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Acta Anaesthesiol Scand. 2017 Jul;61(6):636-640. doi: 10.1111/aas.12898. Epub 2017 Apr 25.

Pharmacokinetics after a single dose of naloxone administered as a nasal spray in healthy volunteers.

Author information

1
Department of Anesthesia and Intensive Care, Visby Hospital, Visby, Sweden.
2
Department of Pediatric Anesthesia and Intensive Care, Astrid Lindgren Children's Hospital, Karolinska University Hospital, Stockholm, Sweden.
3
Department of Chemistry, Environment and Feed Hygiene, National Veterinary Institute (SVA), Uppsala, Sweden.
4
Childhood Cancer Research Unit, Department of Woman and Child Health, Karolinska University Hospital, Karolinska Institutet, Stockholm, Sweden.
5
Department of Physiology and Pharmacology, Karolinska Institutet, Stockholm, Sweden.

Abstract

BACKGROUND:

There 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.

METHODS:

Twenty 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.

RESULTS:

Median 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 min was 37.1 ± 15.0 ng*min/ml. Elimination half-life estimated from the median concentration data was 28.2 min.

CONCLUSION:

Our 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.

PMID:
28444856
DOI:
10.1111/aas.12898
[Indexed for MEDLINE]

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