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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.
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Citations
Cited by
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Self-citationIncidence, Prevalence, and Management of Opioid Bowel Dysfunction
Pappagallo, M. (2001) · The American Journal of Surgery · doi:10.1016/s0002-9610(01)00782-6 · Cited by 531
Management of opioid side effects in cancer-related and chronic noncancer pain: a systematic review
McNicol, E., Horowicz-Mehler, N., Fisk, R. A., Bennett, K., Gialeli-Goudas, M., Chew, P. W., Lau, J., & Carr, D. (2003) · The Journal of Pain · doi:10.1016/s1526-5900(03)00556-x · Cited by 466
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Taguchi, A., Sharma, N., Saleem, R. M., Sessler, D. I., Carpenter, R. L., Seyedsadr, M., & Kurz, A. (2001) · New England Journal of Medicine · doi:10.1056/nejmoa010564 · Cited by 318
Meissner, W., Leyendecker, P., Mueller‐Lissner, S., Nadstawek, J., Hopp, M., Ruckes, C., Wirz, S., Fleischer, W., & Reimer, K. (2009) · European Journal of Pain · doi:10.1016/j.ejpain.2008.06.012 · Cited by 257
Metadata
- Authors
- Culpepper-Morgan, J. A., Inturrisi, C. E., Portenoy, R. K., Foley, K., Houde, R. W., Marsh, F., & Kreek, M. J.
- Venue
- Clinical Pharmacology and Therapeutics
- Publisher
- Wiley
- Published
- 1992-07
- Volume
- 52
- Issue
- 1
- Pages
- 90-95
- ISSN
- 0009-9236 (ISSN-L)
- 1532-6535
- OpenAlex
- W1974076297
- Cited by
- 208
- References
- 0
- FWCI
- 4.34
- Type
- journal article
- Language
- en
- Open access
- closed
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- Culpepper-Morgan, J. A., Inturrisi, C. E., Portenoy, R. K., Foley, K., Houde, R. W., Marsh, F., & Kreek, M. J. (1992). Treatment of opioid-induced constipation with oral naloxone: A pilot study. Clinical Pharmacology and Therapeutics. https://doi.org/10.1038/clpt.1992.106
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
