Active substanceOrlistatOrlistat
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  • Dosage form: & nbsptoapsules
    Composition:

    Per one capsule:

    Active substance: orlistat substance-pellets 50% - 120,00 mg, in terms of orlistat - 60,00 mg.

    Auxiliary substances of substance-pellets: cellulose microcrystalline - 49.32 mg, sodium carboxymethyl starch - 5.04 mg, sodium lauryl sulfate - 3.12 mg, povidone-K30 - 2.52 mg.

    Capsule body composition: indigocarmine - 0,017%, iron dye oxide yellow - 0,25%, titanium dioxide - 2,0%, gelatin - up to 100%.

    Composition of cap capsule: indigokarmin - 0.0312%, titanium dioxide - 4.0%, gelatin - up to 100%.

    Description:

    Hard gelatin capsules number 2. The capsule body is light green, the lid is light blue, opaque.

    The contents of the capsules are white or almost white pellets.

    Pharmacotherapeutic group:Lipase GIT inhibitor
    ATX: & nbsp

    A.08.A.B.01   Orlistat

    Pharmacodynamics:

    Orlistat is a potent, specific 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. Undisintegrated triglycerides are not absorbed, and therefore the intake of calories in 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. Increases the concentration of fat in the contents of the intestine 24-48 hours after ingestion. After the drug is withdrawn, the fat content in the intestinal contents after 48-72 hours usually returns to the level that occurred before the start of therapy.

    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: Ml (four-membered hydrolyzed lactone ring) and M3 (M1 with a split residue N-formylleucine). 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 approximately 97% of the dose taken, 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 intestine and kidneys) is 3-5 days. The ratio of pathways for orlistat in individuals with normal body weight and obesity was similar.

    Indications:

    Reduction of excess body weight (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 of the components of the drug;

    - syndrome of chronic malabsorption;

    - cholestasis;

    - concomitant therapy with indirect anticoagulants (warfarin) or other oral anticoagulants;

    - concomitant therapy with cyclosporine;

    - simultaneous application with sitagliptin;

    - period of pregnancy and breastfeeding;

    - children's age till 18 years.

    Pregnancy and lactation:

    Clinical data on the use of orlistat during pregnancy are absent, the use of the drug Orlixen 60 during pregnancy is contraindicated.

    Due to the fact that there are no data on the penetration of orlistat into breast milk, the use of Orlixen 60 during the period of breastfeeding is contraindicated.

    Dosing and Administration:

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

    Within 24 hours you can take no more than three capsules of 60 mg of the drug Orlixen 60. The course of treatment should not exceed 6 months.

    Efficacy and safety of orlistat in patients with impaired liver and / or kidney function, as well as in elderly patients was not investigated, however, given that orlistat absorption is minimal, dose adjustment in the elderly and in persons with impaired liver and / or kidney function is not required.

    Side effects:

    Adverse events were noted when taking orlistat mainly from the gastrointestinal tract and were driven by higher amounts of fat in the feces. With prolonged therapy with orlistat, the incidence of adverse events decreases.

    The following side effects are given in accordance with the following gradations of their occurrence frequency: Often (≥ 1/10); often (≥ 1/100, < 1/10); infrequently (≥1/1000 ,<1/100); rarely (≥1/10000, <1/1000); rarely (<1/10000); frequency unknown - according to available data to establish the frequency of occurrence is not possible.

    Disorders from the gastrointestinal tract: Often - oily discharges from the rectum, the passage of gases with a certain amount of detachable, imperative desires for defecation, steatorrhea; often - abdominal pain, fecal incontinence, loose stool, frequent bowel movements.

    Disorders of the psyche: often - sense of anxiety.

    Postmarketing observations

    Violations of the blood and lymphatic system: frequency unknown - a decrease in prothrombin, an increase in INR (the international normalized ratio). These side effects were observed with the simultaneous use of orlistat and anticoagulants.

    Disorders from the gastrointestinal tract: frequency unknown - minor bleeding from the rectum, diverticulitis, pancreatitis.

    Disturbances from the liver and bile ducts: frequency unknown - increased activity of "liver" transaminases, alkaline phosphatase, hepatitis, cholelithiasis.

    Disorders from the kidneys and urinary tract: hyperoxalaturia; oxalate nephropathy, which can sometimes lead to the development of renal failure.

    Disturbances from the skin and subcutaneous tissues: frequency unknown - bullous rash.

    Immune system disorders: frequency unknown - skin 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 have experience with 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 overdose with orlistat, either the absence of undesirable events was reported, or the undesirable events did not differ from those 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, and therefore it is necessary to monitor the content of cyclosporine in the blood plasma. The simultaneous use of orlistat and cyclosporine is contraindicated.

    With the simultaneous use of orlistat with amiodarone, there was a decrease in the concentration of amiodarone in the blood plasma 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 prothrombin concentration and an increase in INR may occur, which leads to a change in the haemostatic parameters. The simultaneous use of orlixen 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 diarrhea, the use of an additional method of contraception is recommended.

    When taking concomitantly with levothyroxine sodium, due to a decrease in absorption inorganic iodine and / or levothyroxine sodium, hypothyroidism and / or decreased 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 and ethanol.

    There have been cases of a decrease in the effectiveness of antiretroviral drugs for the treatment of HIV (human immunodeficiency virus), antidepressants and antipsychotics (including lithium preparations) that coincide with the onset of orlistat in previously compensated patients.

    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 use of Orlixen 60 should be discontinued if, after 12 weeks of therapy, body weight decreased by less than 5% compared to the initial body weight.

    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 an improvement in metabolic control in patients with diabetes mellitus, those who receive hypoglycemic drugs should consult their physician before starting to use Orlixen 60 and, if necessary, adjust the dose hypoglycemic agents.

    Decreased body weight may be accompanied by an improvement in blood pressure and a decrease in cholesterol concentration. Patients taking medications for hypertension or hypercholesterolemia should be consulted with a doctor when using Orlixen 60 and, if necessary, correct the dose of these drugs.

    When orlistat was used, cases of rectal bleeding were observed. If severe and / or persistent bleeding symptoms occur, additional testing is necessary.

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

    If symptoms such as weakness, fatigue, fever, jaundice and darkening of the urine occur, you should consult your doctor to rule out liver damage.

    When Orlistat was used, rare cases of development of hypothyroidism and / or violation of its control were noted. The mechanism of development of this phenomenon is unknown, but it can be caused by a decrease in absorption of iodized salt and / or levothyroxine sodium.

    Orlistat has the potential to reduce the absorption of antiretroviral drugs to treat HIV and to reduce the effectiveness of antiretroviral therapy. Before starting orlistat therapy, you should carefully evaluate the benefit / risk ratio in such patients.

    When using orlistat, the development of oxalate nephropathy is possible, which can sometimes lead to the development of renal failure. An increased risk is noted in patients with chronic renal failure and / or dehydration.

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

    There was no any negative influence of the orlisken on the ability to drive vehicles and mechanisms.

    Form release / dosage:

    Capsules, 60 mg.

    Packaging:

    For 5 or 10 capsules in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

    10, 20, 30, 40, 50, 100 or 120 capsules into cans of polyethylene terephthalate for medicinal products sealed with caps screwed on with the first opening or by a "push-turn" system of polypropylene or polyethylene or polypropylene cans for medicines,sealed with caps tightened with the control of the first opening of polyethylene or cans of polypropylene for medicinal products sealed with lids pulled with the control of the first opening of high pressure polyethylene.

    One bank or 1, 2, 3, 4, 5, 6, 8, 9, 10 or 16 contour mesh packages together with the instruction for use are placed in a cardboard package.

    It is allowed to bundle 2 or 3 cardboard packages (packs) into a group package (shipping container) from cardboard for consumer packaging.

    Storage conditions:

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

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:Without recipe
    Registration number:LP-003800
    Date of registration:19.08.2016
    Expiration Date:19.08.2021
    The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia
    Manufacturer: & nbsp
    Representation: & nbspOZONE LLC OZONE LLC Russia
    Information update date: & nbsp11.06.2017
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