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常见镇痛药和解热药的药代动力学考量

Pharmacokinetic considerations of common analgesics and antipyretics.

作者信息

Hartwig-Otto H

出版信息

Am J Med. 1983 Nov 14;75(5A):30-7. doi: 10.1016/0002-9343(83)90230-9.

DOI:10.1016/0002-9343(83)90230-9
PMID:6606362
Abstract

Knowledge of pharmacokinetics (action of organisms on drugs) and pharmacodynamics (drug action on living organisms) allows for the proper assessment of the most suitable dose, dosing intervals, route of administration, as well as dose adjustment when clinically indicated. The basic physical scientific principles of the movement of drug particles across biologic barriers, their subsequent conversion to other chemical forms, and their elimination are reviewed in general terms. The specific metabolic pathways for aspirin and paracetamol (acetaminophen) are then discussed in more detail. Elimination of salicylate involves two saturable (nonlinear) major pathways and three apparently first-order (linear) minor pathways; these mixed order kinetics lead to somewhat complex mathematics affecting elimination half-life which, in turn, can have implications for anticipating side effects and toxicity. The kinetics of acetaminophen also involve various pathways, but studies have shown a good correlation between the expected and the observed elimination half-life of this drug. Comparison is made between the in vivo handling of the two analgesics, but it is stressed that these data apply only to healthy adults under normal conditions and cannot be extrapolated to patients with underlying disease processes.

摘要

了解药物代谢动力学(生物体对药物的作用)和药效学(药物对生物体的作用)有助于正确评估最合适的剂量、给药间隔、给药途径以及临床指征时的剂量调整。本文将概述药物颗粒穿过生物屏障的运动、随后转化为其他化学形式以及消除的基本物理科学原理。然后将更详细地讨论阿司匹林和对乙酰氨基酚(扑热息痛)的具体代谢途径。水杨酸盐的消除涉及两条可饱和(非线性)主要途径和三条明显的一级(线性)次要途径;这些混合顺序动力学导致影响消除半衰期的数学计算有些复杂,这反过来又可能对预测副作用和毒性有影响。对乙酰氨基酚的动力学也涉及各种途径,但研究表明该药物的预期消除半衰期与观察到的消除半衰期之间有良好的相关性。本文对这两种镇痛药的体内处理进行了比较,但强调这些数据仅适用于正常条件下的健康成年人,不能外推至有潜在疾病过程的患者。

相似文献

1
Pharmacokinetic considerations of common analgesics and antipyretics.常见镇痛药和解热药的药代动力学考量
Am J Med. 1983 Nov 14;75(5A):30-7. doi: 10.1016/0002-9343(83)90230-9.
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Comparative pharmacokinetics of aspirin and acetaminophen.
Arch Intern Med. 1981 Feb 23;141(3 Spec No):279-81. doi: 10.1001/archinte.141.3.279.
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Ther Drug Monit. 1982;4(2):147-80. doi: 10.1097/00007691-198206000-00003.
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[Acute paracetamol and aspirin poisoning].[对乙酰氨基酚和阿司匹林急性中毒]
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Interactions of aspirin with acetaminophen and caffeine in rat stomach: pharmacokinetics of absorption and accumulation in gastric mucosa.阿司匹林与对乙酰氨基酚和咖啡因在大鼠胃中的相互作用:胃黏膜吸收和蓄积的药代动力学
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Pharmacokinetics and metabolism of non-steroidal anti-inflammatory drugs.非甾体抗炎药的药代动力学与代谢
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Pharmacokinetics of acetaminophen in children.对乙酰氨基酚在儿童体内的药代动力学。
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Pharmacokinetics of common analgesics, anti-inflammatories and antipyretics in children.儿童常用镇痛药、抗炎药和解热药的药代动力学
Clin Pharmacokinet. 1989;17 Suppl 1:116-37. doi: 10.2165/00003088-198900171-00009.

引用本文的文献

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Mol Cell Proteomics. 2017 Feb;16(2):310-326. doi: 10.1074/mcp.O116.065219. Epub 2016 Dec 2.
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A Reaction of Aspirin with Ferrous Gluconate.阿司匹林与葡萄糖酸亚铁的反应。
AAPS PharmSciTech. 2015 Dec;16(6):1495-9. doi: 10.1208/s12249-015-0316-y. Epub 2015 Mar 14.
3
Release of tumor necrosis factor-alpha and prostanoids in whole blood cultures after in vivo exposure to low-dose aspirin.体内暴露于低剂量阿司匹林后全血培养物中肿瘤坏死因子-α和类前列腺素的释放。
Mediators Inflamm. 2001 Apr;10(2):81-8. doi: 10.1080/09629350120054554.
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Non-narcotic analgesics. Problems of overdosage.非麻醉性镇痛药。过量用药问题。
Drugs. 1986;32 Suppl 4:177-205. doi: 10.2165/00003495-198600324-00013.