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Rapid Absorption of Naloxone from Eye Drops

Naloxone as emergency treatment for opioid overdosing can be administered via several routes. However, the available administration methods are invasive or may be associated with incomplete or slow naloxone absorption. We evaluated pharmacokinetics and local tolerance of naloxone ocular drops in hea...

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Autores principales: Tuunainen, Johanna, Saloranta, Lasse, Levijoki, Jouko, Lindstedt, Jenni, Lehtisalo, Jenni, Pappinen, Sari, Ramela, Meri, Virtanen, Sami, Joensuu, Heikki
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9143859/
https://www.ncbi.nlm.nih.gov/pubmed/35631356
http://dx.doi.org/10.3390/ph15050532
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author Tuunainen, Johanna
Saloranta, Lasse
Levijoki, Jouko
Lindstedt, Jenni
Lehtisalo, Jenni
Pappinen, Sari
Ramela, Meri
Virtanen, Sami
Joensuu, Heikki
author_facet Tuunainen, Johanna
Saloranta, Lasse
Levijoki, Jouko
Lindstedt, Jenni
Lehtisalo, Jenni
Pappinen, Sari
Ramela, Meri
Virtanen, Sami
Joensuu, Heikki
author_sort Tuunainen, Johanna
collection PubMed
description Naloxone as emergency treatment for opioid overdosing can be administered via several routes. However, the available administration methods are invasive or may be associated with incomplete or slow naloxone absorption. We evaluated pharmacokinetics and local tolerance of naloxone ocular drops in healthy beagle dogs. Naloxone administration as eye drops produced fast absorption with time to maximum plasma concentration (t(max)) achieved in 14 to 28 min, high plasma exposure (C(max) 10.3 ng/mL to 12.7 ng/mL), and good bioavailability (41% to 56%). No signs of ocular irritability were observed in the scored ocular tolerability parameters, and the reactions of dogs suggesting immediate ocular discomfort after the dosing were sporadic and short lasting. Slight and transient increase in the intraocular pressure and transient decrease in the tear production were recorded. The results suggest that eye drops may provide a fast and an effective non-invasive route for naloxone administration to reverse opioid overdosing, and clinical studies in the human are warranted.
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spelling pubmed-91438592022-05-29 Rapid Absorption of Naloxone from Eye Drops Tuunainen, Johanna Saloranta, Lasse Levijoki, Jouko Lindstedt, Jenni Lehtisalo, Jenni Pappinen, Sari Ramela, Meri Virtanen, Sami Joensuu, Heikki Pharmaceuticals (Basel) Article Naloxone as emergency treatment for opioid overdosing can be administered via several routes. However, the available administration methods are invasive or may be associated with incomplete or slow naloxone absorption. We evaluated pharmacokinetics and local tolerance of naloxone ocular drops in healthy beagle dogs. Naloxone administration as eye drops produced fast absorption with time to maximum plasma concentration (t(max)) achieved in 14 to 28 min, high plasma exposure (C(max) 10.3 ng/mL to 12.7 ng/mL), and good bioavailability (41% to 56%). No signs of ocular irritability were observed in the scored ocular tolerability parameters, and the reactions of dogs suggesting immediate ocular discomfort after the dosing were sporadic and short lasting. Slight and transient increase in the intraocular pressure and transient decrease in the tear production were recorded. The results suggest that eye drops may provide a fast and an effective non-invasive route for naloxone administration to reverse opioid overdosing, and clinical studies in the human are warranted. MDPI 2022-04-25 /pmc/articles/PMC9143859/ /pubmed/35631356 http://dx.doi.org/10.3390/ph15050532 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Tuunainen, Johanna
Saloranta, Lasse
Levijoki, Jouko
Lindstedt, Jenni
Lehtisalo, Jenni
Pappinen, Sari
Ramela, Meri
Virtanen, Sami
Joensuu, Heikki
Rapid Absorption of Naloxone from Eye Drops
title Rapid Absorption of Naloxone from Eye Drops
title_full Rapid Absorption of Naloxone from Eye Drops
title_fullStr Rapid Absorption of Naloxone from Eye Drops
title_full_unstemmed Rapid Absorption of Naloxone from Eye Drops
title_short Rapid Absorption of Naloxone from Eye Drops
title_sort rapid absorption of naloxone from eye drops
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9143859/
https://www.ncbi.nlm.nih.gov/pubmed/35631356
http://dx.doi.org/10.3390/ph15050532
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