[Investigation of neuromuscular blocking agents at Richter Ltd].

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Karpati E, Biro K, Kukorelli T

[Investigation of neuromuscular blocking agents at Richter Ltd].

Acta Pharm Hung. 2002;72(1):37-48.

PubMed ID

12426786 [ View in PubMed

]

Abstract

Investigation of new neuromuscular blocking agents was started 30 years ago in Richter Ltd. This paper presents the results obtained by Richter's scientists. 2 compounds out of 100 bisquaternary ammonio steroid having androstane skeleton were selected for further pharmacological study. One of these agents, pipecuronium bromide (Arduan) elicited long-lasting block of neuromuscular transmission without cardiovascular side effects in both animal experiments and clinical studies. Arduan is a powerful competitive antagonist of acetylcholine, since it can bind pre- and postsynaptic (N1) receptors of the transmitters. It has no remarkable cumulative effect. Neostigmine rapidly and completely antagonized the neuromuscular blockade caused by pipecuronium. Arduan was introduced into clinical practice. The second compound, RGH-4201 (Duador) evoked a neuromuscular block of short duration. It showed slight atropin-like cardio-vagolytic effect in animal experiments. In the clinical studies, however, the cardiovascular side effects were found to be too strong. Therefore, it was not introduced in clinical practice.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Pipecuronium	Muscarinic acetylcholine receptor M2	Protein	Humans	Unknown	Antagonist	Details
Pipecuronium	Muscarinic acetylcholine receptor M3	Protein	Humans	Unknown	Antagonist	Details
Pipecuronium	Neuronal acetylcholine receptor subunit alpha-2	Protein	Humans	Yes	Antagonist	Details