氟卡胺的药代动力学与药效动力学

Pharmacokinetics and pharmacodynamics of flecainide

氟卡胺是抑制心脏传导间期AH,HV,QRS,QT的抗心律不齐新药。犬iv 2,4 mg/kg氟卡胺后呈二室型代谢动力学特点,其t_(1/2)为60～70min。健康人po 200 mg/kg与小鼠sc 10 mg/kg氟卡胺后呈一级吸收一室型,t_(1/2)为60～76 min。 以抑制传导间期为药效指标,犬iv 4 mg/kg氟卡胺后测各传导间期变化,计算药效动力学,公式为:△％=(△_(max)％)c^(-kt)。以血药浓度对数对相应时间传导间期变化(△％)作图呈线性相关,计算公式为:C=ae^b(△％)。

Flacainide is a new anti-arrythmic agent which inhibits the heartconduction intervals(AH,HV,QRS,QT).The pharmacokinetic properties of flecainidc in dogs after iv 2 or 4 mg/kg is of two-compartment open model with t1/2 of 60-70 min.But in human after oral 200 mg and in mice after sc 10mg/kg,flccainidc is of one-compartment open model and the t1/2 were 60-76 min.On measuring the time course of the change of conduction intervals(AH,HV,QRS,QT)after iv 4 mg/kg flecainidc to dogs,the pharmacodynamic properties were calcu-lated by the equation:△%=△max% e-kt.A linear relationship between the ln(blood drug concentration)and the change of conduction intervals was obtained with the equation C=aeb(△%).