Xenobese 120-MG Capsule

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%.

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.

Reduction in cyclosporine plasma levels when Xenobese was coadministered with cyclosporine. Xenobese inhibited absorption of a vitamin E acetate supplement. The effect of Xenobese 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 Xenobese and levothyroxine. Patients treated concomitantly with Xenobese and levothyroxine should be monitored for changes in thyroid function. Administer levothyroxine and Xenobese at least 4 hours apart. Vitamin K absorption may be decreased with Xenobese. Patients on chronic stable doses of warfarin who are prescribed Xenobese should be monitored closely for changes in coagulation parameters. Convulsions have been reported in patients treated concomitantly with Xenobese and antiepileptic drugs. Patients should be monitored for possible changes in the frequency and/or severity of convulsions.

Orlistat is contraindicated in patients with chronic malabsorption syndrome, in patients with cholestasis and in patients who are hypersensitive to orlistat or to any of the other ingredients of the capsules.

Common: Undesirable effects of Xenobese are largely gastrointestinal in nature. Common gastrointestinal side effects are oily spotting from the rectum, flatulence, fecal urgency, oily or fatty stool, abdominal discomfort etc.

Rare: Influenza, anxiety. headache, fatigue etc may rarely occur in some patients. Rare cases of hypersensitivity have been reported. Main clinical symptoms are pruritus, exanthema, urticaria, angioedema and anaphylaxis.

Organic causes of obesity (e.g. hypothyroidism) should be excluded before prescribing Xenobese. Xenobese and cyclosporine should not be coadministered. Cyclosporine should be taken at least 2 hours before or after Xenobese in patients taking both drugs. Cyclosporine level should be measured and frequently monitored.

In clinical trial, the decrease in body weight with Xenobese therapy was less in type II diabetic patients than in non-diabetic patients. Antidiabetic drug treatment should be closely monitored during Xenobese therapy. Because of the improvement in glycemic control, the dose of oral antidiabetics or of insulin may need to be adjusted.

Patients should be advised to adhere to the dietary recommendations. The probability of occurrence of gastrointestinal side effects may increase when Xenobese is taken with a fatty meal. The daily intake of fat should be distributed between three main meals. Patients should be strongly encouraged to take a multivitamin supplement that contains fat soluble vitamins to ensure adequate nutrition because Xenobese has been shown to reduce the absorption of some fat soluble vitamins & beta-carotene. In addition, the levels of vitamin D & beta carotene may be low in obese patients compared with non-obese patients.

Single doses of 800 mg Xenobese 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 Xenobese 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 Xenobese should be rapidly reversible.

Appetite suppressant drugs/Anti-obesity drugs

Store in cool & dry place below 30°C, protect from light & moisture. Keep out of reach of children.