Tablet Presentation

Each film coated tablets contains:

1.Atorvastatin Calcium eq. to Atorvastatin IP              10 mg Ezetimibe                                   10 mg

2.Atorvastatin Calcium eq. to Atorvastatin IP              40 mg Ezetimibe                                   10 mg

Before knowing its combination, we should need to know how they work individually so we know that Atorvastatin Calciumis a selective, competitive HMG-CoA reductase inhibitor. Atorvastatin Calcium is the only drug in its class specifically indicated for lowering both elevated LDL-cholesterol and triglycerides in patients with hypercholesterolemia. It prevents coronary atherosclerosis and reduces the risk of heart attack.
Ezetimibe is in a class of lipid-lowering compounds that selectively inhibits the intestinal absorption of cholesterol and related phytosterols.

Indications

This combination(Atorvastatin Ezetimibe Tablet) is used for the treatment of dyslipidemia and the prevention of cardiovascular disease.
Ezetimibe is a prescription drug that is used to treat high cholesterol and a rare genetic condition called s

Pharmacology

Atorvastatin

After oral administration, Atorvastatin is rapidly absorbed, with peak serum concentrations reaching within 1 to 2 hours. Extent of absorption increases in proportion to Atorvastatin dose. The absolute bioavailability of Atorvastatin is approximately 14% and the systemic availability of HMG-CoA reductase inhibitory activity is approximately 30%. Mean volume of distribution is approximately 381 liters. Atorvastatin is ≥ 98% bound to plasma proteins. Atorvastatin is extensively metabolized to ortho-and para hydroxylated derivatives and various beta-oxidation products. Approximately 70% of circulatory inhibitory activity for HMG-CoA reductase is attributed to active metabolites. Atorvastatin and its metabolites are eliminated primarily in bile following hepatic and/or extrahepatic metabolism; however the drug does not appear to undergo enterohepatic recirculation. Mean plasma elimination half life of Atorvastatin in humans is approximately 14 hrs, but the half life of inhibitory activity for HMG-CoA reductase is 20-30 hours due to contribution of active metabolites.

Ezetimibe

Ezetimibe is rapidly absorbed and conjugated after oral administration. Tmax of Ezetimibe and Ezetimibe-glucuronide are 4-12 hrs and 1-2 hrs respectively. Concomitant food administration (high fat or non-fat meals) has no effect on the extent of absorption of Ezetimibe. Ezetimibe can be administered with or without food. Ezetimibe and Ezetimibe-glucuronide are highly bound (>90%) to human plasma proteins. In humans, Ezetimibe gets rapidly metabolized to Ezetimibe-glucuronide. Ezetimibe and Ezetimibe glucuronide are the major drug-derived compounds detected in plasma, constituting approximately 10-20% and 80-90% of the total drug in plasma, respectively. Both Ezetimibe and Ezetimibe-glucuronide are slowly eliminated from plasma with a half-life of approximately 22 hours for both Ezetimibe and Ezetimibe-glucuronide.
From the pharmacokinetic profile, it is clear that both the drugs are rapidly absorbed after oral administration. The Tmax for Atorvastatin and Ezetimibe glucuronide (pharmacologically active metabolite of Ezetimibe) are also same (i.e. 1-2 hours) which further supports their use in fixed dose combination as a single dose. Further Atorvastatin and Ezetimibe can be administered as a single dose at any time of the day with or without food.

Mechanism of Action

Atorvastatin belongs to the category of statins, which inhibits 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase. Synthesis of mevalonic acid is impeded, which is a rate-limiting step in cholesterol biosynthesis. This results in a decrease in intracellular cholesterol leading to an increase in the number of synthesis of LDL receptors and increased clearance of LDL cholesterol in plasma. HMG-CoA reductase inhibitors may also lower plasma cholesterol levels by decreasing hepatic production of VLDL and LDL cholesterol.
Ezetimibe is a selective cholesterol absorption inhibitor, which potently and selectively prevents absorption of cholesterol from dietary and biliary sources by preventing transport of cholesterol through the intestinal wall. This reduces the overall delivery of cholesterol to the liver, thereby promoting the synthesis of LDL receptors and a subsequent reduction in serum LDL-C.Ezetimibe does not affect the absorption of fat-soluble vitamins.

Drug Interactions

BEFORE TAKING THIS TABLET TELL THE DOCTOR ABOUT ANY MEDICAL PROBLEMS AN ALLERGIES THAT CHILD HAS NOW OR HAS HAD.
This tablet is the combination of Atorvastatin and Ezetimibe and has unique duel mode of action i.e in this combination, atorvastatin used to treat cardiovascular disease and ezetimibe used to treat high cholesterol. Drug interactions occur when it is taken with another drug or with food. Atorvastatin help to Increases digoxin levels and increases anticoagulant effect of warfarin. Avoid the combination of HMG-CoA reductase inhibitors and fibrates. Ezetimibe: Cholestyramine decreases AUC of ezetimibe by approx 55%, ciclosporin may increase ezetimibe levels.

Side Effects

The Atorvastatin Calcium and Ezetimibe Tablet combination have some side effects which are Headache, Flatulence, Dyspepsia, Rash, Allergy, Infection and Back pain.

Contraindications

• Caution in pregnancy.
• Caution in lactation.
• Caution in Hypersensitivity.

Conclusions

From the above discussion, it can be concluded that this Atorvastatin and Ezetimibe tablet could improve the quality of life with cardiovascular disease and sitosterolemia. We are making superior quality Atorvastatin & Ezetimibe tablet that is used to treat cardiovascular disease. Our offered tablet is processed using high grade chemical compounds and other required drugs by our experienced quality controllers that ensure its quality, purity and chemical properties. Highly treasured among the clients for its reliability, accurate composition, excellent physical and purity, this tablet is offered to our esteemed clients at the market leading prices.