Belaube P, Garcin G, Marchand J P, Privat Y
Sem Hop. 1983 Dec 8;59(45):3101-4.
Thalidomide (alpha-N-phtalimido-glutarimide) was withdrawn from sale in 1961 since it was held responsible for the birth of hundreds of phocomelus children. Despite this teratogenic potential, thalidomide remains a useful tool in the treatment of erythema nodosum leprosum, as well as in discoid lupus erythematosus when antimalarial drugs are ineffective or contraindicated. In addition, good results have been reported in several diseases such as actinic prurigo, polymorphous light eruption, Behçet syndrome, Weber-Christian disease, prurigo nodularis, pyoderma gangrenosum and ulcerative colitis. The mechanism of action is under debate but it is likely that thalidomide has immunomodulating properties by controlling T-suppressor lymphocytes, and anti-inflammatory effects, particularly an inhibition of neutrophil chemotaxis. Several attempts at synthesis of effective thalidomide derivatives devoid of teratogenic effects are ongoing.
沙利度胺(α-N-邻苯二甲酰谷氨酸亚胺)于1961年被撤市,因为它被认为是导致数百名海豹肢症患儿出生的原因。尽管有这种致畸潜力,但沙利度胺在治疗麻风结节性红斑以及抗疟药无效或禁忌时的盘状红斑狼疮方面仍是一种有用的药物。此外,在多种疾病如光化性瘙痒症、多形性日光疹、白塞综合征、韦格纳-克里斯蒂安病、结节性痒疹、坏疽性脓皮病和溃疡性结肠炎中也报道了良好的疗效。其作用机制仍在争论中,但沙利度胺可能通过控制T抑制淋巴细胞具有免疫调节特性,以及具有抗炎作用,特别是抑制中性粒细胞趋化性。目前正在进行多项合成无致畸作用的有效沙利度胺衍生物的尝试。