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Flutamide: Anti-Androgen Prostate Cancer Hormone Treatment

Indications for Flutamide

Anti-androgen hormone treatment of prostate cancer with flutamide is a therapeutic option against prostate cancer in the following situations:

• Hormonal treatment of advanced prostate cancer, either alone or in combination with a GnRH agonist, GnRH antagonist or surgical castration.
• Adjuvant androgen deprivation therapy of advanced prostate cancer after surgery or radiation therapy.
• Short course of 14 days to prevent the testosterone flare at the beginning of GnRH agonist therapy.

Mechanism of Action of Flutamide

Flutamide is a nonsteroidal anti-androgen drug which binds without biological activity to the androgen receptor (competitive antagonism). The central inhibition of androgen receptors leads to an increase in LH, testosterone and estrogen.

Pharmacokinetics of Flutamide

• Hepatic metabolism to active metabolites. Mostly renal elimination. Elimination half life: 6–8 h.

Side Effects of Flutamide

• Flutamide shows typical side effects of antiandrogens: gynecomastia, hot flushes, decreased libido, decreased erectile function. Sexual side effects are less pronounced than with LHRH treatment.
• Abdominal pain, diarrhea or nausea, rarely vomiting.
• Increased liver enzymes (7%) or jaundice. Fatal liver necrosis due to flutamid has been reported.
• Fluid retention, cardiac decompensation
• Anemia (frequently), rarely leukopenia, thrombocytopenia
• Allergic reactions
• Greenish discoloration of urine

Contraindications for Flutamide

Liver insufficiency. Increased liver enzymes during flutamide treatment warrant dose reduction and regular laboratory monitoring. Flutamide should be stopped in progressive elevation of liver transaminases without evidence of liver metastases. Further contraindications are allergy, flutamide has no indications in women and children.

Dosage of Flutamide

250 mg 1-1-1 p.o.

References

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Perdona u.a. 2005 PERDONA, S. ; AUTORINO, R. ; DE PLACIDO, S. ; D’ARMIENTO, M. ; GALLO, A. ; DAMIANO, R. ; PINGITORE, D. ; GALLO, L. ; DE SIO, M. ; BIANCO, A. R. ; DI LORENZO, G.: Efficacy of tamoxifen and radiotherapy for prevention and treatment of gynaecomastia and breast pain caused by bicalutamide in prostate cancer: a randomised controlled trial.
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Sieber u.a. 2004 SIEBER, P. R. ; KEILLER, D. L. ; KAHNOSKI, R. J. ; GALLO, J. ; MCFADDEN, S.: Flutamide 150 mg maintains bone mineral density during monotherapy for localized or locally advanced prostate cancer.
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Smith u.a. 2004b SMITH, M. R. ; GOODE, M. ; ZIETMAN, A. L. ; MCGOVERN, F. J. ; LEE, H. ; FINKELSTEIN, J. S.: Bicalutamide monotherapy versus leuprolide monotherapy for prostate cancer: effects on bone mineral density and body composition.
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Tyrrell u.a. 2004 TYRRELL, C. J. ; PAYNE, H. ; TAMMELA, T. L. ; BAKKE, A. ; LODDING, P. ; GOEDHALS, L. ; VAN ERPS, P. ; BOON, T. ; VAN DE BEEK, C. ; ANDERSSON, S. O. ; MORRIS, T. ; CARROLL, K.: Prophylactic breast irradiation with a single dose of electron beam radiotherapy (10 Gy) significantly reduces the incidence of bicalutamide-induced gynecomastia.
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Widmark u.a. 2003 WIDMARK, A. ; FOSSA, S. D. ; LUNDMO, P. ; DAMBER, J. E. ; VAAGE, S. ; DAMBER, L. ; WIKLUND, F. ; KLEPP, O.: Does prophylactic breast irradiation prevent antiandrogen-induced gynecomastia? Evaluation of 253 patients in the randomized Scandinavian trial SPCG-7/SFUO-3.
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