Organophosphorous poisoning: Treatment and analytical methodologies applied in evaluation of reactivation and inhibition of acetylcholinesterase

Abstract

Organophosphorus derivatives inhibit the enzyme acetylcholinesterase promoting cholinergic hyperstimulation, irreversible damage and death. These compounds are used by civil and military organizations as pesticides or chemical weapons, respectively, and are responsible for over three million annual cases of poisoning, as well as more than 250,000 deaths per year from intentional self-poisoning, accounting 30% of suicides in the world. The organophosphorus sarin, soman, tabun and VX are been employed as weapons of war by different terrorist groups. Oxime derivatives (pralidoxime and obidoxima) have been used as antidote in detoxification step, but the results are still not satisfactory, because these drugs have low penetration into blood-brain barrier and an inefficient nucleophilic action against organophosphorus. Thus, different analytical methods can be used to monitor the efficiency of drugs with property to reactivate or inhibit the acetylcholinesterase enzyme. This paper provides an overview of the derivatives of oximes currently used as potential reactivators and inhibitors, as well as of the main methodologies used in monitoring or reactivation or inhibition of acetylcholinesterase.