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壬二酸。对其药理学特性以及在痤疮和色素沉着性皮肤病中的治疗效果的综述。

Azelaic acid. A review of its pharmacological properties and therapeutic efficacy in acne and hyperpigmentary skin disorders.

作者信息

Fitton A, Goa K L

机构信息

Adis Drug Information Services, Auckland, New Zealand.

出版信息

Drugs. 1991 May;41(5):780-98. doi: 10.2165/00003495-199141050-00007.

Abstract

Azelaic acid is a naturally occurring saturated dicarboxylic acid which, on topical application (usually as a 20% cream), has been shown to be effective in the treatment of comedonal acne and inflammatory (papulopustular, nodular and nodulocystic) acne, as well as various cutaneous hyperpigmentary disorders characterised by hyperactive/abnormal melanocyte function, including melasma and, possibly, lentigo maligna. In addition, azelaic acid has an antiproliferative and cytotoxic effect on the human malignant melanocyte, and preliminary findings indicate that it may arrest the progression of cutaneous malignant melanoma. The mechanism of this selective cytotoxic action of azelaic acid is unclear, but may possibly be related to its inhibition of mitochondrial oxidoreductase activity and DNA synthesis. In controlled studies, topical azelaic acid demonstrated comparable anti-acne efficacy to topical tretinoin, benzoyl peroxide, erythromycin and oral tetracycline, while in patients with melasma azelaic acid proved at least as effective as topical hydroquinone. On topical application azelaic acid is well tolerated, with adverse effects apparently limited to a generally mild and transient local cutaneous irritation. Thus, topical azelaic acid, employed either as monotherapy or in combination with other treatments, is likely to prove of value in the management of acne and several hyperpigmentary disorders, most notably melasma.

摘要

壬二酸是一种天然存在的饱和二羧酸,局部应用(通常为20%乳膏)已显示对粉刺性痤疮和炎性(丘疹脓疱性、结节性和结节囊肿性)痤疮以及各种以黑素细胞功能亢进/异常为特征的皮肤色素沉着障碍有效,包括黄褐斑以及可能的恶性雀斑样痣。此外,壬二酸对人恶性黑素细胞具有抗增殖和细胞毒性作用,初步研究结果表明它可能会阻止皮肤恶性黑色素瘤的进展。壬二酸这种选择性细胞毒性作用的机制尚不清楚,但可能与其抑制线粒体氧化还原酶活性和DNA合成有关。在对照研究中,局部应用壬二酸显示出与局部应用维甲酸、过氧化苯甲酰、红霉素和口服四环素相当的抗痤疮疗效,而在黄褐斑患者中,壬二酸被证明至少与局部应用氢醌一样有效。局部应用壬二酸耐受性良好,不良反应显然仅限于一般轻度和短暂的局部皮肤刺激。因此,局部应用壬二酸,无论是作为单一疗法还是与其他治疗联合使用,在痤疮和几种色素沉着障碍(最显著的是黄褐斑)的治疗中可能都具有价值。

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