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[静脉麻醉药药代动力学的现代概念]

[Modern concepts in pharmacokinetics of intravenous anesthetics].

作者信息

Heidegger T, Minto C F, Schnider T W

机构信息

Institut für Anästhesiologie, Kantonsspital St. Gallen, St. Gallen, Switzerland.

出版信息

Anaesthesist. 2004 Jan;53(1):95-110. doi: 10.1007/s00101-003-0628-2.

DOI:10.1007/s00101-003-0628-2
PMID:14994741
Abstract

From a pharmacological perspective, anesthesia is concerned with controlling the time course of drug effect. Mathematical models are commonly used to relate the administered drug dose to the measured drug concentration (a pharmacokinetic model) and to relate the measured drug concentrations to the measured drug effects (a pharmacodynamic model). With such models, the time course of the drug effect for different drug regimens can be predicted. Although the conventional pharmacokinetic parameters such as the volume of distribution, clearance, distribution and elimination half-lives can be used to accurately describe the time course of the plasma concentration, the plasma is usually not the site of drug effect. An understanding of the "effect compartment concept" and the "time of the peak effect site concentration," together with the concepts of" context sensitive"half-time and "relevant decrement time,' contribute substantially to the anesthetist's understanding of the principles governing the onset and offset of drug effect. As part of a computer-controlled infusion system, the pharmacokinetic model facilitates optimized and rational dosing. These systems, also called target-controlled infusion systems (TCI), calculate the infusion rates for rapidly achieving and then maintaining a target concentration.

摘要

从药理学角度来看,麻醉涉及控制药物效应的时间进程。数学模型通常用于将给药剂量与测得的药物浓度相关联(药代动力学模型),并将测得的药物浓度与测得的药物效应相关联(药效动力学模型)。利用这些模型,可以预测不同给药方案的药物效应时间进程。尽管传统的药代动力学参数,如分布容积、清除率、分布半衰期和消除半衰期,可用于准确描述血浆浓度的时间进程,但血浆通常不是药物作用的部位。对“效应室概念”和“效应部位浓度峰值时间”的理解,以及“上下文敏感”半衰期和“相关衰减时间”的概念,极大地有助于麻醉医生理解药物效应起效和消退的原理。作为计算机控制输注系统的一部分,药代动力学模型有助于优化和合理给药。这些系统,也称为靶控输注系统(TCI),计算输注速率以快速达到并维持目标浓度。

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1
[Modern concepts in pharmacokinetics of intravenous anesthetics].[静脉麻醉药药代动力学的现代概念]
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Clin Pharmacokinet. 2006;45(11):1051-60. doi: 10.2165/00003088-200645110-00001.
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[Effect compartment equilibration and time-to-peak effect. Importance of a pharmacokinetic-pharmacodynamic principle for the daily clinical practice].

本文引用的文献

1
Using the time of maximum effect site concentration to combine pharmacokinetics and pharmacodynamics.利用效应室浓度达峰时间结合药代动力学和药效学。
Anesthesiology. 2003 Aug;99(2):324-33. doi: 10.1097/00000542-200308000-00014.
2
Identification and targeting policies for computer-controlled infusion pumps.计算机控制输液泵的识别与定位策略
Crit Rev Biomed Eng. 2000;28(1-2):179-85. doi: 10.1615/critrevbiomedeng.v28.i12.300.
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Targeting effect compartment or central compartment concentration of propofol: what predicts loss of consciousness?
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Anaesthesist. 2005 Oct;54(10):1021-31. doi: 10.1007/s00101-005-0864-8.
丙泊酚的靶向效应室或中央室浓度:什么能预测意识消失?
Anesthesiology. 1999 Jan;90(1):92-7. doi: 10.1097/00000542-199901000-00014.
4
Determination of the distribution volume that can be used to calculate the intravenous loading dose.用于计算静脉注射负荷剂量的分布容积的测定。
Clin Pharmacokinet. 1998 Jul;35(1):1-7. doi: 10.2165/00003088-199835010-00001.
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A physiological model of induction of anaesthesia with propofol in sheep. 1. Structure and estimation of variables.绵羊丙泊酚麻醉诱导的生理模型。1. 变量的结构与估计
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Context-sensitive half-times and other decrement times of inhaled anesthetics.吸入麻醉药的情境敏感半衰期及其他衰减时间。
Anesth Analg. 1997 Sep;85(3):681-6. doi: 10.1097/00000539-199709000-00036.
7
Influence of age and gender on the pharmacokinetics and pharmacodynamics of remifentanil. I. Model development.年龄和性别对瑞芬太尼药代动力学和药效学的影响。I. 模型建立。
Anesthesiology. 1997 Jan;86(1):10-23. doi: 10.1097/00000542-199701000-00004.
8
Pharmacokinetic parameters relevant to recovery from opioids.与阿片类药物恢复相关的药代动力学参数。
Anesthesiology. 1994 Oct;81(4):833-42. doi: 10.1097/00000542-199410000-00010.
9
Technique for quantifying the duration of intravenous anesthetic effect.静脉麻醉效果持续时间的量化技术。
Anesthesiology. 1995 Nov;83(5):1095-103. doi: 10.1097/00000542-199511000-00024.
10
Performance of computer-controlled infusion of propofol: an evaluation of five pharmacokinetic parameter sets.丙泊酚计算机控制输注的性能:五种药代动力学参数集的评估
Anesth Analg. 1995 Dec;81(6):1275-82. doi: 10.1097/00000539-199512000-00026.