Xenalten Light - instructions for use, dose, side effects, contraindications

Excipients: cellulose microcrystalline 29.8 mg, sodium lauryl sulfate 5.0 mg, carboxymethyl starch sodium (sodium starch glycolate) 19 mg, povidone K-30 5 mg, talc 1.2 mg;

capsule hard gelatinous №З: body - titanium dioxide 2%, gelatin up to 100%, lid - titanium dioxide 2%, dye blue patented 0.0176%, dye diamond black 0.0051%, gelatin - up to 100%.

Description:Hard gelatin capsules No. 3 with a white body and a blue lid. The contents of the capsules are a mixture of powder and granules of white or almost white color.

Pharmacotherapeutic group:Inhibitor of gastrointestinal tract lipases

ATX: & nbsp

A.08.A.B.01 Orlistat

Pharmacodynamics:

Orlistat is a potent, specific and reversible inhibitor of long-acting gastrointestinal lipases. It acts in the lumen of the stomach and small intestine, forming a covalent bond with the active serine portion of the gastric and pancreatic lipases. The inactivated enzyme is not able to break down the food fats coming in the form of triglycerides, up to the absorbed free fatty acids and monoglycerides.

Undivided triglycerides are not absorbed, in connection with which, the intake of calories in the body decreases, which leads to a decrease in body weight. Orlistat at a dose of 60 mg three times a day blocks the absorption of approximately 25% of edible fat. The therapeutic effect of the drug is carried out without absorption into the systemic bloodstream. Increases the concentration of fat in the contents of the intestine 24-48 hours after its use inside. After the drug is withdrawn, the fat content in the intestinal contents after 48-72 hours usually returns to the level that occurred before the start of therapy.

In adults with BMI (body mass index) ≥28 kg / m² orlistat in a dose of 60 mg three times a day is effective in combination with a low-fat hypocaloric diet. In this case, the main weight loss occurs during the first 6 months of treatment.

The decrease in body weight, caused by the use of orlistat at a dose of 60 mg three times a day, is accompanied by another beneficial effect: a decrease in the concentration of total cholesterol, LDL cholesterol (low-density lipoproteins), and a decrease in the waist circumference.

Pharmacokinetics:

Suction

Absorption is low. After 8 hours after ingestion in a dose of 360 mg unchanged orlistat in blood plasma is practically not determined (concentration <5 ng / ml).Signs of cumulation are absent, which is consistent with the minimum absorption of the drug.

Distribution

The volume of distribution can not be established, since orlistat is practically not absorbed and does not have established systemic pharmacokinetics. Orlistat more than 99% associated with blood plasma proteins in vitro (mainly with lipoproteins and albumin). Orlistat in minimal amounts can penetrate into the red blood cells. Metabolism

Metabolism of orlistat is carried out, mainly, in the intestinal wall with the formation of pharmacologically inactive metabolites: M1 (four-membered hydrolyzed

lactone ring) and M3 (M1 with a split residue N-formleleucine). Molecules M1 and M3 have an open beta-lactone ring and extremely weakly inhibit lipase (respectively, 1000 and 2500 times weaker than orlistat).

Excretion

The main way of excretion through the intestine is about 97% of the dose, 83% of which is unchanged orlistat. Total excretion by the kidneys of all metabolites of orlistat is <2% of the accepted dose of orlistat. The time of complete excretion (through the intestines and kidneys) is 3-5 days. The ratio of orlistat excretion pathways in individuals with normal body weight and obesity was similar.

Indications:

Reduction in overweight in adults over 18 years (body mass index ≥28 kg / m²) when used in conjunction with a moderately hypocaloric diet with a low fat diet.

Contraindications:

Hypersensitivity to orlistat or any other components of the drug; syndrome of chronic malabsorption; cholestasis; simultaneous use with indirect anticoagulants (warfarin) or other oral anticoagulants; simultaneous application with cyclosporine; pregnancy; Breastfeeding period: children under 18 years.

Pregnancy and lactation:

Clinical data on the use of orlistat during pregnancy are absent, therefore the drug Xenalten® Light should not be used during pregnancy.

Due to the fact that data on the penetration of orlistat into breast milk are not available, the use of Xenalten® Light during breastfeeding is contraindicated.

Dosing and Administration:

Inside, 1 capsule (60 mg) three times a day, washed down with water, with each main meal, immediately before, during or no later than one hour after ingestion.If food intake is missed or food is fat-free, Xenalten® Light can also be taken.

Within 24 hours, you can take no more than three capsules of 60 mg of Xenalten® Light. The course of treatment should not exceed 6 months.

If, after 12 weeks of taking Xenalten® Light, a decrease in body weight does not occur (no more than 5% of the original body weight), the patient should consult a physician to determine whether further use is advisable.

The efficacy and safety of orlistat in patients with impaired hepatic and / or renal function, as well as in elderly patients was not investigated, however, given that orlistat absorption is minimal, dose adjustments in elderly people and in persons with impaired liver and / or kidney function it takes.

Side effects:

Adverse events with orlistat were noted mainly from the gastrointestinal tract (GIT) and were caused by an increase in the amount of fat in the feces. With prolonged therapy with orlistat, the incidence of adverse events decreases.

The indicated bottome side effects are given in accordance with the WHO classification incidence of side effects:

Often - ≥1/10 appointments

often from ≥1 / 100 to <1/10 of assignments

infrequently - from ≥1 / 1000 to <1/100 of the assignments

rarely from ≥1 / 10000 to <1/1000 assignments

very rarely - <1/10000 prescriptions

frequency is not known - according to available data, it is not possible to establish the frequency of occurrence.

Disorders from the gastrointestinal tract

Often: oily discharges from the rectum, the escape of gases with a certain amount of detachable, imperative urges for defecation, steatorrhea.

Often: abdominal pain, fecal incontinence, loose stool, frequent bowel movements.

Postmarketing observations

Violations of the blood and lymphatic system

Frequency not known: decreased prothrombin, increased INR (international normalized ratio). These side effects were observed with the simultaneous use of orlistat and anticoagulants.

Ongastrointestinal disruption

Frequency not known: minor bleeding from the rectum, diverticulitis. Disturbances from the liver and bile ducts

Frequency not known: increased activity of "liver" transaminases, alkaline

phosphatase, hepatitis, cholelithiasis

Disturbances from the skin and subcutaneous tissues

Frequency not known: bullous rash.

Onimmunosuppression

Frequency not known: itching. rash, hives, angioedema, bronchospasm, anaphylaxis.

Overdose:

Receiving single doses of 800 mg or taking 400 mg 3 times a day for 15 days, both in patients with normal body weight and patients with obesity was not accompanied by significant adverse events. In addition, patients with obesity experience the use of orlistat 240 mg 3 times a day for 6 months, which was not accompanied by a significant increase in the incidence of adverse events.

In cases of an overdose of orlistat, either the absence of adverse events was reported, or undesirable phenomena did not differ from those. which are observed when taking the drug in therapeutic doses.

In case of an overdose, consult a doctor. In cases of severe overdose, it is recommended that the patient be observed for 24 hours. According to preclinical and clinical studies, the systemic effects associated with lipase inhibitory properties of orlistat should be rapidly reversible.

Interaction:

With the simultaneous use of orlistat and cyclosporine, a decrease in the concentration of cyclosporine in the blood plasma is possible, in connection with which, it is necessary to monitor the content of cyclosporine in the blood plasma. Simultaneous use of the drug Xenalten® Light and cyclosporine is contraindicated.

With the simultaneous use of orlistat with amiodarone, the concentration of amiodarone in the blood plasma was reduced after a single application, but due to the complicated pharmacokinetics of amiodarone, the clinical significance of this phenomenon is not clear. Simultaneous use of orlistat and amiodarone is possible only on the advice of a doctor.

The drug interaction of orlistat with warfarin was not revealed, however, with the simultaneous administration of orlistat and warfarin or other anticoagulants, a decrease in the concentration of prothrombin and an increase in INR may be observed. which leads to a change in hemostatic indicators. Simultaneous use of the drug Xenalten® Light and warfarin or other oral anticoagulants is contraindicated.

Orlistat may reduce the absorption of fat-soluble vitamins A, D, E, K and beta-carotene.If the reception of multivitamins is indicated, they should be taken no earlier than 2 hours after taking orlistat or before bedtime.

Orlistat may reduce the absorption of antiepileptic drugs, which can lead to seizures.

Given the lack of studies of pharmacokinetic interaction, the combined use of orlistat and acarbose is not recommended.

In some cases orlistat can indirectly reduce the bioavailability of oral contraceptives. In the case of severe diarrhea, the use of an additional contraceptive method is recommended.

When taking with sodium levothyroxine concurrently, in connection with a decrease in absorption of inorganic iodine and / or levothyroxine sodium, hypothyroidism and / or a decrease in the control of hypothyroidism may develop.

There was no drug interaction with amitriptyline, atorvastatin, biguanides, digoxin, fibrates, fluoxetine, losartan, phenytoin, oral contraceptives, phentermine, pravastatin, nifedipine, sibutramine, ethanol.

Special instructions:

Patients should point out the need to adhere to their dietary recommendations.

Diet and exercise are an important component of the program to reduce body weight. It is recommended to begin the diet program and physical exercises before the beginning of therapy with the drug. During the use of the drug, the patient should receive a moderately hypocaloric diet with a balanced nutrient content, in which approximately 30% is fat. Daily intake of fat should be distributed among the three main meals. It is recommended that food be rich in fruits and vegetables. The program of diet and exercise should be continued after the drug has been discontinued.

The likelihood of side effects from the gastrointestinal tract is higher if a single meal or diet as a whole is characterized by a high fat content. A diet low in fat reduces the likelihood of developing adverse events from the gastrointestinal tract.

Patients with kidney disease should consult with a physician, since possibly the development of hyperoxaluria and nephropathy.

Since weight loss may be accompanied by improved metabolic control in patients with diabetes mellitus, those who receive hypoglycemic drugs before starting the drug Xenalten® Light should consult with a doctor and, if necessary, adjust the dose of hypoglycemic agents.

Decreased body weight may be accompanied by an improvement in blood pressure and a decrease in cholesterol concentration. Patients taking drugs for hypertension or hypercholesterolemia, when using the drug Xenalten® Light should consult with a doctor and, if necessary, adjust the dose of these drugs.

In patients using orlistat, cases of bleeding from the rectum are described. If this phenomenon occurs, the patient should consult a physician.

It is recommended to use an additional method of contraception to prevent possible ineffectiveness of oral contraceptives in the event of severe diarrhea.

When there are such symptoms as weakness, fatigue, fever, jaundice and darkening of urine,it is necessary to consult a doctor to rule out the liver function disorder.

Effect on the ability to drive transp. cf. and fur:

There was no adverse effect of the drug Xenalten® Light on the ability to drive vehicles and mechanisms.

Form release / dosage:

Capsules of 60 mg.

Packaging:

For 7 or 21 capsules in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 1, 2, 3, 4 contour squares, together with instructions for use, are placed in a pack of cardboard.

Storage conditions:

In dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 of the year.

Do not use after the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:LP-002925

Date of registration:23.03.2015

Expiration Date:23.03.2020

The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Manufacturer: & nbsp

OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Representation: & nbspOBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSCOBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSCRussia

Information update date: & nbsp05.02.2018

Illustrated instructions

Instructions

Xenalten® Light (Kcenalten® Lite)