Suppression of calcium current in a snail neurone by eperisone and its analogues

Effect of tolperisone on the resting brain and on evoked responses, an phMRI BOLD study

“…Although tolperisone has long been used worldwide, the exact mechanism of its action was revealed only in the last decade. Its therapeutic effect is mediated by several signalization pathways; however, the main targets of tolperisone are voltage gated sodium and calcium channels (Novales-Li et al, 1989;Kocsis et al, 2005;Hofer et al, 2006). Tolperisone reveals a strong reflex inhibitory action (Pratzel et al, 1996;Dulin et al, 1998) and several studies report its analgesic properties in rodents (Sakaue et al, 2004) and in humans (Svensson et al, 2003).…”

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

“…The mechanism underlying cardiotoxicity in this case may be as follows: Voltage clamp experiments performed on snail neurons have shown that the inhibition of voltage-dependent calcium flow by eperisone depends on the extracellular concentration of the drug. 6 The hypotension and bradycardia observed on arrival may be attributed to the negative inotropic effects associated with the calcium antagonist action; these effects consist of peripheral vasodilation, bradycardia, and reduced cardiac contractility. Additionally, in the isolated canine atrium, eperisone produces a cardiac depressant effect by inhibiting nicotinic and muscarinic receptors.…”

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

“…Eperisone acts as a calcium antagonist on smooth muscle tissues of the guinea pig basilar artery and is an antispastic agent (3). Eperisone is also a calcium antagonist in the snail neuron (9). Calcium antagonists induce the negative chrono tropic and inotropic effects, which are not affected by atropine, in the isolated, blood perfused dog heart preparations (10-13).…”