Active substanceOrlistatOrlistat
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  • Dosage form: & nbspcapsules
    Composition:

    One capsule contains:

    Active substance: Orlistat 60 mg.

    Excipients: microcrystalline cellulose, sodium carboxymethyl starch, sodium lauryl sulfate, povidone, talc; capsule: gelatin, titanium dioxide, indigocarmine, sodium lauryl sulfate, sorbitan laurate, black opaque inks (Opacode) S-1-17822 / 23 (shellac, iron stain oxide black E172, propylene glycol); gelatinous fringe: gelatin, polysorbate-80, indigocarmine.

    Description:

    Hard gelatin capsules No. 2, with an opaque turquoise cap, an opaque turquoise shell, with a blue border; inscription "alli"It is printed in black ink on the lid.The contents of the capsules are white or almost white granules.

    Pharmacotherapeutic group:Inhibitor of gastrointestinal tract lipases
    ATX: & nbsp

    A.08.A.B.01   Orlistat

    Pharmacodynamics:

    Orlistat is a potent specific inhibitor of long-acting gastrointestinal lipases. It manifests its therapeutic activity 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 loses the ability to hydrolyze dietary fats (triglycerides) into absorbable free fatty acids and monoglycerides. Undivided triglycerides are not absorbed, which leads to Reducing the number of calories absorbed by the body, and reducing body weight.The therapeutic effect of the drug is thus carried out without being absorbed into the systemic bloodstream. According to the results of clinical studies, orlistat, taken daily at a dose of 60 mg three times a day, blocks the absorption of approximately 25 % fats included in the daily diet.

    Along with a decrease in body weight, with a prolonged intake of orlistat at a dose of 60 mg, there are decreases in such indicators as waist circumference, total cholesterol level and low density lipoprotein cholesterol (LDL cholesterol). After 6 months of treatment with orlistat in a dose of 60 mg, the average level of total cholesterol is reduced by an average of 2.4%, LDL cholesterol by 3.5%. The waist circumference after half a year of taking the drug decreases on average by 4.5 cm.

    Pharmacokinetics:

    Absorption

    Absorption of the drug is minimal.

    Excretion

    About 97% of the administered dose of the drug is secreted through the intestine, 83% of this amount is unchanged.

    The excretion of orlistat and its metabolites through the kidneys is less than 2% of the dose taken. The drug is completely eliminated after 3-5 days. Excretion of orlistat as in volunteers with normal body weight, and in obese patients is similar.

    Indications:

    Reduction in overweight in adults (over 18 years) with a body mass index (BMI)> 28 kg / m2. It is used only in combination with a moderately hypocaloric diet containing not more than 30% of the daily caloric value in the form of fats.

    Contraindications:

    - Hypersensitivity to orlistat or to any of the components of the drug;

    - syndrome of chronic malabsorption;

    - cholestasis;

    - concomitant administration of cyclosporine;

    - concomitant reception of indirect anticoagulants (warfarin)

    - concomitant use of sitagliptin

    - pregnancy and lactation;

    - age to 18 years.

    Pregnancy and lactation:

    Alli should not be used during pregnancy due to the lack of reliable clinical data confirming the safety of its use.

    It is not established whether the orlistat in breast milk, in connection with which the use of Alli during lactation (breastfeeding) is not recommended.

    Dosing and Administration:

    For adults, the recommended dose of Alli is 60 mg (1 capsule) 3 times a day with each main meal in combination with a moderately hypocaloric diet with a low fat content. The capsule should be taken immediately before meals, during meals or no later than 1 hour after meals, with water.If ingestion is missed or if the food does not contain fat, then taking the drug Alli should be skipped.

    Within a day, you can take no more than three capsules of the drug.

    The drug should be taken only at recommended doses.

    Treatment is recommended not more than 6 months. It is recommended to discuss the results of weight loss with a doctor. If, after 12 weeks of using the Alli drug, there is no decrease in body weight (ie, a decrease in body weight is less than 5% from the initial), it is necessary to consult a doctor to decide whether to continue taking the drug.

    Side effects:
    Undesirable reactions when taking the drug are usually observed from the side of the gastrointestinal tract and are caused by the pharmacological action of the drug. The frequency of undesirable reactions is determined as follows: very often (≥ 1/10); often (≥ 1/100, but <1/10); infrequently (≥ 1/1000, but <1/100); rarely (≥ 1/10000, but <1/1000) and very rarely (<1/10000), including individual messages.

    Below is the frequency of reactions from various organs and systems.

    Clinical studies of orlistat in a dose of 60 mg for a period of 18 to 24 months revealed unwanted reactions from the gastrointestinal tract, which were generally light and reversible.Usually they were manifested at the beginning of treatment. Compliance with a diet low in fat reduces the likelihood of such reactions.

    From the gastrointestinal tract were observed: very often - oily discharge from the rectum, the passage of gases with a certain amount of detachable, imperative urges for defecation, steatorrhea; often - abdominal pain, fecal incontinence, loose stool, frequent bowel movements.

    As a rule, these adverse reactions are mild and transient. They occur in the early stages of treatment (in the first 3 months), and in most patients there was not more than one episode of such reactions.

    Postmarketing research

    During the postmarketing application of orlistat, the following undesirable reactions were noted, the frequency of which is unknown:

    The circulatory system: a decrease in the level of prothrombin and an increase in the international standardized ratio (INR) in patients taking orlistag together with indirect anticoagulants.

    Gastrointestinal tract: mild rectal bleeding, diverticulitis.

    Skin and subcutaneous tissue: bullous rash.

    The immune system: hypersensitivity reactions, including itching, rash, hives, angioedema, bronchospasm and anaphylaxis.

    Liver and biliary excretion withsystem: cholelithiasis, hepatitis, an increase in the level of hepatic transaminases and alkaline phosphatase.
    Overdose:

    When using orlistat 800 mg once and at a dose of up to 400 mg three times a day daily for 15 days both in individuals with normal body weight and in obese patients, no significant adverse effects have been identified. When using orlistat 240 mg three times a day for 6 months, the increase in the frequency of dose-dependent side effects was not noted.

    In most reports of overdoses of orlistat in the postmarketing period, indications of unwanted reactions are either absent or they are similar to those that can be after receiving the recommended doses of the drug.

    In case of an overdose, consult a doctor. If a significant overdose of orlistat is recommended, follow the patient for 24 hours. Based on the data of the study in humans and animals, any general reactions of the body due to inhibition of lipase are, as a rule, quickly reversible.

    Interaction:

    Cyclosporin. Several studies of the drug interaction of cyclosporin, when used simultaneously with orlistat, report a decrease in the plasma cyclosporine concentration. Potentially, this can lead to a decrease in the immunosuppressive effectiveness of the latter. The simultaneous use of orlistat and cyclosporine is contraindicated.

    Indirect anticoagulants. With the simultaneous use of warfarin or other oral anticoagulants with orlistat may change the value of INR.

    Fat-soluble vitamins. Orlistat may potentially impair the absorption of fat-soluble vitamins (A, D, E and K).

    Acarbose. Due to the lack of data on pharmacokinetic interactions, it is not recommended to use orlistat together with acarbose.

    Amiodarone. At simultaneous application with orlistatom there was a decrease in the level of amiodarone in the plasma after a single dose. The clinical significance of this effect for patients taking amiodarone, is unclear. Simultaneous use of orlistat and amiodarone is possible only on the advice of a doctor.

    Lack of interaction. Orlistat does not interact with amitriptyline, phenytoin, fluoxetine, sibutramine, phentermine; atorvastatin, pravastatin, fibrates; biguanides; digoxin, nifedipine, losartan; alcohol.
    Special instructions:

    Diet and exercise are an integral part of the program to reduce body weight. It is recommended to begin to follow the diet and exercise before starting orlistat.

    Taking orlistat, it is necessary to adhere to a fractional balanced, moderately hypocaloric diet, with a fat content of not more than 30% of the daily caloric intake (for example, with a diet of 2000 kcal /not more than 66 g / day). Patients should adhere to the recommendations received on diet and physical activity both during and after discontinuation of the drug.

    The use of orlistat leads to an increase in the amount of fats in the stool after 24-48 hours after the start of the admission. After discontinuation of the use of the drug, the fat content in the feces usually returns to the initial for 48-72 hours. The likelihood of side effects from the gastrointestinal tract increases when taking orlistat with food,containing a large amount of fat.

    The intake of orlistat can potentially impair the absorption of fat-soluble vitamins (A, D, E and K, betacarotene). The overwhelming majority of patients who received orlistat in the course of four-year clinical trials, concentrations vitamins A, D, E and K, betacarotene were within the normal range. With the preventive purpose, it is recommended to take multivitamins at night.

    Since weight loss is usually accompanied by an improvement in carbohydrate metabolism, patients with type 2 diabetes mellitus should first consult with a physician before starting to take orlistat, in order to adjust the dose of hypoglycemic drugs if necessary. Decreased body weight during treatment can be accompanied by a decrease in blood pressure and cholesterol. Patients taking drugs for the treatment of hypertension or hypercholesterolemia should consult a physician to adjust the doses of the above drugs if necessary.

    In clinical studies, there was no interaction between oral contraceptives and orthostat. But, orlistat can indirectly reduce the bioavailability of oral contraceptives, which can lead to the development of unwanted pregnancies. It is recommended to use additional methods of contraception in case of development of acute diarrhea.

    Patients suffering from kidney disease should consult with a doctor, as possible the development of hyperoxaluria and nephropathy. Patients receiving amiodarone, warfarin or other oral anticoagulants, also need to be consulted by a physician before proceeding with orlistat treatment, since changes in the INR indicator are possible.

    Patients should stop taking orlistat and consult a doctor if symptoms such as icteric staining of the sclera or skin, itching, darkening of the urine and loss of appetite occur.

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

    Orlistat does not affect the ability to drive a car, other modes of transport and use mechanisms.

    Form release / dosage:

    Capsules of 60 mg.

    Packaging:

    For 21, 42 and 84 capsules in a wide-necked can of white color from high-density polyethylene, with a moisture absorber (silica gel).Banks are sealed with polypropylene lids with a child protection system and sealed with a foil liner. Caps are equipped with a mechanism that allows you to open the bottle only when you simultaneously press and rotate the lid.

    1 can of 21, 42 or 84 capsules together with instructions for use and a plastic case for 3 capsules; packed in a cardboard box.

    Storage conditions:

    Store at a temperature not exceeding 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years. Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:Without recipe
    Registration number:LSR-006089/10
    Date of registration:29.06.2010
    Expiration Date:Unlimited
    The owner of the registration certificate: Glaxo Group, Limited Glaxo Group, Limited United Kingdom
    Manufacturer: & nbsp
    Representation: & nbspGlaxoSmithKline Helsker GlaxoSmithKline Helsker United Kingdom
    Information update date: & nbsp10.07.2017
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