Rapid Absorption of Naloxone from Eye Drops

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Tuunainen , J , Saloranta , L , Levijoki , J , Lindstedt , J , Lehtisalo , J , Pappinen , S , Ramela , M , Virtanen , S & Joensuu , H 2022 , ' Rapid Absorption of Naloxone from Eye Drops ' , Pharmaceuticals , vol. 15 , no. 5 , 532 . https://doi.org/10.3390/ph15050532

Title: Rapid Absorption of Naloxone from Eye Drops
Author: Tuunainen, Johanna; Saloranta, Lasse; Levijoki, Jouko; Lindstedt, Jenni; Lehtisalo, Jenni; Pappinen, Sari; Ramela, Meri; Virtanen, Sami; Joensuu, Heikki
Contributor organization: University of Helsinki
Department of Oncology
Heikki Joensuu / Principal Investigator
HUS Comprehensive Cancer Center
Date: 2022-05
Language: eng
Number of pages: 11
Belongs to series: Pharmaceuticals
ISSN: 1424-8247
DOI: https://doi.org/10.3390/ph15050532
URI: http://hdl.handle.net/10138/345814
Abstract: 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.
Subject: naloxone
ocular administration
opiate
pharmacokinetics
tolerability
FDA-APPROVED INTRANASAL
PHARMACOKINETIC PROPERTIES
3125 Otorhinolaryngology, ophthalmology
Peer reviewed: Yes
Rights: cc_by
Usage restriction: openAccess
Self-archived version: publishedVersion


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