Listata Mini

General characteristics. Structure:

Active ingredient: 60 mg of an orlistat.

Excipients: sodium lauryl sulfate, acacias gum, лудифлэш (Mannitolum - 84,00-92,00%, кросповидон - 4,00-6,00%, polyvinyl acetate - 3,50-6,00%, povidone - 0,25-0,60%), коповидон, кросповидон, magnesium stearate.

Structure of a cover: опадрай the II blue (85F30720) (polyvinyl alcohol - 40,00%, titanium dioxide - 21,40%, a macrogoal-3350 - 20,20%, talc - 14,80%, indigo carmine - 3,50%, a varnish aluminum quinolinic yellow - 0,10%). Опадрай silvery (63F97546) (polyvinyl alcohol - 47,03%, talc - 27,00%, a macrogoal-3350 - 13,27%, a nacreous pigment - 10,00%, polysorbate-80 - 2,70%).

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 communication with what receipt of calories in an organism decreases that leads to decrease in body weight. 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 drug withdrawal the content of fat in fecal masses usually is returned to initial level in 48-72 h.

Pharmacokinetics. Absorption. Absorption - low. 8 hours later after intake of a therapeutic dose not changed орлистат in a blood plasma practically is not defined (concentration <5 ng/ml). Signs of cumulation are absent that will be coordinated with the minimum absorption of drug.

Distribution. The volume of distribution 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). Orlistat in the minimum quantities 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 lactonic ring) and MZ(M1 with the chipped-off N-formilleytsina rest).

Removal. About 97% of the entered dose are brought through intestines, 83% 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:

Decrease in excess body weight (IMT body weight index> of 28 kg/m 2) at use in combination with moderately hypocaloric diet with the low content of fats.

Route of administration and doses:

Drug is accepted inside. The recommended dose makes 60 mg 3 times a day with each main meal in combination with moderately hypocaloric diet with the low content of fat. It is necessary to take a pill just before food, during food or not later than in 1 hour after food, washing down with water. If meal is missed or food does not contain fat, administration of drug of Listat Mini has to be missed.

During the day it is possible to take no more than 3 pill on 60 mg.

Treatment is recommended to spend no more than 6 months. If after 12 weeks of therapy decrease in body weight (i.e. decrease in body weight makes less than 5% of initial) is not observed, consultation of the doctor is necessary for the solution of a question of drug use continuation.

With abnormal liver functions and kidneys of dose adjustment are not required from elderly patients, patients.

Listat Mini's drug is not recommended to be applied at children and teenagers up to 18 years because of insufficiency of data on safety and efficiency.

Features of use:

The diet and physical exercises are important components of the program of decrease in body weight. It is recommended to begin the dietary program and physical exercises prior to therapy with Listat Mini's drug. The patient has to receive moderately hypocaloric diet containing no more than 30% of calories in the form of fats (for example, at the caloric content of 2000 kcal/days food has to contain no more than 67 g of fat). Daily consumption of fats has to be distributed between three main meals.

The diet with the low content of fats reduces probability of development of the undesirable phenomena from digestive tract.

The patients accepting antiepileptic drugs should consult with the doctor before use of drug of Listat Mini as change of frequency and weight of spasms is possible. In these cases it is possible to consider a question of reception of an orlistat and antiepileptic drugs at different times.

Patients with diseases of kidneys need to consult with the doctor since development of a hyperoxaluria and nephropathy is possible.

Due to decrease in body weight against the background of administration of drug of Listat Mini, improvement of carbohydrate metabolism at patients with a diabetes mellitus 2 types in this connection it is necessary to consult with the attending physician is possible and, in case of need, to reduce a dose of hypoglycemic drugs.

Decrease in body weight can be followed by a lowering of arterial pressure and concentration of cholesterol. The patients accepting hypotensive and hypolipidemic drugs should consult with the doctor before reception of an orlistat and, in case of need, to carry out dose adjustment of these medicines.

At emergence of such symptoms as weakness, fatigue, fervescence, jaundice and darkening of urine, it is necessary to consult with the doctor for an exception of an abnormal liver function.

Influence on ability to driving of motor transport and to control of mechanisms. Orlistat does not exert impact on ability to manage vehicles and mechanisms.

Pregnancy. Due to the lack of clinical data on use for pregnant women, орлистат it is contraindicated at pregnancy.

Lactation. As it is not established whether gets орлистат into breast milk, it is contraindicated during breastfeeding.

Side effects:

The undesirable phenomena at reception of an orlistat are observed, generally from digestive tract and are caused by pharmacological effect of drug.

The side effects registered during clinical trials
the chastota of side effects is presented as follows:
■Очень it is frequent (≥ 1/10).
■Часто (≥ 1/100, <1/10).
■Нечасто (≥ 1/1000, <1/100).
■Редко (≥ 1/10000, <1/1000).
■Очень it is rare (<1/10000), including separate messages.

From digestive tract. Very often - oily allocations from a rectum; a passage of flatus with a quantity separated, imperative desires on defecation, a steatorrhea.

Often - an abdominal pain, an incontience a calla, a liquid chair; increase in frequency of defecations.

From digestive tract. Insignificant proctorrhagia; diverticulitis.

From a liver and biliary tract. Increase in activity of "hepatic" transaminases and alkaline phosphatase, hepatitis, cholelithiasis.

From skin and hypodermic cellulose. Violent rash.

From immune system. Hypersensitivity reactions (itch, rash, urticaria, Quincke's disease, bronchospasm and anaphylaxis).

Others. Decrease in concentration of a prothrombin, increase in an indicator of the International normalized relation (MHO) at the patients accepting орлистат together with indirect anticoagulants.

Interaction with other medicines:

At simultaneous use of an orlistat and cyclosporine decrease in concentration of cyclosporine in a blood plasma in this connection it is necessary to monitorirovat the content of cyclosporine in a blood plasma is possible. Simultaneous use of drug of Listat Mini and cyclosporine contraindicated.

At simultaneous use of an orlistat with Amiodaronum decrease in concentration of Amiodaronum in a blood plasma is possible. Clinically the importance of this effect is not clear. At a concomitant use of an orlistat and warfarin or other peroral anticoagulants decrease in concentration of a prothrombin and increase in an indicator of MHO can be observed. Simultaneous use of drug of Listat Mini and warfarin or other peroral anticoagulants contraindicated.

Orlistat can reduce absorption of fat-soluble A, D, E, K vitamins and beta carotene. If reception of polyvitamins is shown, then they should be accepted not earlier than in 2 hours after reception of an orlistat or before going to bed.

Orlistat can reduce absorption of antiepileptic drugs that can lead to developing of spasms.

Due to the lack of researches of pharmacokinetic interaction, joint primeney the orlistat and acarbose is not recommended.

In some cases орлистат can reduce in the indirect way bioavailability of oral contraceptives. In case of heavy diarrhea use of an additional method of contraception is recommended.

At a concomitant use with sodium left thyroxine, in connection with reduction of absorption of inorganic iodine and/or left thyroxine of sodium, the hypothyroidism and/or decrease in control of a hypothyroidism can develop.

Medicinal interaction with amitriptyline, atorvastatiny, guanyl guanidines, digoxin, fibrata, fluoxetine, lozartany, Phenytoinum, phentermine, pravastatiny, nifedipine, sibutraminy and ethanol is not revealed.

Contraindications:

■ Hypersensitivity to any of drug components.
■ Syndrome of chronic malabsorption.
■ Cholestasia.
■ Simultaneous use with indirect anticoagulants (warfarin) or other peroral anticoagulants.
■ Simultaneous use with cyclosporine.
■ pregnancy Period.
■ Lactation.
■ Children's age up to 18 years.

Overdose:

Symptoms: at use of an orlistat in a dose of 800 mg once and in a dose to 400 mg 3 times a day daily within 15 days both at persons with normal body weight, and at patients with obesity, the considerable undesirable phenomena are not revealed. At use of an orlistat in a dose of 240 mg 3 times a day within 6 months at patients with obesity of increase in dozozavisimy side effects are noted.

Treatment: in the majority of messages on cases of overdose of an orlistat it was told about lack of undesirable reactions, or undesirable reactions were similar to those which were observed at use of an orlistat in the recommended doses. In case of considerable overdose of an orlistat observation of the patient for 24 hours is recommended. According to preclinical and clinical trials, the system effects connected with lipazoingibiruyushchy properties of an orlistat have to be quickly reversible.

Storage conditions:

To store in the place protected from light at a temperature not above 25 °C. A period of validity - 2 years. To store in places unavailable to children. Not to use after expiry date.

Issue conditions:

Without recipe

Packaging:

In 1 blister of 10 tablets. In cardboard packaging 3 blisters.