Ledain L, Page A, Favreau L, Besse P
Arch Mal Coeur Vaiss. 1982 May;75(5):605-12.
Mexiletine was used in 12 patients. Serum drug levels and the antiarrhythmic effects were studied in a therapeutic protocol comprising an initial intravenous administration (3,5 mg/Kg over 10 mins, then 450 mg in 5 hours) followed by oral administration (200 mg eight hourly). The serum drug levels of Mexiletine were high (1,46 +/- 0,47 microgram/ml) as from the first hour in all patients, and remained constant during intravenous administration (average: 1,59 +/- 0,72 microgram/ml). On oral therapy the average mexiletine level was 1,18 +/- 0,21 microgram/ml with two lows (1,02 microgram/ml) six to eight hours after the ingestion of the 200 mg gelules. Ventricular extrasystoles completely regressed after the initial rapid intravenous injection in 7 out of the 12 patients (58,3 p. 100) and this efficacity was maintained throughout the trial. In two patients with low serum mexiletine levels at the end of oral therapy (less than 1 microgram/ml), ventricular extrasystoles were much less frequent during the intravenous phases but reappeared during oral therapy. The clinical, electrocardiographic and hemodynamic tolerance was good (withdrawn in only one patient). The dose should be adapted to the patient's weight and hemodynamic status. When ineffective, the serum mexiletine level can be estimated and when less than 1 microgram/ml, the dose may be increased, in particular by adjusting oral dosage to 200 mg six hourly.
12名患者使用了美西律。在一个治疗方案中研究了血清药物水平和抗心律失常作用,该方案包括初始静脉给药(10分钟内给予3.5mg/kg,然后在5小时内给予450mg),随后口服给药(每8小时200mg)。所有患者从第一小时起美西律的血清药物水平就很高(1.46±0.47μg/ml),在静脉给药期间保持恒定(平均:1.59±0.72μg/ml)。口服治疗时,美西律的平均水平为1.18±0.21μg/ml,在服用200mg胶囊后6至8小时出现两个低水平(1.02μg/ml)。12名患者中有7名(58.3%)在初始快速静脉注射后室性期前收缩完全消退,并且这种疗效在整个试验中得以维持。在口服治疗结束时血清美西律水平较低的两名患者(低于1μg/ml)中,室性期前收缩在静脉给药阶段频率明显降低,但在口服治疗期间再次出现。临床、心电图和血流动力学耐受性良好(仅1名患者退出)。剂量应根据患者体重和血流动力学状态进行调整。无效时,可评估血清美西律水平,当低于1μg/ml时,可增加剂量,特别是将口服剂量调整为每6小时200mg。