• E Vanky, L Hellmundt, U Bondesson, S Eksborg, and S Lundeberg.
• Department of Anesthesia and Intensive Care, Visby Hospital, Visby, Sweden.
• Acta Anaesthesiol Scand. 2017 Jul 1; 61 (6): 636-640.

BackgroundThere is increasing interest in the use of intranasal naloxone to reverse adverse opioid effects during management of procedural pain in children and in adults after overdose. There are limited data on the pharmacokinetics of intranasal naloxone so in this study we aimed to detail the pharmacokinetic profile of the commercially marketed injectable solution of naloxone 0.4 mg/ml when administered as an intranasal spray.MethodsTwenty healthy volunteers received naloxone as an intranasal spray at a dose of 10 μg/kg. Venous blood sampling was carried out for 90 min after administration to determine the time profile of the plasma concentrations of using tandem mass spectrometry. Pharmacokinetic parameters were calculated using a one-compartment model.ResultsMedian time to maximum naloxone concentration (Tmax) was 14.5 (95% CI: 9.0-16.5) min, mean maximum naloxone concentration (Cmax) was 1.09 ± 0.56 ng/ml and mean AUC0-90 minwas 37.1 ± 15.0 ng*min/ml. Elimination half-life estimated from the median concentration data was 28.2 min.ConclusionOur results show a faster uptake of intranasal naloxone to maximum concentration compared with previous studies although with a marked variation in maximum concentration. The findings are consistent with our clinical experience of the time profile for reversing the effects of sufentanil sedation in children.© 2017 The Acta Anaesthesiologica Scandinavica Foundation. Published by John Wiley & Sons Ltd.

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