van Lemmen Maarten A, van Velzen Monique, Sarton Elise Y, Dahan Albert, Niesters Marieke, van der Schrier Rutger M
Department of Anesthesiology, Leiden University Medical Center, Leiden, the Netherlands.
Department of Anesthesiology, Amsterdam University Medical Center, Amsterdam, the Netherlands.
Nat Commun. 2025 May 19;16(1):4659. doi: 10.1038/s41467-025-59932-7.
Severe opioid-induced respiratory depression (OIRD) can be treated with intranasal (IN) or intramuscular (IM) naloxone. It is relevant to compare their efficacy and determine the optimal strategy to restore breathing following OIRD. In this open label, crossover, one-on-one randomized trial, conducted in a research unit of an academic medical center, we compared the required number of IM (5 mg/0.5 mL) versus IN (4 mg/0.1 mL) naloxone doses following 10 µg/kg intravenous fentanyl-induced apnea in opioid-naïve participants and participants who chronically use an opioid. After 2 min of apnea, IM or IN naloxone was given at 2 min intervals until return of adequate ventilation. The primary outcome was the number of naloxone doses needed to achieve full reversal of breathing. If necessary, rescue intravenous naloxone was administered. Eighteen opioid-naïve participants were randomized, 16 analyzed. The required median IM naloxone doses were 1.5 (IQR 1-2) versus 2 (1-3) for IN naloxone (p = 0.0002); one participant required rescue naloxone. No serious adverse events occurred. Similarly, in participants who chronically used an opioid, IM was more effective than IN naloxone. In these participants, adverse effects included muscle rigidity in the IN treated participants and mild to moderate withdrawal irrespective of treatment. Here we show the superiority of IM over IN naloxone in the number of doses required for full reversal of breathing following opioid-induced apnea. While the trial shows superiority for IM naloxone with products used in the community, we relate our findings to the higher naloxone plasma concentrations after IM naloxone compared to IN naloxone. The study was registered at https://doi.org/10.1186/ISRCTN21068708 .
严重的阿片类药物所致呼吸抑制(OIRD)可用鼻内(IN)或肌内(IM)纳洛酮治疗。比较二者的疗效并确定OIRD后恢复呼吸的最佳策略具有重要意义。在这项开放标签、交叉、一对一随机试验中,我们在一所学术医疗中心的研究单位进行了研究,比较了在未使用过阿片类药物的参与者和长期使用阿片类药物的参与者中,静脉注射10µg/kg芬太尼诱发呼吸暂停后,肌内注射(5mg/0.5mL)与鼻内注射(4mg/0.1mL)纳洛酮所需的剂量。呼吸暂停2分钟后,每隔2分钟给予肌内或鼻内纳洛酮,直至恢复充分通气。主要结局是实现呼吸完全恢复所需的纳洛酮剂量。如有必要,给予静脉注射纳洛酮进行抢救。18名未使用过阿片类药物的参与者被随机分组,16名接受分析。肌内注射纳洛酮所需的中位数剂量为1.5(四分位间距1 - 2),而鼻内注射纳洛酮为2(1 - 3)(p = 0.0002);1名参与者需要抢救用纳洛酮。未发生严重不良事件。同样,在长期使用阿片类药物的参与者中,肌内注射比鼻内注射纳洛酮更有效。在这些参与者中,不良反应包括鼻内注射治疗的参与者出现肌肉僵硬,且无论治疗方式如何均有轻至中度戒断反应。在此我们表明,在阿片类药物诱发呼吸暂停后实现呼吸完全恢复所需的剂量方面,肌内注射纳洛酮优于鼻内注射纳洛酮。虽然该试验显示社区使用的产品中肌内注射纳洛酮具有优势,但我们将我们的发现与肌内注射纳洛酮后比鼻内注射纳洛酮更高的纳洛酮血浆浓度联系起来。该研究已在https://doi.org/10.1186/ISRCTN21068708上注册。