Roll Antonie, Reich Kristian, Boer Almut
Department of Dermatology, Dermatologikum, Hamburg, Germany.
Indian J Dermatol Venereol Leprol. 2007 Mar-Apr;73(2):133-7. doi: 10.4103/0378-6323.31908.
Fumaric acid esters (FAE) are chemical compounds derived from the unsaturated dicarbonic acid fumaric acid. The usage of FAEs in treatment of psoriasis was introduced in the late 1950's. In the 1980s more standardized oral preparations of FAEs were developed containing dimethylfumarate (DMF) and salts of monoethylfumarate (MEF) as main compounds. In 1994, Fumaderm an enteric-coated tablet containing DMF and calcium, magnesium and zinc salts of MEF was approved for the treatment of psoriasis in Germany and since then has become the most commonly used systemic therapy in this country. Fumaric acids have been proven to be an effective therapy in patients with psoriasis even though the mechanisms of action are not completely understood. About 50-70% of the patients achieve PASI 75 improvement within four months of treatment and without any long-term toxicity, immunosuppressive effects or increased risk of infection or malignancy. Tolerance is limited by gastrointestinal side effects and flushing of the skin. This article reviews pharmacokinetics, uses, contraindications, dosages and side effects of treatment with FAEs.
富马酸酯(FAE)是源自不饱和二元羧酸富马酸的化合物。20世纪50年代末引入了富马酸酯在银屑病治疗中的应用。20世纪80年代开发出了更标准化的富马酸酯口服制剂,其主要成分包含富马酸二甲酯(DMF)和富马酸单乙酯(MEF)盐。1994年,含有DMF以及MEF的钙、镁和锌盐的肠溶衣片剂Fumaderm在德国被批准用于治疗银屑病,自那时起它已成为该国最常用的全身治疗方法。富马酸已被证明对银屑病患者是一种有效的治疗方法,尽管其作用机制尚未完全了解。约50 - 70%的患者在治疗四个月内实现银屑病面积和严重程度指数(PASI)改善75%,且无任何长期毒性、免疫抑制作用或感染或恶性肿瘤风险增加。耐受性受胃肠道副作用和皮肤潮红的限制。本文综述了富马酸酯治疗的药代动力学、用途、禁忌证、剂量和副作用。