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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| Format: | Article |
| Language: | English |
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MDPI AG
2022-04-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/15/5/532 |
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| author | Johanna Tuunainen Lasse Saloranta Jouko Levijoki Jenni Lindstedt Jenni Lehtisalo Sari Pappinen Meri Ramela Sami Virtanen Heikki Joensuu |
| author_facet | Johanna Tuunainen Lasse Saloranta Jouko Levijoki Jenni Lindstedt Jenni Lehtisalo Sari Pappinen Meri Ramela Sami Virtanen Heikki Joensuu |
| author_sort | Johanna Tuunainen |
| collection | DOAJ |
| 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<sub>max</sub>) achieved in 14 to 28 min, high plasma exposure (C<sub>max</sub> 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. |
| first_indexed | 2024-03-10T03:10:30Z |
| format | Article |
| id | doaj.art-7559035102a94e858d86ff1ed4786416 |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-10T03:10:30Z |
| publishDate | 2022-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-7559035102a94e858d86ff1ed47864162023-11-23T12:34:02ZengMDPI AGPharmaceuticals1424-82472022-04-0115553210.3390/ph15050532Rapid Absorption of Naloxone from Eye DropsJohanna Tuunainen0Lasse Saloranta1Jouko Levijoki2Jenni Lindstedt3Jenni Lehtisalo4Sari Pappinen5Meri Ramela6Sami Virtanen7Heikki Joensuu8Orion Corporation Orion Pharma, Orionintie 1A, FIN-02200 Espoo, FinlandOrion Corporation Orion Pharma, Orionintie 1A, FIN-02200 Espoo, FinlandOrion Corporation Orion Pharma, Orionintie 1A, FIN-02200 Espoo, FinlandOrion Corporation Orion Pharma, Orionintie 1A, FIN-02200 Espoo, FinlandOrion Corporation Orion Pharma, Orionintie 1A, FIN-02200 Espoo, FinlandOrion Corporation Orion Pharma, Orionintie 1A, FIN-02200 Espoo, FinlandOrion Corporation Orion Pharma, Orionintie 1A, FIN-02200 Espoo, FinlandOrion Corporation Orion Pharma, Orionintie 1A, FIN-02200 Espoo, FinlandDepartment of Oncology, Helsinki University Hospital, Haartmaninkatu 8, FIN-00290 Helsinki, FinlandNaloxone 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<sub>max</sub>) achieved in 14 to 28 min, high plasma exposure (C<sub>max</sub> 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.https://www.mdpi.com/1424-8247/15/5/532naloxoneocular administrationopiatepharmacokineticstolerability |
| spellingShingle | Johanna Tuunainen Lasse Saloranta Jouko Levijoki Jenni Lindstedt Jenni Lehtisalo Sari Pappinen Meri Ramela Sami Virtanen Heikki Joensuu Rapid Absorption of Naloxone from Eye Drops Pharmaceuticals naloxone ocular administration opiate pharmacokinetics tolerability |
| 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 | naloxone ocular administration opiate pharmacokinetics tolerability |
| url | https://www.mdpi.com/1424-8247/15/5/532 |
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