ヒトにおけるテスラノシドの薬物速度論

概要

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The pharmacokinetics of deslanoside was studied in four healthy volunteers and five patients with cardiac failure. It was found that the homogeneous enzyme immunoassay (EMIT^[○!R]) for digoxin was able to apply for the determination of deslanoside serum levels. The curve of the average serum levels of deslanoside in four healthy volunteers after intravenous administration was typically adapted to two compartment model, and a half life time (t_<1/2>) and an apparent volume of distribution (V_d) were calculated to be 41 hours and 10 l/kg, while t_<1/2> and V_d in the cases of five patients were 61 hours and 6.4 l/kg on average, respectively. An equation of β=0.69×10^<-4>C_<er>+0.0089 (γ=0.69) was obtained in an investigation to know a relationship between elimination rate constant (β) and creatinine clearance (C_<er>), indicating good correlation between renal function and urinary excretion. Metabolism of deslanoside to digoxin was examined in analysis of urine collected during 24 hours after administration of three healthy volunteers by means of a combination of high performance liquid chromatography and homogeneous enzyme immunoassay, and convertion ratio of deslanoside to digoxin was found to be 4-7%. Toxic serum level of deslanoside was able to be defined as 2.0-2.5 ng/ml by 22 measurements of deslanoside serum levels in 12 patients with cardiac failure.
社団法人日本薬学会の論文
1982-11-25