Pyridostigmine (bromide)

Pyridostigmine is an inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE; IC₅₀s = 0.35 and 1 μM, respectively, for the human enzymes).¹ Pyridostigmine (10 µM) reduces decreases in AChE activity induced by the organophosphate pesticides diisopropyl fluorophosphate, chlorpyrifos-oxon, diazinon-oxon, paraoxon, and malaoxon in isolated bovine red blood cells.² It also reduces soman-induced membrane depolarization and decreases in AChE activity in isolated human muscle bundles in a concentration-dependent manner.³ Pyridostigmine (3 mg/kg per day for four weeks) prevents tachycardia and increases in sympathetic tone in mice following myocardial infarction induced by left coronary artery ligation.⁴ Formulations containing pyridostigmine have been used in the treatment of myasthenia gravis and as neuromuscular protective agents against organophosphate poisoning.

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1. Strelnik, A.D., Petukhov, A.S., Zueva, I.V., et al. Novel potent pyridoxine-based inhibitors of AChE and BChE, structural analogs of pyridostigmine, with improved in vivo safety profile. Bioorg. Med. Chem. Lett. 26(16), 4092-4094 (2016).

2. Henderson, J.D., Glucksman, G., Leong, B., et al. Pyridostigmine bromide protection against acetylcholinesterase inhibition by pesticides. J. Biochem. Mol. Toxicol. 26(1), 31-34 (2012).

3. Maselli, R.A., Henderson, J.D., Ng, J., et al. Protection of human muscle acetylcholinesterase from soman by pyridostigmine bromide. Muscle Nerve 43(4), 591-595 (2011).

4. Durand, M.T., Becari, C., de Oliveira, M., et al. Pyridostigmine restores cardiac autonomic balance after small myocardial infarction in mice. PLoS One 9(8), e104476 (2014).