The DOI matches its Crossref record; 18 of the 18 references it cites were found in a registry or an index.
Ketoconazole Blocks Testosterone Synthesis
Abstract
Ketoconazole, a new oral drug used to treat systemic and superficial mycoses, inhibits sterol synthesis in fungi. The development of gynecomastia in two patients prompted us to investigate the effect of the drug on testosterone production. After a 200-, 400-, or 600-mg dose, volunteer male testosterone serum concentrations fell markedly, but returned toward baseline eight to 24 hours later as ketoconazole serum concentrations waned. A marked but transient drop in testosterone levels occurred in patients receiving long-term therapy, and continuous testosterone depression was noted in one. A block of synthesis was demonstrated in vitro. Ketoconazole at concentrations achievable in serum with currently used doses blocked basal and gonadotropin-stimulated testosterone production by rat Leydig cells. The diminution of testosterone synthesis could be significant as further therapeutic trials may use larger doses or more than once-daily administration. The paucity of reports of endocrinologic toxicity may relate to the "escape" from the block demonstrated in vivo.
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Burton, K. (1956) · Biochemical Journal · doi:10.1042/bj0620315 · Cited by 14,090
Ketoconazole Blocks Adrenal Steroid Synthesis
PONT, A., WILLIAMS, P. L., LOOSE, D. S., FELDMAN, D., REITZ, R. E., BOCHRA, C., & STEVENS, D. A. (1982) · Annals of Internal Medicine · doi:10.7326/0003-4819-97-3-370 · Cited by 422
Self-citationIn vitro and in vivo effects of the antimycotic drug ketoconazole on sterol synthesis
Van den Bossche, H., Willemsens, G., Cools, W., Cornelissen, F., Lauwers, W. F., & van Cutsem, J. M. (1980) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.17.6.922 · Cited by 276
Midgley, A. R., & Niswender, G. D. (1970) · Acta Endocrinologica · doi:10.1530/acta.0.065s320 · Cited by 268
Dufau, M. L., Mendelson, C. R., & Catt, K. J. (1974) · The Journal of Clinical Endocrinology & Metabolism · doi:10.1210/jcem-39-3-610 · Cited by 267
Mechanism of Action of Antifungal Drugs, with Special Reference to the Imidazole Derivatives
Borgers, M. (1980) · Clinical Infectious Diseases · doi:10.1093/clinids/2.4.520 · Cited by 215
Disposition of ketoconazole, an oral antifungal, in humans
Brass, C., Galgiani, J. N., Blaschke, T. F., Defelice, R., O'Reilly, R. A., & Stevens, D. A. (1982) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.21.1.151 · Cited by 210
MOYLE, W. R., & RAMACHANDRAN, J. (1973) · Endocrinology · doi:10.1210/endo-93-1-127 · Cited by 197
Gynecomastia with Ketoconazole
DeFelice, R., Johnson, D. G., & Galgiani, J. N. (1981) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.19.6.1073 · Cited by 159
Ketoconazole, an oral antifungal: laboratory and clinical assessment of imidazole drugs
Borelli, D., Bran, J. L., Fuentes, J., Legendre, R., Leiderman, E. A., Levine, H. B., Restrepo-M., A., & Stevens, D. A. (1979) · Postgraduate Medical Journal · doi:10.1136/pgmj.55.647.657 · Cited by 146
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The Decline of Androgen Levels in Elderly Men and Its Clinical and Therapeutic Implications
Kaufman, J. M., & Vermeulen, A. (2005) · Endocrine Reviews · doi:10.1210/er.2004-0013 · Cited by 1,079
Inhibition of Adrenal Steroidogenesis by the Anesthetic Etomidate
Wagner, R. L., White, P. F., Kan, P. B., Rosenthal, M. H., & Feldman, D. (1984) · New England Journal of Medicine · doi:10.1056/nejm198405313102202 · Cited by 555
The Treatment of Cushing's Disease
Pivonello, R., De Leo, M., Cozzolino, A., & Colao, A. (2015) · Endocrine Reviews · doi:10.1210/er.2013-1048 · Cited by 465
Hormonal Therapy for Prostate Cancer
Desai, K., McManus, J. M., & Sharifi, N. (2021) · Endocrine Reviews · doi:10.1210/endrev/bnab002 · Cited by 447
The use of ketoconazole as an inhibitor of steroid production
Oates, J. A., Wood, A. J. J., & Sonino, N. (1987) · New England Journal of Medicine · doi:10.1056/nejm198709243171307 · Cited by 395
Metadata
- Authors
- Pont, A.
- Venue
- Archives of Internal Medicine
- Publisher
- American Medical Association (AMA)
- Published
- 1982-11-01
- Volume
- 142
- Issue
- 12
- Pages
- 2137
- ISSN
- 0003-9926 (ISSN-L)
- OpenAlex
- W2073435592
- Cited by
- 296
- References
- 18
- FWCI
- 12.94
- Type
- journal article
- Language
- en
- Open access
- closed
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