Mazur N A, Liakishev A A, Podrid F D, Piotrovskiĭ V K
Kardiologiia. 1979 Oct;19(10):17-21.
The anti-arrhythmic activity of mexitil was studied in 36 patients with frequent, prognostically unfavourable ventricular extrasystoles of various etiology. Quantitative and qualitative assessment of rhythm disorders was accomplished by bicycle ergometry and ECG recording for 24 hours by means of portable monitors. The disorders of rhythm were appraised prior to treatment, during mexitil medication in daily doses of 750--1200 mg/24 hrs administered for 3--5 days, and against the background of placebo. The effect of a single 250 to 600 mg dose of mexitil was appraised by monitoring the ECG for three and a half hours. The concentration of mexitil in blood plasma and saliva was tested by gas-fluid chromatography. A positive effect of mexitil treatment manifested in complete correction of ventricular extrasystoles or the reduction of their number by more than half and complete elimination of group extrasystoles and paroxysms of ventricular tachycardia was produced in 66 per cent of patients according to the daily ECG monitoring finds and in 76 per cent of patients according to the results of bicycle ergometry. The antiarrhythmic effect developed 62 minutes, on the average, after oral administration of a single 250--600 mg dose of mexitil and lasted 5--8 hours and more. The therapeutic concentration of mexitil ranged from 0.6 to 0.9 micrograms/ml in blood plasma and from 10.3 to 15.8 micrograms/ml in saliva. In 36 per cent of patients side effects (mainly muscular tremor, lassitude and headache) were noted. It is concluded that mexitil possesses high anti-arrhythmic activity in ventricular extrasystole. To avoid side effects it is recommended to begin treatment in a dose of 250 mg given three times daily, and if necessary gradually increase the single dose to 400 mg and the daily dose to 1200 mg.
对36例病因各异、频发且预后不良的室性期前收缩患者进行了美西律抗心律失常活性的研究。通过自行车测力计及借助便携式监测仪进行24小时心电图记录,对心律失常进行定量和定性评估。在治疗前、美西律每日剂量750 - 1200mg/24小时给药3 - 5天期间以及安慰剂背景下,对心律失常进行评估。通过监测三小时半的心电图来评估单次250至600mg剂量美西律的效果。采用气液色谱法检测血浆和唾液中美西律的浓度。根据每日心电图监测结果,66%的患者美西律治疗产生了积极效果,表现为室性期前收缩完全纠正或数量减少一半以上,且完全消除了成组期前收缩和室性心动过速发作;根据自行车测力计结果,76%的患者有此效果。口服单次250 - 600mg剂量美西律后,抗心律失常作用平均在62分钟后出现,持续5 - 8小时甚至更长时间。美西律的治疗浓度在血浆中为0.6至0.9微克/毫升,在唾液中为10.3至15.8微克/毫升。36%的患者出现了副作用(主要为肌肉震颤、乏力和头痛)。结论是美西律在室性期前收缩方面具有高抗心律失常活性。为避免副作用,建议开始治疗时剂量为每日三次,每次250mg,如有必要可逐渐将单次剂量增至400mg,每日剂量增至1200mg。