当前使用和未来的潜在作用在皮肤类维生素a。

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

当前使用和未来的潜在作用在皮肤类维生素a。

药。1997年3月,53 (3):358 - 88。

PubMed ID

9074840 (在PubMed

]

文摘

因为他们介绍15年前,类维生素a被越来越多地用于局部和全身治疗牛皮癣和其他角化过的和parakeratotic皮肤疾病,角化病的genodermatoses,严重的痤疮和acne-related皮肤病,也用于治疗和/或化学预防皮肤癌和其他肿瘤。氧化代谢物的维生素A(视黄醇)自然类维生素A在外周血中的低水平。合成类维生素a分为3代包括nonaromatic单芳和聚芳的化合物。他们在等离子体检测30 - 60分钟后系统管理,并达到最大浓度2到4小时后。消除半衰期是10到20小时异维甲酸,etretinate 80 - 175天,2到4天,trans-acitretin;后者,然而,部分转化为etretinate。类维生素a浓度在皮肤与皮下脂肪组织相当低。细胞、类维生素a与胞质蛋白和特定的核受体。已经提出两类核受体调解类维生素a活动在分子水平上,rar和rxr。类维生素a受体组织特定的表达式; 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.

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药物靶点

药物	目标	类	生物	药理作用	行动
Acitretin	视黄酸受体α	蛋白质	人类	是的	受体激动剂	细节
Acitretin	视黄酸受体RXR-alpha	蛋白质	人类	是的	受体激动剂	细节
Acitretin	视黄酸受体RXR-gamma	蛋白质	人类	是的	受体激动剂	细节
Etretinate	视黄酸受体α	蛋白质	人类	是的	受体激动剂	细节
Etretinate	视黄酸受体RXR-alpha	蛋白质	人类	是的	受体激动剂	细节