Barth L, Dannhorn R
Prakt Anaesth. 1979 Aug;14(4):303-12.
In 48 patients anaesthetized with nitrous oxide-oxygen and hexobarbitone the neuromuscular (n-m) block (greater than or equal to 95% depression) produced by roughly equipotent doses of d-tubocurarine (dTC), gallamine (GALL), pancuronium (PANC) or alcuronium (ALC), respectively, was antagonized by 10 mg of pyridostigmine (P) applied intravenously 35-460 min after the relaxant at variable levels of spontaneous recovery from n-m block. Muscular reactions to tetanic stimulation (30 to 400 Hz, 4-5 s each) of the ulnar nerve transmitted by a force-displacement system served as a measure for calculating the relative amount of n-m receptors liberated from relaxant molecules. Within 3-10 min after its injection P increased the number of relaxant-free n-m receptors by 16 +/- 6% (M +/- SD). Thereafter recovery progressed at similar speed as before. Reinjections of 5-10 mg P were comparably as effective as the first injection. No correlations were to be found between the effectiveness of P and the dose of relaxant applied (r = 0,12 to 0,27), the level of recovery reached before P (r = 0,32), or the time at which P was injected after the relaxant (r = -0,39), respectively. However, the amount of receptors liberated by P decreased with increasing recovery from n-m block and with increasing time interval between the relaxant and the antidote injection. P was significantly more effective (P less than 0,01), when applied within 150 min after the relaxant than at applications after that time. The relative number of receptors liberated by this drug was insignificantly larger in the PANC-and GALL-block than in the ALC-and dTC-block.
在48例接受氧化亚氮 - 氧气和己巴比妥麻醉的患者中,分别给予大致等效剂量的d - 筒箭毒碱(dTC)、加拉明(GALL)、泮库溴铵(PANC)或阿库氯铵(ALC)产生神经肌肉(n - m)阻滞(大于或等于95%抑制),在肌肉松弛剂作用后35 - 460分钟,于不同程度的n - m阻滞自发恢复水平下,静脉注射10毫克新斯的明(P)进行拮抗。通过力 - 位移系统传递的尺神经强直刺激(30至400赫兹,每次4 - 5秒)引起的肌肉反应,作为计算从松弛剂分子释放的n - m受体相对数量的指标。注射后3 - 10分钟内,P使无松弛剂的n - m受体数量增加了16±6%(均值±标准差)。此后恢复速度与之前相似。再次注射5 - 10毫克P的效果与首次注射相当。P的有效性与所用松弛剂剂量(r = 0.12至0.27)、P给药前达到的恢复水平(r = 0.32)或松弛剂后注射P的时间(r = -0.39)之间均未发现相关性。然而,随着n - m阻滞恢复程度的增加以及松弛剂与解毒剂注射时间间隔的延长,P释放的受体数量减少。与松弛剂注射后150分钟之后给药相比,在150分钟内给药时P的效果显著更佳(P<0.01)。该药物释放的受体相对数量在PANC和GALL阻滞中比在ALC和dTC阻滞中略大。