Treatment of opioid-induced constipation with oral naloxone: A pilot study

摘要: 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 determine if naloxone could reverse opioid-induced without precipitating abstinence or recrudescence pain opioid-dependent individuals. Concentrations unmetabolized total naloxone, including glucuronide, were measured radioimmunoassay. A dose-related increase symptoms laxation resulted all three patients studied that paralleled active plasma levels. Withdrawal occurred with area under concentration—time curves above 550 ng · min/ml dosing intervals less than 3 hours. Peak levels did not predict withdrawal. Oral ameliorates persons. Titration dose a maximum 12 mg at least 6 hours apart may be needed avoid adverse reactions. Clinical Pharmacology Therapeutics (1992) 52, 90–95; doi:10.1038/clpt.1992.106