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异维A酸

Isotretinoin.

作者信息

Khalil Nasr Y, Darwish Ibrahim A, Al-Qahtani Abdulmohsen A

机构信息

Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.

Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia; Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Assiut University, Assiut, Egypt.

出版信息

Profiles Drug Subst Excip Relat Methodol. 2020;45:119-157. doi: 10.1016/bs.podrm.2019.10.005. Epub 2019 Dec 6.

Abstract

Isotretinoin is chemically named as: (2Z, 4E, 6E, 8E)-3,7-Dimethyl-9-(2,6,6-trimethylcyclohex-1-enyl)nona-2,4,6,8-tetraenoic acid. It is an orally active retinoic acid derivative for the treatment of severe refractory nodulocystic acne. It acts primarily by reducing sebaceous gland size and sebum production, and as a result alters skin surface lipid composition. Using isotretinoin for 1-2mg/kg/day for 3-4 months produces 60%-95% clearance of inflammatory lesions in patients with acne. Doses as low as 0.1mg/kg/day have also proven successful in the clearance of lesions. Encouraging results have also been seen in small numbers of patients with rosacea, Side effects affecting the mucocutaneous system and raised serum triglyceride levels occur in most patients receiving isotretinoin. Isotretinoin is strictly contraindicated in women of childbearing potential. This profile discusses and explains names of isotretinoin, its physical and chemical characteristics. It also includes methods of preparation, thermal and spectral behavior, methods of analysis, and pharmacology.

摘要

异维A酸的化学名称为:(2Z, 4E, 6E, 8E)-3,7-二甲基-9-(2,6,6-三甲基环己-1-烯基)壬-2,4,6,8-四烯酸。它是一种口服活性维甲酸衍生物,用于治疗重度难治性结节囊肿性痤疮。其主要作用是减小皮脂腺大小并减少皮脂分泌,从而改变皮肤表面脂质成分。以1 - 2mg/kg/天的剂量使用异维A酸3 - 4个月,可使痤疮患者的炎性皮损清除率达到60% - 95%。低至0.1mg/kg/天的剂量在皮损清除方面也已证实有效。在少数酒渣鼻患者中也观察到了令人鼓舞的效果。大多数接受异维A酸治疗的患者会出现影响黏膜皮肤系统的副作用以及血清甘油三酯水平升高。育龄期女性严格禁用异维A酸。本简介讨论并解释了异维A酸的名称、其物理和化学特性。还包括其制备方法、热行为和光谱行为、分析方法以及药理学。

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