Kitzman J V, Wilson R C, Booth N H, Hendricks H L, Bush P B
Department of Physiology and Pharmacology, College of Veterinary Medicine, The University of Georgia, Athens, GA 30602, USA.
Am J Vet Res. 1984 Jul;45(7):1333-5.
The pharmacokinetics of 4-aminopyridine (4-AP), a drug capable of antagonizing nondepolarizing neuromuscular blocking drugs, as well as several classes of injectable sedative and anesthetic agents, were studied in 6 intact, awake horses. Plasma samples were assayed for 4-AP over a frequent sampling schedule for 8 hours after IV administration. The plasma 4-AP vs time data best fit a 2-compartment pharmacokinetic model. Distribution half-life was 7.4 minutes, elimination half-life was 259 minutes, volume of the central compartment was 0.89 L/kg, volume of distribution (area) was 1.98 L/kg, volume of distribution at steady state was 1.9 L/kg, and total clearance was 5.3 ml min(-1) kg(-1). The 259-minute elimination halflife observed in the present study is consistent with prolonged clinical effectiveness observed in a previous study of antagonism of xylazine/ketamine anesthesia by 4-AP in horses.
在6匹健康、清醒的马身上研究了4-氨基吡啶（4-AP）的药代动力学，4-AP是一种能够拮抗非去极化神经肌肉阻滞剂以及几类注射用镇静剂和麻醉剂的药物。静脉给药后，按照频繁采样计划在8小时内对血浆样本进行4-AP检测。血浆4-AP浓度与时间数据最符合二室药代动力学模型。分布半衰期为7.4分钟，消除半衰期为259分钟，中央室容积为0.89 L/kg，分布容积（面积）为1.98 L/kg，稳态分布容积为1.9 L/kg，总清除率为5.3 ml·min⁻¹·kg⁻¹。本研究中观察到的259分钟消除半衰期与先前一项关于4-AP拮抗马的赛拉嗪/氯胺酮麻醉的研究中观察到的临床效果延长一致。
