Carmeliet E, Janssen P A, Marsboom R, Van Nueten J M, Xhonneux R
Arch Int Pharmacodyn Ther. 1978 Jan;231(1):104-30.
Lorcainide hydrochloride or N-(4-chlorophenyl)-N-[1-(1-methyl-ethyl)-4-piperidinyl]benzeneacetamide mono-hydrochloride (R 15889) is a new anti-arrhythmic drug. Studies in dogs show that lorcainide is effective against post-infarction and ouabain-induced ventricular arrhythmias, and abolishes acetylcholine and aconitine-induced atrial fibrillation; it elevates the threshold of electrically induced ventricular fibrillation. In isolated dog and cow Purkinje fibers, in dog ventricular and in guinea-pig auricular muscle preparations, lorcainide decreases the rate of rise of the transmembrane action potential, the conduction velocity and spontaneous activity. It prolongs the refractory period of isolated Purkpinje and ventricular muscle preparations, and the functional refractory period of the AV node in the guinea-pig heart. It has no effect on Ca mediated electrical activity. Isometric force measurements in isolated cat papillary muscles and hemodynamic studies in anaesthetized and unanaesthetized dogs indicate that lorcainide moderately decreases myocardial contractility. Side effects observed at large doses are of central origin and include salivation, tremor and vomiting. Intravenous injection induces transient peripheral vasodilatation. Lorcainide is an antiarrhythmic of the local anaesthetic type. It is characterized by a good oral absorption, a long duration of action and a large safety factor.
盐酸劳卡尼，即N -（4 - 氯苯基）- N - [1 -（1 - 甲基乙基）- 4 - 哌啶基]苯乙酰胺单盐酸盐（R 15889），是一种新型抗心律失常药物。对犬类的研究表明，劳卡尼对心肌梗死后及哇巴因诱发的室性心律失常有效，能消除乙酰胆碱和乌头碱诱发的心房颤动；它能提高电诱导室颤的阈值。在离体犬和牛浦肯野纤维、犬心室及豚鼠心房肌标本中，劳卡尼可降低跨膜动作电位的上升速率、传导速度及自发活动。它能延长离体浦肯野纤维和心室肌标本的不应期，以及豚鼠心脏房室结的功能不应期。它对钙介导的电活动无影响。在离体猫乳头肌上进行的等长力测量及在麻醉和未麻醉犬身上进行的血流动力学研究表明，劳卡尼可适度降低心肌收缩力。大剂量时观察到的副作用源于中枢神经系统，包括流涎、震颤和呕吐。静脉注射会引起短暂的外周血管扩张。劳卡尼是一种局部麻醉类型的抗心律失常药物。其特点是口服吸收良好、作用持续时间长且安全系数大。
