Index of drugs

Treatment of advanced prostate cancer when inhibition of testosterone is indicated. In combination with luteinizing hormone-releasing hormone (LHRH) agonists in the treatment of limited prostate cancer (stage B2 or T2b) and in the treatment of advanced prostate cancer infiltrating a tumor beyond the glandular capsule (stage C or T3-T4), without metastases or local involvement lymph nodes. It is also used as a supportive medicine in patients previously treated with an LHRH agonist, in patients after orchiectomy and in patients who have responded poorly or have poorly tolerated other types of hormonal treatment.

1 tabl contains 250 mg of flutamide (and 40.2 mg of lactose).

A non-steroidal androgen antagonist. It inhibits uptake of androgens and their binding in the nucleus of target tissue cells. The effect of flutamide on testosterone metabolism at the cell level supplements the chemical castration obtained with the use of an LHRH agonist that inhibits testosterone production by inhibiting the release of luteinizing hormone. After oral administration, flutamide is absorbed quickly and completely from the gastrointestinal tract. It is metabolized quite quickly. The main active metabolite (2-hydroxyflutamide) reaches C_max in plasma within 2 h, and its T_0,5 is about 6 hours (in elderly patients T_0,5 it is prolonged and is 8 hours after a single dose and 9.6 hours at steady state). Flutamide binds plasma proteins in 94-96% and hydroxyflutamide in more than 90%. The drug and its metabolites are mainly excreted in the urine. The action of the drug at the cellular level occurs about 2 hours after administration. In patients with advanced prostate cancer, pain reduction was observed after 2-4 weeks of treatment.

Hypersensitivity to the active substance or to any of the excipients.

Starting treatment with flutamide should be under the control of a specialist. The drug should be used with caution in patients with hepatic insufficiency and a tendency to clot. In patients with liver failure, long-term treatment with flutamide may be recommended only after a careful assessment of the individual benefits of treatment compared with the risk of side effects. Before starting treatment with flutamide, the patient should check serum aminotransferases. Flutamide treatment is not recommended for patients with transaminase levels 2-3 times higher than ULN. Laboratory liver function should be checked periodically. Appropriate laboratory tests should be performed monthly during the first 4 months of treatment and then periodically monitored for liver function. You should also carry out appropriate laboratory tests in the event of first signs of liver dysfunction, such as pruritus, dark urine, persistent lack of appetite, jaundice, pain under the right rib cage, or unexplained flu-like symptoms. Treatment with flutamide should be discontinued or the dose reduced if: liver damage or jaundice documented in laboratory tests, the biopsy did not show metastases to the liver; 2-3 fold increase in aminotransferase levels without clinical symptoms. Patients should be advised that they should stop taking the medicine and seek medical advice immediately after any symptoms of liver toxicity. The flutamide metabolite - 4-nitro-3-fluoro-methylaniline - can exert aniline toxic effects: methaemoglobinaemia, haemolytic anemia and congestive jaundice. These symptoms have been observed in animal studies and in patients with increased sensitivity to aniline, e.g. in persons with G-6-PD deficiency in smokers. Monitoring of methaemoglobin concentration is indicated in these patients. Caution should be exercised when using flutamide in patients with impaired renal function. Determination of the concentration of specific antigen for the prostate (PSA) may be useful for monitoring the patient's response to treatment.In the case of a constant, significant increase in PSA levels during treatment with flutamide and an LHRH agonist, the patient's clinical condition should be assessed. When stating the progression of the neoplastic process at the same time as increasing the PSA concentration, one should consider continuing the treatment with only the LHRH agonist. In patients with circulatory insufficiency, the drug should be used with extreme caution, because it causes water retention in the body. Patients who have a history of QT prolongation or are at increased risk for this disorder, and patients taking concomitant medications that may prolong QT interval, should assess the benefit-risk balance before taking flutamide, taking into account the risk of tachycardia chamber typetorsade de pointes. During prolonged treatment or severe liver damage an increase in serum AST and ALT is observed. In addition, there may be an increase in bilirubin, creatinine, estradiol and serum testosterone. In severe cases, this may lead to an increased risk of angina and heart failure. Therefore, caution should be exercised when using flutamide in the presence of cardiovascular disease. Flutamide may increase swelling and swelling around the ankles in susceptible patients. Increased estradiol levels when using flutamide increases the patient's compliance to thromboembolic events. The product contains lactose - should not be used in patients with rare hereditary problems of galactose intolerance, lactase deficiency (Lapp type) or malabsorption of glucose-galactose.

The preparation is intended only for men. Contraceptive precautions should be taken during treatment. Flutamide may cause fetal harm when administered to a pregnant woman or may be present in breast milk of a nursing mother. Flutamide affects male fertility by reducing the number of sperm in semen. In addition, the reduction in fertility may also result from the inhibition of testosterone release by the LHRH agonist used simultaneously with flutamide. In men treated chronically with flutamide without prior pharmacological or surgical castration, the sperm count should be checked at regular intervals.

Monotherapy. Very often: gynecomastia, compression soreness of the mammary glands, mycotox. Common: increased appetite, insomnia, diarrhea, nausea, vomiting, fatigue, transient deviations in liver function indicators, hepatitis. Rare: shingles, lymphoedema, lupus-like syndrome, loss of appetite, anxiety, depression, headache and dizziness, blurred vision, pulmonary embolism, hot flushes, non-specific abdominal discomfort, ulcer-like pain, heartburn, constipation, pruritus, ecchymosis, weakness of libido, decreased sperm count, swelling, weakness, unwellness, thirst, chest pains. Very rare: neoplastic changes in the mammary glands, cough, sensitivity of the skin to light. Frequency unknown: extension of the OT segment.Combination therapy (flutamide + LHRH agonist). Very often: hot flushes, diarrhea, nausea, vomiting, decreased libido, impotence. Common: liver dysfunction. Uncommon: hepatitis, gynecomastia. Rare: anemia, leukopenia, thrombocytopenia, loss of appetite, depression, anxiety, numbness, drowsiness, confusion, nervousness, irritability, hypertension, non-specific abdominal discomfort, liver dysfunction, jaundice, rash, neuromuscular symptoms, arthralgia, muscle pain, genitourinary symptoms (painful or difficult urination, changes in frequency of urination), edema, irritation at the injection site (in the case of injection in combination with an LHRH agonist), increased blood urea nitrogen (BUN), increased serum creatinine . Very rare: haemolytic anemia, macrocytic anemia, methaemoglobinaemia, sulphhemoglobinemia, hyperglycemia, worsening of diabetes, pulmonary symptoms (e.g. dyspnoea), interstitial pneumonitis, congestive jaundice, hepatic encephalopathy, hepatic cirrhosis, death due to hepatotoxicity, photosensitivity reactions, erythema, ulcerations, bullous rash, epidermal necrolysis, change of urine to orange or greenish-yellow. Frequency unknown: thromboembolism.

Orally. Adults.Limited prostate cancer (stage B2 or T2b): 1 tabl 3 times a day (every 8 hours). When initiating treatment with an LHRH agonist, the frequency and severity of the exacerbation of disease symptoms can be significantly reduced, which sometimes occurs with the administration of an LHRH agonist if flutamide is administered before the agonist and not simultaneously with it. It is recommended to start therapy with flutamide in a dose of 1 tablet. 3 times daily for at least 3 days before initiating LHRH agonist administration and then continuing at the same dose. Treatment with flotamide in combination with an LHRH agonist should be started 8 weeks before the start of radiotherapy and continue during its duration, usually also for about 8 weeks. The whole treatment in this case will last about 16 weeks.Advanced prostate cancer (stage C or T3-T4): the drug should be administered with an LHRH agonist and continue treatment for improvement; if the tumor regresses or stabilizes its growth, treatment continues as long as the patient responds positively to the drug.Special groups of patients. In patients with liver failure, long-term treatment with flutamide may be recommended only after a careful assessment of the individual benefits of treatment compared with the risk of side effects. This treatment should not be used in patients with elevated aminotransferases levels 2-3 times higher than normal. No dosage adjustment is necessary for patients with impaired renal function.Method of administration. For the patient's convenience, a table is provided in the leaflet and on the outer packaging of the medicine for a graphical representation of how it is used. This gives you the opportunity to mark the individual dosage of the drug, as well as check the patient's regularity immediately before taking the drug.