Orsotene - instructions for use, dose, side effects, contraindications

Capsules of hypromellose. The cap and capsule body are white to white with a yellowish hue. The contents of the capsules are microgranules or a mixture of powder and microgranules of white or almost white color. It is allowed to have caked agglomerates that easily break down when pressed.

Pharmacotherapeutic group:Lipase GIT inhibitor

ATX: & nbsp

A.08.A.B.01 Orlistat

Pharmacodynamics:Orlistat is a specific inhibitor of gastrointestinal lipases, which has a long-lasting effect. It has a therapeutic effect in the lumen of the stomach and small intestine, forming a covalent bond with the active serine portion of the gastric and intestinal lipases. Inactivated in this way, the enzyme loses the ability to break down food fats that come in the form of triglycerides, to sucking free fatty acids and monoglycerides.Since uncleaved triglycerides are not absorbed, the intake of calories into 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 bloodstream. The action of orlistat leads to an increase in the fat content in the feces after 24-48 hours after taking the drug. After the drug is withdrawn, the fat content in the stool usually returns to the initial level after 48-72 hours.

Pharmacokinetics:

Suction

Absorption of orlistat is low. 8 hours after ingestion of the therapeutic dose, unchanged orlistat in blood plasma is practically not determined (concentration <5 ng / ml). Signs of cumulation are absent, which confirms the minimal absorption of the drug.

Distribution

In vitro orlistat more than 99% associated with plasma proteins (mainly with lipoproteins and albumin). In minimum quantities orlistat can penetrate into erythrocytes.

Metabolism

Orlistat is metabolized mainly in the intestinal wall with the formation of pharmacologically inactive metabolites: M1 (hydrolysed four-membered lactone ring) and M3 (M1 with split N-formleleucine residue).

Excretion

The main way of elimination is through the intestine - about 97% of the dose taken, where 83% orlistat in unmodified form.

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

Indications:

Orsotene is indicated for prolonged treatment of obese patients with a body mass index (BMI) ≥ 30 kg / m², or patients with an overweight (BMI ≥ 28 kg / m²), including those associated with obesity risk factors, combined with a moderately low-calorie diet.

Orsotenum can be prescribed in combination with hypoglycemic drugs and / or a moderately low-calorie diet for patients with type 2 diabetes mellitus with excessive body weight or obesity.

Contraindications:

- Syndrome of chronic malabsorption;

- cholestasis;

- hypersensitivity to orlistat or any other components of the drug;

- pregnancy and lactation;

- children under 18 years of age (efficacy and safety not studied).

Pregnancy and lactation:

According to the results of preclinical studies: teratogenicity and embryotoxicity were not observed when taking orlistat. Clinical data on the use of orlistat during pregnancy are not available, therefore, should not be prescribed orlistat during pregnancy. Since there is no data on application during lactation, orlistat should not be taken during lactation.

Dosing and Administration:

The recommended single dose of orlistat is one 120 mg capsule that is taken orally, washed down with water, immediately before each main meal, during meals or no later than one hour after a meal. If food intake is missed or if the food does not contain fat, you can skip the intake of orlistat. Doses of orlistat over 120 mg 3 times a day do not enhance its therapeutic effect. The duration of therapy is not more than 2 years. Correction of the dose is not required for elderly patients or patients with impaired liver or kidney function.

The safety and effectiveness of orlistat in the treatment of children under the age of 18 years is not established.

Side effects:

Adverse reactions to orlistat mainly observed from the gastrointestinal tract and were due to an increased amount of fat in the stool. Usually observed adverse reactions are mild and transitory. The appearance of these phenomena was observed at the initial stage of treatment during the first three months (but not more than one case). With prolonged use of orlistat, the incidence of side effects is reduced. There are meteorism accompanied by secretions from the rectum, urges for defecation, fat / oil stools, oily discharge from the rectum, loose stools, soft stools, fats in the stool (steatorrhea), pain / discomfort in the abdomen, more bowel movements, pain / discomfort in the rectum, imperative urges for defecation, stool incontinence, tooth and gum disease; hypoglycemia in patients with type 2 diabetes mellitus, headache, anxiety, flu, fatigue, upper respiratory infections, urinary tract infections, dysmenorrhea, rarely: allergic reactions (eg, itching, rash, urticaria, angioedema, bronchospasm, anaphylaxis ); very rarely: diverticulitis, cholelithiasis, hepatitis,possibly a severe degree, bullous rash, increased levels of hepatic transaminases and alkaline phosphatase.

Overdose:

Cases of overdose are not described. The administration of a single dose of orlistat 800 mg or multiple doses up to 400 mg 3 times a day for 15 days was not accompanied by significant adverse reactions. In addition, a dose of 240 mg 3 times a day, prescribed to patients with obesity for 6 months, did not cause a significant increase in side effects.

In case of an overdose of orlistat it is recommended to observe the patient within 24 hours.

Interaction:

In patients who received warfarin or other anticoagulants and orlistat, there may be a decrease in the level of prothrombin, an increase in the international coefficient of normalization (INR), which leads to changes in the haemostatic parameters.

Interaction with amitriptyline, biguanides, digoxin, fibrates, fluoxetine, losartan, phenytoin, oral contraceptives, phentermine, nifedipine GITS, nifedipine, sustained release, sibutramine, furosemide, captopril, atenolol, glibenclamide, or ethanol was not observed.Increases the bioavailability and hypolipidemic effect of pravastatin, increasing its plasma concentration by 30%. Lower body weight can improve metabolism in diabetic patients, so it is necessary to reduce the dose of oral hypoglycemic agents. Orlistat treatment can potentially impair the absorption of fat-soluble vitamins (A, D, E, K). If multivitamins are recommended, 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 level of cyclosporine concentration in the blood plasma was noted, therefore it is recommended to conduct a more frequent determination of the level of cyclosporin concentration in the blood plasma.

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

Special instructions:

Orlistat is effective for prolonged monitoring of body weight (weight loss, maintenance at an appropriate level and prevention of repeated weight gain).Treatment with orlistat 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 reduction in visceral fat

Decreased 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 can reduce the dose of hypoglycemic drugs.

To ensure adequate nutrition of patients it is recommended to take multivitamin preparations.

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

The likelihood of developing adverse reactions from the gastrointestinal tract may increase if orlistat take on a diet rich in fats (for example, 2000 kcal / day,> 30% of the daily calorie intake comes in the form of fats, which is about 67 grams of fat).Patients should be aware that the more precisely they observe a diet (especially regarding the allowed amount of fat), the less likely the development of adverse reactions. A low-fat diet reduces the likelihood of adverse reactions from the gastrointestinal tract (GIT) and helps patients to monitor and regulate fat intake.

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

Form release / dosage:Capsules of 120 mg.

Packaging:

For 7 or 21 capsules in a contour mesh package. 3, 6 or 12 contour cell packs (7 capsules each) or 1, 2 or 4 contour cell packs (21 capsules each) along with the instructions for use are placed in a pack of cardboard.

Storage conditions:

Store at a temperature of no higher than 25 ° C, in the original packaging.

Keep out of the reach of children.

Shelf life:3 years.
Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-007799/08

Date of registration:03.10.2008 / 09.10.2012

Expiration Date:Unlimited

The owner of the registration certificate:KRKA-RUS, LLC KRKA-RUS, LLC Russia

Manufacturer: & nbsp

KRKA-RUS, LLC Russia

Information update date: & nbsp11.10.2016

Illustrated instructions

Instructions

Orsotene® (Orsoten®)