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methylnaltrexone (Relistor)
Indications:
- opioid-induced constipation in palliative care patients who aren't getting relief from laxatives
Dosage:
- given SC every other day
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:
- generally mild
- nausea, dizziness, diarrhea
Mechanism of action:
- opioid antagonist
- blocks opioid effects on the gut without blocking its CNS analgesic effects
General
gastrointestinal agent
naltrexone (ReVia, Trexan, Vivitrol, Vivitrex)
Database Correlations
PUBCHEM correlations
References
- Prescriber's Letter 15(6): 2008
New Drug: Relistor (Methylnaltrexone)
Detail-Document#: 240608
(subscription needed) http://www.prescribersletter.com
- Thomas J et al,
Methylnaltrexone for opioid-induced constipation in advanced
illness.
N Engl J Med 2008, 358:2332
PMID: 18509120