Universal reference book for medicines
Name of the drug: ORSOTEN (ORSOTEN ® )

Active substance: orlistat

Type: An agent for the treatment of obesity - an inhibitor of gastrointestinal lipases

Manufacturer: КРКА-РУС (Russia)
Composition, form of production and packaging
Capsules
from white to white with a yellowish shade of color;
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.
1 caps.

orsotene semi-finished granules * 225.6 mg,

which corresponds to the content of orlistat 120 mg

* 100 g of semi-finished granules contain: orlistat - 53.1915 g, microcrystalline cellulose.

Excipients: microcrystalline cellulose.

Composition of the body and cap capsules: hypromellose, water, titanium dioxide (E171).

7 pcs.
- packings cellular planimetric (3) - packs cardboard.
7 pcs.
- packings cellular planimetric (6) - packs cardboard.
7 pcs.
- packings cellular planimetric (12) - packs cardboard.
21 pcs.
- packings of cellular contour (1) - packs cardboard.
21 pcs.
- packings cellular planimetric (2) - packs cardboard.
21 pcs.
- packings cellular planimetric (4) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2015.

PHARMACHOLOGIC EFFECT

A specific inhibitor of gastrointestinal lipases, which has a prolonged effect.
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 feces after 24-48 hours after taking the drug. After the drug is withdrawn, the fat content in the stools usually returns to the initial level after 48-72 hours.
PHARMACOKINETICS

Suction

Absorption of orlistat is low.
8 hours after oral administration of the therapeutic dose, unchanged orlistat in blood plasma is practically not detected (concentration less than 5 ng / ml). Signs of cumulation are absent, which confirms the minimal absorption of the drug.
Distribution

In vitro, orlistat more than 99% binds to plasma proteins (mainly lipoproteins and albumin).
In minimal quantities orlistat can penetrate into the 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 the cleaved N-formylleucine residue).

Excretion

The main way of elimination is through the intestine - about 97% of the dose of the drug, of which 83% - unchanged.

The cumulative excretion of all substances structurally related to orlistat by the kidneys 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

- prolonged treatment of obese patients with a body mass index (BMI) of 30 kg / m 2 , or patients with an overweight (BMI = 28 kg / m 2 ), incl.
having associated with obesity risk factors, in combination with a moderately low-calorie diet.
Orthoten ® 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.

DOSING MODE

The recommended single dose is 1 caps.
(120 mg).
The capsule is taken with water, taking in immediately before each main meal, during meals or not later than 1 hour after a meal.
If food is missed or if the food does not contain fat, you can skip the intake of orlistat.
Doses of orlistat more than 120 mg 3 times / day do not enhance its therapeutic effect.
Duration of therapy - no 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 efficacy of orlistat treatment for children and adolescents under the age of 18 years is not established.

SIDE EFFECT

Adverse reactions were mainly noted on the part of the gastrointestinal tract and were caused by an increased amount of fat in the stool.
Usually observed adverse reactions are mild and transitory. The appearance of these reactions 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 incidence of side effects is reduced.
From the digestive system: flatulence, 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, Increased defecation, pain / discomfort in the rectum, mandatory urge to defecate, stool incontinence, tooth and gum disease;
very rarely - diverticulitis, cholelithiasis, hepatitis, possibly severe, increased activity of hepatic transaminases and alkaline phosphatase.
On the part of metabolism: hypoglycemia in patients with type 2 diabetes mellitus.

From the side of the central nervous system: headache, a sense of anxiety.

Allergic reactions: rarely -
itching, rash, hives, angioedema, bronchospasm, anaphylaxis.
From the skin: very rarely - bullous rash.

Other: flu-like syndrome, fatigue, upper respiratory infections, urinary tract infections, dysmenorrhea.

CONTRAINDICATIONS

- Syndrome of chronic malabsorption;

- cholestasis;

- Pregnancy;

- the period of lactation (breastfeeding);

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

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

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 in pregnancy are absent, so you should not prescribe the drug in this period.
Because
data on application during lactation are absent, orlistat should not be prescribed during lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER

Correction of the dose is not required for patients with impaired renal function.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Dose adjustment is not required for patients with impaired liver function.

APPLICATION FOR CHILDREN

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

APPLICATION IN ELDERLY PATIENTS

Correction of the dose is not required for elderly patients.

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 mellitus, 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 adverse reactions from the GI tract may increase if orlistat is taken amid 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 g 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 and helps patients control and regulate fat intake.
If after 12 weeks of therapy there was no decrease in body weight, at least 5%, orlistat should be stopped.

OVERDOSE

Cases of overdose are not described.

Symptoms: taking a single dose of orlistat 800 mg or multiple doses up to 400 mg 3 times / day for 15 days was not accompanied by significant adverse reactions.
In addition, a dose of 240 mg 3 times / day, prescribed to patients with obesity for 6 months, did not cause a significant increase in adverse reactions.
Treatment: in case of an overdose of orlistat it is recommended to observe the patient for 24 hours.

DRUG INTERACTION

Patients receiving warfarin or other anticoagulants and orlistat may experience a decrease in the level of prothrombin, an increase in INR, leading to changes in haemostatic parameters.

Interactions with amitriptyline, biguanides, digoxin, fibrates, fluoxetine, losartan, phenytoin, oral contraceptives, phentermine, nifedipine (including delayed release), sibutramine, furosemide, captopril, atenolol, glibenclamide or ethanol have not been observed.

Increases the bioavailability and hypolipidemic effect of pravastatin, increasing its concentration in plasma by 30%.

A decrease in body weight can improve metabolism in diabetic patients, and as a result, it is necessary to reduce the dose of oral hypoglycemic agents.

Treatment with orlistat may potentially interfere with 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.

Patients receiving amiodarone should be more carefully monitored and monitored by the ECG;
cases of a decrease in the level of amiodarone concentration in the blood plasma are described.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of the reach of children, in the original package, at a temperature of no higher than 25 ° C.
Shelf life - 3 years.
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