Orlistat (marketed as Xenical by Roche) is a drug designed to treat obesity. Its primary function is to prevent the absorption of dietary fats, thereby reducing caloric intake. It is intended for use in conjunction with a physician-supervised reduced calorie diet.
Pharmacology
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. Only trace amounts of orlistat are absorbed systemically, the primary effect is local lipase inhibition within the
GI tract after an oral dose. The primary route of elimination is through the
feces.
At the standard prescription dose of 120 mg three times daily before meals, orlistat prevents approximately 30% of dietary fat from being absorbed.
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