Abstract

To assess the pharmacokinetic properties of community-use formulations of naloxone for emergency treatment of opioid overdose. Systematic literature review based on searches of established databases and congress archives. 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. The pharmacokinetics of im./sc. auto-injector 2mg and approved intranasal spray (2 and 4mg) 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.

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