ABSTRACT
This chapter aims to turn readers’ attention to antidotal therapy with acetylcholinesterase (AChE) reactivators. It describes the history of the development of the AChE reactivators, especially within the last 25 years, and their basic pharmacokinetic and pharmacodynamic properties. The positive charge at the pyridinium ring of oxime reactivators provides strong affinity for binding at the active site of AChE. The main benefit of administration of an oxime after exposure to organophosphorus compounds (OPC) is its potency to reactivate OPC-inhibited AChE and restore its basic physiological function—hydrolysis of the neurotransmitter ACh after it has fulfilled its physiological function. In the case of poisoning with organophosphorus insecticides (OPI), the effectiveness of oximes depends on the chemical structure of the OPI. A pathway for increasing the antidotal performance is to improve the pharmacokinetic properties of oximes, allowing critical levels to be reached in crucial areas such as central nervous system regions and diaphragm.
