Orlistat
- PMID: 31194359
- Bookshelf ID: NBK542202
Orlistat
Excerpt
Orlistat (tetrahydrolipstatin) is an anti-obesity medication approved by the US Food and Drug Administration (FDA). This medication is a saturated derivative derived from the endogenous lipstatin found in Streptomyces toxytricini. Orlistat is used to manage obesity by reversibly inhibiting gastric and pancreatic lipases within the gut. These lipases play a crucial role in the digestion of dietary fat by breaking down triglycerides into absorbable free fatty acids and monoglycerides. Orlistat binds covalently to the serine residues of the active sites of these lipases, rendering them inactive. This inactivation of lipase prevents the hydrolysis of triglycerides, thereby impeding the absorption of free fatty acids.
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- Sjöström L, Rissanen A, Andersen T, Boldrin M, Golay A, Koppeschaar HP, Krempf M. Randomised placebo-controlled trial of orlistat for weight loss and prevention of weight regain in obese patients. European Multicentre Orlistat Study Group. Lancet. 1998 Jul 18;352(9123):167-72. - PubMed
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- Torgerson JS, Hauptman J, Boldrin MN, Sjöström L. XENical in the prevention of diabetes in obese subjects (XENDOS) study: a randomized study of orlistat as an adjunct to lifestyle changes for the prevention of type 2 diabetes in obese patients. Diabetes Care. 2004 Jan;27(1):155-61. - PubMed
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- Hampl SE, Hassink SG, Skinner AC, Armstrong SC, Barlow SE, Bolling CF, Avila Edwards KC, Eneli I, Hamre R, Joseph MM, Lunsford D, Mendonca E, Michalsky MP, Mirza N, Ochoa ER, Sharifi M, Staiano AE, Weedn AE, Flinn SK, Lindros J, Okechukwu K. Clinical Practice Guideline for the Evaluation and Treatment of Children and Adolescents With Obesity. Pediatrics. 2023 Feb 01;151(2) - PubMed
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