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阿达帕林。对其药理学特性及治疗轻至中度痤疮临床潜力的综述。

Adapalene. A review of its pharmacological properties and clinical potential in the management of mild to moderate acne.

作者信息

Brogden R N, Goa K E

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs. 1997 Mar;53(3):511-9. doi: 10.2165/00003495-199753030-00010.

Abstract

Adapalene, a naphthoic acid derivative with retinoid-like activity, is used for the topical treatment of mild to moderate acne vulgaris. It binds to retinoic acid receptors found predominantly in the terminal differentiation zone of epidermis and is more active than tretinoin in modulating cellular differentiation. Adapalene exhibits anti-inflammatory activity in various in vitro and in vivo models. To date, adapalene 0.1% gel and lotion formulations have been compared only with tretinoin 0.025% gel. In these comparisons, adapalene 0.1% aqueous gel was at least as effective as tretinoin and in some studies was significantly better at reducing the numbers of noninflammatory, inflammatory and total facial lesions in patients with mild to moderate acne. In such comparisons, the cutaneous tolerability of adapalene aqueous gel was generally better than that of tretinoin. On the basis of published data, adapalene aqueous 0.1% gel is an effective and generally better tolerated alternative to tretinoin 0.025% gel for the topical treatment of patients with mild to moderate acne.

摘要

阿达帕林是一种具有类视黄醇活性的萘甲酸衍生物,用于局部治疗轻至中度寻常痤疮。它与主要在表皮终末分化区发现的维甲酸受体结合,在调节细胞分化方面比维甲酸更具活性。阿达帕林在各种体外和体内模型中均表现出抗炎活性。迄今为止,仅将0.1%的阿达帕林凝胶和洗剂配方与0.025%的维甲酸凝胶进行了比较。在这些比较中,0.1%的阿达帕林水凝胶至少与维甲酸一样有效,并且在一些研究中,在减少轻至中度痤疮患者的非炎性、炎性和面部总皮损数量方面明显更好。在这类比较中,阿达帕林水凝胶的皮肤耐受性通常优于维甲酸。根据已发表的数据,0.1%的阿达帕林水凝胶是一种有效且耐受性通常更好的替代药物,可用于替代0.025%的维甲酸凝胶对轻至中度痤疮患者进行局部治疗。

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