Flutamide is indicated for use in combination with LHRH agonists for the management of locally confined Stage B2-C and Stage D2 metastatic carcinoma of the prostate. Stage B2-C Prostatic Carcinoma: Treatment with Flutamide and the LHRH agonist should start 8 weeks prior to initiating radiation therapy and continue during radiation therapy. Stage D2 Metastatic Carcinoma: To achieve benefit from treatment, Flutamide should be initiated with the LHRH agonist and continued until progression.
In animal studies, flutamide demonstrates potent antiandrogenic effects. It exerts its antiandrogenic action by inhibiting androgen uptake and/or by inhibiting nuclear binding of androgen in target tissues or both. Prostatic carcinoma is known to be androgen-sensitive and responds to treatment that counteracts the effect of androgen and/or removes the source of androgen, e.g. castration.
The recommended dosage of Flutamide in combination with orchiectomy or in combination with an LHRH agonist is one 250 mg tablet three times a day at eight-hour intervals. In combination with an LHRH agonist, either the two agents may be initiated simultaneously, or Flutamide tablet therapy may be started 24 hours prior to initiation of the LHRH agonist. In the management of bulky locally advanced Stage B 2 and Stage C prostatic carcinoma, the recommended dosage is one 250 mg tablet, three times a day at eight-hour intervals. Flutamide should be started simultaneously or 24 hours prior to initiation of the LHRH agonist. Administration of Flutamide should begin eight weeks prior to external beam radiation therapy and continue through the course of radiation therapy.
Interactions between Flutamide Tablets and leuprolide have not occurred. In patients receiving long-term oral-anticoagulant therapy, increases in prothrombin time have been reported after flutamide monotherapy was initiated. Therefore close monitoring of prothrombin time is recommended and adjustment of the anticoagulant dose may be necessary when flutamide tablets are administered concomitantly. Cases of increased theophylline plasma concentrations have been reported in patients receiving concomitant theophylline and flutamide tablets. Theophylline is primarily metabolized by CYP1A2, which is the primary enzyme responsible for the conversion of flutamide to its active agent 2-hydroxyflutamide.
Flutamide tablets are contraindicated in patients who have shown hypersensitivity to flutamide or any component of this preparation. Flutamide is contraindicated in patients with severe hepatic impairment. Flutamide has not been studied in women and is not indicated for this population, particularly for nonserious or non-threatening conditions.
Cardiovascular System: hypertension in 1% of patients. Rarely thrombophlebitis, pulmonary embolism, myocardial infarction.
Central Nervous System: CNS (drowsiness/confusion/depression/anxiety/nervousness) reactions occurred in 1% of patients. Rarely insomnia, tiredness, headache, dizziness, weakness, malaise, blurred vision and decreased libido have been reported.
Endocrine System: gynecomastia in 9% of patients. Rarely breast tenderness sometimes accompanied by galactorrhoea.
Gastrointestinal System: nausea/vomiting occurred in 11%; diarrhea 12%, anorexia 4%, and other gastrointestinal disorders occurred in 6% of patients. Increased appetite, indigestion and constipation have also been reported.
Hematopoietic System: anaemia occurred in 6% of patients, leukopenia 3%, thrombocytopenia 1%.
Liver and Biliary System: clinically evident hepatitis and jaundice occurred in <1% of patients.
Skin: irritation at the injection site and rash occurred in 3% of patients. Photosensitivity reactions have been reported in five patients.
No studies have been conducted in pregnant or lactating women. Therefore, the possibility that Flutamide may cause fetal harm if administered to a pregnant woman, or may be present in the breast milk of lactating women must be considered.
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
.png&w=384&q=75)