类维生素a在皮肤科的目前用途和未来潜在作用。

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Orfanos CE, Zouboulis CC, Almond-Roesler B, Geilen CC

类维生素a在皮肤科的目前用途和未来潜在作用。

药物。1997年3月53(3):358-88。

PubMed ID

9074840 (查看PubMed

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摘要

自15年前推出以来，类维生素a已越来越多地用于银屑病和其他角化过度和角化不全性皮肤病、角化遗传性皮肤病、严重痤疮和痤疮相关皮肤病的局部和全身治疗，也用于皮肤癌和其他肿瘤的治疗和/或化学预防。维生素A的氧化代谢物(视黄醇)是天然的类维生素A，在外周血中存在低水平。合成的类维生素a可分为三类，包括非芳香族、单芳香族和多芳香族化合物。全身给药后30-60分钟可在血浆中检测到，并在2 - 4小时后达到最大浓度。异维甲酸的消除半衰期为10至20小时，乙维甲酸为80至175天，反式阿维甲酸为2至4天;而后者则部分转化为乙替甲酸。与皮下脂肪组织相比，皮肤中的类维生素a浓度相当低。在细胞内，维甲酸与胞质蛋白和特定的核受体相互作用。两类核受体被认为在分子水平介导类视黄酮活性，RARs和RXRs。类视黄酮受体的表达是组织特异性的; skin mainly espresses RAR gamma and RXR alpha. Retinoids affect epidermal cell growth and differentiation as well as sebaceous gland activity and exhibit immunomodulatory and anti-inflammatory properties. Current retinoid research targets the development of receptor-selective retinoids for tailoring and/or improving their therapeutic profile. Currently, tretinoin is used systemically for acute promyelocytic leukaemia, etretinate and acitretin for psoriasis and related disorders, as well as other disorders of keratinisation and isotretinoin for seborrhoea, severe acne, rosacea and acneiform dermatoses. Systemic retinoids are also applied for chemoprevention of epithelial skin cancer and cutaneous T cell lymphoma. The major adverse effect of retinoids is teratogenicity; all other adverse effects are dose-dependent and controllable. Contraception is, therefore, essential during retinoid treatment in women of child-bearing age. Clinical monitoring requires physical examination for adverse effects every 3 to 4 weeks and proper laboratory investigations, also including analysis of retinoid bioavailability in selected cases. Topical retinoids are rapidly developing at present and seem promising for the future; their clinical application includes acne, aging, photodamage, precanceroses, skin cancer and disorders of skin pigmentation. The development of receptor-specific retinoids for topical treatment of psoriasis and/or acne may lead to interesting new compounds based on our current concepts of retinoid function.

引用本文的药库数据

药物靶点

药物	目标	种类	生物	药理作用	行动
Acitretin	视黄酸受体	蛋白质	人类	是的	受体激动剂	细节
Acitretin	视黄酸受体rxr -	蛋白质	人类	是的	受体激动剂	细节
Acitretin	视黄酸受体rxr	蛋白质	人类	是的	受体激动剂	细节
Etretinate	视黄酸受体	蛋白质	人类	是的	受体激动剂	细节
Etretinate	视黄酸受体rxr -	蛋白质	人类	是的	受体激动剂	细节