注射用替加环素临床前安全性研究.PDF

Drug Evaluation Research 第 37 卷 第 5 期 2014 年 10 月 - 441 - 注射用替加环素临床前安全性研究 赵 涛，牟丽丽，李 斌，王现珍，张莹莹，王恩力，李 欣* 鲁南制药集团股份有限公司新药安评中心，山东 临沂 273400 摘 要：目的 评价注射用替加环素的安全性。方法 对注射用替加环素进行血管刺激、肌肉刺激、溶血性及被动皮肤过敏、 全身主动过敏性、类过敏性试验。结果 注射用替加环素对血管无明显刺激性、对肌肉组织产生轻度可逆性的刺激，对家兔 红细胞无溶血、凝聚作用，大鼠被动皮肤过敏反应（PCA ）试验未出现过敏反应；豚鼠全身主动过敏反应（ASA ）试验部分 豚鼠出现过敏反应；注射用替加环素与已上市药品 Tygacil 在同等剂量下，豚鼠出现同等程度的类过敏反应。结论 注射用 替加环素可能会引起肌肉刺激性及过敏、类过敏反应，临床应用时应关注患者给药后的反应。 关键词：注射用替加环素；血管刺激；肌肉刺激；溶血性；被动皮肤过敏；过敏及类过敏 中图分类号：R965.3 文献标志码：A 文章编号：1674 - 6376 (2014) 05 - 0441 - 04 DOI: 10.7501/j.issn.1674-6376.2014.05.015 Preclinical safety of Tigecycline for injection ZHAO Tao, MU Li-li, LI Bin, WANG Xian-zhen, ZHANG Ying-ying, WANG En-li, LI Xin Center for New Drug Safety Evaluation of Lunan Pharmaceutical Group Corporation, Linyi 273400, China Abstract: Objective To evaluate the safety of Tigecycline for injection. Methods The reactions of stimulation on blood vessel and muscle of rabbit, hemolysis, PCA on SD rat, ASA and anaphylactoid on Guinea pig were studied. Results No hypersensitive action was found on blood vessel, red cell, and PCA of rabbit, and mild reversible reactions on muscle tissue was observed. Anaphylactic and anaphylactoid reactions were found on some Guinea pigs. Tigecycline for injection and marketed drug Tygacil can cause anaphylactoid reaction in Guinea pigs with the same degree at an equivalent dose. Conclusion Tigecycline for injection may cause muscle stimulation, allergy, and anaphylactoid reaction, and the patients should be followed after taking the medicine. Key words: Tigecycline for injection; vascular irritation; muscle irritation; hemolysis; PCA; anaphylactic and anaphylactoid reactions 替加环素是第一个用于临床的甘氨酰四环素， 瓶，山东新时代药业有限公司。白蛋白（鸡蛋），批 经过结构改造使其抗菌活性优于四环素，抗菌谱广， 号 110209，规格 1 g/瓶，上海伯奥生物科技有限公 特别是临床上的多重耐药菌，如耐甲氧西林金黄色