Prevention of drug absorption in simulated theophylline overdose

Abstract

1 The effects of emesis, gastric lavage and oral activated charcoal on theophylline absorption were compared in healthy volunteers. 2 One of four regimes (ipecacuanha-induced emesis, gas tric lavage, oral activated charcoal and no treatment) was randomly chosen one hour after a simulated over dose with sustained-release theophylline on four sepa rate occasions in twelve healthy volunteers. 3 Syrup of ipecacuanha produced emesis in all twelve volunteers but only seven vomited any tablets. Gastric lavage yielded tablets in only one volunteer. 4 The mean systemic availabilities (areas under the con centration-time curves relative to control) of theo phylline for ipecacuanha-induced emesis, gastric lavage and charcoal, were 107.1%, 101.1% and 16.9%, respectively. 5 Oral activated charcoal was thus highly effective, while gastric lavage and emesis were ineffective in pre venting theophylline absorption. Activated charcoal is potentially the most effective first-line treatment for acute overdosage with sustained-release theophylline tablets.