Orlistat 60mg is a peripherally acting anti-obesity agent, classified as a lipase inhibitor. It is indicated for weight management in conjunction with a reduced-calorie diet. It acts locally in the gastrointestinal tract to inhibit dietary fat absorption by approximately 30%. In India, it is widely used as an over-the-counter (OTC) aid for weight loss in adults with a Body Mass Index (BMI) of 25 kg/m² or above.
Adult: One 60mg capsule taken orally three times daily with each main meal containing fat (during or up to 1 hour after the meal). If a meal is missed or contains no fat, the dose should be omitted.
Note: Take with a glass of water. Should be taken during or within 1 hour of a main meal. Daily fat intake should be distributed over three main meals. A daily multivitamin supplement containing fat-soluble vitamins (A, D, E, K) should be taken at least 2 hours before or after orlistat (e.g., at bedtime).
Orlistat is a potent, reversible inhibitor of gastrointestinal lipases, primarily pancreatic and gastric lipase. These enzymes are essential for the hydrolysis of dietary triglycerides into absorbable free fatty acids and monoglycerides. By covalently binding to the active serine site of these lipases in the gastric and intestinal lumen, orlistat inactivates them. This prevents the digestion of approximately 30% of ingested dietary fat, which is then excreted unchanged in the feces.
Pregnancy: Category X. Contraindicated. Weight loss offers no potential benefit during pregnancy and may cause fetal harm.
Driving: No known effects. However, patients experiencing fecal urgency or incontinence should be cautious.
| Cyclosporine | Orlistat may significantly decrease cyclosporine absorption, reducing its plasma levels and efficacy. Risk of transplant rejection. | Major |
| Levothyroxine | Orlistat may decrease levothyroxine absorption, potentially causing hypothyroidism. Dosing should be separated by at least 4 hours. | Major |
| Warfarin/Acenocoumarol | Orlistat may affect vitamin K absorption, potentially altering INR. Monitor INR closely, especially when starting or stopping orlistat. | Major |
| Antiepileptics (e.g., Valproate, Lamotrigine) | Potential for reduced absorption and decreased efficacy. Monitor seizure control. | Moderate |
| Antiretroviral drugs (e.g., Atazanavir, Lopinavir) | Potential for reduced absorption. Avoid concomitant use. | Major |
| Amiodarone | Potential for reduced absorption. Monitor efficacy. | Moderate |
| Fat-soluble Vitamins (A, D, E, K) and Beta-carotene | Orlistat reduces their absorption. Supplementation is required, taken at a 2+ hour separation. | Moderate |