Flutamide

Pharmacological properties

Flutapharm femin is a non-steroidal drug with antiandrogenic action.

In women with hyperandrogenic conditions accompanied by infertility and disorders of the ovarian-menstrual cycle (for example, scleropolycystic ovary syndrome), Flutapharm Femina 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 severity of symptoms of hyperandrogenism (hirsutism) decreases, menstruation resumes, folliculogenesis and the menstrual cycle improve, which probably leads to the restoration of fertility in some patients.

Pharmacokinetics Flutamide is well absorbed in the digestive tract. C_max in the blood is observed 2 hours after oral administration. It is rapidly metabolized to form the active metabolite of 2-hydroxyflutamide and other substances. T_½ the active metabolite is 5–6 hours. It is eliminated mainly with urine. In 2 days, 91% is excreted from the body, in 3 days - 98% of the administered dose.

Indications

Treatment of women with functional hyperandrogenism, which is accompanied by violations of the ovarian-menstrual cycle, hirsutism, scleropolic cystic ovary syndrome and infertility.

Application

For women with hyperandrogenic conditions, Flutapharm femin should be administered orally by 1 tablet (125 mg) 3 times a day for 3–6 months. take during or after meals. mandatory is the use of non-hormonal contraceptives, in particular barrier.

Children. The drug should not be used to treat children.

Contraindications

Hypersensitivity to flutamide or other components of the drug. hyperandrogenism of organic origin (tumors of the ovaries and adrenal cortex). severe liver failure (baseline liver enzymes should be assessed before treatment).

Side effects

The following adverse reactions were observed with the use of the drug in men.

With monotherapy

Reproductive system: gynecomastia and / or pain in the area of ​​the mammary glands, sometimes accompanied by galactorrhea. These reactions disappear after discontinuation of treatment or a reduction in the dose of the drug. The incidence of gynecomastia is significantly reduced with the simultaneous use of LHRH agonists. Decreased libido, decreased sperm count.

Infections and infestations: herpes zoster.

Blood and lymphatic system: edema, ecchymosis, lymphostasis.

Immune system: lupus-like syndrome.

Mental disorders: depression, anxiety, embarrassment, anxiety.

Nervous system: insomnia, headache, dizziness.

Organ of vision: blurred vision.

Respiratory system: dyspnea, cough.

Alimentary tract: diarrhea, nausea, vomiting, increased appetite, gastrointestinal tract dysfunction, stomach pain, ulcerative pain, heartburn, constipation, anorexia, thirst.

Hepatobiliary system: increased activity of liver enzymes, transient disorders of liver function, jaundice, hepatitis.

Skin and subcutaneous tissue: itching, rash.

Common disorders: fatigue, malaise, weakness, fever, chest pain.

Disorders from the cardiovascular system occur much less frequently compared with the use of diethylstilbestrol.

special instructions

Patients should be under constant medical supervision. special attention should be paid to the effect of the drug on liver function.

Treatment with the drug should not be started if the levels of hepatic transaminases in blood plasma are 2-3 times higher than the upper limit of normal. Monitoring liver function should be carried out during the entire period of treatment with the drug.Plasma transaminases should be determined prior to the initiation of flutamide therapy, monthly for the first 4 months of taking the drug, periodically thereafter and with the first symptoms of liver dysfunction (for example, itching, dark urine, nausea, vomiting, fatigue, anorexia, jaundice, pain right hypochondrium or incomprehensible flu-like symptoms). When jaundice occurs or an increase in liver transaminase activity is 2–3 times higher than normal (in the absence of liver metastases confirmed by biopsy), flutamide should be stopped immediately and liver function carefully monitored until the situation is clarified.

Patients should immediately consult a doctor if the first symptoms of liver function impairment appear, such as skin itching, dark urine, nausea, vomiting, persistent anorexia, yellowing of the sclera and skin, soreness in the right hypochondrium and flu-like symptoms.

Liver lesions are usually reversible after discontinuation of therapy, and in some patients even after a dose reduction.

Flutamide is excreted mainly by the kidneys, so dose adjustment in patients with renal failure may be required.

Since plasma levels of testosterone and estradiol increase during flutamide treatment, fluid retention in body tissues is possible. Therefore, flutamide should be used with caution in patients with heart disease. In addition, increasing estradiol levels may increase the risk of thromboembolism.

Patients with latent or actual glucose-6-phosphate deficiency may develop methemoglobinemia. In the case of cyanosis, methemoglobinemia, a possible factor for overdosing should be considered.

Flutamide contains lactose, so patients with rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome should not use the drug.

Before using the drug Flutapharm Femina, women need to exclude hyperandrogenism of organic origin (tumors of the ovaries and adrenal cortex).

During treatment should not drink alcohol.

Use during pregnancy and lactation. When using the drug, women should pay special attention to the prevention of pregnancy with the help of non-hormonal, in particular barrier, contraceptives. In case of a positive pregnancy test result, the drug should be stopped immediately. Sexual relations for the purpose of having a desired pregnancy can be resumed no earlier than 48 hours after the last administration of Flutapharm Femina.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. Until the patients individual reaction to the drug is clarified, one should refrain from driving vehicles or other mechanisms, given that during treatment with flutamide increased fatigue, sometimes dizziness, drowsiness, and visual disturbances were observed.

Interactions

In patients receiving long-term warfarin, an increase in prothrombin time is noted after initiation of monotherapy with flutamide. therefore, with the combined use of the drug Flutapharm femin and warfarin, careful monitoring of prothrombin time and, possibly, dose adjustment of the anticoagulant are necessary.

Flutamide can slow down the metabolism of corticosteroids.

The combined use of flutamide with potentially hepatotoxic drugs should be avoided.

When using flutamide simultaneously with theophylline, an increase in theophylline concentration in blood plasma is possible.

Excessive alcohol consumption during flutamide treatment should be avoided.

Overdose

A single dose of flutamide, which would cause overdose symptoms or be life threatening, has not been established.

In case of an overdose, dialysis is ineffective, given the high degree of binding of flutamide to plasma proteins.

As with the treatment of an overdose of any drug, the possibility of simultaneous administration of several drugs should be considered. In case of overdose, if there is no spontaneous vomiting, vomiting should be induced. Gastric lavage may be required.

Standard supportive measures are shown with constant monitoring of the patient and vital functions.

Storage conditions

In the original packaging at a temperature not exceeding 25 ° c.