Adults: Orlistat is indicated in combination with a mildly hypocaloric diet for the treatment of obese patients with a body mass index (BMI) >30 kg/m² and overweight patients (BMI >28 kg/m²) with associated risk factors such as type II diabetes, hyperlipidemia.

Orlistat is a potent, specific, and long-acting lipase inhibitor. It acts locally in the lumen of the stomach and upper small intestine by forming a covalent bond with the active serine site of gastric and pancreatic lipases. This inactivates the enzymes and prevents the hydrolysis of dietary triglycerides into absorbable free fatty acids and monoglycerides. Since undigested triglycerides cannot be absorbed, a caloric deficit is created, which contributes to weight reduction. Systemic absorption of orlistat is not required for its activity. At the recommended dose of 120 mg three times daily, orlistat inhibits dietary fat absorption by approximately 30%.

The recommended dose of Orlistat is one 120 mg capsule to be taken immediately before, during or up to one hour after each main meal. If a meal is missed or contains no fat the dose of Orlistat should be omitted. Doses of Orlistat above 120 mg three times daily have not been shown to provide additional benefits. The effect of Orlistat results in an increase in fecal fat 24-48 hours after dosing. Upon discontinuation of therapy, fecal fat content usually returns to pretreatment levels within 48-72 hours.

The safety & efficacy of Orlistat were investigated in clinical studies lasting up to 4 years. The recommended dose of Orlistat for adolescents is as same as adults.

Special dosage instruction: The tolerability and efficacy of Orlistat have not been studied in elderly patients, or patients with hepatic and/ or renal impairments.

A reduction in cyclosporine plasma levels has been observed when Orlistat is coadministered with cyclosporine. Orlistat may inhibit the absorption of vitamin E acetate supplements. The effect on absorption of supplemental vitamin D, vitamin A, and dietary vitamin K is not clearly known. Hypothyroidism has been reported in patients receiving Orlistat together with levothyroxine. Thyroid function should be monitored in such cases, and levothyroxine and Orlistat should be taken at least 4 hours apart. Vitamin K absorption may be reduced with Orlistat. Patients on warfarin should be closely monitored for changes in coagulation parameters. Convulsions have been reported in patients receiving Orlistat with antiepileptic drugs; therefore, monitoring for changes in seizure frequency or severity is recommended.

Orlistat is contraindicated in patients with chronic malabsorption syndrome, cholestasis, and in patients with known hypersensitivity to orlistat or any capsule ingredients.

Common: Gastrointestinal side effects are most common, including oily spotting from the rectum, flatulence, fecal urgency, oily or fatty stools, and abdominal discomfort.

Rare: Influenza, anxiety, headache, fatigue. Rare hypersensitivity reactions have been reported, including pruritus, rash (exanthema), urticaria, angioedema, and anaphylaxis.

Pregnancy: Orlistat is Pregnancy Category X. It is contraindicated during pregnancy as weight loss provides no benefit and may cause fetal harm. Minimum weight gain is recommended during pregnancy, even in overweight or obese women. If exposure occurs during pregnancy, the patient should be informed about potential fetal risks.

Lactation: It is not known whether Orlistat is excreted in human milk. Caution is advised when administering to breastfeeding women.

Organic causes of obesity (e.g. hypothyroidism) should be ruled out before treatment. Orlistat should not be coadministered with cyclosporine; if necessary, cyclosporine should be taken at least 2 hours before or after Orlistat, with close monitoring of levels.

In clinical studies, weight loss was less in type II diabetic patients compared to non-diabetic patients. Antidiabetic therapy should be closely monitored, as dose adjustments of insulin or oral antidiabetic drugs may be required due to improved glycemic control.

Patients should follow dietary recommendations. Gastrointestinal side effects increase with high-fat meals. Fat intake should be distributed across three main meals. Multivitamin supplementation (containing fat-soluble vitamins) is recommended, as Orlistat reduces absorption of vitamins A, D, E, K, and beta-carotene.

Single doses up to 800 mg and repeated doses up to 400 mg three times daily for 15 days have been studied without serious adverse effects. In case of significant overdose, the patient should be observed for 24 hours. Systemic effects related to lipase inhibition are expected to be rapidly reversible.

Appetite suppressant drugs / Anti-obesity drugs.

Store in a cool, dry place below 30°C. Protect from light and moisture. Keep out of reach of children.