Calvey T N, Wareing M, Williams N E, Chan K
Br J Clin Pharmacol. 1979 Feb;7(2):149-55. doi: 10.1111/j.1365-2125.1979.tb00915.x.
1 The pharmacokinetics of neostigmine was studied in six patients during the reversal of neuromuscular block induced by tubocurarine chloride. The effect of the drug on neuromuscular function was simultaneously assessed by electromyography. 2 Neostigmine was rapidly eliminated from plasma after intravenous administration. The decline in the plasma concentration of the drug was invariably resolved into two exponential components. The fast disposition (distribution) half-life of the drug was invariably less than 1 min; the slow disposition (elimination) half-life ranged from 15.4--31.7 min. 3 Neostigmine usually increased the amplitude of the compound muscle action potential and diminished electromyographic decrement within 2 min of intravenous injection. The pharmacological effect of neostigmine was usually maximal between 7 and 15 min. There was an inverse relationship between the plasma concentration of the drug and the facilitation of neuromuscular transmission. 4 Red cell acetylcholinesterase activity was almost completely inhibited within 2--3 min of intravenous injection of neostigmine. Enzyme activity recovered to approximately 28% of control values by 30 min and to 55% by 60 min.
1 在6例由氯化筒箭毒碱引起神经肌肉阻滞逆转过程中的患者身上研究了新斯的明的药代动力学。同时通过肌电图评估该药对神经肌肉功能的影响。2 静脉注射后新斯的明迅速从血浆中消除。该药血浆浓度的下降总是分解为两个指数成分。该药的快速处置（分布）半衰期总是小于1分钟；缓慢处置（消除）半衰期为15.4 - 31.7分钟。3 新斯的明通常在静脉注射后2分钟内增加复合肌肉动作电位的幅度并减少肌电图衰减。新斯的明的药理作用通常在7至15分钟之间达到最大。该药的血浆浓度与神经肌肉传递的易化之间存在反比关系。4 静脉注射新斯的明后2 - 3分钟内红细胞乙酰胆碱酯酶活性几乎完全被抑制。到30分钟时酶活性恢复到对照值的约28%，到60分钟时恢复到55%。
