Prevention of drug absorption in simulated theophylline overdose.

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, gastric lavage, oral activated charcoal and no treatment) was randomly chosen one hour after a simulated overdose with sustained-release theophylline on four separate 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 concentration-time curves relative to control) of theophylline 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 preventing theophylline absorption. Activated charcoal is potentially the most effective first-line treatment for acute overdosage with sustained-release theophylline tablets.