Pharmacokinetic properties of intranasal and injectable formulations of naloxone for community use: a systematic review

Abstract

Aim: To assess the pharmacokinetic properties of community-use formulations of naloxone for emergency treatment of opioid overdose.

Methods: Systematic literature review based on searches of established databases and congress archives.

Results: Seven studies met inclusion criteria: two of US FDA-approved intramuscular (im.)/subcutaneous (sc.) auto-injectors, one of an FDA-approved intranasal spray, two of unapproved intranasal kits (syringe with atomizer attachment) and two of intranasal products in development.

Conclusion: The pharmacokinetics of im./sc. auto-injector 2 mg and approved intranasal spray (2 and 4 mg) demonstrated rapid uptake and naloxone exposure exceeding that of the historic benchmark (0.4 mg im.), indicating that naloxone exposure was adequate for reversal of opioid overdose.

Keywords: auto-injector; bioavailability; community use; drug overdose; intramuscular; intranasal; naloxone; nasal spray; pharmacokinetics; reversal.