Hommel L, Geiger J M, Harms M, Saurat J H
Department of Dermatology, University Hospital, Genève, Switzerland.
Dermatology. 1996;193(2):127-30. doi: 10.1159/000246227.
It is generally accepted that the inhibition of sebum excretion has a predictive value for anti-acne activity. Whereas oral 13-cisretinoic acid (13-cis-RA) decreases sebum excretion, it has not been shown so far if oral all-trans-retinoic acid (tretinoin, tRA) does so. The aim of this exploratory study was to investigate the effect of oral tRA on the sebum excretion rate (SER) in young male subjects.
12 healthy volunteers with a baseline SER above 1.0 microgram/cm2/min were treated with 20 mg/day tRA for 4 weeks. The SER was measured at weeks 2 and 4. Adverse reactions were recorded.
The mean SER varied from 1.56 at baseline to 1.65 at week 2 and to 1.49 micrograms/cm2/min at week 4. Comparison with values obtained in the same subjects previously treated with either 13-cis-RA or 9-cis-retinoic acid indicated that tRA less sebosuppressive. Mucocutaneous reactions and headache were the most frequent side effects of oral tRA.
The lack of effect on the SER suggests that oral tRA would probably be ineffective against acne. The fact that, of the three isomers tested, only 13-cis-RA (which does not bind to nuclear receptors) shows activity may suggest that sebosuppression is not nuclear receptor mediated. We discuss other hypotheses related to pharmacokinetics.
普遍认为抑制皮脂分泌对抗痤疮活性具有预测价值。口服13-顺式维甲酸（13-cis-RA）可降低皮脂分泌，但口服全反式维甲酸（维甲酸，tRA）是否有此作用目前尚未得到证实。本探索性研究的目的是调查口服tRA对年轻男性受试者皮脂分泌率（SER）的影响。
12名基线SER高于1.0微克/平方厘米/分钟的健康志愿者接受20毫克/天tRA治疗4周。在第2周和第4周测量SER。记录不良反应。
平均SER从基线时的1.56变化至第2周时的1.65，以及第4周时的1.49微克/平方厘米/分钟。与先前用13-顺式维甲酸或9-顺式维甲酸治疗的同一受试者获得的值进行比较表明，tRA的皮脂抑制作用较小。皮肤黏膜反应和头痛是口服tRA最常见的副作用。
对SER缺乏影响表明口服tRA可能对痤疮无效。在所测试的三种异构体中，只有13-顺式维甲酸（不与核受体结合）显示出活性，这一事实可能表明皮脂抑制不是由核受体介导的。我们讨论了与药代动力学相关的其他假设。
