Active substanceFlutamideFlutamide
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  • Dosage form: & nbspfilm coated tablets
    Composition:

    1 tablet coated film contains:

    active substance:

    flutamide 250 mg

    Excipients: cellulose microcrystalline 140 mg, lactose monohydrate 250 mg, sodium croscarmellose 17 mg, magnesium stearate 2 mg, silicon dioxide colloidal 1 mg.

    Composition of the film shell:

    hypromellose (hydroxypropylmethylcellulose) 2910 - 9 mg, giprolase (hydroxypropylcellulose) 400 CPS - 5 mg, macrogol (polyethylene glycol) 3350 - 2 mg, titanium dioxide (E 171) - 5.94 mg, aluminum lacquer based on the dye Honolin yellow (E 104) 0.06 mg, carnauba wax 0.033 mg

    Description:

    Round biconvex tablets, film-coated lightlol-yellow color. On one side engraving made inscriptions "FLUT" and "250", separated by a horizontal line, on the other side of the engraving: "NU" or "APO", or "PRO".

    Pharmacotherapeutic group:Antitumor agent, antiandrogen.
    ATX: & nbsp

    L.02.B.B.01   Flutamide

    Pharmacodynamics:

    Flutamide is a non-steroidal antiandrogenic antitumor drug. Competitively blocks the interaction of androgens with their cellular receptors. The mechanism of action is based on inhibition of androgen uptake and / or inhibition of androgen binding in target cell nuclei. Its ability to inhibit the action of testosterone at the cellular level is in addition to the drug "castration" caused by gonadotropin-releasing hormone (GnRH) agonists. The target organ of the pharmacological action of flutamide is the prostate gland and seminal vesicles. Flutamide does not possess estrogenic, antiestrogenic, progestagenic and anti-gestagenic activity.


    Pharmacokinetics:The drug is completely and rapidly absorbed after ingestion, undergoing biotransformation in the liver.The main metabolite found in blood plasma, the maximum concentration of which is reached after 2 hours, is a biologically active a-hydroxylated derivative (2-hydroxyflutamide). 94-96% flutamide and 92-94% a-hydroxylated metabolite binds to proteins. From the body, the drug is excreted mainly by the kidneys, about 4.2% is secreted through the intestine within 72 hours. The half-life of the active metabolite from the plasma is about 6 hours (in elderly patients - 8 hours after a single dose and 9.6 hours at a stable concentration). After taking flutamide intravenously, 250 mg 3 times a day, a stable concentration levelof the drug and its active metabolite in plasma is achieved after a fourth dose of the drug.
    Indications:
    Treatment of metastatic prostate cancer when suppression of testosterone is indicated:
    • at the beginning of treatment in combination with GnRH agonists;
    • as an additional treatment for patients already receiving therapy with GnRH agonists;
    • in patients with surgical castration;
    • treatment of patients in whom other types of hormone therapy were ineffective or when intolerance of suchtreatment.

    Contraindications:

    - Hypersensitivity to flutamide or to any other component of the drug.

    - Pronounced hepatic understatics.

    - Childhood (safety and efficacy not established).

    Carefully:

    in patients with decreased liver function, with susceptibility to thrombosis and withof cardiovascular diseases, and also in conditions, predisposinganiline intoxication (one of the metabolites of flutamide -methylaniline derivative): deficiency of glucose-6-phosphate dehydrogenase, smoking, hemoglobinopathy (M-hemoglobin).

    Dosing and Administration:

    Inside for 250 mg 3 times a day eachthe last 8 hours. If applies until the appearance of signs progression of tumor disease.

    In the case of combined therapy with GnRH agonists, both drugs may be assigned at the same time or reception flutamide begin three days before the first admission of agonist GnRH.

    Side effects:

    Frequency of development of side effects is stated in accordance with the followinggradation: most often (10 % and higher), less often (from 1 to 10%), rarely (less than 1%).

    When the drug is used in monotherapy

    Most often: gynecomastia and / or pain in the mammary gland, sometimes followed by galactorrhea. These phenomena disappear after abolition of ledose reduction.

    Less often: diarrhea, nausea, vomiting, increased appetite, insomnia, increased fatigue, transient liver dysfunction.

    Rarely: hepatitis or jaundice (including cholestatic), liver necrosis, hepatic encephalopathy, increased transaminase activity (these side effects are usually reversible after discontinuation of therapy, but there have been reports of fatal outcomes due to severe hepatic insufficiency with flutamide therapy); subcutaneous hemorrhages, shingles, skin itching, lupus-like syndrome; anorexia, heartburn, constipation, diarrhea; decreased libido, headache, hot flashes (fever, sweating), increased blood pressure, dizziness, weakness, visual acuity, thirst, chest pain, swelling (fingers, feet, shins), anxiety , depression and thrombocytopenia. With prolonged treatment, suppression of spermatogenesis was noted.Some cases of development of hemolytic anemia, macrocytic anemia, methemoglobinemia, reaction of increased photosensitivity (including erythema, ulceration of the skin, bullous rash, epidermal necrolysis) have been noted. Sometimes, patients experience a change in the color of urine from amber to yellow-green.

    When treated in combination with GnRH agonists

    Most often: "hot flashes" (fever, increased sweating), decreased libido, impotence, diarrhea, nausea, vomiting. The incidence of these side effects, with the exception of diarrhea (more pronounced when used in conjunction with flutamins - home), is the same as in monotherapy with agonists G nRG.

    Less often: gynecomastia, anemia, leukopenia, thrombocytopenia, lack of appetite, swelling, symptoms of neuromuscular disorders, difficulty urinating, increased blood pressure and side effects from the central nervous system (drowsiness, depressionthis, confusion, anxiety, neurosis).

    Rarely: impaired respiration, hepaticinsufficiency, hepatitis, cholestattic jaundice, liver necrosis, hepatic encephalopathy, increasedphotosensitivity, methemoglobinemia.

    Overdose:
    In case of an overdose, if the patient is conscious and without spontaneous vomiting, vomiting should be induced. It is necessary to use symptomatic therapy with constant monitoring of the patient and vital functions.

    Interaction:
    In view of the possible increase in anticoagulant action with simultaneous use of indirect anticoagulants and flutamide, the dose of anticoagulant should be selected under the control of prothrombin time.

    Special instructions:
    Treatment with flutamide should be performed under the control of hepatic enzyme activity in blood serum (once a month for the first 4 months and then regularly).
    If the activity of hepatic enzymes is increased 2-3 times in comparison with the upper limit of normal values ​​and / or the appearance of jaundice in the absence of metastases in the liver, the use of flutamide should be discontinued. Patients should receive a recommendation to consult a doctor immediately when the first symptoms of liver dysfunction occur, such as pruritus, darkening of the urine, nausea, vomiting, persistent loss of appetite, jaundice of the skin or sclera, pain in the right hypochondrium or influenza-like symptoms.

    Form release / dosage:
    The tablets covered with a cover on 250 mg.
    Packaging:
    For 10,20,30,50,84, 90, 100 and 500 tablets in bottles made of high pressure polyethylene, sealed with lids.
    1 bottle with instructions for use in cardboard pack
    Storage conditions:
    In a dry, the dark place at a temperature of 15 to 30 ° C. Keep out of the reach of children. List B.

    Shelf life:
    3 years.
    The drug should not be used after the expiry date indicated on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:P N014283 / 01
    Date of registration:16.01.2008
    The owner of the registration certificate:New Farm Inc.New Farm Inc.
    Information update date: & nbsp23.10.2015
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