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[阿维A酯可代谢回异维A酸。对口服维甲酸治疗的重要性]

[Trans-acitretin is metabolized back to etretinate. Importance for oral retinoid therapy].

作者信息

Almond-Roesler B, Orfanos C E

机构信息

Universitäts-Hautklinik und Poliklinik, Klinikum Benjamin Franklin der Freien Universität Berlin.

出版信息

Hautarzt. 1996 Mar;47(3):173-7. doi: 10.1007/s001050050398.

Abstract

The oral retinoid etretinate (Tigason) has recently been replaced by trans-acitretin (Neotigason) in the treatment of severe psoriasis, primarily because of its short half-life and the assumption that a shorter period of subsequent contraception would be required. After introduction of the new drug, however, circulating quantities of etretinate were detected in patients treated with trans-acitretin. Thus far, re-esterification has been detected in at least 83 cases. The 2-month period of strict contraception initially recommended after oral intake of trans-acitretin has been extended to 2 years, as with etretinate. We review some aspects of trans-acitretin metabolism, with special emphasis on etretinate formation. Re-esterification of trans-acitretin into etretinate takes place under varying conditions in volunteers and patients, as well as in animal models. Ethanol is a co-factor for the enzymatic re-esterification of trans-acitretin. It is unclear whether the introduction of trans-acitretin has been of any significant benefit to patients. Monitoring of plasma retinoid levels during and after retinoid therapy remains of decisive importance in managing difficult cases and or in approving decisions for pregnancy.

摘要

口服维甲酸依曲替酯(银屑灵)在重度银屑病治疗中最近已被阿维A(新银屑灵)所取代,主要是因为其半衰期短,且假定后续所需避孕期较短。然而,在使用阿维A治疗的患者中检测到了依曲替酯的循环量。到目前为止,至少在83例病例中检测到了再酯化现象。口服阿维A后最初建议的2个月严格避孕期已延长至2年,与依曲替酯情况相同。我们回顾了阿维A代谢的一些方面,特别强调依曲替酯的形成。阿维A再酯化形成依曲替酯在志愿者、患者以及动物模型的不同条件下都会发生。乙醇是阿维A酶促再酯化的辅助因子。阿维A的引入对患者是否有任何显著益处尚不清楚。在维甲酸治疗期间及之后监测血浆类视黄醇水平对于处理疑难病例和/或批准妊娠决定仍然至关重要。

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