Prevention of drug absorption in simulated theophylline overdose

To assess the effectiveness of oral activated charcoal and catharsis in preventing theophylline absorption, 12 healthy subjects, aged 20-35 years, received 3 x 200 mg sustained-release theophylline tablets and 16 radio-opaque placebo tablets on six occasions. On each occasion, they received either no treatment (control) or one of five treatments. Treatments were a) oral activated charcoal (Carbomix): 50 g at 1 h, 25 g at 5 h and 9 h; b) sorbitol 70%: 150 mL at 1 h; c) activated charcoal: 50 g at 6 h, 25 g at 10 h and 14 h; d) sorbitol 70%: 150 mL at 6 h; e) charcoal commencing at 6 h plus sorbitol at 6 h (i.e. a combination of treatments c and d). Plasma theophylline concentrations were measured and all stools collected over 36 h to assess placebo tablet recovery by radiography. Charcoal administration at 1 h was 91.2% effective in preventing theophylline absorption and at 6 h was 57.3% effective, while combined charcoal and catharsis at 6 h was 63.3% effective. Sorbitol-induced catharsis at 1 h and 6 h did not reduce theophylline absorption despite greater tablet recovery. Oral activated charcoal may be the most effective treatment for sustained-release theophylline overdose, with maximum benefit when administered soon after an overdose, though later administration might still be of value. Sorbitol catharsis is of no benefit either alone or in combination with charcoal.