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
Published Studies Related to Naloxone
The acceptability, safety, and tolerability of methadone/naloxone in a 50:1 ratio. [2009.06]
Methadone is an effective therapy for heroin addiction, but the public health benefits are compromised by diversion and injection of prescribed methadone. Combination with naloxone is one way to reduce the risk of diversion and injection... Methadone-naloxone in 50:1 ratio has the pharmacological properties to be a useful combination product for treatment of heroin addiction with reduced risk of injection.
Ultra low-dose naloxone and tramadol/acetaminophen in elderly patients undergoing joint replacement surgery: a pilot study. [2009.03]
OBJECTIVE: A pilot study was conducted to assess whether both the rationale and feasibility exist for future randomized clinical trials to evaluate the combined use of naloxone infusion and tramadol/acetaminophen as opioid-sparing drugs in elderly patients undergoing lower extremity joint replacement surgery... CONCLUSION: Consequently, a randomized, double-blinded clinical trial comparing standard therapy versus standard therapy plus these two drugs seems warranted. In such a trial, it would require approximately 20 subjects per treatment arm to detect a 80% decrease in morphine use.
Combined prolonged-release oxycodone and naloxone improves bowel function in patients receiving opioids for moderate-to-severe non-malignant chronic pain: a randomised controlled trial. [2009.03]
BACKGROUND: This randomised, double-blind, double-dummy, parallel-group multicentre study assessed the impact of a total daily dose of 60-80 mg oral oxycodone prolonged-release (PR)/naloxone PR (OXN PR) as fixed-ratio combination for patients with opioid-induced constipation (OIC) having moderate-to-severe, non-malignant pain... CONCLUSION: This study shows that the fixed-ratio combination of OXN PR is superior to OXY PR alone in terms of bowel function, while providing effective equivalent analgesia.
The effect of naloxone-3-glucuronide on colonic transit time in healthy men after acute morphine administration: a placebo-controlled double-blinded crossover preclinical volunteer study. [2008.12.01]
BACKGROUND: Constipation is a significant side effect of opioid therapy. We have previously demonstrated that naloxone-3-glucuronide (NX3G) antagonizes the motility-lowering-effect of morphine in the rat colon. AIM: To find out whether oral NX3G is able to reduce the morphine-induced delay in colonic transit time (CTT) without being absorbed and influencing the analgesic effect... CONCLUSIONS: Orally administered NX3G is able to reverse the morphine-induced delay of CTT in humans without being detected in peripheral blood samples. Therefore, NX3G may improve symptoms of constipation in-patients using opioid medication without affecting opioid-analgesic effects.
Analgesic efficacy and safety of oxycodone in combination with naloxone as prolonged release tablets in patients with moderate to severe chronic pain. [2008.12]
This randomized, double-blind, placebo- and active-controlled, parallel-group study was designed to demonstrate the superiority of oxycodone in combination with naloxone in a prolonged release (PR) formulation over placebo with respect to analgesic efficacy.Not only does oxycodone PR/naloxone PR demonstrate analgesic efficacy comparable with oxycodone PR, but it also improves opioid-induced bowel dysfunction, and may therefore improve the acceptability of long-term opioid treatment for chronic pain.
Clinical Trials Related to Naloxone
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.
Preference for Subutex® (Buprenorphine) Versus Suboxone® (Buprenorphin/Naloxone) in Opioid Dependent Patients on Subutex (Study P05094)(COMPLETED) [Completed]
This study is designed to determine if opioid dependent subjects who are already receiving
Subutex prefer the Suboxone tablet over the Subutex tablet after switching from Subutex to
Suboxone. Subjects who are selected to participate in this study will continue their
prescribed dose of Subutex (buprenorphin 2 to 16 mg daily) for the first two days of the
study (Day 1 and Day 2) then switch to and receive an equivalent dose of Suboxone
(buprenorphine 2 to 16 mg daily) for the last 3 days of the study (Day 3, Day 4 and Day 5).
The Day 5 Visit will be the subject's last study visit. Upon completing the study, subjects
will continue their pre-study prescribed dosage of Subutex.
Abuse Potential of Buprenorphine/Naloxone [Terminated]
Buprenorphine is a treatment for opioid dependence. Naloxone is given in addition to
buprenorphine in order to limit the abuse potential that is commonly associated with
buprenorphine. The purpose of this study is to determine the abuse potential of high doses
of buprenorphine/naloxone in opioid dependent individuals.
Determine the Safety of a Sublingual Tablet Formulation of Buprenorphine and Naloxone by Extending the Combination Tablet Availability to Physicians in Office-Based Practice [Completed]
The CS 1018 study will recruit a total of 600 patients seeking treatment for opiate
dependence. They will be recruited from six states (Florida, New York, Texas, California,
Washington, and Illinois), with up to ten private physician sites or clinics participating in
each state. Coordination of the participating sites and clinics in each of the six states
will be performed from an associated Department of Veterans Affairs Medical Center (Tampa
VAMC, New York City VAMC, San Antonio VAMC, Long Beach VAMC, Seattle VAMC, and Hines VAMC).
The Principal Investigator (PI) at each of the six VAMC?s will be a physician experienced in
the treatment of opiate dependent patients.
Patients will be recruited by any of numerous strategies including word of mouth,
self-referral, local fliers, newspapers, and radio advertisements. This study will be
conducted open label with no random assignment or stratification. Patients may be accepted
for detoxification or longer-term treatment (6 to 12 months of buprenorphine/naloxone
therapy). Patients under the age of 21 will initially be admitted for detoxification; longer
treatment of these patients will be based on physician judgement of the necessary of
continued treatment. Patients will be inducted directly into buprenorphine/naloxone 4: 1
combination tablets. Patients treated in private practice will be asked to sign a treatment
contract which will delineate the terms and conditions of treatment.
Pharmacokinetic Interactions Between Buprenorphine and Tipranavir/Ritonavir [Completed]
The main purpose of this study is to examine the effect of tipranavir combined with
ritonavir, medications for the treatment of HIV-infection, on buprenorphine/naloxone (BUP) in
people who have been receiving the same dose of buprenorphine/naloxone for at least 3 weeks
before study entry.
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Page last updated: 2009-10-20
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