Orsoten, 120mg capsules, 42pcs

Composition

1 capsule contains:

Active ingredient:  

orsoten semi-finished pellets;

Auxiliary substance:  

microcrystalline cellulose.

Pharmacological action

Orsoten is a long-acting specific inhibitor of gastrointestinal lipases. It has a therapeutic effect in the lumen of the stomach and small intestine, forming a covalent bond with the active serine site of gastric and intestinal lipases.

Inactivated in this way, the enzyme loses its ability to break down dietary fats coming in the form of triglycerides into absorbed free fatty acids and monoglycerides. Since undivided triglycerides are not absorbed, the intake of calories in the body decreases, which leads to a decrease in body weight.

The therapeutic effect of the drug is carried out without absorption into the systemic circulation. The effect of orlistat leads to an increase in the fat content in the feces as early as 24-48 hours after taking the drug. After discontinuation of the drug, the fat content in fecal masses usually returns to the initial level after 48-72 hours

. Pharmacokinetics

Suction. Orlistat absorption is low. 8 hours after oral use of the therapeutic dose, unchanged orlistat is practically not detected in the blood plasma (concentration —

Distribution. In vitro, orlistat binds more than 99% to plasma proteins (mainly lipoproteins and albumin). In minimal amounts, orlistat can penetrate red blood cells.

Metabolism. Orlistat is mainly metabolized in the intestinal wall to form pharmacologically inactive metabolites: M1 (hydrolyzed four-membered lactone ring) and M3 (M1 with a cleaved N-formylleucine residue).

Output. The main route of elimination is elimination through the intestine — about 97% of the dose of the drug taken, of which 83% is orlistat in unchanged form.

The cumulative elimination of all substances structurally related to orlistat through the kidneys is less than 2% of the drug dose taken. The total elimination time is 3-5 days. Orlistat and its metabolites may be excreted in the bile.

Indications

Weight loss in overweight adults (over 18 years of age) (body mass index BMI ≥ 28 kg/m2).

It is used only in combination with a moderate hypocaloric diet with low-fat food.

Use during pregnancy and lactation

According to the results of preclinical studies: teratogenicity and embryotoxicity were not observed when taking orlistat.

There are no clinical data on the use of orlistat during pregnancy, so you should not prescribe orlistat during pregnancy.

Since there are no data on use during lactation, orlistat should not be taken during lactation.

Contraindications

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

Side effects

Adverse reactions to orlistat were mainly observed from the gastrointestinal tract and were caused by an increased amount of fat in the stool. Usually, the observed adverse reactions are mild and transient. The occurrence of these phenomena was observed at the initial stage of treatment during the first 3 months (but not more than one case). With prolonged use of orlistat, the number of cases of side effects decreases.

They meet:  flatulence accompanied by discharge from the rectum, urge to defecate, greasy/oily stools, oily discharge from the rectum, loose stools, soft stools, inclusions of fat in the feces (steatorrhea), pain/discomfort in the abdomen, increased bowel movement, pain/discomfort in the rectum, imperative urge to defecate, fecal incontinence, tooth and gum damage; hypoglycemia in patients with type 2 diabetes, headache, anxiety, flu, fatigue, upper respiratory tract infections, urinary tract infections, dysmenorrhea, rarely: allergic reactions (e. g. pruritus, rash, urticaria, angioedema, bronchospasm, anaphylaxis); very rarely — diverticulitis, cholelithiasis, hepatitis (possibly severe), bullous rash, increased levels of hepatic transaminases and alkaline phosphatase.

Interaction

Patients receiving warfarin or other anticoagulants and orlistat may experience a decrease in prothrombin levels, an increase in the international normalization factor (INR), which leads to changes in hemostatic parameters.

Interactions with amitriptyline, biguanides, digoxin, fibrates, fluoxetine, losartan, phenytoin, oral contraceptives, phentermine, nifedipine GITS, nifedipine delayed release, sibutramine, furosemide, captopril, atenolol, glibenclamide or ethanol were not observed. Increases the bioavailability and hypolipidemic effect of pravastatin, increasing its plasma concentration by 30%.

Weight loss can improve the metabolism of diabetic patients, so it is necessary to reduce the dose of oral hypoglycemic agents. Treatment with orlistat may potentially impair the absorption of fat-soluble vitamins (A, D, E. K).

If a multivitamin is recommended, then they should be taken no earlier than 2 hours after taking orlistat or before bedtime.

With simultaneous use of orlistat and cyclosporine, a decrease in the level of cyclosporine concentration in blood plasma was noted, so it is recommended to determine the level of cyclosporine concentration in blood plasma more often.

In patients receiving amiodarone, more careful clinical monitoring and ECG monitoring should be carried out, since cases of a decrease in the level of amiodarone concentration in blood plasma have been described.

How to take, course of use and dosage

Inside, washed down with water, immediately before each main meal, during a meal, or no later than an hour after a meal.

The recommended single dose of orlistat is 1 capsule of 120 mg. If the meal is skipped or the food does not contain fat, then you can skip taking orlistat.

Doses of orlistat over 120 mg 3 times a day do not enhance its therapeutic effect. Duration of therapy-no more than 2 years. No dose adjustment is required for elderly patients or patients with impaired liver or kidney function.

The safety and efficacy of orlistat in the treatment of children under 18 years of age has not been established.

Special instructions

Orlistat is effective for long-term weight control (reducing body weight, maintaining it at the appropriate level and preventing repeated weight gain). Treatment with orlistat improves the profile of risk factors and diseases associated with obesity (including hypercholesterolemia, impaired glucose tolerance, hyperinsulinemia, hypertension, type 2 diabetes mellitus) and reduces the amount of visceral fat.

Weight loss during treatment with orlistat may be accompanied by improved compensation of carbohydrate metabolism in patients with type 2 diabetes, which may allow reducing the dose of hypoglycemic drugs.

To ensure adequate nutrition, patients are advised to take multivitamins.

Patients should follow the dietary guidelines. They should receive a balanced, moderately low-calorie diet containing no more than 30% of calories in the form of fat. Daily fat intake should be divided into three main meals.

The probability of developing adverse reactions from the gastrointestinal tract may increase if orlistat is taken against the background of a diet rich in fat (for example,2000 kcal/day, more than 30% of the daily calorie intake comes in the form of fat, which is approximately 67 g of fat). Patients should be aware that the more accurately they follow the diet (especially regarding the allowed amount of fat), the less likely they are to develop adverse reactions. A low-fat diet reduces the likelihood of gastrointestinal side effects and helps patients control and regulate their fat intake.

If no weight loss of at least 5% has occurred after 12 weeks of therapy, orlistat should be discontinued.

Form of production

Capsules

Storage conditions

At a temperature not exceeding 25 °C

Shelf life

2 years

Active ingredient

Orlistat

Conditions of release from pharmacies

By prescription

Dosage form

Capsules