Töpert M
Research Laboratories of Schering AG, Berlin, West Germany.
Drugs. 1988;36 Suppl 5:1-8. doi: 10.2165/00003495-198800365-00003.
In dermatotherapy, potent drugs are needed which can be used as alternatives to corticosteroids, but which are without unwanted local and systemic effects. Three theoretical possibilities for the development of such advanced drugs have been presented. Firstly, dissociation of wanted and unwanted effects by selection of a certain corticosteroid structure is proposed. However, this is impossible, because corticosteroid receptors are ubiquitous and all display the same specificity. Secondly, manipulation of the pathways of the inflammatory response may be more feasible. Because of increasing knowledge of the mechanism of inflammation and the pathogenesis of cutaneous inflammatory diseases, it is predictable that effective nonsteroidal anti-inflammatory drugs for topical use will be developed some time in the future. Lastly, the effects and side effects can now be limited to the site of application, thus avoiding systemic risks, by optimising corticosteroid activity with respect to receptor binding and pharmacokinetic properties. However, it is realistic to assume that, even in the future, corticosteroids will always possess both desirable and undesirable properties.
在皮肤病治疗中，需要强效药物作为皮质类固醇的替代品，但这些药物不能有不良的局部和全身效应。已经提出了开发此类先进药物的三种理论可能性。首先，有人提出通过选择某种皮质类固醇结构来分离所需效应和不良效应。然而，这是不可能的，因为皮质类固醇受体无处不在，且都表现出相同的特异性。其次，操纵炎症反应途径可能更可行。由于对炎症机制和皮肤炎症性疾病发病机制的了解不断增加，可以预见在未来的某个时候会开发出有效的局部用非甾体抗炎药。最后，通过优化皮质类固醇在受体结合和药代动力学特性方面的活性，现在可以将效应和副作用限制在应用部位，从而避免全身风险。然而，现实的假设是，即使在未来，皮质类固醇也将始终具有 desirable 和 undesirable 的特性。 （注：原文中“desirable”和“undesirable”未明确中文释义，保留英文）
