Haffajee C I, Sacks G M, Alpert J S, Howe J P, Ockene I S, Paraskos J A, Dalen J E
Clin Cardiol. 1983 Feb;6(2):72-8. doi: 10.1002/clc.4960060206.
Tocainide, an oral analog of lidocaine, was evaluated as a long-term antiarrhythmic agent in 21 patients with symptomatic complex ventricular ectopic activity (10 with hemodynamically significant ventricular tachycardia) refractory to currently available antiarrhythmics singly, and in combination for periods of 3 days to 35 months (mean 13.6 months). Tocainide appeared to be an effective and safe agent for the control of these refractory symptomatic ventricular arrhythmias in 14 of the 21 patients (66%). Minor central nervous system and gastrointestinal side effects were present in most of the patients, usually early on in therapy, and only precluded long-term use in 2 patients. Furthermore, lidocaine responsiveness was a good predictor of tocainide effectiveness in this group of patients. Tocainide precipitated atrioventricular (A-V) block in one patient with pre-existing A-V nodal disease; two patients developed a skin rash while on tocainide therapy. These two patients had previously developed lupus-like syndromes and skin rashes while on procainamide. The ANA titers had been falling in these two patients while on tocainide, and in one of these patients with true systemic lupus erythematosus, rechallenge with tocainide failed to produce skin rash. Tocainide's long plasma half-life and high oral bioavailability permit an 8-h regime. We conclude that tocainide is an effective, safe antiarrhythmic agent with tolerable side effects.
妥卡尼是利多卡因的口服类似物,在21例有症状的复杂性室性异位活动患者(其中10例有血流动力学意义的室性心动过速)中被评估为一种长期抗心律失常药物,这些患者对目前可用的抗心律失常药物单独或联合治疗均无效,治疗时间为3天至35个月(平均13.6个月)。在21例患者中的14例(66%),妥卡尼似乎是控制这些难治性有症状室性心律失常的一种有效且安全的药物。大多数患者出现轻微的中枢神经系统和胃肠道副作用,通常在治疗早期出现,仅2例患者因此而不能长期使用。此外,利多卡因反应性是该组患者妥卡尼疗效的一个良好预测指标。妥卡尼使1例原有房室结疾病的患者发生了房室传导阻滞;2例患者在妥卡尼治疗期间出现皮疹。这2例患者在使用普鲁卡因胺时曾出现过狼疮样综合征和皮疹。在使用妥卡尼期间,这2例患者的抗核抗体滴度一直在下降,其中1例患有真正系统性红斑狼疮的患者再次使用妥卡尼未出现皮疹。妥卡尼的血浆半衰期长且口服生物利用度高,允许采用8小时给药方案。我们得出结论,妥卡尼是一种有效、安全且副作用可耐受的抗心律失常药物。