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透皮治疗芬太尼系统(TTS-F)。

Transdermal therapeutic fentanyl-system (TTS-F).

作者信息

Mystakidou Kyriaki, Katsouda Emmanuela, Tsilika Eleni, Parpa Efi, Vlahos Lambros

机构信息

Department of Radiology, University of Athens, School of Medicine, Korinthias 27, Athens 115 26, Greece.

出版信息

In Vivo. 2004 Sep-Oct;18(5):633-42.

Abstract

Fentanyl, a surgical analgesic and general anaesthetic, is a lipophilic short-acting synthetic opioid, having a selective potent effect on mu receptors. The transdermal therapeutic fentanyl-system (TTS-F) allows for a continued and sustained titratable amount of fentanyl to be delivered without the inconvenience of the typical 24-h administration of other analgesics. Although incidences of respiratory depression led to TTS-F being contraindicated for postoperative analgesia, it is currently undergoing Phase III trials for nociceptive, neuropathic and chronic moderate to severe pain in a variety of settings. It demonstrates a slow pharmacokinetic profile and incidences of breakthrough pain may still require rapid analgesia, for which intravenous and bolus administration of rapid acting opioids remain 'gold standard' However, TTS-F is finding uses for chronic pain of cancer origin where it offers a solution for step 3-pain (WHO) management on the WHO analgesic ladder. More recent data indicates that TTS-F is not only effective for neuropathic but also nociceptive non-cancer and cancer pain alike. This review presents an overview of the synthesis, delivery, pharmacokinetics, toxicity and clinical pharmacology of the transdermal delivery of fentanyl.

摘要

芬太尼是一种外科手术镇痛药和全身麻醉药,是一种亲脂性短效合成阿片类药物,对μ受体具有选择性强效作用。透皮治疗性芬太尼系统(TTS-F)能够持续、稳定地递送可滴定剂量的芬太尼,避免了其他镇痛药通常需要24小时给药带来的不便。尽管呼吸抑制的发生率导致TTS-F被禁止用于术后镇痛,但目前它正在多种情况下针对伤害性、神经性和慢性中度至重度疼痛进行III期试验。它呈现出缓慢的药代动力学特征,爆发性疼痛的发生率可能仍需要快速镇痛,对此静脉注射和推注速效阿片类药物仍然是“金标准”。然而,TTS-F正在被用于癌症引起的慢性疼痛,它为世界卫生组织镇痛阶梯上的3级疼痛(世界卫生组织)管理提供了一种解决方案。最新数据表明,TTS-F不仅对神经性疼痛有效,对伤害性非癌性和癌性疼痛也同样有效。本综述概述了芬太尼透皮给药的合成、递送、药代动力学、毒性和临床药理学。

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