Structural requirements for chelate antidotal efficacy in acute antimony(III) intoxication.
The LD50 for i.p. potassium antimonyl tartrate was determined to be 54.6 mg/kg in mice, with a 95% confidence range of 48.4 to 61.7 mg/kg. An examination of the antidotal efficacy of a number of different structural types of chelating agents showed that very few types were able to act as antidotes when potassium antimonyl tartrate was administered i.p. to mice at a level of 120 mg/kg. The most effective antidotes, by a substantial margin, were the water soluble vicinal dithiols: 2,3-dimercaptosuccinic acid and sodium 2.3-dimercaptopropane-1-sulfonate, with the first of these being significantly better than the second. Appreciably less effective, but still useful, was D-penicillamine. At this level of administration of antimony(III), BAL is not an effective antidote. Among other chelating agents which were also not effective at this level of antimony(III) are tartaric acid, EDTA, cysteine, sodium diethyldithiocarbamate and potassium dithiooxalate.
D000818:Animals; D000931:Antidotes / Q000627:therapeutic use*; D000965:Antimony / Q000037:antagonists & inhibitors / Q000506:poisoning*; D002614:Chelating Agents / Q000627:therapeutic use*; D004112:Dimercaprol / Q000627:therapeutic use; D008297:Male; D051379:Mice; D010396:Penicillamine / Q000627:therapeutic use; D013329:Structure-Activity Relationship; D004113:Succimer / Q000627:therapeutic use
D000931:Antidotes; D002614:Chelating Agents; D004112:Dimercaprol; D000965:Antimony; D004113:Succimer; D010396:Penicillamine