Orsoten, 120 mg, 42 pcs.

1 capsule contains:

Active substance: 

orsoten semi-finished product granules;

Excipient: 

microcrystalline cellulose.

Orsotene is a long-lasting 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. 

Thus inactivated, the enzyme loses the ability to break down dietary fats in the form of triglycerides into absorbed free fatty acids and monoglycerides. Since the undigested triglycerides are not absorbed, the intake of calories in the body is reduced, which leads to a decrease in body weight.

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

Pharmacokinetics

Suction. The absorption of orlistat is low. 8 hours after ingestion of a therapeutic dose, unchanged orlistat in blood plasma is practically undetectable (concentration -

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

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

Excretion. The main way of elimination is excretion through the intestines - about 97% of the taken dose of the drug, of which 83% is orlistat in unchanged form.

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

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.

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

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

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

• 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.

Adverse reactions to orlistat were mainly noted from the gastrointestinal tract and were due to an increased amount of fat in the feces. Usually the observed side reactions are mild and transient. The appearance 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 side effects decreases.

Occurs: flatulence accompanied by rectal discharge, urge to defecate, oily / oily stools, oily rectal discharge, loose stools, soft stools, fat inclusions in the stool (steatorrhea), pain / discomfort in the abdomen, increased frequency of bowel movements, pain / discomfort in the rectum, urge to defecate, fecal incontinence, damage to the teeth and gums; hypoglycemia in patients with type 2 diabetes mellitus, headache, anxiety, flu, fatigue, upper respiratory tract infections, urinary tract infections, dysmenorrhea, rarely: allergic reactions (for example, itching, rash, urticaria, angioedema, bronchospasm, anaphylaxis) ; very rarely - diverticulitis, gallstone disease, hepatitis (possibly severe), bullous rash, increased levels of hepatic transaminases and alkaline phosphatase.

In patients receiving warfarin or other anticoagulants and orlistat, there may be a decrease in prothrombin levels, an increase in the international normalization rate (INR), which leads to changes in hemostatic parameters.

Interaction with amitriptyline, biguanides, digoxin, fibrates, fluoxetine, losartan, phenytoin, oral contraceptives, phentermine, nifedipine GITS, sustained-release nifedipine, sibutramine, furosemide, neoblastolamidomopril. Increases the bioavailability and hypolipidemic effect of pravastatin, increasing its plasma concentration by 30%. 

Weight loss can improve metabolism in diabetic patients, as a result of which it is necessary to reduce the dose of oral hypoglycemic agents. Orlistat treatment can potentially interfere with the absorption of fat-soluble vitamins (A, D, E. K). 

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

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

In patients receiving amiodarone, clinical observation and ECG monitoring should be carried out more closely, because cases of a decrease in the level of concentration of amiodarone in blood plasma are described.

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

The recommended single dose of orlistat is 1 capsule of 120 mg. If the meal is skipped or the meal does not contain fat, then 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 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 using orlistat in the treatment of children under the age of 18 has not been established.

Orlistat is effective for long-term control of body weight (reducing body weight, maintaining it at an appropriate level and preventing re-weight gain). Orlistat treatment leads to an improvement in the profile of risk factors and diseases associated with obesity (including hypercholesterolemia, impaired glucose tolerance, hyperinsulinemia, arterial hypertension, type 2 diabetes mellitus) and a decrease in the amount of visceral fat.

A decrease in body weight during treatment with orlistat may be accompanied by an improvement in the compensation of carbohydrate metabolism in patients with type 2 diabetes, which may allow a decrease in the dose of hypoglycemic drugs.

Patients are advised to take multivitamins to ensure adequate nutrition.

Patients should adhere to dietary recommendations. They should eat a balanced, moderately low-calorie diet with no more than 30% of their calories as fat. Divide your daily fat intake into three main meals.

The likelihood of developing adverse reactions from the gastrointestinal tract may increase if orlistat is taken on a diet rich in fats (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 closely they follow the diet (especially in relation to the allowed amount of fat), the less likely it is to develop adverse reactions. A low-fat diet reduces the likelihood of gastrointestinal side reactions and helps patients control and regulate their fat intake.

If after 12 weeks of therapy there has been no decrease in body weight by at least 5%, orlistat should be discontinued.