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Management of Opioid-Induced Constipation in Cancer Patients

Focus on Methylnaltrexone

  • Review Article
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Abstract

Opioids are one of the most widely used therapies for the palliative treatment of cancer pain; however, despite their proven analgesic efficacy, they are associated with several adverse effects. Associated with psychological distress and multiple concomitant clinical concerns, constipation is the most commonly occurring adverse effect of chronic opioid therapy in cancer patients. Whilst prophylaxis remains the first-line management option, methylnaltrexone is a recommended treatment option for opioid-related constipation if administration of laxatives is ineffective.

Due to its inability to cross the blood-brain barrier, methylnaltrexone exerts a peripheral inhibition of opioid-related effects without influencing the opioid-induced central effects; as a result, the analgesic effect of opioids is unaffected. Moreover, multiple clinical trials, albeit not always conducted specifically in cancer patients, have demonstrated that up to 4 months' treatment with either intravenous or subcutaneous methylnaltrexone provides effective relief from opioid-related constipation and is well tolerated. Preliminary evidence indicates that the addition of methylnaltrexone to standard care for opioid-related constipation may also be advantageous from a pharmacoeconomic perspective. In addition, preliminary data suggest that methylnaltrexone could be associated with some further clinical benefits other than the treatment of opioid-related constipation, such as the improvement of gastric emptying, the relief of nausea/vomiting, and the reduction of the risk of regurgitation and pulmonary aspiration.

This narrative review examines the most recent evidence and evaluates the current role of methylnaltrexone in the management of opioid-related constipation, and its potential efficacy in cancer patients. The pharmacokinetics, pharmacodynamics, efficacy and tolerability of methylnaltrexone are discussed.

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Acknowledgements

Editorial assistance for the writing of this review was provided by Luca Giacomelli, PhD and Andrea Bothwell on behalf of inScience Communications, Springer Healthcare. This assistance was funded by Pfizer.

The authors have no conflicts of interest relating to the contents of this article.

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Authors and Affiliations

  1. Emergency Care, Critical Care Medicine, Pain Medicine and Anaesthesiology Department at Tor Vergata Polyclinic, University of Rome-Tor Vergata, Viale Oxford, 81, 00133, Rome, Italy

    Antonio Gatti & Alessandro Fabrizio Sabato

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  1. Antonio Gatti
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  2. Alessandro Fabrizio Sabato
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Correspondence to Antonio Gatti.

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Gatti, A., Sabato, A.F. Management of Opioid-Induced Constipation in Cancer Patients. Clin Drug Investig 32, 293–301 (2012). https://doi.org/10.2165/11598000-000000000-00000

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