Orlistat

Xenical

Approved uses

• XENICAL is indicated for obesity management including weight loss and weight maintenance when used in conjunction with a reduced-calorie diet.
• XENICAL is also indicated to reduce the risk for weight regain after prior weight loss.
• XENICAL is indicated for obese patients with an initial body mass index (BMI) ≥30 kg/m 2 or ≥27 kg/m 2 in the presence of other risk factors (e.g., hypertension, diabetes, dyslipidemia).
• Table 1 illustrates body mass index (BMI) according to a variety of weights and heights.

Forms and strengths

• XENICAL 120 mg turquoise capsules imprinted with XENICAL 120 in black ink.
• Capsules: 120 mg.

How it is taken

• One 120-mg capsule three times a day with each main meal containing fat (during or up to 1 hour after the meal).
• Advise patients to take a nutritionally balanced, reduced-calorie diet that contains approximately 30% of calories from fat.
• Distribute the daily intake of fat, carbohydrate, and protein over three main meals.
• Advise patients to take a multivitamin containing fat-soluble vitamins to ensure adequate nutrition.
• Take the vitamin supplement at least 2 hours before or after the administration of XENICAL, such as at bedtime.
• For patients receiving both XENICAL and cyclosporine therapy, administer cyclosporine 3 hours after XENICAL.

Must not be used when

• XENICAL is contraindicated in: Pregnancy Patients with chronic malabsorption syndrome Patients with cholestasis Patients with known hypersensitivity to XENICAL or to any component of this product Pregnancy Chronic malabsorption syndrome Cholestasis Known hypersensitivity to XENICAL or to any component of this product

Interactions

• Cyclosporine: Reduction in cyclosporine plasma levels was observed when XENICAL was coadministered with cyclosporine.
• Fat-soluble Vitamin Supplements and Analogues: All patients should take a daily multivitamin that contains vitamins A, D, E, K, and beta-carotene.
• Levothyroxine: Patients treated concomitantly with XENICAL and levothyroxine should be monitored for changes in thyroid function.
• Warfarin: Patients on chronic stable doses of warfarin who are prescribed XENICAL should be monitored closely for changes in coagulation parameters.
• Amiodarone: A reduction in exposure to amiodarone was observed when XENICAL was co-administered.
• Antiepileptic Drugs: Convulsions have been reported in patients taking XENICAL with antiepileptic drugs. Patients should be monitored for possible changes in frequency or severity of convulsions.

Warnings and precautions

• XENICAL has drug interactions and can decrease vitamin absorption.
• Take a multivitamin supplement that contains fat-soluble vitamins to ensure adequate nutrition.
• Rare cases of severe liver injury with hepatocellular necrosis or acute hepatic failure have been reported.
• Patients may develop oxalate nephrolithiasis and oxalate nephropathy following treatment with XENICAL. Monitor renal function in patients at risk for renal insufficiency. Discontinue XENICAL if oxalate nephropathy develops.
• Substantial weight loss can increase the risk of cholelithiasis.
• Exclude organic causes of obesity (eg, hypothyroidism) before prescribing XENICAL.
• Gastrointestinal events may increase when XENICAL is taken with a diet high in fat (>30% total daily calories from fat).

Common side effects

• most common adverse events resulting in discontinuation of treatment were gastrointestinal.

Pregnancy

Pregnancy Category X XENICAL is contraindicated during pregnancy, because weight loss offers no potential benefit to a pregnant woman and may result in fetal harm. A minimum weight gain, and no weight loss, is currently recommended for all pregnant women, including those who are already overweight or obese, due to the obligatory weight gain that occurs in maternal tissues during pregnancy.

How it acts

Orlistat is a reversible inhibitor of gastrointestinal 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.

Label holder:

H2-Pharma LLC

Label version:

9 January 2026

This section reports the approved product information. The wording is condensed from the regulator's own summary, and the full document is linked under Sources.