24小时连续注入bivalirudin研究老鼠。

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格里森TG, Chengelis CP,杰克逊CB Lindstrom P

24小时连续注入bivalirudin研究老鼠。

Int J Toxicol。2003 May-Jun; 22 (3): 195 - 206。

PubMed ID

12851152 (在PubMed

]

文摘

的潜在毒性bivalirudin(一种抗凝剂)进行评估静脉输液Sprague-Dawley老鼠学习。Bivalirudin被连续静脉输液管理24小时到六组的老鼠。剂量水平的100、500和2000毫克/公斤/ 24小时选择低收入,中期,和高剂量组。三个12 bivalirudin-treated 12组雄性和雌性都指定的毒理学评估。6 /性/组动物安乐死在完成24小时输液,剩下的动物被分配给14天的恢复期。三个额外的10组大鼠/性/组指定的毒性动力学评估。这项研究包括生理盐水组和一个对照组。没有指出bivalirudin-related毒性。没有治疗相关的对临床病理学参数的影响。没有明确的测试相关文章宏观、器官重量或显微结构变化中被确认。 Three animals in the 500-mg/kg/24 h group, and 7 animals in the 2000-mg/kg/24 h group in the toxicokinetic assessment phase of the study were found dead or euthanized in extremis (following blood sampling). The concurrent clinical signs suggest that the animals hemorrhaged, which is consistent with the pharmacological action of bivalirudin. The extent of systemic exposure was similar in male and female rats, indicating a lack of a sex-related difference. Plasma concentrations of bivalirudin appeared to be linear and dose independent. Based on the results of this study, the no-observed-adverse-effect level (NOAEL) for bivalirudin, administered to rats via intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h. However, the known pharmacological properties of bivalirudin could result in hemorrhage in the presence of an appropriate challenge (e.g., blood collection).

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药物

Bivalirudin