High-Dose Ketoconazole Therapy and Adrenal and Testicular Function in Humans

Pont, Allan; Graybill, John R.; Craven, Philip C.; Galgiani, John N.; Dismukes, William E.; Reitz, Richard E.; Stevens, David A.

doi:10.1097/00006254-198506000-00019

Cited by 22 publications

(40 citation statements)

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“…In addition, glucocorticoid antagonist activity due to occupancy of glucocorticoid receptors has been shown in cultured hepatoma cells (8). Low dose ketoconazole (200 mg) administration to normal men caused a selective and fully reversible block of the Ci7_2o lyase (9), explaining the drug's potent inhibitory effect on testosterone production (9)(10)(11)(12)(13). Clinical data concerning adrenal effects also are available.…”

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confidence: 99%

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Prolonged Treatment of Cushing's Disease by Ketoconazole

Sonino

Boscaro

Merola

et al. 1985

The Journal of Clinical Endocrinology & Metabolism

112

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Ketoconazole, used in clinical practice as an antifungal medication, recently was found to be a potent inhibitor of gonadal and adrenal steroidogenesis in vitro and in vivo. The effects of prolonged treatment with this agent in Cushing's disease were investigated in five patients who had recurrent severe hypercortisolism after selective transsphenoidal surgery. The patients received the drug for at least 2 months. Urinary cortisol markedly decreased in all patients immediately after the beginning of treatment with ketoconazole (800 mg/day) and remained within low normal levels when the daily dose was lowered to 600 mg/day. Plasma cortisol also decreased. After 4-6 weeks of treatment, the clinical features of the disease regressed in all patients without signs of toxicity. These findings indicate that ketoconazole may be a valuable drug for the management of patients with Cushing's disease because of its ability to correct hypercortisolism quickly.

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confidence: 99%

“…Clinical data concerning adrenal effects also are available. In normal subjects, the plasma cortisol response to ACTH was significantly blunted by ketoconazole (5,13). In patients with an adrenal adenoma or Cushing's disease, plasma cortisol was suppressed, and the cortisol response to ACTH was blunted after administration of 800 mg/ day for 2 days (14, 15).…”

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confidence: 99%

Prolonged Treatment of Cushing's Disease by Ketoconazole

Sonino

Boscaro

Merola

et al. 1985

The Journal of Clinical Endocrinology & Metabolism

112

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“…Initially its frequent use was enthusiastically followed but soon some conservative opinions questioned its efficacy, hepatic [16] and endocrine [17,18] toxicity and even a delayed anti-androgenic effect after therapy discontinuation [ 191.…”

Section: Discussionmentioning

confidence: 99%

African histoplasmosis: therapeutic efficacy of itraconazole

Velho

Cabral

Massa

1998

Acad Dermatol Venereol

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“…Ketoconazole, an imidazole, was the first azole to be used for coccidioidomycosis, despite a dismal clinical response rate of 20% to 30%. The use of ketoconazole was also limited by gastrointestinal intolerance, adrenal insufficiency, and gynecomastia [37,38].…”

Section: Azolesmentioning

confidence: 99%