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. Due to its efficacy at reducing systemic androgen levels, ketoconazole has been used with some success as a treatment for androgen-dependent prostate cancer. These findings indicate a delayed effect of ketoconazole on the synthesis of testosterone, although its blood levels are decreased to nearly zero. A single oral dose of 400 mg ketoconazole, a broad-spectrum antifungal drug, administered orally to 5 young men induced a drop in serum and saliva testosterone into the range of hypogonadism, while LH, FSH and prolactin levels remained unchanged. They can monitor for any potential side effects and ensure the continued effectiveness of the treatment, as well as discuss the potential for the ketoconazole shampoo to lower testosterone. Ketoconazole, an imidazole anti-fungal agent, has often produced features of androgen deficiency including decreased libido, gynecomastia, impotence, oligospermia, and decreased testosterone levels, in men being treated for chronic mycotic infections. Most clinicians aim for mid‑normal total testosterone (often ~400–700 ng/dL), individualized to symptom control and side effects. For oral TU, plan regular blood pressure monitoring. The 2023 TRAVERSE trial in high‑risk men found testosterone was non‑inferior to placebo for major cardiac events over follow‑up, though there were slightly higher rates of atrial fibrillation, pulmonary embolism, and acute kidney injury. If you’re trying to conceive, avoid standard testosterone, it suppresses sperm production. 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. However, in the treatment of prostate cancer, concomitant glucocorticoid administration is needed to prevent adrenal insufficiency. It was speculated that antifungal properties of ketoconazole reduce scalp microflora and consequently may reduce follicular inflammation that contributes to alopecia. Ketoconazole shampoo in conjunction with an oral 5α-reductase inhibitor such as finasteride or dutasteride has been used off label to treat androgenic alopecia. Topically administered ketoconazole is usually prescribed for fungal infections of the skin and mucous membranes, such as athlete's foot, ringworm, candidiasis (yeast infection or thrush), jock itch, and tinea versicolor. They received the drug for seven days at a dose of 200 mg daily. A block of synthesis was demonstrated in vitro. Insurers typically require symptoms plus two low morning testosterone results and periodic labs. Work with your clinician to review opioids, glucocorticoids, ketoconazole, spironolactone, and certain antidepressants. Keep alcohol moderate (≤2 drinks/day, with alcohol‑free days each week). 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. Due to incidence of serious liver toxicity, the use of oral ketoconazole was suspended in France in July 2011, following review. When administered orally, ketoconazole is best absorbed at highly acidic levels, so antacids or other causes of decreased stomach acid levels will lower the drug's absorption. Ketoconazole has been found to displace dihydrotestosterone and estradiol from sex hormone-binding globulin in vitro, but this was not found to be relevant in vivo.
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