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Tacrolimus 1994年于日本北部在免疫抑制剂的开发研究中,从土壤真菌streptomyces tsuku-baensinr的发酵液中分离而得,属大环内酯类抗生素,具有23员环状结构.1987年Ochiai报道了本品用于兔子具有免疫抑制活性,1989年Starzl报道了本品首次用于肝移植病人的情况.1993年6月作为肝抑制排斥反应抑制剂首先于日本上市,1994年获得美国FDA批准在美国上市,随后又在欧洲共同体国家上市.在日本、美国、欧洲本上已经得到了较广泛的临床应用,在肝、肾、心、肺、小肠移植病人显示出有效的免疫抑制活性.1 药理作用
Tacrolimus was isolated from the fermentation broth of soil fungus streptomyces tsuku-baensinr in northern Japan in 1994 for its immunosuppressant development and belongs to a macrolide antibiotic with a 23-membered ring structure. In 1987, Ochiai reported This product is used for rabbits with immunosuppressive activity, 1989 Starzl reported the first time this product was used in patients with liver transplantation in 1993 June as a liver suppression rejection inhibitor first listed in Japan in 1994, the United States FDA approved in the United States Listed, and later listed in the European Community countries in Japan, the United States, Europe, has been the majority of the clinical application has been in liver, kidney, heart, lung, small bowel transplantation patients showed effective immunosuppressive activity.1 pharmacological effects