Xenical

Xenical – inhibitor of gastrointestinal lipases, means for treatment of obesity.

Form of release and structure

Dosage form – capsules: No. 1, gelatinous, turquoise color, with firm opaque structure and a text of black color: on the XENICAL 120 case, on a lid of "ROCHE"; in capsules – pellets of almost white or white color (on 21 pieces in blisters, in a cardboard pack 1, 2 or 4 blisters).

Active agent of Xenical – орлистат, in 1 capsule – 120 mg.

Excipients: talc.

Auxiliary components of pellets: sodium carboxymethylstarch (примогель), cellulose microcrystallic, sodium lauryl sulfate, K-30 povidone.

Structure of a cover of the capsule: indigo carmine, gelatin, titanium dioxide.

Indications to use

Use of Xenical is shown in a combination with moderately low-calorie diet at long therapy of obesity or excess weight of a body, including at the patients having risk factors similar to obesity.

Drug appoint the patient with an excess weight or obesity at treatment of a diabetes mellitus 2 types in combination with hypoglycemic means: insulin, metformin, derivatives of sulphonylurea or moderately low-calorie diet.

Contraindications

• Cholestasia;
• Syndrome of chronic malabsorption;
• Period of pregnancy and breastfeeding;
• Hypersensitivity to drug components.

Safety and efficiency of use of drug for patients with a renal failure and a liver, elderly patients and children are younger than 12 years were not investigated.

Route of administration and dosage

Capsules accept inside, in time or at once (within 1 hour) after food.

The recommended dosing: on 1 capsule 3 times a day, during each main meal.

If food does not contain fats or the patient misses a breakfast, a dinner or a lunch, then and the daily dose of drug decreases on the number of the missed meals.

The balanced moderately low-calorie diet of the patient has to contain up to 30% of fats. The standard daily rate of a kalorazh consisting of fats, proteins and carbohydrates should be distributed on three main receptions.

Side effects

At clinical trials of use of Xenical there were following side reactions:

• From digestive tract: very often – strong desires on defecation, allocations from a rectum of oily structure, a steatorrhea, release of gases with insignificant separated, increase of excrements, a liquid chair, discomfort or abdominal pains, a meteorism (frequency increases at increase in content of fat in food); often – abdominal distention, a soft chair, an incontience a calla, pains or discomfort in a rectum, damage of teeth and/or gums;
• Others: very often – a headache, upper respiratory tract infections, flu; often – weakness, a dysmenorrhea, alarm, infections of urinary and lower respiratory tracts, at patients with a diabetes mellitus are 2 types – hypoglycemic states.

In post-marketing observations chances of side effects are described:

• Allergic reactions: seldom – an itch, skin rash, a bronchospasm, a small tortoiseshell, an anaphylaxis, a Quincke's disease; very seldom – violent rash;
• Others: very seldom – increase in activity of an alkaline phosphatase and transaminases, hepatitis, rectal bleedings, a diverticulitis, pancreatitis, a cholelithiasis and an oxalic nephropathy (frequency of emergence is unknown).

Special instructions

Prolonged use of Xenical allows to control decrease and maintenance of body weight at the new level, warning a repeated increase of extra kilos.

Exceeding of the recommended dose of an orlistat does not strengthen its therapeutic effect.

Clinical effect of drug reduces amount of visceral fat and improves a profile of the risk factors and pathologies accompanying obesity including disturbance of tolerance to glucose, a diabetes mellitus 2 types, a giperinsulinemiya, a hypercholesterolemia, arterial hypertension.

The concomitant use of drug with hypoglycemic means (sulphonylurea derivatives, metformin, insulin) and observance of moderately hypocaloric diet allows a sick diabetes mellitus 2 types with obesity or excess weight of a body in addition to improve compensation of carbohydrate metabolism.

At most of patients after four years of use of an orlistat clinical trials confirm contents within norm of a betakaroten and A, D, E, K vitamins. For providing an organism with adequate intake of nutrients purpose of polyvitamins is shown.

Moderately hypocaloric diet has to be balanced, contain many fruit and vegetables and 30% or less kalorazh in the form of fats. The standard daily rate of carbohydrates, fats and proteins should be eaten in three main receptions.

The probability of side effects of drug from digestive tract increases against the background of food rich with fats.

Use of Xenical at a diabetes mellitus 2 types improves compensation of carbohydrate metabolism and can cause requirement of reduction of a dose of hypoglycemic means.

Medicinal interaction

Clinical interaction of Xenical at simultaneous use of amitriptyline, an atorvastatin, guanyl guanidines, digoxin, fibrat, fluoxetine, a lozartan, Phenytoinum, oral contraceptives, phentermine, a pravastatin, warfarin, nifedipine of gastrointestinal therapeutic system and nifedipine with slow release, a sibutramina or alcohol intake is not revealed. Nevertheless, at a combination to peroral anticoagulants, including warfarin, it is recommended to watch indicators of the international normalized relation (INR).

Decrease in absorption of a betakaroten and vitamins D, E therefore polyvitamins should be accepted before going to bed or in 2 hours after administration of drug is noted.

The combination with cyclosporine can lead to decrease in its concentration in a blood plasma therefore it is regularly necessary to determine the plasma content of cyclosporine at a combination with orlistaty.

Due to the lack of results of pharmacokinetic researches contraindicated simultaneous use of acarbose.

Against the background of a concomitant use of Xenical and antiepileptic means cases of development in the patient of spasms were registered. As relationship of cause and effect of this interaction is not established, it is necessary to monitor the frequency and/or weight of a convulsive syndrome at this category of patients.

Terms and storage conditions

To store in the place, dry, unavailable to children, at a temperature up to 25 °C.

Period of validity – 3 years.