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Potentiation of neostigmine and pyridostigmine by 4-aminopyridine in the rat

1978; Oxford University Press; Volume: 30; Issue: 1 Linguagem: Inglês

10.1111/j.2042-7158.1978.tb13368.x

2042-7158

Ronald D. Miller, Peter A F Dennissen, Francien van der Pol, S. Agoston, L.H.D.J. Booij, Jan F. Crul,

Quinazolinone synthesis and applications

Abstract The interaction between 4-aminopyridine and neostigmine or pyridostigmine was studied in vivo in the rat sciatic nerve-anterior tibialis preparation using the constant infusion of pancuronium technique. The ED50 (dose of drug which produced a 50% antagonism) of neostigmine, pyridostigmine and 4-aminopyridine were 18, 49 and 440 μg kg−1 respectively. The addition of 100 μg kg−1 of 4-aminopyridine, which produced no antagonism by itself, decreased the neostigmine ED50 to 7·4 μg kg−1. The addition of 200 μg kg−1 of 4-aminopyridine, which produced a 30% antagonism by itself, decreased the ED50 of pyridostigmine to 11 μg kg−1. We conclude that both neostigmine and pyridostigmine interact with 4-amino-pyrine synergistically.