Effect of anticholinergic drugs on the efficacy of activated charcoal.
BACKGROUND
Although it is a commonly held belief that the ingestion of drugs with an anticholinergic action would prolong the duration of time after drug ingestion for effective gastrointestinal decontamination, data are lacking to support this belief. The purpose of this study is to determine whether activated charcoal is more effective in the presence of concurrent anticholinergic activity.


METHODS
A three-limbed randomized crossover study in 10 healthy volunteers was completed to determine the ability of a 50 g dose of activated charcoal to reduce the bioavailability of a simulated overdose of acetaminophen (12 x 325 mg tablets) in the presence and absence of a concurrently present anticholinergic drug, atropine (0.01 mg/kg I. M. administered 15 min prior to the acetaminophen ingestion).


RESULTS
After the acetaminophen ingestion, median Cmax occurred at 1 h for all three exposures but was lower in the atropine-treated study arm (31+/-19 mg/L) than in the control or charcoal alone intervention arms (49+/-13 and 51+/-16 mg/L, respectively) (P<0.05). Compared to the control area under the serum concentration vs. time curve, a single dose of activated charcoal 1 h after drug ingestion reduced acetaminophen bioavailability by 20% (95% CI 4-36%) and by 47% (95% CI 35-59%) in the presence of atropine (P<0.05 atropine plus charcoal vs. charcoal alone).


CONCLUSIONS
Our data support the belief that activated charcoal is more effective in the presence of anticholinergic activity. Additional study is required to determine whether in patients with anticholinergic drug overdose, activated charcoal is effective at times beyond the recommendation for overdoses of drugs without this pharmacodynamic effect.
Green
Robert
R
Department of Emergency Medicine, Internal Medicine, and Pediatrics and Child Health, Faculty of Medicine, University of Manitoba, Children's Hospital, Winnipeg, Manitoba, Canada.
Sitar
Daniel S
DS
Tenenbein
Milton
M
D000082:Acetaminophen / Q000097:blood / Q000493:pharmacokinetics; D000328:Adult; D018712:Analgesics, Non-Narcotic / Q000097:blood / Q000493:pharmacokinetics; D000931:Antidotes / Q000494:pharmacology*; D019540:Area Under Curve; D001285:Atropine / Q000494:pharmacology; D001682:Biological Availability; D002606:Charcoal / Q000494:pharmacology*; D018680:Cholinergic Antagonists / Q000494:pharmacology*; D018592:Cross-Over Studies; D004347:Drug Interactions; D005260:Female; D006207:Half-Life; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D007408:Intestinal Absorption / Q000187:drug effects; D008297:Male
D018712:Analgesics, Non-Narcotic; D000931:Antidotes; D018680:Cholinergic Antagonists; D002606:Charcoal; D000082:Acetaminophen; D001285:Atropine