A review of methylnaltrexone, a peripheral opioid receptor antagonist, and its role in opioid-induced constipation Journal Article


Authors: Shaiova, L.; Rim, F.; Friedman, D.; Jahdi, M.
Article Title: A review of methylnaltrexone, a peripheral opioid receptor antagonist, and its role in opioid-induced constipation
Abstract: Objectives: Opioid medications are frequently used in pain and palliative care patients with malignancy to manage symptoms such as pain and dyspnea. However, opiates are associated with various side effects. Constipation is a particularly problematic and common side effect of opioid pharmacology. Opioid antagonists have been studied in the management of opioid-induced constipation. Methylnaltrexone (MNTX) is a peripheral opioid antagonist currently under clinical investigation. It offers the potential to reverse undesirable side effects without reversing analgesia. Methods: This article attempts to review existing clinical data, focusing on antagonism of opioid-induced adverse effects on the gastrointestinal system. Results: MNTX seems to be well tolerated with limited or transient side effects. MNTX has been shown to improve oral-cecal transit times in opioid treated patients, induce laxation in chronic opioid users, and neither reverses the analgesic effects of morphine nor cause withdrawal symptoms. Significance of results: Larger clinical trials of MNTX are still necessary to support its use as a standard for treatment of opioid-induced constipation. © 2007 Cambridge University Press.
Keywords: constipation; review; pain; oncology; narcotic analgesic agent; chemically induced disorder; drug derivative; analgesics, opioid; naltrexone; opioid-induced constipation; quaternary ammonium compounds; methylnaltrexone; opioid antagonists; 17 methylnaltrexone; narcotic antagonist; quaternary ammonium derivative; narcotic antagonists
Journal Title: Palliative and Supportive Care
Volume: 5
Issue: 2
ISSN: 1478-9515
Publisher: Cambridge University Press  
Date Published: 2007-06-01
Start Page: 161
End Page: 166
Language: English
DOI: 10.1017/s147895150707023x
PUBMED: 17578067
PROVIDER: scopus
DOI/URL:
Notes: --- - "Cited By (since 1996): 10" - "Export Date: 17 November 2011" - "Source: Scopus"
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  1. Faye Haeju Rim
    1 Rim
  2. Maryam Jahdi
    4 Jahdi