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ALIMENTARY TRACT AND METABOLISM › ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS › ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS › Peripherally acting antiobesity products
orlistat
A08AB01
Forms & Strengths
- Capsule, oral: 60 mg
- Capsule, oral: 120 mg
Adult Dosing
- Weight loss: 120 mg orally three times daily with each main meal containing fat
- Administer during or up to 1 hour after the meal
- Omit dose if meal is missed or contains no fat
- Supplement with a multivitamin containing fat-soluble vitamins at least 2 hours before or after orlistat
Pediatric Dosing
- Adolescents >= 12 years: 120 mg orally three times daily with each fat-containing meal
- Children < 12 years: Safety and efficacy not established
Indications
- Management of obesity including weight loss and weight maintenance when used in conjunction with a reduced-calorie diet
- Reduction in risk for weight regain after prior weight loss
Mechanism of Action
- Reversible inhibitor of gastric and pancreatic lipases
- Forms a covalent bond with the active serine site of lipases in the lumen of the stomach and small intestine
- Inactivates enzymes, preventing hydrolysis of dietary fat into absorbable free fatty acids and monoglycerides
- Results in approximately 30% inhibition of dietary fat absorption
Contraindications
- Chronic malabsorption syndrome
- Cholestasis
- Known hypersensitivity to orlistat or any component of the formulation
- Pregnancy
Adverse Reactions
- Oily spotting
- Flatus with discharge
- Fecal urgency
- Fatty or oily stool
- Oily evacuation
- Increased defecation
- Fecal incontinence
- Rare cases of severe liver injury and oxalate nephropathy
Drug Interactions
- Cyclosporine: Decreases plasma concentrations; administer cyclosporine at least 3 hours after orlistat
- Levothyroxine: May cause hypothyroidism; monitor thyroid function and separate administration by at least 4 hours
- Warfarin: May affect international normalized ratio (INR); monitor coagulation parameters closely
- Fat-soluble vitamins (A, D, E, K, beta-carotene): Absorption is reduced; take multivitamin at least 2 hours before or after orlistat
- Amiodarone: Decreased plasma concentrations and potential loss of efficacy
Curated Content: Needs Vetting Before Put to Clinical Use