An in vitro evaluation of fluoxetine adsorption by activated charcoal and desorption upon addition of polyethylene glycol-electrolyte lavage solution.
BACKGROUND
In drug overdoses, treatment with activated charcoal is frequently used because of its adsorptive properties. Recently, whole-bowel irrigation with polyethylene glycol-electrolyte lavage solution has been used as a gastrointestinal decontamination procedure for ingestions of toxins not well adsorbed to activated charcoal and for toxins with a delayed absorption phase, although well adsorbed to activated charcoal. While a combined approach using activated charcoal and whole-bowel irrigation could theoretically enhance the efficacy of both modalities, this improvement remains speculative, since data demonstrating its clinical advantage in overdose treatment are lacking. Fluoxetine, a selective serotonin uptake inhibitor, is one of the most frequently prescribed antidepressants. Fluoxetine is well adsorbed onto activated charcoal. This in vitro investigation was undertaken to study: a) the effect of polyethylene glycol, as well as polyethylene glycol-electrolyte lavage solution, on the adsorption of fluoxetine to laboratory grade-activated charcoal and a commercial activated charcoal formulation (Carbomix powder) in simulated gastric (pH= 1.2) and intestinal (pH=7.2) fluid environment; b) whether the order of polyethylene glycol-electrolyte lavage solution addition would have any effect on the adsorption of fluoxetine to activated charcoal.


METHODS
Adsorption of fluoxetine to charcoal in the presence of polyethylene glycol was examined: a) by the simultaneous addition of polyethylene glycol and charcoal to fluoxetine solution and b) by the addition of charcoal to fluoxetine solution and subsequent addition of polyethylene glycol. In both cases, the slurries were incubated at 37 degrees C for 1 hour and filtered. Free fluoxetine concentration was determined in the diluted filtrate by a reversed-phase high-performance liquid chromatography method.


RESULTS
The amount of fluoxetine adsorbed to activated charcoal (or Carbomix) was dramatically decreased at gastric and intestinal pH by the presence of polyethylene glycol or polyethylene glycol-electrolyte lavage solution added either concurrently or sequentially to activated charcoal.


CONCLUSIONS
In cases of fluoxetine overdose, administration of activated charcoal is recommended, while a combined approach using activated charcoal and whole-bowel irrigation with polyethylene glycol-electrolyte lavage solution is not recommended since it causes a significant desorption of the drug from activated charcoal.
Atta-Politou
J
J
University of Athens, Greece.
Kolioliou
M
M
Havariotou
M
M
Koutselinis
A
A
Koupparis
M A
MA
D000327:Adsorption / Q000187:drug effects; D002606:Charcoal; D002851:Chromatography, High Pressure Liquid; D062787:Drug Overdose / Q000628:therapy; D005069:Evaluation Studies as Topic; D005473:Fluoxetine / Q000493:pharmacokinetics*; D005751:Gastric Lavage; D006863:Hydrogen-Ion Concentration; D011092:Polyethylene Glycols / Q000494:pharmacology*; D017367:Selective Serotonin Reuptake Inhibitors / Q000493:pharmacokinetics*; D012996:Solutions; D007507:Therapeutic Irrigation
D002606:Charcoal; D005473:Fluoxetine; D011092:Polyethylene Glycols; D017367:Selective Serotonin Reuptake Inhibitors; D012996:Solutions