Connolly S J, Gupta R N, Hoffert D, Roberts R S
Department of Medicine, McMaster University, Hamilton, Ontario, Canada.
Am Heart J. 1988 Jun;115(6):1208-13. doi: 10.1016/0002-8703(88)90010-5.
Twelve patients with frequent ventricular premature depolarizations (VPDs) received amiodarone, 600 mg/day, for up to 8 weeks. On days 0, 1, 4, 8, 15, 22, 36, and 57 of treatment, 24-hour ambulatory ECGs were obtained, and multiple blood samples were taken for determination of amiodarone and desethylamiodarone plasma concentrations. All patients had at least 75% suppression of VPDs. The mean duration of therapy before the onset of antiarrhythmic effect was 13.2 days (range 1 to 36 days). Trough amiodarone and desethylamiodarone plasma concentrations at the time of onset of antiarrhythmic effect were 0.86 +/- 0.48 mg/L and 0.23 +/- 0.15 mg/L, respectively. Sixty-seven percent of patients responded at amiodarone concentrations below 1.0 mg/L. For each patient there was a progressive decrease in frequency of VPDs as both amiodarone and desethylamiodarone concentrations increased. Regression modeling indicated that both amiodarone and desethylamiodarone plasma concentrations explained significant variability in the frequency of VPDs, and amiodarone and desethylamiodarone plasma concentrations were highly correlated with each other. There was a trend for desethylamiodarone to explain more variability in frequency of VPDs than amiodarone.
12例频发室性早搏患者接受胺碘酮治疗，剂量为600mg/天，持续8周。在治疗的第0、1、4、8、15、22、36和57天，进行24小时动态心电图检查，并采集多份血样以测定胺碘酮和去乙基胺碘酮的血浆浓度。所有患者的室性早搏至少有75%得到抑制。抗心律失常作用起效前的平均治疗时间为13.2天（范围1至36天）。抗心律失常作用起效时胺碘酮和去乙基胺碘酮的血浆谷浓度分别为0.86±0.48mg/L和0.23±0.15mg/L。67%的患者在胺碘酮浓度低于1.0mg/L时出现反应。随着胺碘酮和去乙基胺碘酮浓度的增加，每位患者的室性早搏频率逐渐降低。回归模型表明，胺碘酮和去乙基胺碘酮的血浆浓度均能解释室性早搏频率的显著变异性，且胺碘酮和去乙基胺碘酮的血浆浓度彼此高度相关。去乙基胺碘酮比胺碘酮更能解释室性早搏频率变异性的趋势。
