Heuer H, Gülker H, Hasfeld M, Frenking B, Behrenbeck T
Medizinische Klinik und Poliklinik, Abteilung Innere Medizin C, Westfälische Wilhelms-Universität Münster.
Z Kardiol. 1987 Jul;76(7):415-20.
Diprafenone is a new antiarrhythmic drug with a dominant local anaesthetic action and an additional beta-sympathicolytic activity. In this study, the results of long-term treatment (8 months on average) obtained from 27 patients with chronic ventricular arrhythmias are reported. Before diprafenone, all patients were treated unsuccessfully with flecainide, propafenone, sotalol, combined sotalol/flecainide and sotalol/propafenone, and another two to six antiarrhythmic agents. Following diprafenone (300-600 mg/24 h), a substantial reduction in arrhythmic activity (greater than or equal to 80%; Lown classification less than or equal to II) was achieved in 21 cases. In 12 patients, side effects (fatigue, headache, blurred vision, dizziness and heartburn) were apparent. Diprafenone had to be discontinued in five patients, because of these side effects. At dosages greater than or equal to 450 mg/24 h, the PQ interval was significantly lengthened, and QRS duration prolonged. In one patient, an AV block III degree developed. In another case, SGOT and SGPT increased significantly; this increase was reversed after the drug was discontinued. Despite these side effects, further clinical evaluation of the compound seems promising, as the antiarrhythmic potency of diprafenone is very strong and superior to that of propafenone with respect to the required doses.
双苯丙胺是一种新型抗心律失常药物，具有显著的局部麻醉作用和额外的β-交感神经阻滞活性。在本研究中，报告了对27例慢性室性心律失常患者进行长期治疗（平均8个月）的结果。在使用双苯丙胺之前，所有患者使用氟卡尼、普罗帕酮、索他洛尔、索他洛尔/氟卡尼联合用药、索他洛尔/普罗帕酮联合用药以及另外两到六种抗心律失常药物治疗均未成功。使用双苯丙胺（300 - 600 mg/24 h）后，21例患者的心律失常活动大幅降低（大于或等于80%；洛恩分级小于或等于Ⅱ级）。12例患者出现副作用（疲劳、头痛、视力模糊、头晕和烧心）。由于这些副作用，5例患者不得不停用双苯丙胺。在剂量大于或等于450 mg/24 h时，PQ间期显著延长，QRS时限增宽。1例患者发生Ⅲ度房室传导阻滞。另1例患者血清谷草转氨酶（SGOT）和血清谷丙转氨酶（SGPT）显著升高；停药后这种升高得以逆转。尽管有这些副作用，但由于双苯丙胺的抗心律失常效力非常强，且就所需剂量而言优于普罗帕酮，因此对该化合物进行进一步临床评估似乎很有前景。
