Pharmacokinetic Properties of Intranasal and Injectable Formulations of Naloxone for Community use: a Systematic Review
Year: 2018
Type: review
Study design: Systematic Review
Abstract: Practice points• The US FDA has approved two naloxone products for use by laypersons in community settings for emergency treatment of known or suspected opioid overdose: an intranasal spray with a concentrated naloxone dose of 2 or 4 mg in 0.1 ml and an auto-injector for intramuscular (im.) or subcutaneous (sc.) use with a naloxone dose of 0.4 or 2 mg.• In the absence of head-to-head, comparative efficacy studies, which are not feasible for ethical and logistical reasons, pharmacokinetic data provide important information about effective doses and routes of administration of naloxone for opioid overdose reversal.• In pharmacokinetic studies, both the approved intranasal spray and the im./sc.auto-injector demonstrated bioequivalence with a previously approved formulation, indicating that naloxone exposure was adequate to reverse an opioid overdose.• Both the approved intranasal spray and the im./sc.auto-injector demonstrated sufficient plasma exposure within the first 15-20 min after administration.• Usability studies with laypersons in simulated overdose conditions have found that more than 90% of participants were able to successfully administer naloxone using the approved intranasal spray or im./sc.auto-injector without prior training; however, these studies have identified critical errors with the proper assembly and use of unapproved intranasal kits, even when training had been provided.• Approved intranasal naloxone is appropriate for most patients, with the exception of those with known nasal pathology (e.g., polyps and chronic intranasal drug use).• Providing prescriptions for community-use naloxone may reduce future risk in patients who are receiving chronic opioid therapy for pain control or who have histories of illicit opioid use.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.
Source: Pain Management
Authors: Shawn A Ryan, Robert B Dunne
Institutions: University of Cincinnati, Wayne State University
Language: English
Field: Medicine
Domain: Health Sciences
Open Access status: hybrid
OpenAlex ID: W2799697733