维拉帕米的临床药物动力学,硝苯地平和地尔硫卓。

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Echizen H, Eichelbaum M

维拉帕米的临床药物动力学,硝苯地平和地尔硫卓。

Pharmacokinet。1986; 11 - 12月11 (6):425 - 49。doi: 10.2165 / 00003088-198611060-00002。

PubMed ID

3542336 (在PubMed

]

文摘

钙拮抗剂地尔硫卓、硝苯地平、维拉帕米被广泛用于治疗冠心病,动脉高血压、某些室上快速性心律失常和阻塞性肥厚性心肌病。近年来它们的药代动力学特性和新陈代谢更详细地研究了。虽然这些3钙拮抗剂展示伟大的化学结构的多样性,他们表现出共同的药代动力学性质。这些药物广泛被代谢,所以只在尿液改变药物消除的痕迹。他们的系统性等离子体间隙高,依赖于肝血流量。因此,其生物利用度(地尔硫卓40 - 50%;硝苯地平40 - 50%;维拉帕米10到30%)很低,尽管口服后几乎完全吸收。在长期治疗,口服间隙减少和增加生物利用度由于饱和肝初步的新陈代谢。明显内部inter-individual间隙的变化和生物利用度。 In patients with liver cirrhosis the various pharmacokinetic parameters are grossly altered. Clearance decreases, elimination half-life is substantially prolonged, and bioavailability more than doubles. In addition, the volume of distribution increases. Whereas renal disease has no impact on the pharmacokinetics of diltiazem and verapamil, elimination half-life of nifedipine increases in relation to the degree of renal impairment due to an increase in volume of distribution. Systemic clearance, however, remains unchanged. The data so far available indicate that the plasma concentrations of these drugs correlate with both their electrophysiological and haemodynamic effects. However, no effective therapeutic plasma concentration range has been firmly established. As reliable clinical end-points are available for dose titration of calcium antagonists, it is doubtful whether therapeutic drug monitoring will be of great value. Calcium antagonists are often administered in combination with a variety of other drugs. Thus, the potential for both pharmacodynamic and pharmacokinetic drug interaction exists. The interaction between digoxin and these drugs is of clinical importance. Verapamil and diltiazem cause a significant increase in plasma digoxin concentrations. In contrast, nifedipine does not lead to a significant increase in the plasma digoxin concentration. The mechanism responsible for this interaction is inhibition of both renal and non-renal digoxin clearance.(ABSTRACT TRUNCATED AT 400 WORDS)

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药物

维拉帕米