Cholinesterase reactivation in organophosphorus poisoned patients depends on the plasma concentrations of the oxime pralidoxime methylsulphate and of the organophosphate.
We measured in nine patients, poisoned by organophosphorus agents (ethyl parathion, ethyl and methyl parathion, dimethoate, or bromophos), erythrocyte and serum cholinesterase activities, and plasma concentrations of the organophosphorus agent. These patients were treated with pralidoxime methylsulphate (Contrathion), administered as a bolus injection of 4.42 mg.kg-1 followed by a continuous infusion of 2.14 mg.kg-1/h, a dose regimen calculated to obtain the presumed "therapeutic" plasma level of 4 mg.l-1, or by a multiple of this infusion rate. Oxime plasma concentrations were also measured. The organophosphorus agent was still detectable in some patients after several days or weeks. In the patients with ethyl and methyl several days or weeks. In the patients with ethyl and methyl parathion poisoning, enzyme reactivation could be obtained in some at oxime concentrations as low as 2.88 mg.l-1; in others, however, oxime concentrations as high as 14.6 mg.l-1 remained without effect. The therapeutic effect of the oxime seemed to depend on the plasma concentrations of ethyl and methyl parathion, enzyme reactivation being absent as long as these concentrations remained above 30 micrograms.l-1. The bromophos poisoning was rather mild, cholinesterases were moderately inhibited and increased under oxime therapy. The omethoate inhibited enzyme could not be reactivated.
Willems
J L
JL
Heymans Institute of Pharmacology, University of Ghent, Medical School, Belgium.
De Bisschop
H C
HC
Verstraete
A G
AG
Declerck
C
C
Christiaens
Y
Y
Vanscheeuwyck
P
P
Buylaert
W A
WA
Vogelaers
D
D
Colardyn
F
F
D000328:Adult; D000368:Aged; D002800:Cholinesterase Inhibitors / Q000097:blood; D002801:Cholinesterase Reactivators / Q000097:blood*; D002802:Cholinesterases / Q000097:blood; D004117:Dimethoate / Q000097:blood / Q000506:poisoning; D004912:Erythrocytes / Q000201:enzymology; D005260:Female; D006801:Humans; D007306:Insecticides / Q000097:blood / Q000506:poisoning*; D008297:Male; D008743:Methyl Parathion / Q000097:blood / Q000506:poisoning; D008875:Middle Aged; D062025:Organophosphate Poisoning; D009943:Organophosphorus Compounds / Q000097:blood; D063086:Organothiophosphates / Q000097:blood; D010278:Parathion / Q000097:blood / Q000506:poisoning; D011220:Pralidoxime Compounds / Q000097:blood*
D002800:Cholinesterase Inhibitors; D002801:Cholinesterase Reactivators; D007306:Insecticides; D009943:Organophosphorus Compounds; D063086:Organothiophosphates; D011220:Pralidoxime Compounds; D008743:Methyl Parathion; D010278:Parathion; C100092:bromophos; D002802:Cholinesterases; C028797:pralidoxime; D004117:Dimethoate