Orsoten Slim, 60 mg 84 pcs.

Active substance:

orsoten semi-finished product - granules - 112.8 mg, in terms of orlistat - 60 mg (auxiliary substance of the semi-finished product - microcrystalline cellulose granules).

Excipients :

microcrystalline cellulose - 22.20 mg.

Hard gelatin capsules No. 3:

Capsule body:

titanium dioxide (E 171) - 0.58 mg,

gelatin - 28.22 mg.

Capsule cap:

titanium dioxide (E 171) - 0.19 mg,

iron oxide yellow (E172) - 0.04 mg,

  gelatin - 18.97 mg.

Pharmacodynamics

Orlistat is a specific, long-acting inhibitor of gastrointestinal lipases. Its therapeutic activity is realized in the lumen of the stomach and small intestine and consists in the formation of a covalent bond with the active serine site of gastric and pancreatic lipases.

The enzyme inactivated in this way loses the ability to hydrolyze edible fat in the form of triglycerides to absorbable free fatty acids and monoglycerides. Undigested triglycerides are not absorbed, and the resulting caloric deficit can have a positive effect on weight control.

Orlistat 60 mg three times a day blocks the absorption of approximately 25% of dietary fat. The therapeutic effect of orlistat is realized without its systemic absorption. The effect of orlistat leads to the fact that the concentration of fat in the intestinal contents increases within 24–48 hours after its ingestion. After discontinuation of orlistat, the concentration of fat in the intestinal contents usually returns to baseline values ​​after 48–72 hours.

In adults with a BMI (body mass index) ≥ 28 kg / m2, orlistat 60 mg three times daily is effective when combined with a low-fat, hypocaloric diet. Moreover, the main body weight loss occurs during the first 6 months of treatment.

The decrease in body weight caused by the use of orlistat at a dose of 60 mg three times a day is accompanied by other beneficial effects: a decrease in the concentration of total cholesterol, LDL cholesterol (low density lipoproteins), as well as a decrease in waist circumference.

Pharmacokinetics

Suction

Studies in volunteers with normal and increased body weight have shown that the degree of absorption of orlistat is minimal. The concentration of unchanged orlistat in blood plasma is below the limit of quantitative determination (below 5 ng / ml) 8 hours after oral administration of orlistat at a dose of 360 mg. In general, when using therapeutic doses, the determination of unchanged orlistat in blood plasma is sporadic, and its concentration is extremely low (less than 10 ng / ml or 0.02 μmol / l), and there are no signs of cumulation, which indicates a minimum degree of absorption.

Distribution

The volume of distribution cannot be determined, since orlistat is minimally absorbed and has no established systemic pharmacokinetics. Orlistat is more than 99% bound to blood plasma proteins (mainly lipoproteins and albumin). Orlistat can penetrate into red blood cells to a minimum extent.

Metabolism

Orlistat metabolism occurs mainly in the walls of the stomach and small intestine.

Withdrawal

Approximately 97% of the dose is excreted through the intestines, 83% of this amount is in the form of unchanged orlistat. The cumulative renal excretion of all orlistat-containing substances is less than 2% of the dose taken. The time to achieve full excretion (through the intestines and kidneys) is 3 to 5 days.

Weight loss in overweight adults (over 18 years old) (body mass index BMI ≥ 28 kg / m2). Only used in conjunction with a moderate, low-fat, hypocaloric diet.

There are no clinical data on the use of orlistat during pregnancy, therefore, Orsoten® Slim should not be used during pregnancy.

Since it is not known whether orlistat is excreted in breast milk, Orsoten® Slim should not be used during breastfeeding.

• Hypersensitivity to orlistat or to any of the components of the drug;
• glucose-galactose malabsorption syndrome;
• cholestasis;
• concomitant therapy with cyclosporine;
• pregnancy, breastfeeding period;
• age up to 18 years.

Classification of the incidence of side effects (WHO):

• very often> 1/10;
• often from> 1/100 to <1/10;
• infrequently from> 1/1000 to <1/100;
• rarely from> 1/10000 to <1/1000 very rarely from <1/10000, including isolated reports.

Adverse reactions when using orlistat are usually gastrointestinal in nature and are associated with its pharmacological action.

On the part of the digestive system: very often - oily discharge from the rectum, gas with some discharge, urge to defecate, steatorrhea; often - abdominal pain, fecal incontinence, loose stools, increased bowel movements.

During the post-marketing use of orlistat, the following adverse reactions were noted (frequency unknown):

From the hematopoietic system: a decrease in the concentration of prothrombin; an increase in the International Normalized Ratio (INR) in patients taking orlistat simultaneously with anticoagulants.

On the part of the digestive system: slight rectal bleeding, diverticulitis, hepatitis, cholelithiasis, increased activity of "hepatic" transaminases and alkaline phosphatase.

From the skin: bullous rash.

Allergic reactions: itching, rash, urticaria, angioedema, bronchospasm, anaphylaxis.

Cyclosporine

With the simultaneous use of cyclosporine and orlistat, a decrease in the concentration of cyclosporine in the blood plasma is observed, which may be accompanied by a decrease in its immunosuppressive activity.

The simultaneous use of orsoten and cyclosporine is contraindicated.

Oral anticoagulants

With the simultaneous use of warfarin or other oral anticoagulants and orlistat, a change in the value of the International Normalized Ratio (INR) may occur.

Fat-soluble vitamins

Orlistat may impair absorption of fat-soluble vitamins (A, D, E and K).

Acarbose

Due to the lack of data on pharmacokinetic interactions, it is not recommended to use orlistat simultaneously with acarbose.

Amiodarone

With simultaneous use with orlistat, a decrease in the concentration of amiodarone in blood plasma after a single use was noted. The clinical significance of this effect in patients taking amiodarone is unclear. The simultaneous use of orlistat and amiodarone is possible only on the recommendation of a doctor.

Orlistat does not interact with amitriptyline, phenytoin, fluoxetine, sibutramine, phentermine; atorvastatin, pravastatin, fibrates; biguanides; digoxin, nifedipine, losartan; oral contraceptives and ethanol.

Inside, 1 capsule (60 mg) three times a day with water, immediately before, during or within 1 hour after each meal.

If a meal is skipped or the meal does not contain fat, orlistat should be skipped.

Within 24 hours, you can take no more than three capsules of 60 mg of Orsoten® Slim.

Duration of treatment

The course of treatment should not exceed 6 months. If, after 12 weeks of using Orsoten® Slim, there is no decrease in body weight (no more than 5% of the initial weight), the patient should consult a doctor to decide on the appropriateness of further use.

Diet and exercise are important components of a weight loss program. It is recommended to start the dietary program and exercise before starting Orsoten® Slim therapy.

During the use of Orsoten® Slim, the patient should receive a moderately hypocaloric diet with a balanced nutrient content, in which approximately 30% are fats (for example, with a calorie content of 2000 kcal per day, food should contain no more than 67 grams of fat). Your daily intake of fat, carbohydrates, and protein should be split across your three main meals. The diet and exercise program should be continued after the use of Orsoten® Slim is discontinued.

Elderly patients

Data on the use of orlistat in the elderly are limited.

Patients with impaired liver and kidney function

The effects of orlistat in persons with impaired liver and / or kidney function have not been studied, however, given that the absorption of orlistat is minimal, dose adjustment in the elderly and in persons with impaired liver and / or kidney function is not required.

Symptoms: when using orlistat at a dose of 800 mg once and at a dose of up to 400 mg three times a day, daily, for 15 days, both in patients with normal body weight and in patients with obesity, no significant adverse reactions were detected. When using orlistat 240 mg three times a day for 6 months, there was no increase in the frequency of adverse reactions.

Most reports of orlistat overdose in the post-marketing period either do not have specific information about adverse reactions, or describe adverse reactions that do not differ from those observed when using the recommended doses of orlistat.

Treatment: in case of overdose, a doctor's consultation is necessary. In case of a significant overdose of orlistat, observation of the patient for 24 hours is recommended. Based on data from human and animal studies, all systemic effects of orlistat due to lipase inhibition are usually quickly reversible.

Patients should be advised of the need to adhere to their dietary recommendations. The likelihood of side effects from the gastrointestinal tract is higher if a single meal or diet is generally high in fat.

Treatment with Orsoten® Slim can lead to malabsorption of fat-soluble vitamins (A, D, E and K). For this reason, multivitamins should be taken at bedtime.

Since a decrease in body weight may be accompanied by an improvement in metabolic control in patients with diabetes mellitus, those who receive hypoglycemic drugs should consult a doctor before using Orsoten® Slim and, if necessary, adjust the dose of hypoglycemic agents.

Weight loss can be accompanied by an improvement in blood pressure and a decrease in cholesterol concentration.

Patients taking medications for arterial hypertension or hypercholesterolemia, when using Orsoten® Slim, should consult a doctor and, if necessary, adjust the dose of these medications. Patients taking amiodarone should consult a doctor before starting therapy with Orsoten® Slim.

Cases of rectal bleeding have been reported in patients using orlistat. If this phenomenon occurs, the patient should consult a doctor.

The use of an additional method of contraception is recommended to prevent possible ineffectiveness of oral contraceptives in the event of severe diarrhea.

Influence on the ability to drive vehicles and other mechanisms that require increased concentration of attention

Orsoten® Slim has no effect on driving and working with technical devices that require increased concentration of attention and speed of psychomotor reactions.