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家兔静脉注射5mg/kg心得安。药一时曲线呈二室模型。观察了心得安血浆浓度与抑制静止心率,Q—T_C及山静脉注射25μg/kg异丙肾上腺素引起心动过速的相关性。血药浓度与抑制心率全过程的数学式为:E=20·C~(6.32)/(C~(6.32)+29.4~(6.32))。抑制异丙肾上腺素引起心动过速的数学式为:E=100·C~(2.01)/(C~(2.01)+73.7~(2.01))·式中29.4及73.7是相应的C_(50)(ng/ml)。用此数学式可从药效而预测所需血药浓度,或由血药浓度预测药效。大多数药代动力学参数的个体间差异大于8倍。产生50%最大药效的血药浓度C_(50)亦有变异,个体间差异3.6—5.2倍。心得安血浓度100ng/ml抑制心率的药效相差4.4倍。提示在TDM实践中应注意药效学的个体差异。
Rabbits intravenous injection of 5mg / kg propranolol. Drug curve was a two-compartment model. The correlation between propranolol plasma concentration and restrain resting heart rate, Q-T_C and isoproterenol 25μg / kg in mountain vein induced tachycardia was observed. The formula of plasma concentration and heart rate inhibition was E = 20 · C ~ (6.32) / (C ~ (6.32) + 29.4 ~ (6.32)). The equation for inhibiting isoproterenol-induced tachycardia is: E = 100 · C 2.01 / C 2.01 + 73.7 ~ 2.01 · where 29.4 and 73.7 are the corresponding C 50 values, (ng / ml). Use this formula to predict the desired plasma concentration from the potency, or to predict the pharmacodynamic effect from the plasma concentration. The majority of individual pharmacokinetic parameters differ more than 8-fold between individuals. Produce 50% of the maximum efficacy of plasma concentration C_ (50) also variation, individual differences of 3.6-5.2 times. Experience the safety of blood concentration of 100ng / ml inhibition of heart rate difference of 4.4 times. Tip TDM practice should pay attention to individual differences in pharmacodynamics.