Orlistat Capsule

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Capsule Presentation

Each hard gelatin capsule contains:
Orlistat 120 mg

Orlistat is a drug used in the treatment of obesity. Its primary function is preventing the absorption of fats from the human diet, thereby reducing caloric intake. 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.

Indications

  • Obesity
  • Weight maintenance
  • Risk for weight regain after prior weight loss

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.

Interactions

Orlistat inhibits dietary fat absorption by approximately 30%. It works by inhibiting pancreatic lipase, an enzyme that breaks down fat in the intestine. Without this enzyme, fat from the diet is excreted undigested and not absorbed by the body.

Orlistat may reduce the absorption and blood levels of cyclosporine (Sandimmune) when both drugs are administered together. Therefore, cyclosporine should be administered two hours before or after orlistat, and more frequent monitoring of cyclosporine levels may be needed.

Side Effects

  • Oily spotting
  • Loose stools
  • Vomiting
  • Stomach pain
  • Loss of appetite

Contraindication

  • Impaired liver function, and pancreatic disease.
  • Pregnancy and breastfeeding
  • Reduced gallbladder function
  • Malabsorption.

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