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现将钙拮抗剂与地高辛合用时,其相互作用的药物动力学、机制和临床意义综述如下.一、药物动力学(一)异搏停与地高辛:异搏停与地高辛合用,无论动物实验还是临床应用均证明:异搏停可显著增高地高辛的稳态血浓度.异搏停通过减少肾清除率、非肾清除率和表观容量分布,能使血清地高辛浓度(SDC)增加60～80%.Klein等曾观察41例口服地高辛患者于加服异搏停每日240mg 后,SDC 从0.96±0.08增至1.63±0.12ng/ml(P<0.001),其中 SDC 不增高者仅2例.Pedersen 等对8名健康人进行前瞻性研究,结果与上述相似,并显示异搏停可使地高辛的生物半寿期从38.6±8.5延长至50.5±8.3小时.合用时 SDC增加:①与剂量有关:剂量越大,SDC 越高.每日
Now the combination of calcium antagonist and digoxin, pharmacokinetics, mechanism and clinical significance of its interaction are summarized as follows: First, the pharmacokinetics (a) verapamil and digoxin: verapamil and digoxin Combining, both animal experiments and clinical applications have proved: Verapamil can significantly increase the steady-state blood concentration of digoxin.Shortrace stop by reducing the renal clearance, non-renal clearance and the apparent volumetric distribution, can make the serum high (SDC) increased by 60 to 80% .Klein et al observed the increase of SDC from 0.96 ± 0.08 to 1.63 ± 0.12 ng / ml in 41 oral digoxin patients (P <0.001 ), In which SDC did not increase in only 2 cases.Pedersen et al conducted a prospective study of 8 healthy people with the results similar to the above and showed that verapamil can extend the biological half-life of digoxin from 38.6 ± 8.5 to 50.5 ± 8.3 hours SDC increase in combination: ① dose-related: the higher the dose, the higher SDC daily