Yanagisawa T, Satoh K, Taira N
Arch Int Pharmacodyn Ther. 1979 Feb;237(2):316-29.
The effects of trimetazidine on the electrical and mechanical activities of the myocardium were investigated in comparison with the effect on the coronary blood flow in blood-perfused preparations excised from dog hearts. In the sinoatrial (SA) node preparation trimetazidine injected into the sinus node artery increased blood flow and depressed SA node automaticity. In the atrioventricular (AV) node preparation trimetazidine injected into the AV node artery or the anterior septal artery increased blood flow and equally prolonged AV conduction time. In the papillary muscle preparation trimetazidine injected into the anterior septal artery increased blood flow and depressed force of contraction. These cardiodepressant actions occurred in the same range of doses of trimetazidine that exerted the vasodilator action. This indicates that trimetazidine has no selective activity on the coronary vasculature alone. Moreover, the vasodilator effect was more short-lived than the cardiodepressant action. Trimetazidine injected into the anterior septal artery affected ventricular bipolar electrograms. This, taken together with the prolongation of AV conduction time obtained with the same route of administration, suggests that the cardiodepressant action of trimetazidine is ascribed to the local anaesthetic or the membrane stabilizing action rather than to the calcium-antagonistic action.
在从狗心脏切除的血液灌注制剂中,研究了曲美他嗪对心肌电活动和机械活动的影响,并与对冠状动脉血流的影响进行了比较。在窦房(SA)结制剂中,注入窦房结动脉的曲美他嗪增加了血流量并降低了窦房结自律性。在房室(AV)结制剂中,注入房室结动脉或前间隔动脉的曲美他嗪增加了血流量并同样延长了房室传导时间。在乳头肌制剂中,注入前间隔动脉的曲美他嗪增加了血流量并降低了收缩力。这些心脏抑制作用发生在曲美他嗪发挥血管舒张作用的相同剂量范围内。这表明曲美他嗪对冠状动脉血管系统没有单独的选择性活性。此外,血管舒张作用比心脏抑制作用持续时间更短。注入前间隔动脉的曲美他嗪影响心室双极电图。这与通过相同给药途径获得的房室传导时间延长一起表明,曲美他嗪的心脏抑制作用归因于局部麻醉或膜稳定作用,而不是钙拮抗作用。