Takeda K, Arase S, Takahashi S
Tokushima University School of Medicine, Japan.
Drugs. 1988;36 Suppl 5:15-23. doi: 10.2165/00003495-198800365-00005.
The goal of topical corticosteroid therapy is to maximise the clinical benefits of this highly effective group of drugs, while minimising their adverse effects. Many types of steroid-induced skin lesions and skin atrophy can occur by such mechanisms as the suppression of cell proliferation, immunosuppression, or hormonal activity, and a trend towards an increased incidence of steroid-induced dermatological disturbances has been observed in recent years. Systemic effects have also been documented. To reduce the risk of local and systemic effects, it is necessary to consider factors such as the intrinsic potency of a drug, type of vehicle used and frequency of application. A potent drug may be changed to a less potent one, or the dosage reduced. Once-daily application is often as effective as three-times-daily application, and intermittent application can also be recommended. The concept of an 'ante-drug' promises new developments in topical corticosteroid therapy. An 'ante-drug', e.g. difluprednate, has potent efficacy but fewer side effects than conventional therapy, since it acts at the application site and then is metabolised to less active or inactive compounds before reaching the systemic circulation. It is likely that future corticosteroids will have the attributes of an ante-drug, thus greatly reducing the risk of systemic effects. At present, however, it is still necessary to recognise the influence of various drug and patient factors that contribute to side effects, in order to balance clinical efficacy with an acceptable side effect profile.
局部用皮质类固醇疗法的目标是在将这类高效药物的不良反应降至最低的同时,最大化其临床益处。多种类型的类固醇诱导性皮肤损伤和皮肤萎缩可通过抑制细胞增殖、免疫抑制或激素活性等机制发生,并且近年来已观察到类固醇诱导性皮肤疾病的发病率有上升趋势。全身效应也有文献记载。为降低局部和全身效应的风险,有必要考虑药物的内在效力、所用赋形剂类型和用药频率等因素。可将强效药物换成效力较弱的药物,或减少剂量。每日一次用药通常与每日三次用药效果相同,也可推荐间歇性用药。“前体药物”的概念有望为局部用皮质类固醇疗法带来新进展。一种“前体药物”,如双氟泼尼酯,具有强效疗效,但副作用比传统疗法少,因为它在用药部位起作用,然后在进入体循环之前代谢为活性较低或无活性的化合物。未来的皮质类固醇可能会具备前体药物的特性,从而大大降低全身效应的风险。然而目前,仍有必要认识到导致副作用的各种药物和患者因素的影响,以便在临床疗效与可接受的副作用之间取得平衡。