Loading
Methylnaltrexone (Relistor) is an injection or tablet that relieves the severe constipation caused by strong painkillers in people with advanced cancer, without blocking the pain relief itself.
Methylnaltrexone was approved by the FDA in April 2008 for opioid-induced constipation in adults with advanced illness receiving palliative care when laxatives have failed, on two randomised placebo-controlled trials in hospice and palliative populations in which about half of patients had a bowel movement within four hours of the first subcutaneous dose versus around 15% on placebo; indications for chronic non-cancer pain and oral tablets followed in 2014 to 2016. The EU authorised Relistor in 2008. It is a standard second-line option in palliative care guidelines after conventional laxatives; naloxegol and naldemedine are oral alternatives. Abdominal pain, flatulence and nausea are common, and gastrointestinal perforation has been reported in patients with structural bowel disease. Marketed by Salix (Bausch Health).
Quaternary derivative of naltrexone that does not cross the blood-brain barrier; blocks mu-opioid receptors in the gut to reverse opioid-induced constipation without reducing analgesia or precipitating withdrawal. Connects to Mu-opioid receptor.
1.Methylnaltrexone slips into a pocket on Mu-opioid receptor.
| Region | Year | Indication |
|---|---|---|
| US | 2008 | Opioid-induced constipation in advanced illness receiving palliative care (chronic non-cancer pain and oral tablets added 2014 to 2016) |
| EU | 2008 | Opioid-induced constipation in advanced illness receiving palliative care when laxatives are insufficient (Relistor) |
Country and place are remembered in this browser only. A postcode is sent to OpenStreetMap's Nominatim service to find coordinates when you press the button; nothing else leaves your device.
Query for this drug: (TITLE:"Methylnaltrexone" OR ABSTRACT:"Methylnaltrexone" OR TITLE:"Relistor" OR ABSTRACT:"Relistor") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Methylnaltrexone, not a curated reading list.
Shares Cancer pain management, Early integrated palliative care and the tag supportive.
Shares Early integrated palliative care and the tag supportive.
Shares Early integrated palliative care and the tag supportive.
Shares Cancer pain management and the tag supportive.
Shares Cancer pain management and the tag supportive.
Shares Early integrated palliative care and the tag supportive.
Shares Cancer pain management and the tag supportive.
Shares Early integrated palliative care and the tag supportive.