Orsoten, 120 mg capsules 21 pcs

Orsotene is an inhibitor of gastrointestinal lipases.

Pharmacodynamics

Orlistat is a specific inhibitor of gastrointestinal lipases with prolonged 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 is practically not detected in blood plasma (concentration – < 5 ng/ml). There are no signs of cumulation, which confirms the minimal absorption of the drug.

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

Continued treatment of patients with conditions such as:

Orsotene may be prescribed in combination with hypoglycemic drugs and/or a moderately low calorie diet in patients with type 2 diabetes who are overweight or obese.

Active ingredient

Composition

Active substance:

Orsotene semi-finished pellets 225.6 mg (in terms of the active ingredient orlistat – 120 mg);

Ancillary substances:

MCC

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 the bioavailability and hypolipidemic effect of pravastatin, increasing its plasma concentration by 30%. Reduction of body weight may improve metabolism in patients with diabetes mellitus, due to which it is necessary to reduce the dose of oral hypoglycemic agents. Treatment with orlistat may potentially impair absorption of fat-soluble vitamins (A, D, E, K). If taking multivitamins is recommended, they should not be taken earlier than 2 hours after taking orlistat or before going to bed.

With simultaneous use of orlistat and cyclosporine, a decrease in plasma levels of cyclosporine has been noted, and therefore more frequent determination of plasma levels of cyclosporine 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 body weight control (weight loss, maintaining body 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.

Overdose

No cases of overdose have been described.

The administration of a single dose of orlistat 800 mg or multiple doses up to 400 mg 3 times daily for 15 days was not accompanied by significant adverse reactions.

In addition, the dose of 240 mg 3 times daily administered to obese patients for 6 months did not cause a significant increase in adverse events. In case of orlistat overdose, it is recommended to observe the patient for 24 hours.

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