Treatment of opioid‐induced constipation with oral naloxone: A pilot study Journal Article
| Authors: | Culpepper‐Morgan, J. A.; Inturrisi, C. E.; Portenoy, R. K.; Foley, K.; Houde, R. W.; Marsh, F.; Kreek, M. J. |
| Article Title: | Treatment of opioid‐induced constipation with oral naloxone: A pilot study |
| Abstract: | Opioids cause constipation by binding to specific opioid receptors in the enteric and central nervous systems. First‐pass glucuronidation limits systemic bioavailability of oral naloxone. This study was designed to determine if oral naloxone could reverse opioid‐induced constipation without precipitating abstinence or recrudescence of pain in opioid‐dependent individuals. Concentrations of unmetabolized and total naloxone, including naloxone glucuronide, were measured by radioimmunoassay. A dose‐related increase in symptoms of laxation resulted in all three opioid‐dependent patients studied that paralleled the increase in active and total naloxone plasma levels. Withdrawal symptoms occurred with plasma naloxone area under the plasma concentration—time curves above 550 ng · min/ml and with dosing intervals less than 3 hours. Peak plasma levels did not predict withdrawal. Oral naloxone ameliorates opioid‐induced constipation in opioid‐dependent persons. Titration of dose to a maximum of 12 mg at least 6 hours apart may be needed to avoid adverse reactions. Clinical Pharmacology and Therapeutics (1992) 52, 90–95; doi: © 1992 American Society for Clinical Pharmacology and Therapeutics |
| Keywords: | adult; unclassified drug; constipation; case report; pain; opiate; withdrawal syndrome; dose-response relationship, drug; pilot projects; paracetamol; methadone; substance-related disorders; metoclopramide; naloxone; oxycodone; opiate addiction; oral drug administration; middle age; docusate sodium; laxative; bisacodyl; sodium dihydrogen phosphate; human; male; female; priority journal; article; bile salt; support, non-u.s. gov't; support, u.s. gov't, p.h.s.; senna; bilron; castor oil; fleet enema |
| Journal Title: | Clinical Pharmacology & Therapeutics |
| Volume: | 52 |
| Issue: | 1 |
| ISSN: | 0009-9236 |
| Publisher: | Nature Publishing Group |
| Date Published: | 1992-07-01 |
| Start Page: | 90 |
| End Page: | 95 |
| Language: | English |
| DOI: | 10.1038/clpt.1992.106 |
| PUBMED: | 1623695 |
| PROVIDER: | scopus |
| DOI/URL: | |
| Notes: | Article -- Export Date: 30 July 2019 -- Source: Scopus |
Altmetric
Citation Impact
BMJ Impact Analytics
Related MSK Work