Ketoconazole
This drug got its start as an antifungal agent. Then doctors noticed that men taking it developed breast enlargement—clearly, more than fungal problems were being treated here! Doctors learned that ketoconazole blocks production of testosterone by the testicles as well as androgens made by the adrenal gland. It works quickly; taking 400 milligrams of ketoconazole every eight hours reduces testosterone to the castrate range within twenty-four hours. The drug’s effects are reversible, and testosterone goes back up again as soon as a man stops taking ketoconazole. It’s debatable whether the drug is as effective as other hormonal treatments for long-term use; ketoconazole causes a surge in production of LH that might, over time, overpower the drug’s tight clamp on testosterone. Therefore, ketoconazole generally is used in short-term situations where fast action is needed—in a man with acute spinal pain, for example, or in a man with DIC (disseminated intravascular coagulation, a blood-clotting disorder that develops in some men with advanced prostate cancer). In addition to the hormonal effects, some derivatives of ketoconazole have also been shown to have some effect in directiy blocking the growth of cancer cells; this potential is undergoing intense investigation. One technicality: The drug is not approved by the FDA for use in the treatment of prostate cancer. It can have adverse effects on the liver. Because it can also suppress the production of steroids normally produced by the adrenal gland, ketoconazole should be prescribed along with a corticosteroid such as prednisone (five milligrams a day), to compensate for this loss.
Conclusion: Ketoconazole is not a drug for the long haul, but it is helpful in some situations.
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