. Atorvastatin is 98% bound to plasma proteins. A blood plasma ratio of approximately 0.25 indicates poor drug penetration into red blood cells. Based on observations in rats lipitor, atorvastatin is likely to be secreted in human milk (see CONTRAINDICATIONS lipitor, Pregnancy and Lactation lipitor, and PRECAUTIONS lipitor, Nursing Mothers). Metabolism: Atorvastatin is extensively metabolized to ortho- and parahydroxylated derivatives and various beta-oxidation products. In vitro inhibition of HMG-CoA reductase by ortho- and parahydroxylated metabolites is equivalent to that of atorvastatin. Approximately 70% of circulating inhibitory activity for HMG-CoA reductase is attributed to active metabolites. In vitro studies suggest the importance of atorvastatin metabolism by cytochrome P450 3A4 lipitor, consistent with increased plasma concentrations of atorv.

lipitor Ations in rats lipitor, atorvastatin is likely to be secreted in human milk (see CONTRAINDICATIONS lipitor, Pregnancy and Lactation lipitor, and PRECAUTIONS lipitor, Nursing Mothers). Metabolism: Atorvastatin is extensively metabolized to ortho- and parahydroxylated derivatives and various beta-oxidation products. In vitro inhibition of HMG-CoA reductase by ortho- and parahydroxylated metabolites is equivalent to that of atorvastatin. Approximately 70% of circulating inhibitory activity for HMG-CoA reductase is attributed to active metabolites. In vitro studies suggest the importance of atorvastatin metabolism by cytochrome P450 3A4 lipitor, consistent with increased plasma concentrations of atorva.

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Sclerosis) decreases blood flow and, therefore, the oxygen supply to the heart, brain, and other parts of the body. Lowering blood levels of cholesterol and other fats may help to decrease your chances of getting heart disease, angina (chest pain), strokes, and heart attacks. In addition to taking a cholesterol-lowering medication, making certain changes in your daily habits can also lower your cholesterol blood levels. You should eat a diet that is low in saturated fat and cholesterol (see SPECIAL DIETARY), exercise 30 minutes on most, if not all days, and lose weight if you are overweight. How should this medicine be used?Return to top Atorvastatin comes as a tablet to take by mouth. It is usually taken once a day with or without food. Take atorvastatin at around the same time every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take atorvastatin exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.Your doctor may start you on a low dose of atorvastatin and gradually increase your dose, not more than once every 2-4 weeks.Continue to take atorvastatin even if you feel well. Do not stop taking atorvastatin without talking to your doctor.Other uses for this medicineReturn to top This medication may be prescribed for other uses; ask your doctor or pharmacist for more information.What special precautions should I follow?Return to top Before taking atorvastatin, tell your doctor and pharmacist if you are allergic to atorvastatin or a

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