As with all azole antifungal agents, ketoconazole works principally by inhibiting the enzyme cytochrome P450 14α-demethylase (CYP51A1). A subsequent trial in Europe failed to show a risk to infants of mothers receiving ketoconazole. It should be used for the treatment of certain fungal infections, known as endemic mycoses, only when alternative antifungal therapies are not available or not tolerated. Oral ketoconazole at a dosage range of 400 to 2,000 mg/day has been found to result in a rate of gynecomastia of 21%. In any case, the risk of hepatotoxicity with ketoconazole limits its use in all of these indications, especially in those that are benign such as hirsutism.
As of March 2019, oral levoketoconazole (developmental code name COR-003, tentative brand name Recorlev) is phase III clinical trials for the treatment of Cushing's syndrome. In 2013, oral ketoconazole was withdrawn in the European Union and Australia, and strict restrictions were placed on the use of oral ketoconazole in the United States and Canada. This event triggered an evaluation of oral ketoconazole throughout the rest of the European Union.
Oral ketoconazole has been used clinically as a steroidogenesis inhibitor in men, women, and children at dosages of 200 to 1,200 mg/day. This effect is thought to be quite weak however, even with high oral doses of ketoconazole. It produces this effect through inhibition of 17α-hydroxylase and 17,20-lyase, which are involved in the synthesis and degradation of steroids, including the precursors of testosterone. As an antiandrogen, ketoconazole operates through at least two mechanisms of action. Resistance to ketoconazole has been observed in a number of clinical fungal isolates, including Candida albicans. Lower doses of fluconazole and itraconazole are required to kill fungi compared to ketoconazole, as they have been found to have a greater affinity for fungal cell membranes.
It also inhibits androgen and glucocorticoid synthesis. Thus the link to other proteins binding androgens might be possible. 24 hours after treatment, however, the response of plasma testosterone to hCG was diminished. The diminution of testosterone synthesis could be significant as further therapeutic trials may use larger doses or more than once-daily administration.
The drug may cause adrenal insufficiency so the level of the adrenocortical hormones should be monitored while taking it. Oral ketoconazole has various contraindications, such as concomitant use with certain other drugs due to known drug interactions. Common side effects when taken by mouth include nausea, headache, and liver problems.
Oral ketoconazole is indicated for use in these countries when the indication is a severe or life-threatening systemic infection and alternatives are unavailable. Ketoconazole was introduced as the prototypical medication of the imidazole group of antifungals. Other steroidogenesis inhibitors besides ketoconazole and levoketoconazole include the nonsteroidal compound aminoglutethimide and the steroidal compound abiraterone acetate.citation needed Levoketoconazole is under development for potential clinical use as a steroidogenesis inhibitor with better tolerability and less toxicity than ketoconazole. It is a racemic mixture of two enantiomers, levoketoconazole ((2S,4R)-(−)-ketoconazole) and dextroketoconazole ((2R,4S)-(+)-ketoconazole).
Expect sexual benefits within weeks, energy and mood within 1–2 months, and body composition changes over 3–6 months alongside resistance training and protein intake. Daily gels, patches, and axillary solutions provide steady levels with easy dose adjustments. You’re a candidate when you have both consistent low levels and symptoms. In 2026, you have more evidence-backed options than ever, and the path to feeling like yourself again doesn’t have to be risky or confusing. If you’re struggling with low energy, a stalled libido, slower recovery in the gym, or brain fog that just won’t lift, you’re not imagining it, low testosterone (low T) is common and treatable. Articles from Antimicrobial Agents and Chemotherapy are provided here courtesy of American Society for Microbiology (ASM) Cortisol binding to corticosteroid-binding globulin was unaffected.
Ketoconazole at concentrations achievable in serum with currently used doses blocked basal and gonadotropin-stimulated testosterone production by rat Leydig cells. The development of gynecomastia in two patients prompted us to investigate the effect of the drug on testosterone production. Ketoconazole, a new oral drug used to treat systemic and superficial mycoses, inhibits sterol synthesis in fungi. The .gov means it’s official.

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