Orlistat 120 MG.
BRAND NAME: – ORLAK (Orlistat 120 mg)
Composition: – Each capsule contains 120mg Orlistat
Packing: – 10*10 (Alu-Alu)
1. Pharmacodynamics: – Orlistat is a lipase inhibitor for obesity management that acts by inhibiting the absorption of dietary fats. At the recommended therapeutic dose of 120 mg three times a day, orlistat inhibits dietary fat absorption by approximately 30%. It works by inhibiting pancreatic lipase, an enzyme that breaks down fat in the intestine. Without this enzyme, fat from the diet is excreted undigested and not absorbed by the body. Because some vitamins are fat soluble, the effect of orlistat is to reduce their body absorption. Therefore the drug should only be taken in conjuction with fatty meals, and a multivitamin tablet containing these vitamins (D E K and beta-carotene) should be taken once a day, at least 2 hours before or after taking the drug. In the March 15, 2004 issue of Cancer Research,  Steven J. Kridel et al. state that orlistat may also inhibit growth of prostate cancer, and in theory may be useful in treating other cancers, by interfering with the metabolism of fats.
a. Absorption: – Systemic absorption of orlistat is minimal, however systemic absorption of the drug is not needed for activity.
b. Protein Binding: – >99% bound to plasma proteins (lipoproteins and albumin were major binding proteins).
c. Metabolism: – Metabolized primarily within the gastrointestinal wall forming relatively inactive metabolites. Metabolites M1 (4-member lactone ring hydrolyzed) and M3 (M1 with N-formyl leucine moiety cleaved) accounted for approximately 42% of total radioactivity in plasma. M1 and M3 have an open beta-lactone ring and extremely weak lipase inhibitory activity (1000- and 2500-fold less than orlistat, respectively).
d. Route of Elimination: – Following a single oral dose of 360 mg 14C-orlistat in both normal weight and obese subjects, fecal excretion of the unabsorbed drug was found to be the major route of elimination. Orlistat and its M1 and M3 metabolites were also subject to biliary excretion.
e. Half-Life: – 1 to 2 hours
f. Toxicity: – The results of a massive overdose of Xenical are unknown, although the drug seems relatively harmless.
1. Orlistat 120 mg (Anti Obesity ) Capsule is used for the treatment of obesity.
2. It also leads to a modest reduction in blood pressure.
3. Reduce the risk of high cholesterol levels.
4. Use in weight loss.