Naloxone (Naloxone Hydrochloride) - Summary

NALOXONE SUMMARY

Naloxone hydrochloride, a narcotic antagonist, is a synthetic congener of oxymorphone. In structure it differs from oxymorphone in that the methyl group on the nitrogen atom is replaced by an allyl group.17-Allyl-4,5α-epoxy-3,14-dihydroxymorphinan-6-one hydrochlorideC₁₉H₂₁NO₄• HCl          363.84

Naloxone hydrochloride injection is indicated for the complete or partial reversal of narcotic depression, including respiratory depression, induced by opioids including natural and synthetic narcotics, propoxyphene, methadone and certain narcotic-antagonist analgesics: nalbuphine, pentazocine and butorphanol. Naloxone hydrochloride is also indicated for the diagnosis of suspected acute opioid overdosage.

Naloxone hydrochloride injection may be useful as an adjunctive agent to increase blood pressure in the management of septic shock.

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NEWS HIGHLIGHTS

Media Articles Related to Naloxone

Suboxone Maker Pulls Pills in Favor of Film
Source: MedPage Today Product Alert [2012.09.25]
The buprenorphine-naloxone combination product (Suboxone) in sublingual tablet form will soon be pulled from the U.S. market because its child-resistant packaging isn't effective enough.

News from Annals of Family Medicine January/February 2015
Source: Alcohol / Addiction / Illegal Drugs News From Medical News Today [2015.01.14]
Few Rural Physicians Trained to Provide Treatment for Opioid Use DisorderAmid rising rates of opioid use disorder and related unintentional lethal opioid overdoses, particularly in rural areas of...

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Published Studies Related to Naloxone

Pharmacological challenge with naloxone and cue exposure in alcohol dependence: results of a randomized, double-blind placebo-controlled trial. [2013]
dependency was reported... CONCLUSIONS: We could not replicate the result, that blocking of the endogenous

A randomised controlled trial of sublingual buprenorphine-naloxone film versus tablets in the management of opioid dependence. [2013]
(substance use, psychosocial function)... CONCLUSIONS: The study demonstrated dose equivalence and comparable clinical

A comparison of oxycodone prolonged-release vs. oxycodone + naloxone prolonged-release after laparoscopic hysterectomy. [2013]
for short-term post-operative pain management... CONCLUSION: Addition of naloxone to oxycodone PR tablets in a pain regimen

A randomized, double-blind, active-controlled, double-dummy, parallel-group study to determine the safety and efficacy of oxycodone/naloxone prolonged-release tablets in patients with moderate/severe, chronic cancer pain. [2012]
prolonged-release tablets (OxyPR) in patients with moderate/severe cancer pain... CONCLUSIONS: OXN PR provides superior bowel function in cancer pain patients,

Adjunctive counseling during brief and extended buprenorphine-naloxone treatment for prescription opioid dependence: a 2-phase randomized controlled trial. [2011.12]
CONTEXT: No randomized trials have examined treatments for prescription opioid dependence, despite its increasing prevalence. OBJECTIVE: To evaluate the efficacy of brief and extended buprenorphine hydrochloride-naloxone hydrochloride treatment, with different counseling intensities, for patients dependent on prescription opioids... CONCLUSIONS: Prescription opioid-dependent patients are most likely to reduce opioid use during buprenorphine-naloxone treatment; if tapered off buprenorphine-naloxone, even after 12 weeks of treatment, the likelihood of an unsuccessful outcome is high, even in patients receiving counseling in addition to SMM. Trial Registration clinicaltrials.gov Identifier: NCT00316277.

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Clinical Trials Related to Naloxone

Subjective Analgesic Effects of Naloxone and Virtual Reality [Not yet recruiting]
This study is designed to test a specific hypothesis exploring the neurophysiologic mechanism(s) that underlie the pain- relieving effects of immersive Virtual Reality (VR) as a non-pharmacologic pain management technique, using healthy volunteers experiencing carefully controlled thermal and/or electrical pain in the laboratory. Over the past decade, our research group has performed a series of NIH-funded investigations of VR

analgesia - in both the clinical pain and laboratory pain settings - demonstrating its

clinical efficacy and safety. In the current study we will test pharmacologic manipulation of VR analgesia (with the opioid analgesia antagonist naloxone). We anticipate that this theoretical work will provide a foundation for future clinical applications of immersive VR

- whether used alone or in combination with other analgesic agents - and make immersive VR a

more effective and more widely used analgesic tool for the treatment of clinical pain.

Our previous work with immersive VR indicates that its use during a painful event can reduce subjective pain reports during both acute clinical and laboratory pain by 20-50% [1]. Furthermore, we have shown that effective VR analgesia is associated with reduced pain-related brain activity that is quantitatively and qualitatively comparable to clinically relevant doses of systemic opioid analgesics [2]. The laboratory pain protocol proposed in the current application is identical to the UW HSD-approved protocol used in our

previous studies (#25296 - "Reducing Brief Thermal and Electrical Pain"). What is

specifically different in the current protocol is the use of naloxone to determine whether VR analgesia operates through an endogenous opioid-dependent mechanism or not. The results of this study will not only suggest the mechanism of action of VR analgesia, but also allow us to more effectively apply immersive VR analgesia in the clinically pain setting through its thoughtful combination with well-established pharmacologic analgesic techniques, such as opioid analgesia administration.

The specific aim of this study and the hypothesis it tests are as follows: To determine the extent to which subjective analgesic effects of VR analgesia are inhibited by opioid

receptor antagonism with naloxone. Hypothesis - VR analgesia will not be inhibited by

systemic opioid receptor antagonism, suggesting that VR analgesia is not mediated by release of endogenous opiates and/or by activation of opioid-dependent descending central nervous system pathways.

Safety and Tolerability of Buprenorphine/Naloxone Film Strips [Active, not recruiting]
This study will evaluate the safety and tolerability on the oral mucosa of buprenorphine/naloxone film strips administered either sublingually or buccally daily for 12 weeks in opioid dependent individuals who are already on a stable regimen of buprenorphine/naloxone.

A Study to Evaluate the Pharmacokinetic Effect of SCH 503034 (Boceprevir) on Methadone or Buprenorphine/Naloxone Plasma Concentrations (P08123 AM3) [Recruiting]
In this study, participants on methadone or buprenorphine/naloxone maintenance therapy will be given boceprevir. Blood samples will be taken at specified intervals to find out whether boceprevir affects the pharmacokinetics of methadone or buprenorphine/naloxone.

Optimal Dose of Prophylactic Naloxone in Reducing Opioid-Induced Side Effects in Children/Adolescents [Recruiting]
This is an investigator initiated dose finding study designed to determine the optimal dose of naloxone to prevent or minimize the most common side effects induced by opioids, namely itching, nausea, and vomiting. Male and female inpatients of the Children’s Center of the Johns Hopkins Hospital, who are greater than 6 and less than 18 years of age with acute, moderate to severe pain, and who are to be treated with IVPCA morphine will be eligible for inclusion in this study. Patients will be recruited by a study investigator prior to the initiation of IVPCA therapy. The majority of patients will be post operative patients, and will start therapy and the investigational drug in the Post Anesthesia Care Unit or the Pediatric Intensive Care Unit. We plan on studying between 10 and 99, male and female patients over a 2 year period.

Naloxone SR Capsules in Patients With Opioid Induced Constipation [Recruiting]
For many patients taking opioids for pain relief one of the most distressing side effects is constipation. Naloxone is effective in the reversal of the effects of opioids and is used following opioid overdose. If naloxone is given by mouth it would relieve the effects of constipation but as it goes into the blood stream very quickly, it would also reverse the effects of the opioid and therefore stop the pain relief. The aim of this study is to examine a slow release formulation of naloxone to see if is can reduce constipation without reducing the pain relieving effects of the opioid.

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Reports of Suspected Naloxone Side Effects

Confusional State (5),  Accidental Overdose (5),  Bradykinesia (5),  Drug Withdrawal Syndrome (5),  Bradyphrenia (5),  Dyskinesia (4),  Pulmonary Oedema (4),  Toxicity TO Various Agents (4),  Anxiety (4),  Diarrhoea (4), more >>