Indicated to reduce the risk for weight regain after prior weight loss. Also 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 (e.g., hypertension, diabetes, dyslipidemia).
Lipase inhibitor; Antiobesity preparation
Orlistat is a potent, specific and long-acting lipase inhibitor. It exerts its therapeutic activity 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. The inactivated enzyme is thus rendered unable to hydrolyze dietary fats in the form of triglycerides into absorbable free fatty acids and monoglycerides. As undigested triglycerides can not be absorbed, a caloric deficit arises which has a positive effect on weight control. Systemic absorption of orlistat is therefore not needed for the activity. At the recommended therapeutic dose of 120 mg three times a day, orlistat inhibit dietary fat absorption by approximately 30%.
ORAL Obesity: Adult: 120 mg tid w/ each main meal containing fat; omit dose if meal is occasionally missed or has no fat. Child: 12 yr: 120 mg tid w/ each main meal containing fat; omit dose if meal is occasionally missed or has no fat.
Reduction in cyclosporine plasma levels when Orlistat was coadministered with cyclosporine. Orlistat inhibited absorption of a vitamin E acetate supplement. The effect of Orlistat on the absorption of supplemental vitamin D, vitamin A, and nutritionally-derived vitamin K is not known. Hypothyroidism has been reported in patients treated concomitantly with Orlistat and levothyroxine. Patients treated concomitantly with Orlistat and levothyroxine should be monitored for changes in thyroid function. Administer levothyroxine and Orlistat at least 4 hours apart. Vitamin K absorption may be decreased with Orlistat. Patients on chronic stable doses of warfarin who are prescribed Orlistat should be monitored closely for changes in coagulation parameters. Convulsions have been reported in patients treated concomitantly with Orlistat and antiepileptic drugs. Patients should be monitored for possible changes in the frequency and/or severity of convulsions.
Chronic malabsorption syndrome. Cholestasis. Lactation. Distribute daily intake of fat over 3 main meals. Fat-soluble vitamins supplements may be required during longterm therapy. Discontinue use if 5% body wt loss is not achieved during the 1st 12 wk, History of hyperoxaluria or Ca oxalate nephrolithiasis. DM. Pregnancy.
Faecal urgency & incontinence, flatulence, fatty stools or discharge, increased defecation; headache, anxiety, fatigue, menstrual irregularities; abdominal pain/discomfort. Anaphylaxis; angloedema.
Use is contraindicated during pregnancy. If pregnancy occurs while taking this drug, the mother should be apprised of the potential hazard of maternal weight loss to the fetus. Use with caution while breastfeeding.
Single doses of 800 mg Orlistat and multiple doses of up to 400 mg three times a day for 15 days have been studied in normal-weight and obese subjects without significant adverse findings. Should a significant overdose of Orlistat occur, it is recommended that the patient be observed for 24 hours. Based on human and animal studies, systemic effects attributable to the lipase-inhibiting properties of Orlistat should be rapidly reversible.
Store in cool & dry place below 30°C, protect from light & moisture. Keep out of reach of children.
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