]> 2013-06-19T02:11:59-07:00 Orlistat taken from DrugBank http://www.drugbank.ca/drugs/DB01083 Orlistat is a drug designed to treat obesity. Its primary function is preventing the absorption of fats from the human diet, thereby reducing caloric intake. Orlistat works by inhibiting pancreatic lipase, an enzyme that breaks down triglycerides in the intestine. Without this enzyme, triglycerides from the diet are prevented from being hydrolyzed into absorbable free fatty acids and are excreted undigested. Pharmacology: Orlistat is a lipase inhibitor for obesity management that acts byinhibiting the absorption of dietary fats. At the recommendedtherapeutic dose of 120 mg three times a day, orlistat inhibitsdietary fat absorption by approximately 30%. It works by inhibitingpancreatic lipase, an enzyme that breaks down fat in theintestine. Without this enzyme, fat from the diet is excretedundigested, and not absorbed by the body. Because some vitamins arefat soluble, the effect of orlistat is to reduce their bodyabsorption. Therefore the drug should only be taken in conjuction withfatty meals, and a multivitamin tablet containing these vitamins (D EK and beta-carotene) should be taken once a day, at least 2 hoursbefore or after taking the drug. In the March 15, 2004 issue of CancerResearch, (1) 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. Mechanism of action: Orlistat is a reversible inhibitor of lipases. It exerts its therapeutic activity in the lumen of the stomach and small intestine by forming a covalent bond with the active serine residue site of gastric and pancreatic lipases. The inactivated enzymes are thus unavailable to hydrolyze dietary fat in the form of triglycerides into absorbable free fatty acids and monoglycerides. As undigested triglycerides are not absorbed, the resulting caloric deficit may have a positive effect on weight control. Drug type: Approved. Investigational. Small Molecule. Drug category: Anti-Obesity Agents. Enzyme Inhibitors DB01083 Orlistat 2010-02-04T00:00:00 Molecule (-)-Tetrahydrolipstatin Orlipastat Orlipastatum (INN-Latin) Tetrahydrolipstatin orlistat Alli Xenical Molecule Synonym SuperCategory Fatty acid synthase Pancreatic triacylglycerol lipase Lipoprotein lipase RelatedTo ModifiedDate Label Id Drug Has role Definition DefiningCitation Ab Curator Comment