Jogestrand T, Andersson K
Department of Clinical Physiology, Karolinska Hospital, Stockholm, Sweden.
J Cardiovasc Pharmacol. 1989 Jul;14(1):73-6. doi: 10.1097/00005344-198907000-00013.
Blood samples were taken repeatedly and urine was collected for digoxin assays on two occasions from 12 healthy male volunteers after an oral maintenance dose of digoxin. On one occasion the subjects exercised intermittently on a bicycle ergometer for 8 h after the dose. On the other occasion they rested in the supine position during the study period. Thirty and 45 min after the intake of digoxin, the serum digoxin concentration was significantly higher during exercise compared with rest, indicating increased absorption rate during exercise. Two and 4 h after the intake of digoxin, the serum digoxin concentration was significantly lower during exercise than during rest. Furthermore, the intermittent bicycle exercise decreased the renal excretion of digoxin during the study period. It also increased the steady state digoxin concentration measured after a terminating standardized period of rest. The most probable reason for these changes in the pharmacokinetics is a previously described increased binding of digoxin to exercising muscles. According to the results, there is reason to believe that the daily physical activity performed by digoxin-treated patients will determine to some extent the body content of digoxin. Changes in activity from day to day may therefore cause variations in the effect of the drug.
对12名健康男性志愿者口服维持剂量的地高辛后，多次采集血样，并在两个不同时间点收集尿液进行地高辛检测。一次是在服药后让受试者在自行车测力计上间歇性运动8小时。另一次是在研究期间让他们仰卧休息。服用地高辛后30分钟和45分钟，运动时的血清地高辛浓度显著高于休息时，表明运动期间吸收率增加。服用地高辛后2小时和4小时，运动时的血清地高辛浓度显著低于休息时。此外，在研究期间，间歇性自行车运动减少了地高辛的肾脏排泄。它还增加了在终止标准化休息期后测得的地高辛稳态浓度。这些药代动力学变化最可能的原因是先前描述的地高辛与运动肌肉的结合增加。根据这些结果，有理由相信接受地高辛治疗的患者日常的体力活动将在一定程度上决定地高辛在体内的含量。因此，每天活动量的变化可能会导致药物效果的差异。
