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应用高效液相色谱法测定11例阵发性室上性心动过速静脉注射心律平和15例室性心律失常口服心律平的药浓度时间曲线。静脉注射者药动学符合二室开放模型,主要药动学参数:分布相半衰期(T(1/2)α)0.055±0.01h,清除半衰期(T(1/2)β)2.99±0.53h,中央分布容积(Vc)0.048±0.011L/kg,终止室上性心动过速有效血浓度1032.6±624.1μg/ml。口服者药动学参数T(1/2)α0.33±0.2h,T(1/2)β6.89±2.7h,TPK1.95±0.4h,CST243±161μg/ml。13例口服450mg/d控制室性早搏有效率69.2%,有效血浓度297.7±264.6ng/ml。提示心律平代谢93%为强代谢型,应用同等剂量,血浓度差别甚大,有效血浓度个体间差异也不小,因此不能根据剂量估测血浓度高低,也不能根据血浓度预测疗效和促心律失常反应,其治疗应根据临床观察、个体化剂量予以调整。
Application of high performance liquid chromatography determination of 11 cases of paroxysmal supraventricular tachycardia intravenous rhythm and 15 cases of ventricular arrhythmia oral rhythm of drug concentration time curve. Pharmacokinetics of intravenous injection in line with two-compartment open model, the main pharmacokinetic parameters: distribution phase half-life (T (1/2) α) 0.055 ± 0.01h, clearance half-life .99 ± 0.53h, the central distribution volume (Vc) 0.048 ± 0.011L / kg, the effective blood concentration of the termination of supraventricular tachycardia was 1032.6 ± 624.1μg / ml. Oral pharmacokinetic parameters T (1/2) α0.33 ± 0.2h, T (1/2) β6.89 ± 2.7h, TPK1.95 ± 0.4h, CST243 ± 161μg / ml. 13 cases of oral administration of 450mg / d premature ventricular contractions efficiency 69.2%, effective blood concentration 297.7 ± 264.6ng / ml. Suggesting that 93% of the heart rate metabolism is a strong metabolic type, the application of the same dose, the blood concentration varies greatly, the effective blood concentration between individuals is not small, so the dose can not be estimated according to the level of blood concentration, blood concentration can not predict the efficacy and promote heart rhythm Abnormal reactions, the treatment should be based on clinical observation, individual dose to be adjusted.