Inhibitors of the acetylcholinesterase enzyme were first described in the
latter part of the 19th century. Some of these inhibitors also inhibit the butyrylcholinesterase
enzyme. Therapeutic uses of the cholinesterase inhibitors include
ophthalmology, anesthesia, myasthenia gravis, muscarinic antagonist overdose and
Alzheimer’s disease. Many pesticides act by inhibiting cholinesterase, with the
potential for accidental or deliberate poisoning. Cholinesterase inhibitors were also
developed as nerve agents for chemical warfare.
This chapter describes the discovery and early studies on the effects and mechanism of
action of cholinesterase inhibitors. Subsequent development led to the discovery of a
large and varied group of cholinesterase inhibitors. These drugs will be discussed with
regard to their therapeutic uses and clinical considerations. Finally, concerns regarding
cholinesterase inhibitor toxicity when used as pesticides and nerve agents will be
discussed.
Keywords: Acetylcholinesterase, Acetylcholine, Alzheimer’s disease, Atropine,
Butyrylcholinesterase, Donepezil, Edrophonium, Galantamine, Glaucoma,
Myasthenia gravis, Neostigmine, Nerve agent, Organophosphate, Physostigmine,
Pesticide, Pralidoxime, Pyridostigmine, Rivastigmine.
