Ketoconazole inhibition of testicular secretion of testosterone and displacement of steroid hormones from serum transport proteins

D. S. Grosso, T. W. Boyden, R. W. Pamenter, David G Johnson, D. A. Stevens, John N Galgiani

Research output: Contribution to journalArticle

45 Citations (Scopus)

Abstract

In vivo perfusion of canine testes with ketoconazole inhibited the stimulation of testosterone production by human chorionic gonadotropin in a dose-dependent manner. Ketoconazole also selectively displaced steroids from serum-binding globulins. Dihydrotestosterone and estradiol binding to sex hormone-binding globulin were inhibited by ketoconazole. Cortisol binding to corticosteroid-binding globulin was unaffected. The concentrations of ketoconazole that inhibited human chorionic gonadotropin stimulation of testicular androgen production and displaced sex steroids from sex hormone-binding globulin were in the range of blood levels found in patients on higher therapeutic dosage regimens. Suppression of testicular testosterone synthesis and displacement of estrogens from sex hormone-binding globulin may decrease the androgen/estrogen ratio of the blood and contribute to the development of gynecomastia that has been reported in some ketoconazole-treated patients.

Original languageEnglish (US)
Pages (from-to)207-212
Number of pages6
JournalAntimicrobial Agents and Chemotherapy
Volume23
Issue number2
StatePublished - 1983
Externally publishedYes

Fingerprint

Ketoconazole
Testosterone
Blood Proteins
Carrier Proteins
Steroids
Sex Hormone-Binding Globulin
Hormones
Chorionic Gonadotropin
Androgens
Estrogens
Transcortin
Gynecomastia
Serum Globulins
Dihydrotestosterone
Hydrocortisone
Canidae
Testis
Estradiol
Perfusion

ASJC Scopus subject areas

  • Pharmacology (medical)

Cite this

Ketoconazole inhibition of testicular secretion of testosterone and displacement of steroid hormones from serum transport proteins. / Grosso, D. S.; Boyden, T. W.; Pamenter, R. W.; Johnson, David G; Stevens, D. A.; Galgiani, John N.

In: Antimicrobial Agents and Chemotherapy, Vol. 23, No. 2, 1983, p. 207-212.

Research output: Contribution to journalArticle

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