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Orlistat is a reversible inhibitor of gastrointestinal lipasesIt 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 lipasesThe inactivated enzymes are thus unavailable to hydrolyze dietary fat in the form of triglycerides into absorbable free fatty acids and monoglyceridesAs undigested triglycerides are not absorbedthe resulting caloric deficit may have a positive effect on weight control.

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