Low-dose ketoconazole treatment in hirsute women

Abstract

Ketoconazole is an orally active antimycotic agent and a potent inhibitor of gonadal and adrenal steroidogenesis. As inhibitor of steroid production, it has been employed in Cushing's syndrome, prostatic cancer and precocious puberty due to autonomous Leydig-cell hyperfunction. By virtue of its selective action on androgen synthesis at low doses by inhibition of C17-20 lyase, this drug could be of potential therapeutic utility in hirsutism. We evaluated the hormonal and clinical effects of a low-dose regimen (400 mg/day) for 3 months in 16 women with a spectrum of disorders from idiopathic hirsutism to polycystic ovary syndrome. Four of them completed 6-month treatment. At 3 months, DHEA-S decreased from 9.9 +/- 1.0 (mean +/- SE) to 6.9 +/- 1.0 mumol/L (p less than 0.01), androstenedione from 13.3 +/- 1.5 to 8.3 +/- 1.3 nmol/L (p less than 0.005), and testosterone from 4.2 +/- 0.4 to 3.1 +/- 0.4 nmol/L (p less than 0.05). No significant changes were observed in LH, FSH, prolactin and estradiol levels. In patients treated for 6 months, androgens were within normal limits at the end of the study. Eleven out of 16 women (about 70%) reported some improvement in their hirsutism. There was a significant decrease in Ferriman-Gallwey's score (p less than 0.001) and mean hair-shaft diameter (p less than 0.001). The patients treated for 6 months showed a further improvement. Pelvic ultrasonography, when repeated (n = 8), was either unchanged or improved. Side effects (polymenorrhea, gastrointestinal reaction, somnolence) were generally mild and transient. Of 20 women who entered the study the dropout rate was 20% (n = 4).(ABSTRACT TRUNCATED AT 250 WORDS)

Diagnosis and management of the dermatologic manifestations of the polycystic ovary syndrome

“…The antifungal ketoconazole also has some antiandrogen effects. Ketoconazole (400 mg a day) had some efficacy in the off‐label treatment application for hirsutism and acne (105–107). One study suggests it to be more effective than low dose OCP, cyproterone acetate or spironolactone (105).…”

Hair: What is New in Diagnosis and Management?

“…Hyperandrogenic women with FPHL can benefit from the antiandrogenic mechanism of ketoconazole. 47 Adjunctive Therapies…”

Female pattern hair loss—An update

“…[ 38 ] Recent research studies focus on drugs that are able to block the PG-D2 receptor (GPR44). Setipiprant (KITH-105) is an orally administered GPR44 receptor inhibitor which may be helpful[ 39 ] Ketoconazole: It has an anti-inflammatory property and also acts as the androgen-receptor antagonist which may explain the efficacy of topical ketoconazole in AGA[ 40 41 ] Melatonin: Melatonin is known to have strong anti-oxidant properties and the ability to actively capture free radicals. [ 42 ] Melatonin has been found to modulate hair growth, pigmentation, and molting in many species including humans.…”

“…Ketoconazole: It has an anti-inflammatory property and also acts as the androgen-receptor antagonist which may explain the efficacy of topical ketoconazole in AGA[ 40 41 ]…”