Pharmacokinetic-Pharmacodynamic Model for the Reversal of Neuromuscular Blockade by Sugammadex

苏伽马德克斯 罗库溴铵 神经肌肉阻滞 医学 药效学 药代动力学 麻醉 封锁 药理学 内科学 异丙酚 受体
作者
Bart A. Ploeger,Jean Smeets,Ashley Strougo,Henk‐Jan Drenth,G.S.F. Ruigt,Natalie Houwing,Meindert Danhof
出处
期刊:Anesthesiology [Lippincott Williams & Wilkins]
卷期号:110 (1): 95-105 被引量:42
标识
DOI:10.1097/aln.0b013e318190bc32
摘要

Background Sugammadex selectively binds steroidal neuromuscular blocking drugs, leading to reversal of neuromuscular blockade. The authors developed a pharmacokinetic-pharmacodynamic model for reversal of neuromuscular blockade by sugammadex, assuming that reversal results from a decrease of free drug in plasma and/or neuromuscular junction. The model was applied for predicting the interaction between sugammadex and rocuronium or vecuronium. Methods Noninstantaneous equilibrium of rocuronium-sugammadex complex formation was assumed in the pharmacokinetic-pharmacodynamic interaction model. The pharmacokinetic parameters for the complex and sugammadex alone were assumed to be identical. After development of a pharmacokinetic-pharmacodynamic model for rocuronium alone, the interaction model was optimized using rocuronium and sugammadex concentration data after administration of 0.1-8 mg/kg sugammadex 3 min after administration of 0.6 mg/kg rocuronium. Subsequently, the predicted reversal of neuromuscular blockade by sugammadex was compared with data after administration of up to 8 mg/kg sugammadex at reappearance of second twitch of the train-of-four; or 3, 5, or 15 min after administration of 0.6 mg/kg rocuronium. Finally, the model was applied to predict reversal of vecuronium-induced neuromuscular blockade. Results Using the in vitro dissociation constants for the binding of rocuronium and vecuronium to sugammadex, the pharmacokinetic-pharmacodynamic interaction model adequately predicted the increase in total rocuronium and vecuronium plasma concentrations and the time-course of reversal of neuromuscular blockade. Conclusions Model-based evaluation supports the hypothesis that reversal of rocuronium- and vecuronium-induced neuromuscular blockade by sugammadex results from a decrease in the free rocuronium and vecuronium concentration in plasma and neuromuscular junction. The model is useful for prediction of reversal of rocuronium and vecuronium-induced neuromuscular blockade with sugammadex.

科研通智能强力驱动
Strongly Powered by AbleSci AI
更新
PDF的下载单位、IP信息已删除 (2025-6-4)

科研通是完全免费的文献互助平台,具备全网最快的应助速度,最高的求助完成率。 对每一个文献求助,科研通都将尽心尽力,给求助人一个满意的交代。
实时播报
风趣的烨磊完成签到,获得积分10
1秒前
越啊发布了新的文献求助20
1秒前
过氧化氢发布了新的文献求助10
1秒前
yanaiqi关注了科研通微信公众号
3秒前
bkagyin应助王汉韬采纳,获得10
3秒前
4秒前
4秒前
crazy发布了新的文献求助10
4秒前
量子星尘发布了新的文献求助10
5秒前
nightmare发布了新的文献求助10
6秒前
Lili发布了新的文献求助10
7秒前
kingwill应助南韵采纳,获得20
8秒前
10秒前
Poik完成签到,获得积分10
10秒前
刘娅铷发布了新的文献求助10
10秒前
12秒前
小小吴完成签到,获得积分10
13秒前
不孤独的发卡完成签到,获得积分20
13秒前
潘善若发布了新的文献求助30
16秒前
zzzjh完成签到,获得积分10
16秒前
香蕉觅云应助超级采纳,获得10
18秒前
18秒前
安然完成签到 ,获得积分10
23秒前
桔子完成签到,获得积分10
23秒前
23秒前
落后的哈密瓜完成签到,获得积分10
24秒前
潘善若发布了新的文献求助10
25秒前
Rainbow完成签到 ,获得积分10
26秒前
28秒前
SciGPT应助momo采纳,获得10
28秒前
28秒前
Lili完成签到,获得积分10
29秒前
29秒前
30秒前
congyjs完成签到,获得积分20
32秒前
超级发布了新的文献求助10
33秒前
33秒前
潘善若发布了新的文献求助10
34秒前
Rondab应助胡图图采纳,获得10
34秒前
34秒前
高分求助中
A new approach to the extrapolation of accelerated life test data 1000
ACSM’s Guidelines for Exercise Testing and Prescription, 12th edition 500
‘Unruly’ Children: Historical Fieldnotes and Learning Morality in a Taiwan Village (New Departures in Anthropology) 400
Indomethacinのヒトにおける経皮吸収 400
Phylogenetic study of the order Polydesmida (Myriapoda: Diplopoda) 370
基于可调谐半导体激光吸收光谱技术泄漏气体检测系统的研究 350
Robot-supported joining of reinforcement textiles with one-sided sewing heads 320
热门求助领域 (近24小时)
化学 材料科学 医学 生物 工程类 有机化学 生物化学 物理 内科学 纳米技术 计算机科学 化学工程 复合材料 遗传学 基因 物理化学 催化作用 冶金 细胞生物学 免疫学
热门帖子
关注 科研通微信公众号,转发送积分 3989297
求助须知:如何正确求助?哪些是违规求助? 3531418
关于积分的说明 11253893
捐赠科研通 3270097
什么是DOI,文献DOI怎么找? 1804884
邀请新用户注册赠送积分活动 882087
科研通“疑难数据库(出版商)”最低求助积分说明 809158