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健康人体志愿者肌内注射 F(ab')2 型蝎毒抗血清的药代动力学。

Pharmacokinetics of a F(ab')2 scorpion antivenom administered intramuscularly in healthy human volunteers.

机构信息

Laboratorios Silanes SA de CV, México.

出版信息

Int Immunopharmacol. 2010 Nov;10(11):1318-24. doi: 10.1016/j.intimp.2010.08.018. Epub 2010 Sep 17.

Abstract

This paper presents the first study of F(ab')(2) scorpion antivenom pharmacokinetics in humans after intramuscular (im) administration. The specific anti-Centruroides scorpion antivenom was used in 6 human healthy volunteers. The fabotherapeutic was administered as a 47.5mg im bolus. Blood samples were drawn at 0, 5, 15, 30, 45, 60 , 90, 120, and 180 min, 6h and at 1, 2, 3, 4, 10 and 21 days after antivenom administration. We measured antivenom concentrations in serum using a specific high sensitivity ELISA method for F(ab')(2). Antivenom concentration in serum was fit to a 3 compartment model (inoculation site, plasma and extra vascular extracellular space), it was assumed that the venom may also be irreversibly removed from plasma. Calculated time course of antivenom content shows that at any time no more that 16.6 (5.3, 31.9)% (median and 95% confidence interval) of the antivenom bolus is present in plasma. The time to peak plasma [F(ab')(2)] was 45 (33, 74) h. The most significant antivenom pharmacokinetic parameters determined were: AUC(im,∞)=803 (605, 1463) mg·h·L(-1); V(c)=8.8 (2.8, 23.6) L; V(ss,im)=55 (47, 64) L; MRT(im)=776(326, 1335) h; CL(t)=3.7 (0.6, 1.9) mL·min(-1); f(im,)V(ss)=0.300 (0.153, 0.466). Comparing these parameters with the ones obtained intravenously by Vázquez et al., the parameters were more disperse between subjects, determined with more uncertainty in each individual subject, and the peak F(ab')(2) in plasma occurred with considerable delay; all indicating that the IM route should not be used to administer the antivenom, with the possible exception of cases occurring very far from hospitals, as an extreme means to provide some protection before the IV route becomes available.

摘要

本文首次研究了肌内(IM)给予 F(ab')(2) 蝎毒抗血清后在人体内的药代动力学。在 6 名健康志愿者中使用了特异性抗 Centruroides 蝎毒抗血清。Fab 治疗剂以 47.5mg IM 推注给药。在抗血清给药后 0、5、15、30、45、60、90、120 和 180 分钟、6 小时以及 1、2、3、4、10 和 21 天采血。我们使用针对 F(ab')(2) 的特异性高灵敏度 ELISA 方法测量血清中的抗血清浓度。将血清中抗血清浓度拟合到 3 室模型(接种部位、血浆和血管外细胞外空间),假设毒液也可能从血浆中不可逆地清除。计算抗血清含量的时间过程表明,在任何时候,都不会有超过 16.6(5.3,31.9)%(中位数和 95%置信区间)的抗血清推注剂量存在于血浆中。血浆中 [F(ab')(2)] 的达峰时间为 45(33,74)h。确定的最重要的抗血清药代动力学参数为:AUC(im,∞)=803(605,1463)mg·h·L(-1);V(c)=8.8(2.8,23.6)L;V(ss,im)=55(47,64)L;MRT(im)=776(326,1335)h;CL(t)=3.7(0.6,1.9)mL·min(-1);f(im,)V(ss)=0.300(0.153,0.466)。将这些参数与 Vázquez 等人静脉内获得的参数进行比较,表明各参数在个体之间更为分散,在每个个体中确定的不确定性更大,并且血浆中 F(ab')(2) 的峰值出现明显延迟;所有这些都表明,除了在远离医院的非常情况下,作为在获得静脉途径之前提供一些保护的极端手段,不应该使用肌内途径给予抗血清。

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