The Medical Letter on Drugs and Therapeutics
Methylnaltrexone (Relistor) for Opioid-Induced Constipation
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The FDA has approved subcutaneous injection of methylnaltrexone (Relistor – Wyeth/Progenics), a selective mu-opioid receptor antagonist, for treatment of opioid-induced constipation in patients with advanced illness (such as incurable cancer or end-stage chronic obstructive pulmonary disease) who are receiving palliative care. Another mu-opioid receptor antagonist, alvimopan (Entereg – GlaxoSmithKline/Adolor), has been approved only for short-term, in-hospital use to treat postoperative ileus. It will be reviewed in a future issue.

OPIOID-INDUCED CONSTIPATION — Although patients develop tolerance to the analgesia, respiratory depression and other central-nervous system effects of opioids, they do not develop tolerance to constipation, which can be dose-limiting.1 It is usually treated with laxatives and stool softeners.

MECHANISM OF ACTION — ... more      

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Title: Methylnaltrexone (Relistor) for Opioid-Induced Constipation
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