Treatment of locally advanced or metastatic prostate cancer as a means of monotherapy (with or without orchiectomy) or in combination with luteinizing hormone releasing hormone (lgrg) agonists in patients who have not previously been prescribed any treatment, or treatment of patients who do not respond or who have developed resistance to or intolerance to hormone therapy in order to achieve maximum androgen blockade. In combination therapy – as one of the means for the treatment of locally limited prostate cancer B2-C2 (T2B-T4), to reduce the volume of the tumor, strengthen control over the tumor and increase the period between exacerbations of the disease.
Flutafarm (flutamide) Composition
active substance: flutamide;
1 tablet contains flutamide in terms of 100% substance – 250 mg (0.25 g);
excipients: potato starch, lactose, colloidal silicon dioxide, calcium stearate.
Flutafarm (flutamide) Dosage form
Basic physical and chemical properties: tablets of light yellow color, with a flat surface, scored and beveled.
Flutafarm (flutamide) Pharmacotherapeutic group
Hormone antagonists and similar agents. Antiandrogenic agents. ATX code L02B B01.
Flutapharm is an antiandrogenic drug with a non-steroidal structure. Flutamide and its metabolites do not have agonistic or antagonistic properties at the glucocorticoid, estrogen, progestin, and mineralocorticoid receptors.
Flutamide blocks the androgen receptors of target cells in the prostate, hypothalamus and pituitary gland and inhibits the biological effects of endogenous androgens. However, flutamide does not inhibit the effect on androgen-mediated secretion of gonadotropin-releasing hormone (GTRH) by the hypothalamus or does not affect the sensitivity of the pituitary gland to GTRH. This leads to an increase in the content of gonadotropic hormones (luteinizing and follicle-stimulating), as a result of which testosterone hyperproduction is stimulated.
Flutamide and its metabolites inhibit the interaction of dihydrotestosterone with nuclear androgen receptors. Receptor blockade can also occur at the level of the cell membrane and the cytoplasm of the cell. The main metabolite is 2-hydroxyflutamide. Its affinity with androgen receptors is 25 times higher than in flutamide, which allows it to be considered as the active form of flutamide.
The combination of flutamide with chemical or surgical castration results in the testicular and adrenal effects of androgens.
In women with hyperandrogenic conditions, accompanied by infertility and disorders of the ovarian-menstrual cycle (for example, scleropolycystic ovary syndrome), Flutapharm blocks the pathogenic effect of endogenous androgens on the ovaries and other reproductive organs, as well as on the hypothalamic-pituitary system. Due to this, the symptoms of hyperandrogenism (hirsutism) are weakened in patients, menstruation is restored, folliculogenesis and the menstrual cycle are improved, which probably leads to the restoration of reproductive potential in some patients.
After taking Flutapharm, it is well absorbed from the gastrointestinal tract. The maximum concentration in blood plasma is reached within 2 hours. Experiments with the use of tritiated flutamide indicate its rapid metabolism in the biologically active form – 2-hydroxyflutamide and in other metabolites. The half-life of the drug is 5-6 hours. There are approximately 10 metabolites of flutamide. More than 90% of flutamide and 2-hydroxyflutamide binds to blood plasma proteins. It is excreted mainly by the kidneys. Approximately 4% of the dose taken is excreted in the feces.
Treatment of locally or metastatic prostate cancer as monotherapy (with or without orchiectomy) or in combination with luteinizing hormone releasing hormone (LHRH) agonists in patients who have not previously received any treatment or treatment in patients who do not respond or who have developed resistance to hormone therapy or its intolerance in order to achieve maximum androgenic blockade.
In combination therapy – as one of the means for the treatment of locally limited prostate cancer B2 – C2 (T2b – T4), to reduce tumor volume, enhance tumor control and increase the period between exacerbations of the disease.
Treatment of women with functional hyperandrogenism, which is accompanied by disorders of the ovarian-menstrual cycle, hirsutism, scleropolycystic ovary syndrome and infertility.
Hypersensitivity to flutamide or other components of the drug. For women, additional contraindications for taking Flutapharm are organic hyperandrogenism (tumors of the ovaries and adrenal cortex). Severe hepatic impairment (baseline liver enzymes should be assessed before starting treatment).