Listata

General characteristics. Structure:

Active ingredient: 60 mg or 120 mg of an orlistat.

Excipients: sodium lauryl sulfate, acacias gum, лудифлэш (Mannitolum — 84–92%, кросповидон — 4–6%, polyvinyl acetate — 3,5–6%, povidone — 0,25–0,6%), коповидон, кросповидон, magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Orlistat — specific inhibitor of gastrointestinal lipases of long action. Works in a gleam of a stomach and small intestine, forming a covalent bond with the active serinovy site of gastric and pancreatic lipases. The inactivated enzyme loses ability to split the food fats arriving in the form of triglycerides to the absorbed free fatty acids and monoglycerides. Not split triglycerides are not soaked up in this connection receipt of calories in an organism decreases that leads to a body degrowth. Therapeutic effect of drug is carried out without absorption in a system blood stream.

The decrease in body weight caused by use of an orlistat in a dose of 60 mg three times a day is followed also by other favorable action: decrease in concentration of the general cholesterol, LPNP cholesterol, and also reduction of a circle of a waist.

Action of an orlistat leads to increase in content of fat in fecal masses already in 24–48 h after administration of drug. After cancellation of an orlistat the content of fat in fecal masses usually is returned to initial level in 48–72 h.

Pharmacokinetics. Absorption. Absorption — low. Later 8 h after intake of a therapeutic dose not changed орлистат in a blood plasma practically is not defined (concentration

Distribution. Vd cannot be established as орлистат it is practically not soaked up and has no the established system pharmacokinetics. Orlistat more than for 99% contacts proteins of a blood plasma of in vitro (generally with lipoproteins and albumine). In the minimum quantities орлистат can get into erythrocytes.

Metabolism. Metabolism of an orlistat is carried out mainly in an intestines wall with formation pharmacological of inactive metabolites — M1 (the four-membered hydrolyzed lactone ring) and M3 (M1 with the chipped-off N-formilleytsina rest).

Removal. Through intestines about 97% of the accepted dose, 83% are brought out of this quantity — in not changed look. Removal of an orlistat and its metabolites kidneys makes less than 2% of the accepted dose. Drug is completely removed in 3–5 days. Removal of an orlistat at persons with normal body weight and patients with obesity similarly.

Indications to use:

Obesity and excess body weight (in combination with moderately hypocaloric diet).

Route of administration and doses:

Listat's drug is appointed on 1 tablet by 3 times in сутк together with the main meals. Drug is accepted during food or no later than in 1 h after food. If meal is missed or if food does not contain fat, Listat's reception can be missed.

Increase in a dose does not give recommended for increase in therapeutic effect above.

Features of use:

Against the background of therapy by Listata the patient has to receive the balanced, moderately hypocaloric diet containing no more than 30% of calories in the form of fats. At higher content of fats in a food allowance the probability of emergence of side reactions from a GIT increases.

Decrease in body weight of patients can improve a metabolism at patients with a diabetes mellitus and demand a dose decline of peroral antidiabetic drugs.

Safety and efficiency of use of Xenical for patients with abnormal liver functions and/or kidneys is not established.

In clinical trials of D, E, K and beta carotene remained with most of the patients receiving Xenical within 2 full years, concentration of vitamins A within norm. In certain cases for adequate intake of all nutrients in an organism it is possible to appoint polyvitamins which follow to accept not less, than in 2 h after Listata's reception or before going to bed.

Use in pediatrics. Safety of use of drug for children is not established.

Use at pregnancy and feeding by a breast. In researches of reproductive toxicity on animals the teratogenic and embriotoksichesky effect of an orlistat was not observed. For lack of teratogenic effect at animals the similar effect at the person is not expected. As there are no clinical data on use of an orlistat during pregnancy, use of drug of Listat for pregnant women is contraindicated.

Because there are no data on allocation of an orlistat with breast milk, use of drug of Listat during breastfeeding is contraindicated.

Side effects:

From a GIT: often — a "soft" chair, pain or discomfort in a rectum, an incontience a calla, abdominal distention, damage of teeth, damage of gums.

Other undesirable reactions: very often — a headache, upper respiratory tract infections, flu; often — lower respiratory tract infections, infections of urinary tract, a dysmenorrhea, alarm, weakness.

Interaction with other medicines:

Medicinal interaction at the combined use of Listata with digoxin, warfarin, metformin, oral contraceptives, nifedipine, statines and ethanol is not established.

At simultaneous use of Listat can reduce absorption of fat-soluble vitamins.

Contraindications:

- syndrome of chronic malabsorption;
- cholestasia;
- hypersensitivity to drug.

Storage conditions:

Drug should be stored in the dry place at a temperature not above 25 °C. A period of validity - 2 years.

Issue conditions:

Without recipe

Packaging:

On 30, 60 or 90 tablets in planimetric packagings and cardboard packs.