Orlovit (Orlistat) is a potent, specific and reversible long acting inhibitor of gastrointestinal lipases for obesity management that acts by inhibiting the absorption of dietary fat. It exerts its therapeutic activity in the human stomach and small intestine by forming a covalent bond with the active serine residue of the active site of gastric and pancreatic lipases.
The inactivated enzymes are thus unable to hydrolyze the dietary fat in the form of triglycerides, into absorbable free fatty acids and monoglycerides. As undigested triglycerides are not absorbed, the resulting calorie deficit has a positive effect on weight control. Systemic absorption of the drug is therefore not needed for activity. At the recommended therapeutic dose of 120 mg three times a day, Orlistat inhibits dietary fat absorption by approximately 30%