What Is Flutamide?

Chemicals, [alias] Flunbutamide, Flutamide, Retarded Tumors, Fuzhier, Fluritam, 2-methyl-N- [4-nitro-3-trifluoromethylphenyl] Propionamide.

Flutamide

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Chemical substance

[Chinese name] Flutamide

[Standard] BP2009 USP34

[English name] Flutamide

[English alias] 2-Methyl-N- [4-nitro-3- (trifluoromethyl) -phenyl] -propionamide

[CAS number] 13311-84-7

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[Pharmacological action] This product is a non-steroidal antiandrogenic drug. Except for the anti-androgen effect, this product does not have any hormone effect. Its metabolite, small hydroxyflutamide, is its main active form. It can bind to androgen receptors in target tissues, block the binding of dihydrotestosterone (androgenic active form) to androgen receptors, and inhibit target tissue uptake. Testosterone, which acts as an anti-androgen. However, this effect can cause an increase in the release of FSH and LH, and increase the plasma concentration of testosterone. When used with gonadotropin-releasing hormone (GnRH) such as leuprolide, it completely blocks androgens and prevents compensatory increases.

[Pharmacokinetics] Oral absorption is rapid and complete. Most are converted to 0-hydroxyflutamide when first passed through the liver. After a single oral administration of 250 mg, the blood concentration reached a peak value of about 10 to 20 g / L, and 2 hours after the administration, the blood concentration of -hydroxyflutamide reached a peak value of about 1.3 mg / L. This product and its main active metabolites are widely bound to its plasma proteins, with plasma t1 / 2 of about 5-6 hours; usually 250mg, 3 times / d administration schedule, the concentration of hydroxyflutamide in the plasma is 3.4-8. 5mo1 / L range. Within 24 hours after administration, 28% were excreted from the urine.

[Indications] For prostate cancer or benign prostatic hypertrophy. This product can be used in combination with leuprolide (it should be started and continued at the same time) to treat metastatic prostate cancer, which can significantly increase the efficacy.

[Usage and Dosage] Orally take 0.25g / times, 3 times / d, and take after meals.

[Adverse reactions] The main adverse reactions are feminization of male breasts (34% to 100%) and gastrointestinal discomfort. Others may include insomnia, fatigue, abnormal liver function, sexual dysfunction, pruritus, shingles, etc.

[Specifications] 250mgx 20 tablets.