Ксеналтен® Light

General characteristics. Structure:

Active ingredient: 60 mg of an orlistat in 1 capsule.

Excipients: cellulose microcrystallic, sodium lauryl sulfate, sodium carboxymethylstarch (sodium of starch glikolit), K-30 povidone, talc.

No. Z gelatinous solid capsule: the case - titanium dioxide, gelatin, a lid - titanium dioxide, dye blue patent, dye diamond black, gelatin.

Pharmacological properties:

Pharmacodynamics. Orlistat - powerful, specific and reversible 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 is not capable to split the food fats arriving in the form of triglycerides to the absorbed free fatty acids and monoglycerides.

The split triglycerides are soaked up in this connection, receipt of calories in an organism decreases that leads to a body degrowth. Orlistat in a dose of 60 mg three times a day blocks absorption about 25% of food fat. Therapeutic effect of drug is carried out without absorption in a system blood stream. Increases concentration of fat in intestines contents in 24-48 hours after its use inside. After drug withdrawal the content of fat in intestines contents in 48-72 hours usually is returned to the level taking place prior to therapy.

At adults with BWI (body weight index)> 28 kg/sq.m орлистат in a dose of 60 mg three times a day it is effective in combination with a hypocaloric diet with the low content of fats. At the same time, the main loss of body weight happens within the first 6 months of treatment.

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 (lipoproteids of low density), and also reduction of a circle of a waist.

Pharmacokinetics. Absorption. Absorption is low. 8 hours later after intake in a dose of 360 mg 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 lactone ring) and M3 (M1 with the chipped-off N-formilleytsina rest). The molecules M1 and M3 have an open beta and lactone ring and extremely poorly inhibit a lipase (respectively, in 1000 and 2500 times are weaker, than орлистат).

Removal. The main way of removal through intestines - about 97% of the accepted dose, from them 83% in the form of not changed orlistat. Total removal by kidneys of all metabolites of an orlistat makes <2% of the accepted dose of an orlistat. Time of full removal (through intestines and kidneys) - 3-5 days. The ratio of ways of removal of an orlistat at persons with the normal body weight and obesity was similar.

Indications to use:

Decrease in excess body weight at adults is more senior than 18 years (a body weight index> of 28 kg/sq.m) at use in combination with moderately hypocaloric diet with the low content of fats of food.

Route of administration and doses:

Inside, on 1 capsule (60 mg) three times a day, washing down with water, with each main meal, just before, in time or no later than in an hour after reception beggars. If meal is missed or food does not contain fat, administration of drug Ksenalten Layt can also be missed.

Within 24 hours it is possible to accept no more than three capsules on 60 mg of drug Ksenalten Layt. The course of treatment should not exceed 6 months.

If after 12 weeks of administration of drug Ksenalten Light decrease in body weight does not occur (no more than 5% of initial body weight), the patient should consult with the doctor for the solution of a question of expediency of further use.

Efficiency and safety of an orlistat at patients with an abnormal liver function and/or kidneys, and also at patients of advanced age was not investigated, however, considering that absorption of an orlistat is minimum, dose adjustment and from persons with an abnormal liver function and/or kidneys is not required from elderly people.

Features of use:

Pregnancy and lactation. Clinical data on use of an orlistat during pregnancy are absent therefore drug Ksenalten Layt should not be used during pregnancy.

Because data on penetration of an orlistat into breast milk are absent, drug use Ksenalten Layt during breastfeeding is contraindicated.

Patients should indicate the need to adhere to the recommendations about a diet received by them.

The diet and physical exercises are an important component of the program of decrease in body weight. It is recommended to begin the dietary program and physical exercises prior to therapy with drug. During drug use the patient has to receive moderately hypocaloric diet with the balanced content of nutrients in which about 30% make fats. Daily consumption of fats has to be distributed between three main meals. It is recommended that food was rich with fruit and vegetables. The program of a diet and physical exercises has to be continued and after use of drug is stopped.

The probability of emergence of side effects from digestive tract is higher if separate meal or a diet in general are characterized by the high content of fats. The diet with the low content of fats reduces probability of development of the undesirable phenomena from digestive tract.

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

As decrease in body weight can be followed by improvement of metabolic control at patients with a diabetes mellitus, to those persons who receive hypoglycemic drugs, before drug use Ksenalten Layt it is necessary to consult with the doctor and if necessary to carry out dose adjustment of hypoglycemic means.

Decrease in body weight can be followed by improvement of indicators of arterial pressure and decrease in concentration of cholesterol. The patients accepting drugs concerning arterial hypertension or a hypercholesterolemia at drug use Ksenalten Layt should consult with the doctor and if necessary to carry out dose adjustment of these medicines.

At the patients applying орлистат cases of proctorrhagias are described. If there is this phenomenon, the patient should consult with the doctor.

Use of an additional method of contraception for prevention of possible inefficiency of peroral kontratsepriv when developing heavy diarrhea is recommended.

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 manage vehicles and mechanisms. Any negative influence of drug Ksenalten Layt on ability to manage vehicles and mechanisms is not revealed.

Side effects:

The undesirable phenomena at reception of an orlistat were noted generally from the gastro intestinal path (GIP) and were caused by increase in amount of fat in Calais. At long therapy orlistaty the quantity of the undesirable phenomena decreases.

The side effects provided below are given according to the WHO classification of frequency of development of side effects:

• very often-> 1/10 appointments
• often - from> 1/100 to <1/10 appointments
• infrequently - from> 1/1000 to <1/100 appointments
• seldom - from> 1/10000 to <1/1000 appointments
• very seldom - <1/10000 appointments
• frequency is not known - according to the available data it is not possible to establish emergence frequency.

Disturbances 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: abdominal pain, incontience calla, liquid chair, defecation increase.

Post-marketing observations.

Disturbances from blood and lymphatic system. Frequency is not known: decrease in a prothrombin, increase INR (the international normalized relation). These side effects were observed at simultaneous use of an orlistat and anticoagulants.

Disturbances from digestive tract. Frequency is not known: insignificant proctorrhagia, diverticulitis.

Disturbances from a liver and biliary tract. Frequency is not known: increase in activity of "hepatic" transaminases, an alkaline phosphatase, hepatitis, a zhelchekamenny disease of Disturbance from skin and hypodermic fabrics. Frequency is not known: violent rash.

Disturbances from immune system. Frequency is not known: skin itch. rash, urticaria, Quincke's disease, bronchospasm, anaphylaxis.

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 Ksenalten Layt and cyclosporine contraindicated.

At simultaneous use of an orlistat with Amiodaronum it is noted to the umenshena of concentration of Amiodaronum in a blood plasma after single use, however in connection with difficult pharmacokinetics of Amiodaronum, the clinical importance of this phenomenon is not clear. Simultaneous use of an orlistat and Amiodaronum is possible only according to the recommendation of the doctor.

Medicinal interaction of an orlistat with warfarin is not revealed, however at a concomitant use of an orlistat and warfarin or other anticoagulants decrease in concentration of a prothrombin and increase in MNO can be observed. what leads to change of haemo static indicators. Simultaneous use of drug Ksenalten Layt 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.

Taking into account lack of researches of pharmacokinetic interaction, combined use of an 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, oral contraceptives, phentermine, pravastatiny, nifedipine, sibutraminy, ethanol is not revealed.

Contraindications:

Hypersensitivity to an orlistat or any other components of drug; syndrome of chronic malabsorption; cholestasia; simultaneous use with indirect anticoagulants (warfarin) or other peroral anticoagulants; simultaneous use with cyclosporine; pregnancy; breastfeeding period: children's age up to 18 years.

Overdose:

Reception of single doses of 800 mg or administration of drug on 400 mg 3 times a day within 15 days as at patients with normal body weight, and patients with obesity was not followed by the essential undesirable phenomena. Besides, patients with obesity have an experience of use of an orlistat on 240 mg 3 times a day within 6 months that was not followed by reliable increase in frequency of the undesirable phenomena.

In overdose cases orlistaty it was reported or about lack of the undesirable phenomena, or the undesirable phenomena did not differ from those. which are observed at administration of drug in therapeutic doses.

In case of overdose consultation of the doctor is necessary. In cases of the expressed overdose it is recommended to watch the patient within 24 hours. According to preclinical and clinical trials, the system effects connected with lipazoingibiruyushchy properties of an orlistat have to be quickly reversible.

Storage conditions:

In the dry place protected from light at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 2 years. Not to apply after a period of validity.

Issue conditions:

Without recipe

Packaging:

Capsules on 60 mg. Packaging: on 7 or 21 capsule in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished. On 1, 2, 3, 4 blister strip packagings together with the application instruction place in a pack from a cardboard.