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鼻腔内芬太尼:从药代动力学和生物利用度到当前的治疗应用。

Intranasal fentanyl: from pharmacokinetics and bioavailability to current treatment applications.

机构信息

Pain Relief & Palliative Care Unit, 1st Department of Radiology, University of Athens School of Medicine, Areteion Hospital, 27 Korinthias Avenue, Ampelokipi, 11526 Athens, Greece.

出版信息

Expert Rev Anticancer Ther. 2010 Jul;10(7):1009-21. doi: 10.1586/era.10.77.

Abstract

Fentanyl, a short-acting synthetic pure opiate, offers an excellent option for the treatment of cancer and chronic pain. While oral administration is not an option, its high potency and lipophilicity have made intranasal administration feasible. Intranasal fentanyl has a bioavailability of 89%, with a short onset of action ( approximately 7 min) and duration times ( approximately 1 h). It bypasses the oral/gastrointestinal route, delivers the analgesic dose in a volume of 150 microl that can be adequately absorbed and, with a pH of 6.4, avoids local irritation. Intranasal fentanyl has been investigated to assess its potential as a well-tolerated acute postoperative breakthrough pain relief medication. It has been shown to be superior to oral transmucosal fentanyl for the treatment of cancer breakthrough pain. Similar analgesic effects to fentanyl or morphine intravenously and orally, with a similar safety profile, have been reported for postoperative or acute pain treatment of children and adults in the prehospital and hospital settings.

摘要

芬太尼是一种短效合成纯阿片类药物,为癌症和慢性疼痛的治疗提供了一个极好的选择。虽然口服不是一种选择,但它的高效和脂溶性使得经鼻给药成为可能。经鼻给予芬太尼的生物利用度为 89%,起效迅速(约 7 分钟),作用持续时间(约 1 小时)。它绕过了口服/胃肠道途径,以 150 微升的体积给予镇痛剂量,能够充分吸收,并且 pH 值为 6.4,避免了局部刺激。已经研究了经鼻给予芬太尼,以评估其作为一种耐受性良好的急性术后爆发性疼痛缓解药物的潜力。研究表明,它在治疗癌症爆发性疼痛方面优于口腔黏膜芬太尼。在院前和医院环境中,对于儿童和成人的术后或急性疼痛治疗,经鼻给予芬太尼与静脉内给予芬太尼或吗啡以及口服给予芬太尼或吗啡具有相似的镇痛效果,且安全性相似。

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