Indications
Orlistat is indicated for obesity management including weight loss and weight maintenance when used in conjunction with a reduced-calorie diet. Orlistat is also indicated for the reduction of the risk of weight regain after prior weight loss. Orlistat 120 mg is indicated for obese patients with an initial body mass index (BMI) ≥30 kg/m2 or ≥27 kg/m2 in the presence of other risk factors (eg, hypertension, diabetes, dyslipidemia) and Orlistat 60 mg is indicated for overweight & obese patients with an initial body mass index (BMI) ≥25 kg/m2.
Therapeutic Class
Appetite suppressant drugs/Anti-obesity drugs
Pharmacology
Orlistat is a reversible inhibitor of gastrointestinal lipase. 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 lipase. 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.
The recommended dose of Orlistat is one 60 mg or 120 mg capsule three times a day with each main meal containing fat (during or up to 1 hour after the meal). The patient should be on a nutritionally balanced, reduced-calorie diet that contains approximately 30% of calories from fat. The daily intake of fat, carbohydrate, and protein should be distributed over three main meals. If a meal is occasionally missed or contains no fat, the dose of Orlistat can be omitted.
Interaction
May reduce the absorption of iodine salts and/or levothyroxine, fat-soluble vit (A, D, E, K) and beta carotene. May decrease plasma levels of ciclosporin and amiodarone. May decrease the efficacy of antiepileptic drugs (e.g. valproate, lamotrigine), antiretrovirals, antidepressants, antipsychotics (including lithium). Additive effect on glycaemic control with antidiabetics. May cause hormonal contraceptive failure. May enhance the anticoagulant effect of warfarin.
Orlistat is contraindicated in Pregnancy, Patients with chronic malabsorption syndrome, Patients with cholestasis, Patients with known hypersensitivity to Orlistat or to any component of this product.
Commonly-observed adverse events associated with the use of Orlistat include oily spotting, flatus with discharge, fecal urgency, fatty/oily stool, oily evacuation, increased defecation, fecal incontinence.
Pregnancy Category X. Orlistat is contraindicated during pregnancy, because weight loss offers no potential benefit to a pregnant woman and may result in fetal harm.
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