Pitfalls of Intranasal Naloxone

Zuckerman, Matthew; Weisberg, Stacy; Boyer, Edward W.

doi:10.3109/10903127.2014.896961

Cited by 44 publications

(39 citation statements)

References 22 publications

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“…Although abbreviated observation periods may be adequate for patients with fentanyl, morphine, or heroin overdose, 102,109,[120][121][122][123] longer periods of observation may be required to safely discharge a patient with life-threatening overdose of a long-acting or sustained-release opioid. 93,124,125 Naloxone administration in post-cardiac arrest care may be considered in order to achieve the specific therapeutic goals of reversing the effects of long-acting opioids (Class IIb, LOE C-EO). The use of ILE therapy was first developed as a treatment for cardiac arrest resulting from the local anesthetic bupivacaine.…”

Section: Observation and Post-resuscitation Carementioning

confidence: 99%

Part 10: Special Circumstances of Resuscitation

Lavonas¹,

Drennan²,

Gabrielli³

et al. 2015

Circulation

239

123

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Section: Observation and Post-resuscitation Carementioning

confidence: 99%

Part 10: Special Circumstances of Resuscitation

Lavonas¹,

Drennan²,

Gabrielli³

et al. 2015

Circulation

239

123

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“…Nonetheless, multiple reports have described the reversal of an apparent opioid overdose using these IN improvised devices. These retrospective reports focus on successful rescues but do not provide insight into treatment failures …”

Section: Discussionmentioning

confidence: 99%

“…In addition to the simplicity associated with a single administration, the 4‐mg IN dose increases the potential for a reversal of opioid overdose compared to either improvised IN devices – or the approved autoinjector that delivers 0.4 mg of naloxone . This is especially relevant because of the dramatic rise in the abuse of high‐potency opioids such as fentanyl that require higher concentrations of naloxone to treat overdose . Based on the selectivity of naloxone for opiate receptors and the human use characteristics described here, this product can be used safely and effectively with no prior training to provide an important and potentially life‐saving intervention for the treatment of opioid overdose.…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetic Properties and Human Use Characteristics of an FDA‐Approved Intranasal Naloxone Product for the Treatment of Opioid Overdose

Krieter

Chiang

Gyaw

et al. 2016

The Journal of Clinical Pharma

106

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Parenteral naloxone has been approved to treat opiate overdose for over 4 decades. Intranasal naloxone, administered "off label" using improvised devices, has been widely used by both first responders and the lay public to treat overdose. However, these improvised devices require training for effective use, and the recommended volumes (2 to 4 mL) exceed those considered optimum for intranasal administration. The present study compared the pharmacokinetic properties of intranasal naloxone (2 to 8 mg) delivered in low volumes (0.1 to 0.2 mL) using an Aptar Unit-Dose device to an approved (0.4 mg) intramuscular dose. A parallel study assessed the ease of use of this device in a simulated overdose situation. All doses of intranasal naloxone resulted in plasma concentrations and areas under the curve greater than those observed following the intramuscular dose; the time to reach maximum plasma concentrations was not different following intranasal and intramuscular administration. Plasma concentrations of naloxone were dose proportional between 2 and 8 mg and independent of whether drug was administered to 1 or both nostrils. In a study using individuals representative of the general population, >90% were able to perform both critical tasks (inserting nozzle into a nostril and pressing plunger) needed to deliver a simulated dose of naloxone without prior training. Based on both pharmacokinetic and human use studies, a 4-mg dose delivered in a single device (0.1 mL) was selected as the final product. This product can be used by first responders and the lay public, providing an important and potentially life-saving intervention for victims of an opioid overdose.

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“…Although IN NLX is gaining acceptance as an alternative first-line treatment of opioid toxicity, there have been no laboratory-controlled studies evaluating the potency of NLX to reverse opioidagonist effects as a function of route of administration. There are also some practitioners who remain skeptical of IN NLX for use in opioid overdose compared with IV or IM delivery (Zuckerman et al, 2014). Secondly, we believed that the use of an antagonist provided greater sensitivity to detect changes in RO with PET imaging, particularly with a small sample size.…”

Section: Discussionmentioning

confidence: 99%

Intranasal Opioid Administration in Rhesus Monkeys: PET Imaging and Antinociception

Saccone

Lindsey

Koeppe

et al. 2016

J Pharmacol Exp Ther

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The goal of this study was to evaluate the effects of intranasally administered opioids in rhesus monkeys using the tail-withdrawal assay, and to correlate these effects with measures of receptor occupancy using positron emission tomography (PET) imaging. Initial experiments characterized the antinociceptive effects of intranasal (IN) fentanyl and buprenorphine relative to intramuscular (IM) injection. Fentanyl (0.010-0.032 mg/kg) and buprenorphine (0.1-1.0 mg/kg) produced dose-dependent increases in tail-withdrawal latency that did not differ between routes of delivery. The second experiment compared the ability of IN and intravenous (IV) naloxone (NLX) to block the antinociceptive effects IV fentanyl, and to measure receptor occupancy at equipotent doses of NLX using PET imaging. IN and IV NLX (0.0032-0.032 mg/kg) produced dose-dependent decreases in fentanyl-induced antinociception. Again, there was no difference observed in overall potency between routes. PET imaging showed that IV and IN NLX produced similar decreases in receptor occupancy as measured by [11 C]carfentanil blocking, although there was a trend for IV NLX to produce marginally greater occupancy changes. This study validated the first procedures to evaluate the IN effects of opioids in rhesus monkeys.

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Pitfalls of Intranasal Naloxone

Cited by 44 publications

References 22 publications

Part 10: Special Circumstances of Resuscitation

Part 10: Special Circumstances of Resuscitation

Pharmacokinetic Properties and Human Use Characteristics of an FDA‐Approved Intranasal Naloxone Product for the Treatment of Opioid Overdose

Intranasal Opioid Administration in Rhesus Monkeys: PET Imaging and Antinociception

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