Yoshikawa K
Department of Dermatology, Osaka University School of Medicine.
Nihon Rinsho. 1993 Apr;51(4):1037-42.
One of the synthetic retinoids Etretinate has been used in dermatology for the various inflammatory keratosis, congenital hyperkeratotic disorders and etc., and plays an important role in the treatment of these otherwise intractable skin diseases. But, it still has various side effects, the most serious among which being teratogenicity, and contraception for at least two years after cessation of the drug is recommended because of its very long half life. Acitretin, a nonesterified analogue with a much shorter half life and Isotretinoin are also used in the USA and Europe. The latter is reported to be very effective to severe cystic acne. Apparently, better compounds with less toxicity and a shorter half life are needed. A topical application of retinoid is under clinical evaluation. A topical application of active vitamin D3 and its analogues are shown to be effective for psoriasis, one of the most common intractable skin diseases. Calcitriol is already used in several European countries, and 1,24-dihydroxyvitamin D3 successfully completed aclinical studies in Japan. Topical vitamin D preparations will be important and useful in dermatology in the near future. Although an action of active vitamin D on the skin is not fully understood, we speculate that it plays an important role in the regulation of epidermal growth and differentiation.
合成维甲酸之一的依曲替酯已用于皮肤科治疗各种炎性角化病、先天性角化过度性疾病等,在治疗这些原本难治的皮肤病中发挥着重要作用。但是,它仍有各种副作用,其中最严重的是致畸性,由于其半衰期很长,建议停药后至少避孕两年。阿维A,一种半衰期短得多的非酯化类似物,以及异维A酸也在美国和欧洲使用。据报道,后者对重度囊肿性痤疮非常有效。显然,需要毒性更小、半衰期更短的更好的化合物。维甲酸的局部应用正在进行临床评估。活性维生素D3及其类似物的局部应用已被证明对银屑病有效,银屑病是最常见的难治性皮肤病之一。骨化三醇已在几个欧洲国家使用,1,24 - 二羟基维生素D3在日本成功完成了临床试验。局部维生素D制剂在不久的将来在皮肤科将很重要且有用。尽管活性维生素D对皮肤的作用尚未完全了解,但我们推测它在调节表皮生长和分化中起重要作用。