Орсотен®

General characteristics. Structure:

Active agent:  
орсотен semi-finished product granule of 225,6 mg
(in terms of active agent орлистат — 120 mg)  
structure of a semi-finished product granules (100 g): орлистат — 53,1915 g; MKTs  
excipients: MKTs  
capsules from a gipromelloza  
structure of a cover of the capsule  
capsule case: gipromelloza; water; titanium dioxide (E171)  
capsule lid: gipromelloza; water; titanium dioxide (E171)  

Description of a dosage form

Capsules from a gipromelloza.

Lid and the case of the capsule from color, white to white with a yellowish shade.

Contents of capsules — microgranules or mix of powder and microgranules of white or almost white color. Availability of the packed agglomerates which are easily scattered when pressing is allowed.

Pharmacological properties:

Pharmacodynamics. Orlistat — the specific inhibitor of gastrointestinal lipases possessing long action. It has therapeutic effect in a gleam of a stomach and small intestine, forming a covalent bond with the active serinovy site of gastric and intestinal lipases. The enzyme inactivated, thus, loses ability to split the food fats arriving in the form of triglycerides on the soaking-up free fatty acids and monoglycerides. As not split triglycerides are not soaked up, 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. 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 of an orlistat low. In 8 hours 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 confirms the minimum absorption of drug.

Distribution. In vitro орлистат more than for 99% contacts proteins of plasma (generally with lipoproteins and albumine). In the minimum quantities орлистат can get into erythrocytes.

Metabolism. Orlistat is metabolized, mainly, in an intestines wall with formation pharmacological of inactive metabolites: M1 (the hydrolyzed four-membered lactonic ring) and M3 (M1 with the chipped-off N-formylleucine rest).

Removal. The main way of elimination is removal through intestines — about 97% of the accepted drug dose, from them 83% — орлистат in not changed look.

Cumulative removal through kidneys of all substances which are structurally connected with orlistaty makes less than 2% of the accepted drug dose. Time of full elimination makes 3–5 days. Orlistat and metabolites can be removed with bile.

Indications to use:

Long treatment of patients at such states, as:

obesity (body weight index (BWI) of ≥30 kg/sq.m);

the excess body weight (IMT of ≥28 kg/sq.m), including the having risk factors associated with obesity, in combination with moderately low-calorie diet.

Orsoten patients can appoint in combination with hypoglycemic drugs and/or moderately low-calorie diet with a diabetes mellitus of type 2 with the excess body weight or obesity.

Route of administration and doses:

Inside, washing down with water, just before each main meal, during food or not later than in an hour after food.

The recommended single dose of an orlistat makes 1 капс. on 120 mg. If meal is missed or food does not contain fat, then reception of an orlistat can be missed.

Doses of an orlistat over 120 mg 3 times a day do not strengthen its therapeutic effect. Therapy duration — no more than 2 years. Dose adjustment is not required for patients of advanced age or patients with abnormal liver functions or kidneys.

Safety and efficiency of use of an orlistat in treatment of children are aged younger than 18 years is not established.

Features of use:

Orlistat is effective for long control of body weight (decrease in body weight, its maintenance at appropriate level and prevention of repeated addition of body weight). Treatment orlistaty leads to improvement of a profile of the risk factors and diseases accompanying obesity (including a hypercholesterolemia, disturbance of tolerance to glucose, a giperinsulinemiya, arterial hypertension, a diabetes mellitus of type 2) and to reduction of amount of visceral fat.

Decrease in body weight during treatment orlistaty can be followed by improvement of compensation of carbohydrate metabolism at patients with diabetes 2 types that is able to afford to lower a dose of hypoglycemic drugs.

For providing adequate food patients are recommended to accept polyvitaminic drugs.

Patients should adhere to recommendations concerning a diet. They have to receive the balanced, moderately low-calorie food containing no more than 30% of calories in the form of fats. Daily consumption of fats should be distributed on three main meals.

The probability of development of side reactions from a GIT can increase if орлистат accept against the background of the food rich with fats (for example 2000 kcal/days, more than 30% of daily consumption of calories arrive in the form of fats that about 67 g of fat equal). Patients have to know that the more precisely they keep to a diet (especially relatively the permitted amount of fat), the probability of development of side reactions is less. The diet with the low content of fats reduces probability of development of side reactions from a GIT and helps patients to control and regulate fat consumption.

If in 12 weeks of therapy there was no decrease in body weight, at least, for 5%, reception of an orlistat should be stopped.

Side effects:

Side reactions on орлистат were generally noted from a GIT and were caused by the increased amount of fat in Calais. Usually observed side reactions are poorly expressed and have passing character. Emergence of these phenomena was observed at the initial stage of treatment within the first 3 months (but no more than one case). At long use of an orlistat the quantity of cases of by-effects decreases.

Meet: the meteorism which is followed by allocations from a rectum, desires on defecation, a fat/oil chair, oily allocations from a rectum, a liquid chair, a soft chair, inclusions of fat in Calais (steatorrhea), pain/feeling of discomfort in a stomach, defecation increase, pain/discomfort in a rectum, imperative desires on defecation, an incontience a calla, damage of teeth and gums; a hypoglycemia at patients with a diabetes mellitus of type 2, a headache, feeling of alarm, flu, feeling of fatigue, an infection of upper parts of respiratory tracts, infections of urinary tract, a dysmenorrhea, it is rare: allergic reactions (for example itch, rash, urticaria, Quincke's disease, bronchospasm, anaphylaxis); very seldom — a diverticulitis, cholelithiasis, hepatitis (it is possible in heavy degree), violent rash, increase in level of hepatic transaminases and ShchF.

Interaction with other medicines:

At the patients receiving warfarin or other anticoagulants and орлистат. decrease in level of a prothrombin, increase in the international coefficient of normalization (INR) can be observed that leads to changes of haemo static parameters.

Interaction with amitriptyline, guanyl guanidines, digoxin, fibrata, fluoxetine, lozartany, Phenytoinum, oral contraceptives, phentermine, GITS nifedipine, nifedipine with the slowed-down release, sibutraminy, furosemide, captopril, atenololy, glibenclamide or ethanol was not observed. Increases bioavailability and hypolipidemic effect of a pravastatin, increasing its concentration in plasma for 30%. Decrease in body weight can improve a metabolism at patients with a diabetes mellitus owing to what it is necessary to reduce a dose of peroral hypoglycemic means. Treatment orlistaty can potentially break absorption of fat-soluble vitamins (A, D, E. К). If reception of polyvitamins is recommended, then they should be accepted not earlier than in 2 h after reception of an orlistat or before going to bed.

At a concomitant use of an orlistat and cyclosporine decrease in level of concentration of cyclosporine in a blood plasma therefore it is recommended to a bowl to carry out determination of level of concentration of cyclosporine in a blood plasma was noted.

At the patients receiving Amiodaronum it is necessary to make more carefully clinical observation and monitoring of an ECG since cases of decrease in level of concentration of Amiodaronum in a blood plasma are described.

Contraindications:

Hypersensitivity to an orlistat or any other components of drug;

syndrome of chronic malabsorption;

cholestasia;

pregnancy;

feeding by a breast;

children's age up to 18 years (efficiency and safety are not studied).

Use at pregnancy and feeding by a breast

By results of preclinical trials: teratogenecity and embriotoxity at reception of an orlistat were not observed. Clinical data on use of an orlistat during pregnancy are absent therefore it is not necessary to appoint орлистат at this time.

Data on use in the period of a lactation are absent therefore орлистат it is not necessary to accept in the period of a lactation.

Overdose:

Cases of overdose are not described. Reception of a single dose of an orlistat of 800 mg or repeated doses to 400 mg 3 times a day within 15 days was not followed by considerable side reactions. In addition, the dose of 240 mg 3 times a day appointed to patients with obesity within 6 months did not cause considerable strengthening of by-effects. In case of overdose of an orlistat it is recommended to observe the patient during 24 h.

Storage conditions:

At a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 2 years.

Issue conditions:

According to the recipe

Packaging:

Capsules, 225,6 mg. On 7 or 21 капс. in a blister strip packaging; in a cardboard pack of 3, 6 or 12 packagings (on 7 капс.) or 1, 2 or 4 packagings (on 21 капс.).