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Related Experiment Video

Updated: Jan 30, 2026

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Ketoconazole blocks adrenal steroid synthesis.

A Pont, P L Williams, D S Loose

    Annals of Internal Medicine
    |September 1, 1982
    PubMed
    Summary

    Ketoconazole, an antifungal medication, was found to inhibit steroid synthesis in humans and rats. This drug can blunt cortisol production and reduce adrenal androgen response, warranting caution with high doses.

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    Area of Science:

    • Endocrinology
    • Pharmacology
    • Mycology

    Background:

    • Ketoconazole is a broad-spectrum antifungal agent.
    • It is known to inhibit sterol synthesis in fungi.
    • Gynecomastia has been observed in patients using ketoconazole.

    Purpose of the Study:

    • To investigate the effects of ketoconazole on steroid synthesis in humans.
    • To examine ketoconazole's impact on steroidogenesis in isolated rat adrenal cells.
    • To understand the mechanism behind ketoconazole-induced gynecomastia.

    Main Methods:

    • Administration of ketoconazole (400-mg or 600-mg doses) to healthy human subjects.
    • Measurement of cortisol response to adrenocorticotropic hormone (ACTH) at various time points.
    • Incubation of isolated rat adrenal cells with ketoconazole to assess corticosterone production.

    Main Results:

    • Ketoconazole significantly blunted the human cortisol response to ACTH for up to 8 hours post-administration.
    • Adrenal androgen response was reduced in humans treated with ketoconazole.
    • Therapeutic concentrations of ketoconazole virtually eliminated corticosterone production in isolated rat adrenal cells.

    Conclusions:

    • Ketoconazole inhibits steroid synthesis in humans and rats.
    • The drug can suppress adrenal steroidogenesis, impacting cortisol and androgen production.
    • Caution is advised when using high or multiple doses of ketoconazole, particularly in clinical trials, due to potential effects on adrenal function. The drug may have therapeutic applications in blocking steroid synthesis.