Carmeliet E, Janssen P A, Heykants J, Niemegeers C J, Remeysen P, Van De Water A, Van Gerven W, Wauquier A, Xhonneux R
Arch Int Pharmacodyn Ther. 1987 Jun;287(2):272-90.
Transcainide was selected as an antiarrhythmic drug with potential clinical application. In isolated dog, sheep and rabbit Purkinje fibres, in dog and guinea-pig trabecular preparations and in the guinea-pig right auricle, transcainide decreases the rate of rise of the transmembrane action potential, with no effect on normal spontaneous activity and calcium-mediated action potentials; it inhibits early after-depolarizations. The effect on the rate of rise is very slow in onset. In vivo a prolongation of QRS duration is observed. In dogs, the drug 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. Hemodynamic studies in anaesthetized and unaesthetized dogs indicate that transcainide moderately decreases contractility, while slightly increasing frequency. No major side effects are seen. Preliminary data on the pharmacokinetics suggest that in the dog the observed effects after i.v. infusion are related to the parent drug. Transcainide is an antiarrhythmic of the local anaesthetic type, with very slow kinetics. It is characterized by a good oral absorption and a long duration of action.
曲卡尼被选为一种具有潜在临床应用价值的抗心律失常药物。在离体的犬、羊和兔浦肯野纤维、犬和豚鼠小梁标本以及豚鼠右心房中，曲卡尼可降低跨膜动作电位的上升速率，对正常自发活动和钙介导的动作电位无影响；它能抑制早期后去极化。对上升速率的影响起效非常缓慢。在体内可观察到QRS时限延长。在犬中，该药物对心肌梗死后和哇巴因诱导的室性心律失常有效，并可消除乙酰胆碱和乌头碱诱导的心房颤动；它可提高电诱导室颤的阈值。对麻醉和未麻醉犬的血流动力学研究表明，曲卡尼适度降低心肌收缩力，同时轻微增加心率。未见重大副作用。药代动力学的初步数据表明，在犬中静脉输注后观察到的效应与母体药物有关。曲卡尼是一种局部麻醉类型的抗心律失常药物，动力学非常缓慢。其特点是口服吸收良好，作用持续时间长。
