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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.
AuthorsJ A Culpepper-Morgan, C E Inturrisi, R K Portenoy, K Foley, R W Houde, F Marsh, M J Kreek
JournalClinical pharmacology and therapeutics (Clin Pharmacol Ther) Vol. 52 Issue 1 Pg. 90-5 (Jul 1992) ISSN: 0009-9236 [Print] United States
PMID1623695 (Publication Type: Case Reports, Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, P.H.S.)
Chemical References
  • Naloxone
  • Oxycodone
  • Methadone
Topics
  • Adult
  • Constipation (chemically induced, drug therapy)
  • Dose-Response Relationship, Drug
  • Female
  • Humans
  • Male
  • Methadone (adverse effects)
  • Middle Aged
  • Naloxone (blood, pharmacokinetics, therapeutic use)
  • Oxycodone (adverse effects)
  • Pilot Projects
  • Substance-Related Disorders

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