Taylor Donald R
Comprehensive Pain Care PC, Marietta, GA, USA.
Clin Pharmacol. 2013 Jul 24;5:131-41. doi: 10.2147/CPAA.S26649. Print 2013.
Breakthrough cancer pain (BTCP) is defined as a transient exacerbation of pain that arises in patients with otherwise controlled persistent pain. BTCP typically has a rapid onset and relatively short duration, but it causes a significant amount of physical and psychological distress for patients. Several rapid-onset fentanyl formulations have been introduced in the USA to replace traditional oral opioids for the treatment of BTCP: a transmucosal lozenge, a sublingual orally disintegrating tablet, a buccal tablet, a buccal soluble film, a pectin nasal spray and, the newest formulation to enter the market, a sublingual spray. This article reviews the six rapid-onset formulations of fentanyl approved in the USA for the management of BTCP with emphasis on describing the published literature on fentanyl sublingual spray. The different fentanyl formulations vary in pharmacokinetic properties and ease of use, but all have a rapid onset and a relatively short duration of analgesia. Fentanyl sublingual spray has demonstrated absorption within 5 minutes of administration, with fentanyl plasma concentrations increasing over the first 30 minutes and remaining elevated for 60-90 minutes in pharmacokinetic studies in healthy subjects. Fentanyl sublingual spray shows linear dose proportionality, and changes in the temperature or acidity of the oral cavity do not alter its pharmacokinetic properties. In patients with BTCP, statistically significant pain relief is measurable at 5 minutes after administration of fentanyl sublingual spray, when compared with placebo, with significant pain relief lasting at least 60 minutes after administration. Adverse events are typical of opioid treatment and are considered mild to moderate in intensity. In summary, fentanyl sublingual spray provides rapid onset of analgesia and is a tolerable and effective treatment for BTCP.
爆发性癌痛（BTCP）的定义是，在原本疼痛已得到控制的持续性疼痛患者中出现的疼痛短暂加剧。BTCP通常起病迅速且持续时间相对较短，但会给患者造成大量身体和心理痛苦。美国已推出几种起效迅速的芬太尼制剂，以取代传统口服阿片类药物来治疗BTCP：一种经黏膜含片、一种口腔崩解片、一种颊含片、一种颊用可溶膜、一种果胶鼻喷雾剂，以及最新进入市场的制剂——一种舌下喷雾剂。本文综述了美国批准用于管理BTCP的六种起效迅速的芬太尼制剂，重点描述了关于芬太尼舌下喷雾剂的已发表文献。不同的芬太尼制剂在药代动力学特性和易用性方面存在差异，但均起效迅速且镇痛持续时间相对较短。在健康受试者的药代动力学研究中，芬太尼舌下喷雾剂在给药后5分钟内即显示吸收，芬太尼血浆浓度在最初30分钟内升高，并在60 - 90分钟内保持升高。芬太尼舌下喷雾剂显示出线性剂量比例关系，口腔温度或酸度的变化不会改变其药代动力学特性。在BTCP患者中，与安慰剂相比，芬太尼舌下喷雾剂给药后5分钟即可测得具有统计学意义的疼痛缓解，给药后显著疼痛缓解至少持续60分钟。不良事件是阿片类药物治疗的典型情况，强度被认为是轻度至中度。总之，芬太尼舌下喷雾剂起效迅速，是一种可耐受且有效的BTCP治疗方法。
