Anti-Nicotinic and Anti-Muscarinic Actions of Eperisone in the Isolated Canine Atrium.

Abstract

ABSTRACT-The effects of eperisone, an antispastic agent, on the chronotropic and inotropic responses to acetylcholine, nicotine or stimulation of intracardiac autonomic nerves were evaluated in isolated, blood-perfused canine atrium. Eperisone (10-300,ug) injected into the sinus node artery of the isolated atrium produced dose-related nega tive chronotropic and inotropic effects, which were not affected by atropine. In the same doses, eperisone inhibited the negative chronotropic and inotropic responses to an injection of acetylcholine and intracardiac parasympathetic stimulation. Eperisone also suppressed the negative followed by positive cardiac responses to nicotine, but did not modify the positive responses to intracardiac sympathetic stimulation or nor epinephrine. The inhibitory effect persisted much longer for the responses to nicotine or parasympathetic stimulation than for those to acetylcholine. These results suggest that eperisone at doses that induce direct cardiac depressant effects exerts its blocking action on nicotinic receptors at parasympathetic ganglia and sympathetic nerve termi nals and on muscarinic receptors at the effector cells in the dog heart.

A case oftorsades de pointesinduced by severe QT prolongation after an overdose of eperisone and triazolam in a patient receiving nifedipine

“…Additionally, in the isolated canine atrium, eperisone produces a cardiac depressant effect by inhibiting nicotinic and muscarinic receptors. 7 In our patient, QT prolongation may have been attributable to the prolonged cardiac repolarization time caused by the potassium channelblocking effect associated with the inhibition of muscarinic receptors by eperisone. However, evidence of eperisonemediated potassium channel blockade has not been reported in the literature.…”

Cytochrome P450 2J2: Potential Role in Drug Metabolism and Cardiotoxicity

“…Eperisone (Saegusa et al, 1991;Yamagiwa et al, 2014) QTc interval prolongation morphology and function in rats for 8 weeks after 1.25 mg/kg DOX demonstrated changes in cardiac function, in particular, cardiac output, stroke volume, and ejection fraction from day 15. Gross morphologic changes and biomarkers associated with cardiomyocyte degeneration occurred much later (Cove-Smith et al, 2014).…”

Tolperisone: A Typical Representative of a Class of Centrally Acting Muscle Relaxants with Less Sedative Side Effects

“…Interestingly, the action of lanperisone was longer lasting than that of eperisone and seemed to act in addition to the spinal circuits via supraspinal elements. In order to study possible cardiac side effects, eperisone was injected into the sinus node artery of isolated canine atrium (Saegusa et al 1991). Dose‐related negative chronotropic and inotropic effects were observed.…”