Mystakidou Kyriaki, Katsouda Emmanuela, Tsilika Eleni, Parpa Efi, Vlahos Lambros
Department of Radiology, University of Athens, School of Medicine, Korinthias 27, Athens 115 26, Greece.
In Vivo. 2004 Sep-Oct;18(5):633-42.
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.
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。
