Mediprobe Research Inc., London, Canada.
Department of Medicine, Division of Dermatology, University of Toronto, Toronto, Canada.
J Dermatolog Treat. 2022 Nov;33(7):2946-2962. doi: 10.1080/09546634.2022.2109567. Epub 2022 Aug 15.
Androgenetic alopecia (AGA) is the most common cause of hair loss, often challenging to treat. While oral finasteride (1 mg/d) is an FDA-approved treatment for male AGA, oral minoxidil and oral dutasteride are not approved yet. However, clinicians have been increasingly using these two drugs off-label for hair loss. Recently, Japan and South Korea have approved oral dutasteride (0.5 mg/d) for male AGA.
A probable efficacy ranking, in decreasing order, is - dutasteride 0.5 mg/d, finasteride 5 mg/d, minoxidil 5 mg/d, finasteride 1 mg/d, followed by minoxidil 0.25 mg/d. Oral minoxidil predominantly causes hypertrichosis and cardiovascular system (CVS) symptoms/signs in a dose-dependent manner, whereas oral finasteride and dutasteride are associated with sexual dysfunction and neuropsychiatric side effects.
The average plasma half-lives of minoxidil, finasteride, and dutasteride are ∼4 h, ∼4.5 h, and ∼5 weeks, respectively. Minoxidil acts through multiple pathways to promote hair growth. It has been shown as a vasodilator, an anti-inflammatory agent, a Wnt/β-catenin signaling inducer, and an antiandrogen. Finasteride inhibits 5α-reductase (5AR) type II isoenzyme, while dutasteride inhibits both type I and type II. Thus, dutasteride suppresses DHT levels more than finasteride in the serum and scalp.
雄激素性脱发(AGA)是最常见的脱发原因,通常难以治疗。虽然口服非那雄胺(1mg/d)是 FDA 批准用于男性 AGA 的治疗方法,但口服米诺地尔和口服度他雄胺尚未获得批准。然而,临床医生越来越多地将这两种药物用于脱发的标签外治疗。最近,日本和韩国已批准口服度他雄胺(0.5mg/d)用于男性 AGA。
可能的疗效排名依次为 - 度他雄胺 0.5mg/d、非那雄胺 5mg/d、米诺地尔 5mg/d、非那雄胺 1mg/d,其次是米诺地尔 0.25mg/d。口服米诺地尔主要以剂量依赖性方式引起多毛症和心血管系统(CVS)症状/体征,而口服非那雄胺和度他雄胺与性功能障碍和神经精神副作用相关。
米诺地尔、非那雄胺和度他雄胺的平均血浆半衰期分别约为 4 小时、4.5 小时和 5 周。米诺地尔通过多种途径作用促进头发生长。它已被证明具有血管扩张作用、抗炎作用、Wnt/β-连环蛋白信号诱导剂和抗雄激素作用。非那雄胺抑制 5α-还原酶(5AR)II 型同工酶,而度他雄胺抑制 I 型和 II 型同工酶。因此,度他雄胺抑制血清和头皮中二氢睾酮水平的能力超过非那雄胺。