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Orlistat: profile and news
Low-dose Orlistat helps in fat war -- but heed warning 16 May 2006 From the analyst's couch: Anti-obesity therapies May 4, 2006 Healthcare: At a Glance - Government Launches Weight-Control ... May 12, 2006 Another Weightloss Pill Poses Health Risks May 3, 2006 Allergan's Weight-Loss Bands Beat Diet, Exercise, Study Says May 1, 2006 The Heavy Burden of Stereotyping May 8, 2006 Stomach surgery may have a role in moderate obesity May 2, 2006 Australian LAP-BAND Study Passes Over Low-Carb Comparison May 3, 2006 Gastric Banding May Help In Moderate Obesity May 2, 2006 LAP-BAND Patients Lose Significantly Greater Amounts of Initial ... May 1, 2006 Gastric Banding Effective for Mild to Moderate Obesity May 1, 2006 Glaxo Launches Weight-Loss Website Prior to FDA Action on Diet ... Apr 26, 2006 Cutting weight without the knife Apr 23, 2006 AACE: Insulin Not Sodium May Be Hypertension's Bad Actor Apr 28, 2006 Other information Indication For the treatment of Obesity including management of weight loss and weight maintenance Pharmacology Orlistat is a lipase inhibitor used for obesity management that acts by inhibiting the absorption of dietary 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 Category Antiobesity Agents; Enzyme Inhibitors; ATC:A08AB01 Brand Names/Synonyms Orlipastat; Orlipastatum [Inn-Latin]; Orlistat; Orlistat [Usan:Inn]; Tetrahydrolipstatin; Xenical Dosage Forms CAPSULE Absorption Not Available Interactions Interactions for Orlistat: Alcohol: In a multiple-dose study in 30 normal weight subjects, coadministration of XENICAL and 40 grams of alcohol (e.g., approximately 3 glasses of wine) did not result in alteration of alcohol pharmacokinetics, orlistat pharmacodynamics (fecal fat excretion), or systemic exposure to orlistat. Cyclosporine: Preliminary data from a XENICAL and cyclosporine drug interaction study indicate a reduction in cyclosporine plasma levels when XENICAL was coadministered with cyclosporine. Digoxin: In 12 normal-weight subjects receiving XENICAL 120 mg three times a day for 6 days, XENICAL did not alter the pharmacokinetics of a single dose of digoxin. Fat-soluble Vitamin Supplements and Analogues: A pharmacokinetic interaction study showed a 30% reduction in beta-carotene supplement absorption when concomitantly administered with XENICAL. XENICAL inhibited absorption of a vitamin E acetate supplement by approximately 60%. The effect of orlistat on the absorption of supplemental vitamin D, vitamin A, and nutritionally-derived vitamin K is not known at this time. Glyburide: In 12 normal-weight subjects receiving orlistat 80 mg three times a day for 5 days, orlistat did not alter the pharmacokinetics or pharmacodynamics (blood glucose-lowering) of glyburide. Nifedipine (extended-release tablets): In 17 normal-weight subjects receiving XENICAL 120 mg three times a day for 6 days, XENICAL did not alter the bioavailability of nifedipine (extended-release tablets). Oral Contraceptives: In 20 normal-weight female subjects, the treatment of XENICAL 120 mg three times a day for 23 days resulted in no changes in the ovulation-suppressing action of oral contraceptives. Phenytoin: In 12 normal-weight subjects receiving XENICAL 120 mg three times a day for 7 days, XENICAL did not alter the pharmacokinetics of a single 300-mg dose of phenytoin. Pravastatin: In a 2-way crossover study of 24 normal-weight, mildly hypercholesterolemic patients receiving XENICAL 120 mg three times a day for 6 days, XENICAL did not affect the pharmacokinetics of pravastatin. Warfarin: In 12 normal-weight subjects, administration of XENICAL 120 mg three times a day for 16 days did not result in any change in either warfarin pharmacokinetics (both R- and S-enantiomers) or pharmacodynamics (prothrombin time and serum Factor VII). Although undercarboxylated osteocalcin, a marker of vitamin K nutritional status, was unaltered with XENICAL administration, vitamin K levels tended to decline in subjects taking XENICAL. Therefore, as vitamin K absorption may be decreased with XENICAL, patients on chronic stable doses of warfarin who are prescribed XENICAL should be monitored closely for changes in coagulation parameters. Chemical IUPAC Name 1-[(3-hexyl-4-oxo-oxetan-2-yl)methyl]dodecyl2-formylamino-4-methyl-pentanoate Chemical Formula C29H53NO5 Half Life 1-2 hours Drug Type Approved Drug # Accession No APRD00255 CAS Registry Number 96829-58-2 |
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