methylnaltrexone (Relistor)
Jump to navigation
Jump to search
Indications
- opioid-induced constipation in palliative care patients who aren't getting relief from laxatives[2][3][4]
Contraindications
Dosage
- given SC every other day
- oral formulation available
- laxative therapy should be discontinued before starting methylnaltrexone[3]
Pharmacokinetics
- methyl group keeps it from crossing into the CNS
- about 1/2 of patients will have a response within 4 hours after the 1st dose
Adverse effects
Mechanism of action
- opioid antagonist
- blocks opioid effects on the gut without blocking its CNS analgesic effects
More general terms
References
- ↑ Prescriber's Letter 15(6): 2008 New Drug: Relistor (Methylnaltrexone) Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=240608&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Jump up to: 2.0 2.1 Thomas J et al, Methylnaltrexone for opioid-induced constipation in advanced illness N Engl J Med 2008, 358:2332 PMID: https://www.ncbi.nlm.nih.gov/pubmed/18509120
- ↑ Jump up to: 3.0 3.1 3.2 3.3 Geriatric Review Syllabus, 12th edition (GRS12) Colburn JL, Wescott AM, Potter JF (eds) American Geriatrics Society, 2025
- ↑ Jump up to: 4.0 4.1 Zhang YY, Zhou R, Gu WJ. Efficacy and Safety of Methylnaltrexone for the Treatment of Opioid-Induced Constipation: A Meta-analysis of Randomized Controlled Trials. Pain Ther. 2021 Jun;10(1):165-179. PMID: https://www.ncbi.nlm.nih.gov/pubmed/33575953 PMCID: PMC8119523 Free PMC article. Review. https://pmc.ncbi.nlm.nih.gov/articles/PMC8119523/