Active substanceFlutamideFlutamide
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  • Dosage form: & nbsppills
    Composition:

    1 tablet contains:

    active substance: 6lutamide 250 mg.

    excipients: lactose monohydrate * 221.7 mg, sodium lauryl sulfate 15.0 mg, cellulose microcrystalline * 100.0 mg, starch corn 162.5 mg, silicon dioxide colloid 0.4 mg, magnesium stearate 0.4 mg.

    * Lactose monohydrate and part of cellulose microcrystalline is used in the form mixture of Microcloan 100 containing lactose monohydrate (Hebrew F.) 75% and cellulose microcrystalline (Hebrew F.) 25%.

    Description:Round double-convex pills of light yellow color with a risk on one side.
    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 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:
    Flutamide when ingested quickly and completely absorbed from the gastrointestinal tract, undergoing biotransformation in the liver. Metabdliziruetsya with the formation of the main biologically active metabolite - a-hydroxylated derivative flutamide (2-oxyflutamide), the maximum concentration of which is 2 hours and is detected within 8 hours after taking the drug. 94-96% flutamide and 92-94% a-hydroxyflutamide bind to plasma proteins.The half-life of a-hydroxyflutamide is 6 hours (in elderly patients - 8 hours).
    It is mainly excreted by the kidneys - 46%, through the intestine - 4.2% within 72 hours.
    After repeated administration of flutamide inside 250 mg 3 times a day, the equilibrium concentration of the drug and its active metabolite in the blood serum is reached after the fourth dose of the drug.

    Indications:
    Treatment of metastatic prostate cancer when suppression of testosterone is indicated:
    -in the beginning of treatment in combination with gonadotropin-releasing hormone agonists;
    - as an additional 'treatment for patients already receiving gonadotropin-releasing hormone agonists;
    patients with surgical castration;
    - Treatment of patients in whom other types of hormone therapy were ineffective or with intolerance of such treatment.

    Contraindications:
    Hypersensitivity to flutamide or any other component of the drug;
    severe hepatic impairment;
    children's age (safety and efficacy not established).

    Carefully:the drug should be used in patients with moderate hepatic insufficiency, renal failure,cardiovascular diseases, in patients with a tendency to thrombosis, in conditions predisposing to intoxication aniline (one of the metabolites flutamide - methylalanyl derivative): deficiency of glucose-6-phosphate dehydrogenase, smoking, hemoglobinopathy (M-hemoglobin), congenital lactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome (because the tablet contains lactose).

    Pregnancy and lactation:
    Flutamide Sandoz® is not suitable for use in women.

    Dosing and Administration:
    Tablets are taken preferably after eating, not liquid, with a small amount of liquid.
    Inside, 250 mg every 8 hours (1 tablet 3 times a day). In case of achieving a positive effect, the drug is used until signs of progression of the tumor develop.
    In the case of combined therapy with gonadotropin-releasing hormone agonists, both drugs can be administered simultaneously or the drug intake Flutamide Sandoz® begins 3 days before the first admission of a gonadotropin-releasing hormone agonist.

    Side effects:
    According to the World Health Organization (WHO), unwanted the effects are classified according to the frequency of their development as follows: very often (> 1/10), often (> 1/100 to <1/10), infrequently (> 1/1000 to <1/100), rarely ( from> 1/10000 to <1/1000), very rarely (<1/10000); frequency is unknown - according to available data, it was not possible to establish the frequency of occurrence.
    Application of the drug in monotherapy
    The most common undesirable phenomena
    (gynecomastia and / or pain in the thoracic region glands, sometimes
    accompanied by galactorrhea) disappear when discontinuation or after a reduction in the dose of the drug.
    Infectious and parasitic diseases
    rarely: herpes zoster.
    Benign, malignant and unspecified neoplasms (including cysts and polyps)
    rarely: malignant neoplasm of mammary glands in men.
    Violations of the blood and lymphatic system
    rarely: lymphogenous edema.
    Immune system disorders
    rarely: lupus-like syndrome.
    Disorders from the metabolism and nutrition
    often: increased appetite;
    rarely: lack of appetite (anorexia).
    Disorders of the psyche
    often: insomnia;
    rarely: anxiety, depression.
    Disturbances from the nervous system
    rarely: dizziness, headache.
    Disturbances on the part of the organ of sight
    rarely: blurred vision.
    Heart Disease
    frequency unknown: QT interval elongation.
    Vascular disorders
    rarely: "flushes" of blood to the face (sensation of heat).
    Disorders from the gastrointestinal tract
    often: diarrhea, nausea, vomiting;
    rarely: nonspecific symptoms from the gastrointestinal tract, heartburn, constipation.
    Disturbances from the liver and bile ducts
    often: hepatitis.
    Disturbances from the skin and subcutaneous tissues
    rarely: skin itch, ecchymosis (bleeding in the skin or mucous membranes);
    very rarely: photosensitization reactions;
    frequency unknown: changes in hair.
    Violations of the genitals and mammary gland
    very often: gynecomastia and / or pain in the mammary gland, galactorrhea;
    rarely: decreased libido, reduced production of seminal fluid; frequency is unknown: an increase in the concentration of testosterone in the blood plasma (in the initial period of therapy).
    General disorders and disorders at the site of administration
    often: feeling tired;
    rarely: swelling, general weakness, malaise, thirst, chest pain.
    Impact on the results of laboratory and instrumental studies
    often: transient violations of the liver.
    Cases of development of malignant neoplasms of the mammary gland in men receiving flutamide therapy have been reported. In one case, the development of malignant neoplasm was noted against the background of pre-existing nodular formation in the mammary gland, revealed 3-4 months before the start of flutamide therapy in a patient with benign prostatic hypertrophy. After the removal and histological examination, a low-differentiated ductal adenocarcinoma was identified. Another report describes the development of gynecomastia two months after the initiation of flutamide therapy and the development of neoplasm - after 6 months in a patient receiving metastatic prostate cancer therapy. After 9 months from the start of therapy, the formation was removed, with histological the study revealed a low-grade ductal adenocarcinoma, T4N0M0 G3.
    The use in combination with analogues of the hormone-releasing hormone (GnRH)
    The most common side effects that develop against a background of combined therapy with flutamide and agonists of GnRH are "hot flashes", decreased libido, impotence, diarrhea, nausea and vomiting. With the exception of diarrhea, all these effects occur with a similar frequency with monotherapy with HGH agonists.
    The incidence of gynecomastia compared with monotherapy with flutamide is significantly reduced when combined therapy is used. In clinical studies, there was no significant difference between the incidence of this undesirable effect with the use of hormone agonists in combination with flutamide and placebo. Violations of the blood and lymphatic system
    rarely: anemia, leukopenia, thrombocytopenia;
    very rarely: hemolytic anemia, macrocytic anemia, methemoglobinemia, sulfogemoglobinemia.
    Disorders from the metabolism and nutrition
    rarely: lack of appetite (anorexia);
    highly rarely: hyperglycemia, aggravation of the severity of the course of diabetes mellitus.
    Disorders of the psyche
    rarely: anxiety, depression.
    Disturbances from the nervous system
    rarely: confusion, nervousness, numbness.
    Heart Disease
    frequency is unknown: extension of the QT interval.
    Vascular disorders
    very often: "tides" of blood to the face (sensation of heat);
    rarely: hypertension;
    frequency unknown: thromboembolism.
    Disturbances from the respiratory system, chest and mediastinal organs
    very rarely: symptoms from the respiratory system, including shortness of breath, interstitial lung disease.
    Disorders from the gastrointestinal tract
    often: diarrhea, nausea, vomiting;
    rarely: nonspecific symptoms from the gastrointestinal tract.
    Disturbances from the liver and bile ducts
    infrequently: hepatitis;
    rarely: liver failure, jaundice;
    rarely: Cholestatic jaundice, hepatic encephalopathy, necrosis of hepatocytes. fatal outcome, as manifestations of severe hepatic insufficiency on background of hepatotoxic action
    preparation.
    Disturbances from the skin and subcutaneous tissues
    rarely: skin rash;
    highly rarely: photosensitivity reaction, erythema, ulceration of the skin, epidermal necrolysis.
    Disturbances from the musculoskeletal and connective tissue are rare: symptoms of impairmentneuromuscular conductivity
    (numbness, paresthesia, myalgia and / or myasthenia gravis in the hands, hands, feet, legs).
    Disorders from the kidneys and urinary tract
    rarely: pollakiuria, nocturia, incontinence;
    very rarely: change of color of urine to amber or greenish-yellow color.
    Violations of the genitals and mammary gland
    Often: decreased libido, impotence;
    infrequently: gynecomastia;
    rarely: dyspareunia.
    General disorders and disorders at the site of administration
    rarely: swelling, irritation at the injection site.
    Impact on results of laboratory and instrumental studies
    rarely: increase in the concentration of urea and / or creatinine in the blood plasma.
    Also, during the post-test trials of flutamide, adverse effects such as acute renal failure, interstitial nephritis, myocardial ischemia, micro-nodular changes in the mammary gland tissue were reported. To date, it is not possible to estimate the incidence of these unwanted effects.





    Overdose:
    Symptoms: when taken at a dose of 1500 mg / day for 36 weeks, there is gynecomastia, tension in the breast,increased activity of aspartate aminotransferase.
    Treatment: gastric lavage. There is no specific antidote. It is necessary to use symptomatic therapy with constant monitoring of the patient and vital functions. Hemodialysis is ineffective.

    Interaction:
    The interaction between flutamide and leuprorelin is not described, however, when co-prescribing it is necessary to take into account the possible side effects of each of these drugs.
    Prothrombin time (PT) should be carefully monitored in patients receiving oral anticoagulants, due to the possibility of elongation of PV on the background of the use of flutamide. You may need to adjust the dose of anticoagulants.
    With the combined use of flutamide and theophylline, an increase in the concentration of theophylline in the blood plasma is possible, since the latter undergoes primary metabolism with the cytochrome CYP 1A2 isoenzyme responsible for converting flutamide to the active metabolite 2-oxyflutamide. With simultaneous application to other drugs, metabolized in the liver by isozymes of cytochrome P450, it is possible to increase their concentration in blood plasma.
    On the background of flutamide therapy, drugs that have a hepatotoxic effect should be prescribed only in cases where the potential benefit exceeds the possible risk of therapy. Due to the known toxic effects of flutamide on the liver and kidneys, alcohol should be avoided during therapy with the drug. When carrying out antiandrogen therapy (androgen blockade), the QT interval can be extended. In this regard, special caution should be exercised when it is necessary to administer drugs that can induce prolongation of the QT interval and / or ventricular torsades de pointes, including antiarrhythmic drugs of class 1 (quinidine, disopyramide), Class III (amiodarone, sotalol, dofetilide, ibutilide), other antiarrhythmic drugs, as well as methadone, moxifloxacin, antipsychotics, etc.




    Special instructions:
    In the event of an initial impairment of liver function, long-term therapy with flutamide should be given only after a thorough assessment of the benefit-risk relationship from the planned therapy. Before the application of the drug should be evaluated liver function. Flutamide should not be prescribed if the activity of "liver" transaminases exceeds the upper limit of the norm by more than 2-3 times. Against the background of flutamide therapy, the development of genototoxicity is possible, including an increase in the activity of "hepatic" transaminases, necrosis of hepatocytes, development of cholestatic jaundice, and hepatic encephalopathy. It is necessary to regularly monitor liver function in patients receiving the drug. The defeat of the liver is usually reversible and resolved with the withdrawal of the drug, however, the development of a lethal outcome due to severe liver damage is possible.
    During the first 4 months of flutamide therapy, the activity of "liver" transaminases should be monitored monthly, then their activity should be monitored regularly, as well as when there are clinical symptoms of liver dysfunction (itching, darkening of the urine, loss of appetite, jaundice, tenderness in the right upper quadrant, the appearance of unexplained glyipopodobnyh symptoms). Patients should receive a recommendation to immediately consult a doctor when the first symptoms of a liver function disorder appear.
    In case of revealing the above listed clinical or laboratory signs of liver damage, jaundice (excluding the presence of histologically confirmed metastatic liver damage), increasing the activity of "liver" transaminases 2-3 times higher than the upper limit of the norm (in the absence of other causes), treatment with flutamide should be discontinued.
    Long-term therapy with flutamide without medical or surgical castration requires regular monitoring of the spermatogram.
    Flutamide is intended for use only in male patients. During treatment with Flutamide Sandoz, you must use reliable methods of contraception.
    Caution should be exercised when flutamide is used in patients with impaired renal function.
    During treatment, it is possible to increase the concentration of estradiol in the blood plasma, which can predispose to the development of thromboembolic complications.
    Against the background of the use of flutamide, an increase in the concentration of testosterone and / or estradiol in the blood plasma can lead to fluid retention in the body. In severe cases, this can lead to an increased risk of developing myocardial ischemia and / or exacerbation of chronic heart failure.Caution should be exercised when flutamide is used in patients with cardiovascular disease.
    Fluttund can promote the development of edema in predisposed patients.
    Against the background of anti-androgen therapy, it is possible to develop an extension of the QT interval. In patients with known prolongation of the QT interval and / or those receiving drugs that are capable of elongating it, the potential benefits and possible risks of therapy should be carefully assessed before administration of flutamide.


    Effect on the ability to drive transp. cf. and fur:
    Because of the likelihood of side effects such as drowsiness, headache and confusion, care should be taken when practicing potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.

    Form release / dosage:Tablets 250 mg
    Packaging:

    By 7, 10, 14, 21 or 28 tablets in blister of aluminum foil and PVC / PVDC film.

    By 1, 2, 3 or 4 blisters to 7 tablets in a cardboard box together with instruction on medical application.

    10 blisters with 10 tablets each cardboard pack together with instruction on medical application.

    For 1, 2, 3, 4 or 6 blisters of 14 tablets per cardboard pack together with instructions for medical use.

    For 1 or 4 blisters of 21 tablets per cardboard pack, along with instructions for medical use.

    For 1, 2 or 3 blisters of 28 tablets per cardboard pack, along with instructions for medical use.

    Storage conditions:
    At a temperature not higher than 25 ° C, out of the reach of children.

    Shelf life:
    5 years.
    Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:PL-000216
    Date of registration:16.02.2011
    The owner of the registration certificate:Sandoz d.Sandoz d. Slovenia
    Manufacturer: & nbsp
    Representation: & nbspSANDOZ SANDOZ Switzerland
    Information update date: & nbsp22.10.2015
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