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Obesity lipase inhibitors

Taxane for breast cancer 15,500 Orlistat for obesity (lipase inhibitor) 46,000... [Pg.917]

Lipase Inhibitor Orlistat (Xenical, Roche) is prescribed for the treatment of obesity. It inhibits the gastrointestinal lipase enzymes by binding to the lipase through the serine site and inactivates the enzyme. Fat in the form of triglycerides cannot be hydrolyzed by the lipase and converted to free fatty acids and monoglycerides. Thus, there is no uptake of fat molecules into the cell tissue. [Pg.36]

Orlistat is a pancreatic lipase inhibitor used in conjunction with a hypocaloric diet to reduce the absorption of dietary fat in obese patients. Orlistat is administered twice daily immediately before, during or up to 1 hour after each meal. If the meal contains no fat there is no need to take Orlistat. [Pg.84]

Pharmacology Orlistat is a reversible lipase inhibitor for obesity management that acts by inhibiting the absorption of dietary fats. It exerts its therapeutic activity in the lumen of the stomach and small intestine. [Pg.1389]

Tetrahydrolipstatin is a lipase inhibitor developed and marketed by Roche (Basel, Switzerland) as an anti-obesity drug. With the incidence of obesity rising rapidly in the industrialized nations, having reached 33% of all adults in the United States and more than a quarter of all French schoolchildren, this problem will rapidly cease to remain one of lifestyle and enter the arena of medical costs associated with the diseases stemming from obesity. [Pg.407]

Heck AM, Yanovski JA, Calis KA (2000) Orlistat, a new lipase inhibitor for the management of obesity. Pharmacotherapy 20 270-279... [Pg.83]

The increased lability of diisopropyl acetals resulting from their steric compression1 lft is useful for retrieving aldehydes in sensitive substrates, A synthesis of Lipstatin [Scheme 2.55], a powerful pancreatic lipase inhibitor used in the treatment of obesity, required conditions for the deprotection of fJ-rm-butyldi-methylsilyloxy aldehyde intermediate 55.5 without competing -elimination.117... [Pg.81]

The fat-soluble vitamins (A, D, E, and K) are absorbed dissolved in lipid micelles, and, therefore, absorption will he impaired when the meal is low in fat. Gastrointestinal pathology that results in impaired fat absorption and steattorhea (e.g., untreated celiac disease) will also impair the absorption of fat-soluble vitamins, because they remain dissolved in the unabsorbed Upid in the intestinal lumen. Lipase inhibitors used for the treatment of obesity and fat replacers (e.g., sucrose polyesters such as Olestra ) will similarly impair the absorption of fat-soluble vitamins. [Pg.9]

Indications Obesity, weight reduction Category Lipase inhibitor Half-life I -2 hours... [Pg.425]

Meier, M.K., Blum-Kahlin, D., Bremer, K., ISLER, D., JOLY, P., Keller-Rupp, P. and Lengsfeld, H. (1991) Preclinical profile of the lipase inhibitor tetrahydrolipstatin (Ro 18-0647, THL), a potential drug for the treatment of obesity. Int. J. Obes. 15, 31... [Pg.192]

Zhi, j.. Mulligan, T. and Hauptman, J. (1999) Long-term systemic exposure of orlistat, a lipase inhibitor, and its metabolites in obese patients. J. Clin. Pharmacol. 39, 41-46... [Pg.192]

Orlistat, a GI lipase inhibitor used for weight loss, was administered over a 4-year period that resulted in a 37% reduction in the progression of type 2 diabetes mellitus in a group of insulin-resistant obese patients. Finally, although... [Pg.519]

Inhibition of Lipid Absorption - Agents which decrease the absorption of dietary lipids specifically by inhibiting pancreatic lipase may be suitable for the treatment of obesity. The reduced rate of lipid absorption produced by fenfluramine in rats is probably due to an inhibition of pancreatic lipase. The structural features of a series of phenethylamines, including fenfluramine, required for lipase inhibition have been described using partially purified rat and human pancreatic lipase. Pluronic L-101, a hydrophobic surfactant is a potent inhibitor of pancreatic lipase vitro and reduces body weight gain and carcass lipid after chronic administration to rats. Fecal excretion of dietary lipid is enhanced by Pluronic L-101, thus supporting its action as a lipase inhibitor. [Pg.162]

Orlistat, a semisynthetic derivative of lipstatin, is a potent and selective inhibitor of pancreatic lipases. It was designed to treat obesity. Orlistat prevents approximately 25% of dietary fat from being absorbed. Very little of the drug itself is absorbed. Its adverse effects are therefore restricted to those related to fat malabsorption, with potential losses of fat-soluble vitamins. It has a relatively small effect on body mass, but enough to realise in one study a 37% reduction in the incidence of type 2 diabetes. [Pg.485]

Regrettably, the pharmacologist must confess that no drugs exist that can be recommended for the purpose of weight reduction. The so-called appetite suppressants (anorexiants) act only, if at all, for a limited period and are fraught with side effects. Most anorexiants are derivatives of metham-phetamine that have been withdrawn from the market. A different mechanism of action is involved in the case of an inhibitor of pancreatic lipase, which is required in the intestines for fat absorption. This inhibitor (orlistat) diminishes fat absorption so that fats reach the lower bowel, where they can cause disturbances flatulence, steatorrhea, and frequent need to relieve the bowels occur in about 30% of affected subjects. These symptoms correspond exactly to those seen in pancreatic hypofunction which are then usually treated with pancreatic lipase. Before an obese person submits to treatment with orlistat, he or she should voluntarily reduce the food fat content by one half to live free of such unpleasant adverse effects. [Pg.328]

Orlistat (32 tetrahydrolipstatin, Xenical ) is a potent inhibitor of pancreatic lipase [23] which has been launched for the treatment of obesity in 1998. Large amounts of 32 required for clinical development were obtained using a route based on the enantioselective reduction of P-ketoester 29 to provide P-hydroxyester R)-30 followed by diastereoselective elaboration strategies (via (S,S,i )-31, Scheme 6)... [Pg.1354]


See other pages where Obesity lipase inhibitors is mentioned: [Pg.161]    [Pg.204]    [Pg.68]    [Pg.11]    [Pg.242]    [Pg.353]    [Pg.242]    [Pg.161]    [Pg.125]    [Pg.224]    [Pg.155]    [Pg.2668]    [Pg.67]    [Pg.83]    [Pg.155]    [Pg.242]    [Pg.253]    [Pg.50]    [Pg.41]    [Pg.164]    [Pg.65]    [Pg.160]    [Pg.253]    [Pg.41]    [Pg.631]    [Pg.843]    [Pg.1340]    [Pg.180]   
See also in sourсe #XX -- [ Pg.2667 , Pg.2668 ]




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