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加巴喷丁类药物:药代动力学、药效学及临床实践考量

Gabapentinoids: pharmacokinetics, pharmacodynamics and considerations for clinical practice.

作者信息

Chincholkar Mahindra

机构信息

Pain Centre, Salford Royal NHS Foundation Trust, Salford, UK.

出版信息

Br J Pain. 2020 May;14(2):104-114. doi: 10.1177/2049463720912496. Epub 2020 Mar 13.

DOI:10.1177/2049463720912496
PMID:32537149
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7265598/
Abstract

The gabapentinoids are often recommended as first-line treatments for the management of neuropathic pain. The differing pharmacodynamic and pharmacokinetic profiles can have implications for clinical practice. This article has summarised these key differences. In addition to their use in managing neuropathic pain, gabapentinoids are increasingly being used for off-label conditions despite the lack of evidence. Prescription rates for off-label conditions have overtaken that for on-label use. Similarly, the use of gabapentinoids in the perioperative period is now embedded in clinical practice despite conflicting evidence. This article summarises the risks associated with this increasing use. There is increasing evidence of the potential to cause harm in vulnerable populations such as the elderly and increasing prevalence of abuse. The risk of respiratory depression in combination with opioids is of particular concern in the context of the current opioid crisis. This article describes the practical considerations involved that might help guide appropriate prescribing practices.

摘要

加巴喷丁类药物常被推荐作为治疗神经性疼痛的一线药物。其不同的药效学和药代动力学特征可能会对临床实践产生影响。本文总结了这些关键差异。除了用于治疗神经性疼痛外,尽管缺乏证据,加巴喷丁类药物越来越多地被用于标签外的病症。标签外病症的处方率已超过标签内使用的处方率。同样,尽管证据相互矛盾,但加巴喷丁类药物在围手术期的使用如今已融入临床实践。本文总结了这种日益增加的使用所带来的风险。越来越多的证据表明,这类药物有可能对老年人等弱势群体造成伤害,且滥用现象日益普遍。在当前阿片类药物危机的背景下,与阿片类药物联合使用导致呼吸抑制的风险尤其令人担忧。本文描述了一些实际考虑因素,可能有助于指导合理的处方实践。

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Pregabalin for neuropathic pain in adults.普瑞巴林用于治疗成人神经性疼痛。
Cochrane Database Syst Rev. 2019 Jan 23;1(1):CD007076. doi: 10.1002/14651858.CD007076.pub3.
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Trends in First Gabapentin and Pregabalin Prescriptions in Primary Care in the United Kingdom, 1993-2017.1993 年至 2017 年英国初级保健中首次开处加巴喷丁和普瑞巴林处方的趋势。
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Transport of Pregabalin Via L-Type Amino Acid Transporter 1 (SLC7A5) in Human Brain Capillary Endothelial Cell Line.培高利特经 L 型氨基酸转运蛋白 1(SLC7A5)在人脑微血管内皮细胞系中的转运。
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