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

Netzer, Peter; Sendensky, Alexander; Wissmeyer, Michael; Baumeler, Stephan; Batista, Catarina; Scheurer, U; Krause, Thomas; Reber, P. U.; Brenneisen, Rudolf

doi:10.1111/j.1365-2036.2008.03855.x

Cited by 11 publications

(7 citation statements)

References 34 publications

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“…Interestingly, the administration of naloxone-3-glucuronide (0.16 mg/kg, p.o. ), a naloxone metabolite, reversed the effect of morphine without any impact on analgesia [92]. Naloxone-3-glucuronide is not absorbed into systemic circulation, there is no penetration through the colonic-mucosal blood barrier.…”

Section: Opioid Receptor Ligandsmentioning

confidence: 99%

Physiology, signaling, and pharmacology of opioid receptors and their ligands in the gastrointestinal tract: current concepts and future perspectives

et al. 2013

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Opioid receptors are widely distributed in the human body and are crucially involved in numerous physiological processes. These include pain signaling in the central and the peripheral nervous system, reproduction, growth, respiration, and immunological response. Opioid receptors additionally play a major role in the gastrointestinal (GI) tract in physiological and pathophysiological conditions. This review discusses the physiology and pharmacology of the opioid system in the GI tract. We additionally focus on GI disorders and malfunctions, where pathophysiology involves the endogenous opioid system, such as opioid-induced bowel dysfunction, opioid-induced constipation or abdominal pain. Based on recent reports in the field of pharmacology and medicinal chemistry, we will also discuss the opportunities of targeting the opioid system, suggesting future treatment options for functional disorders and inflammatory states of the GI tract.

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Section: Opioid Receptor Ligandsmentioning

confidence: 99%

Physiology, signaling, and pharmacology of opioid receptors and their ligands in the gastrointestinal tract: current concepts and future perspectives

et al. 2013

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“…The potency of NLL to precipitate opioid withdrawal from acute morphine dependence has been reported [4]. It has also been demonstrated that NLG can antagonize the mobility-lowering effect of morphine in the rat colon [5,6]. Therefore, development of a bioanalytical method for the quantification of NLX, NLL, and NLG in plasma samples is needed to better understand their toxicokinetic and pharmacokinetic behaviors.…”

Section: Introductionmentioning

confidence: 96%

Development and validation of a sensitive LC/MS/MS method for the simultaneous determination of naloxone and its metabolites in mouse plasma

Jiang

Wang

Shet

et al. 2011

Journal of Chromatography B

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“…The N-dealkylation and reduction of 6-oxo group further precede glucuronidation and naloxone-3-b-D-glucuronide is the predominant metabolite of naloxone in humans [16]. Naloxone-3-b-D-glucuronide has demonstrated peripheral opioid antagonist activity in an ex-vivo model and in humans [20,21]. Therefore, its pharmacokinetics profile was evaluated in this study.…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics of Sublingual Buprenorphine and Naloxone in Subjects with Mild to Severe Hepatic Impairment (Child-Pugh Classes A, B, and C), in Hepatitis C Virus-Seropositive Subjects, and in Healthy Volunteers

et al. 2015

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Severe and moderate hepatic impairment significantly increased exposure of naloxone and to a lesser extent of buprenorphine. Therefore, buprenorphine/naloxone combination products should generally be avoided in patients with severe hepatic impairment and may not be appropriate for patients with moderate hepatic impairment. However, buprenorphine/naloxone products may be used with caution for maintenance treatment in patients with moderate hepatic impairment who have initiated treatment on a buprenorphine product without naloxone [Registered at ClinicalTrials.gov as NCT01846455].

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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

Abstract: SUMMARY BackgroundConstipation 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.

Cited by 11 publications

References 34 publications

Physiology, signaling, and pharmacology of opioid receptors and their ligands in the gastrointestinal tract: current concepts and future perspectives

Physiology, signaling, and pharmacology of opioid receptors and their ligands in the gastrointestinal tract: current concepts and future perspectives

Development and validation of a sensitive LC/MS/MS method for the simultaneous determination of naloxone and its metabolites in mouse plasma

Pharmacokinetics of Sublingual Buprenorphine and Naloxone in Subjects with Mild to Severe Hepatic Impairment (Child-Pugh Classes A, B, and C), in Hepatitis C Virus-Seropositive Subjects, and in Healthy Volunteers

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