Haustein K O, Hentschel H
Int J Clin Pharmacol Res. 1987;7(1):19-25.
The systolic time intervals (STI) corrected for changes in the heart rate, electromechanical systole (QS2c) and left ventricular ejection time (LVETc), and the ECG-derived PQ-time and QT-interval were measured in five female and four male healthy subjects. Each volunteer took 0.15, 0.30, 0.45, 0.60, 0.75 or 0.90 mg pengitoxin over six days, with a glycoside-free interval of two or three weeks between two doses. The glycoside plasma level was measured radioimmunologically. Linear correlations were found between the shortening of QS2, LVET, and QT (delta QS2c, delta LVETc, delta QTc) and the plasma level of 16-acetyl-gitoxin. The PQ-time showed a flat dose-dependent increase. The shortening of STI observed after therapeutic and subtoxic doses of pengitoxin was in accordance with that after intake of digitoxin and digoxin in corresponding doses. The efficacy of pengitoxin estimated by shortening of STI justifies the administration of daily maintenance doses between 0.30 and 0.45 mg.
在5名健康女性和4名健康男性受试者中测量了经心率变化校正的收缩期时间间隔(STI)、机电收缩期(QS2c)和左心室射血时间(LVETc),以及心电图衍生的PQ时间和QT间期。每位志愿者在6天内服用0.15、0.30、0.45、0.60、0.75或0.90毫克喷吉毒素,两次给药之间有两周或三周的无糖苷间隔期。采用放射免疫法测定糖苷血浆水平。发现QS2、LVET和QT的缩短(ΔQS2c、ΔLVETc、ΔQTc)与16-乙酰基洋地黄毒苷的血浆水平之间存在线性相关性。PQ时间呈剂量依赖性平缓增加。治疗剂量和亚中毒剂量的喷吉毒素后观察到的STI缩短与相应剂量的洋地黄毒苷和地高辛摄入后的情况一致。通过STI缩短评估的喷吉毒素疗效证明每日维持剂量在0.30至0.45毫克之间是合理的。