Lipicon EZ

Atorvastatin: In animal models, atorvastatin 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; atorvastatin also reduces LDL production and the number of LDL particles.

Ezetimibe: Ezetimibe reduces blood cholesterol by inhibiting the absorption of cholesterol by the small intestine. The molecular target of ezetimibe has been shown to be the sterol transporter, Niemann-Pick C1-Like 1 (NPC1L1), which is involved in the intestinal uptake of cholesterol and phytosterols. In a 2-week clinical study in 18 hypercholesterolemic patients, ezetimibe inhibited intestinal cholesterol absorption by 54%, compared with placebo. Ezetimibe had no clinically meaningful effect on the plasma concentrations of the fat-soluble vitamins A, D, and E and did not impair adrenocortical steroid hormone production. Ezetimibe does not inhibit cholesterol synthesis in the liver or increase bile acid excretion. Ezetimibe localizes at the brush border of the small intestine and inhibits the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver. This causes a reduction of hepatic cholesterol stores and an increase in clearance of cholesterol from the blood; this distinct mechanism is complementary to that of statins.

• Cyclosporine, HIV protease inhibitors (tipranavir plus ritonavir), hepatitis C protease inhibitor (telaprevir), gemfibrozil: Avoid this tablet
• HIV protease inhibitor (lopinavir plus ritonavir): Use with caution and lowest dose necessary.
• Clarithromycin, itraconazole, HIV protease inhibitors (saquinavir plus ritonavir, darunavir plus ritonavir, fosamprenavir, fosamprenavir plus ritonavir): Do not exceed 10/20 mg this tablet daily.
• HIV protease inhibitor (nelfinavir), hepatitis C protease inhibitor (boceprevir): Do not exceed 10/40 mg this tablet daily.
• Other lipid-lowering medications: Use with fenofibrates or lipid-modifying doses (≥1 g/day) of niacin increases the risk of adverse skeletal muscle effects. Caution should be used when prescribing with this tablet.
• Fenofibrates: Combination increases exposure of ezetimibe. If cholelithiasis is suspected in a patient receiving ezetimibe and a fenofibrate, gallbladder studies are indicated and alternative lipid- lowering therapy should be considered.
• Cholestyramine: Combination decreases exposure of ezetimibe.
• Digoxin: Patients should be monitored appropriately.
• Oral contraceptives: Values for norethindrone and ethinyl estradiol may be increased.
• Rifampin should be simultaneously coadministered with this tablet.

Pregnancy Category X. This tablet is contraindicated in women who are or may become pregnant. Serum cholesterol and triglycerides increase during normal pregnancy. Lipid-lowering drugs offer no benefit during pregnancy, because cholesterol and cholesterol derivatives are needed for normal fetal development. Atherosclerosis is a chronic process, and discontinuation of lipid-lowering drugs during pregnancy should have little impact on long-term outcomes of primary hypercholesterolemia therapy. It is not known whether atorvastatin is excreted in human milk, but a small amount of another drug in this class does pass into breast milk.

Patients should be advised to report promptly any unexplained and/or persistent muscle pain, tenderness, or weakness. This tablet should be discontinued immediately if myopathy is diagnosed or suspected.

Skeletal muscle effects (e.g., myopathy and rhabdomyolysis): Risks increase with higher doses and concomitant use of certain CYP3A4 inhibitors, fibric acid derivatives, and cyclosporine. Predisposing factors include advanced age (>65), uncontrolled hypothyroidism, and renal impairment. Rare cases of rhabdomyolysis with acute renal failure secondary to myoglobinuria have been reported.

Liver enzyme abnormalities: Persistent elevations in hepatic transaminase can occur. Check liver enzyme tests before initiating therapy and as clinically indicated thereafter.

Other lipid regulating drugs

Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.