Orsoten, 120 mg capsules 42 pcs

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

The enzyme, thus inactivated, loses its ability to break down dietary fats that come in the form of triglycerides into absorbable free fatty acids and monoglycerides. Because these uncracked triglycerides are not absorbed, the caloric intake is reduced, resulting in weight loss.

The therapeutic effect of the drug is carried out without absorption into the systemic blood flow. The action of orlistat leads to increase of fat content in feces 24-48 hours after taking the drug. After discontinuation of the drug the content of fat in stool usually returns to the initial level in 48-72 hours.

Pharmacokinetics

Intake. Absorption of orlistat is low. In 8 hours after oral administration of therapeutic dose unchanged orlistat in plasma is practically not determined (concentration –

Distribution. In vitro orlistat is more than 99% bound to plasma proteins (mainly to lipoproteins and albumin). In minimal amounts orlistat can penetrate into erythrocytes.

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

Elimination. The main route of elimination is excretion through the intestine – about 97% of the administered dose of the drug, of which 83% is orlistat in unchanged form.

Cumulative excretion through the kidneys of all the substances structurally related to orlistat is less than 2% of the administered dose of the drug. Total elimination time is 3-5 days. Orlistat and metabolites may be excreted with the bile.

Indications

Limiting body weight in adults (over 18 years) with excessive body weight (BMI ≥ 28 kg/m2).

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

Active ingredient

Composition

1 capsule contains:

The active ingredient:

Orsotene semi-finished pellets;

Excipient:

Microcrystalline cellulose.

How to take, the dosage

Orally with water immediately before each main meal, with a meal, or no later than one hour after a meal.

The recommended single dose of orlistat is 1 120 mg capsule. If a meal is skipped or the food does not contain fat, Orlistat can be skipped.

Doses of orlistat over 120 mg 3 times a day do not increase its therapeutic effect. The duration of therapy is not more than 2 years. Dose adjustment is not required for elderly patients or patients with hepatic or renal dysfunction.

The safety and effectiveness of Orlistat in treatment of children under 18 years of age has not been established.

Interaction

In patients receiving warfarin or other anticoagulants and Orlistat, there may be decreased prothrombin levels, increased international normalization ratio (INR), resulting in changes in hemostatic parameters.

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

Lowering body weight may improve metabolism in patients with diabetes mellitus, whereby the dose of oral hypoglycemic agents should be reduced. Treatment with orlistat may potentially impair absorption of fat-soluble vitamins (A, D, E. K).

If multivitamins are recommended, they should not be taken earlier than 2 hours after taking orlistat or before bedtime.

When taking Orlistat concomitantly with cyclosporine, a decrease in plasma cyclosporine concentrations has been noted, and therefore more frequent determination of plasma cyclosporine concentrations is recommended.

In patients receiving amiodarone, clinical monitoring and ECG monitoring should be performed more carefully, since there have been described cases of decreased plasma amiodarone concentrations.

Special Instructions

Orlistat is effective for long-term weight control (weight loss, maintaining weight at an appropriate level and preventing weight gain again). Treatment with orlistat leads to improvement of the profile of risk factors and diseases accompanying obesity (including hypercholesterolemia, impaired glucose tolerance, hyperinsulinemia, arterial hypertension, type 2 diabetes) and reduction of visceral fat.

The reduction in body weight during treatment with orlistat may be accompanied by improved compensation of carbohydrate metabolism in patients with type 2 diabetes, which may allow reduction of the dose of hypoglycemic drugs.

Patients are advised to take multivitamins to ensure adequate nutrition.

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

The chance of gastrointestinal adverse reactions may increase if Orlistat is taken with a fat-rich diet (e.g., 2000 kcal/d, more than 30% of daily caloric intake comes in the form of fat, which equals approximately 67 g fat). Patients should be aware that the more closely they follow the diet (especially regarding the amount of fat allowed), the less likely they are to develop adverse reactions. A low-fat diet reduces the likelihood of GI adverse reactions and helps patients control and manage their fat intake.

If after 12 weeks of therapy there has not been at least a 5% decrease in body weight, Orlistat should be stopped.

Contraindications

Side effects

Adverse reactions to orlistat have mainly been reported in the gastrointestinal tract and have been caused by increased amounts of fat in the feces. 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 adverse events decreases.

There are cases of: flatulence accompanied by rectal discharge, urge to defecate, greasy/oily stools, oily rectal discharge, liquid stools, soft stools, inclusions of fat in the stool (steatorrhea), pain/feeling of discomfort in the abdominal area, frequent defecation, pain/discomfort in the rectum, imperative defecation urges, stool incontinence, dental and gum damage; hypoglycemia in patients with type 2 diabetes, headache, anxiety, flu, fatigue, upper respiratory tract infections, urinary tract infections, dysmenorrhea, rare: Allergic reactions (e.g. itching, rash, urticaria, angioneurotic edema, bronchospasm, anaphylaxis); very rare: diverticulitis, cholelithiasis, hepatitis (possibly severe), bullous rash, increased liver transaminases and ALP levels.

Pregnancy use

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

There are no clinical data regarding the use of orlistat during pregnancy; therefore, orlistat should not be prescribed during pregnancy.

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

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