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Antiandrogens
Sunday, September 18, 2011 Posted by Piscean


Antiandrogens
Antiandrogens are used as an adjunct therapy with gonadotropin-releasing hormone analogues in treating advanced prostate cancer. These drugs include:
  • flutamide
  • nilutamide
  • bicalutamide.
Pharmacokinetics
After oral administration, antiandrogens are absorbed rapidly and completely.
Metabolism and excretion
Antiandrogens are metabolized rapidly and extensively and excreted primarily in urine.
Pharmacodynamics
Flutamide, nilutamide, and bicalutamide exert their antiandrogenic action by inhibiting androgen uptake or preventing androgen binding in cell nuclei in target tissues.
Pharmacotherapeutics
Antiandrogens are used with a gonadotropin-releasing hormone analogue, such as leuprolide, to treat metastatic prostate cancer.
Special feature: no flareup
Concomitant administration of antiandrogens and a gonadotropin-releasing hormone analogue may help prevent the disease flare that occurs when the gonadotropin-releasing hormone analogue is used alone.

Drug interactions
Antiandrogens don’t interact significantly with other drugs. However, flutamide and bicalutamide may affect prothrombin time (a test to measure clotting factors) in a patient receiving warfarin.

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