Xenical, 120 mg

Composition 1 Capsules contains 120 mg of orlistat.

Action strong, specific and long-acting inhibitor of lipases produced in the gastrointestinal tract. It works in the light of the stomach and small intestine by binding to the active site serinoic gastric and pancreatic lipase. Devoid of enzyme activity hydrolyses the fat is not adopted in the diet in the form of triglycerides to be absorbed free fatty acids and monoglycerides. Greater than the dose of orlistat 120 mg 3 times a day does not lead to additional benefits. Effect of orlistat on the increase in faecal fat is already present after 24-48 h of drug use. After discontinuation of treatment in fat in the stool returns to pre-treatment values after 48-72 h virtually Orlistat is not absorbed from the gastrointestinal tract. It is metabolized in the gastrointestinal tract to the pharmacologically insignificant metabolites. Approximately 97% of the administered dose is excreted in faeces (83% unchanged), less than 2% of the dose is excreted in the urine. Total drug elimination time is 3-5 days.

Indications in conjunction with a mildly hypocaloric diet for the treatment of obese patients with body mass index (BMI) equal to or greater than 30 kg/m2 or overweight patients - with a body mass index (BMI) equal to or greater than 28 kg/m2 with frequent both factors risk. Treatment orlistat should be discontinued after 12 weeks if patients were not able to reduce body weight by at least 5% relative to body weight at the start of treatment.
Contra-indications Hypersensitivity to the active or other ingredients. Chronic malabsorption. Cholestasis. Lactation.

Precautions In clinical studies of orlistat weight loss was less pronounced in patients with type 2 diabetes compared to patients without diabetes. The efficacy of orlistat has not been studied in patients with hepatic and (or) renal impairment, children and patients in the elderly. Orlistat is not intended to treat children.

Use during pregnancy and breast feeding no clinical data on the effect of orlistat on pregnancy. Not recommended for use during pregnancy orlistat. The drug is contraindicated during breast-feeding.
Adverse reactions In most cases, are gastrointestinal disorders. The incidence of adverse reactions decreased with longer-term adoption of orlistat. The potential for adverse gastrointestinal may increase if orlistat is taken with a diet high in fat (e.g. in the case of a calorie diet of 2000 kcal / day, in which more than 30% of energy provides over 67 grams of fat). During the first year of treatment the following side effects. Very common: Fat spotting from the rectum, abdominal pain / discomfort, gas with discharge, need to pass stool, fatty / oily stools, flatulence passing gas, liquid stools, fatty spotting, frequent passing of stool, flu, hypoglycemia, headache, infections of the upper airways. Common: loose stools, fecal incontinence, a feeling of swelling, pain in the anus / discomfort, tooth, gum disease, anxiety, lower respiratory tract infection, urinary tract infection, irregular menstruation, fatigue. It was observed rare cases of hypersensitivity (itching, skin rash, urticaria, angioedema and anaphylaxis), elevated liver enzymes.
Interaction In the absence of pharmacokinetic interaction of drugs is not recommended for concomitant administration of orlistat with acarbose. During concomitant administration of warfarin or other anticoagulants should be monitored with orlistat INR. There was no interaction with amitriptyline, atorvastatin, biguanide, digoxin, fibrates, fluoxetine, losartan, phenytoin, oral contraceptives, phentermine, pravastatin, nifedipine GITS, nifedipine extended release, sibutramine and alcohol. Treatment with orlistat may potentially impair the absorption of fat-soluble vitamins (A, D, E, F) - in order to ensure proper nutrition, patients on a low calorie diet should be recommended a diet rich in fruits and vegetables and to consider the administration of a multivitamin in the case of a multivitamin recommendation , should be taken at least 2 hours after taking orlistat or at bedtime. In a study on drug-drug interaction observed decrease in plasma concentrations of cyclosporine and reported in several cases lower levels of cyclosporine during concomitant use of orlistat. This can lead to a reduction of immunosuppressive efficacy. Therefore, such a connection is not recommended. It should be frequently monitored patients treated with cyclosporine after starting treatment with both orlistat and after discontinuation orlisat. Concentrations of cyclosporin levels should be monitored until stabilized. After administration of a single dose of amiodarone during orlistat therapy several healthy volunteers observed a slight decrease in the concentration of amiodarone in blood - in patients treated with amiodarone clinical relevance of this observation remains unknown, but may be minimal, but patients treated with amiodarone at the same time it is reasonable to monitor the clinical and ECG.
Oral Dosage. Adults: The recommended dose is 120 mg (1 caps) immediately before, during or within 1 h after each main meal and drink water. If the patient cannot eat a meal, or if the meal contains no fat, the dose should be omitted.