Hansson L H
Department of Medicine, University of Göteborg, Ostra Hospital, Sweden.
J Cardiovasc Pharmacol. 1989;14 Suppl 10:S36-9; discussion S59-62.
Dihydropyridine calcium antagonists play an important role in the treatment of arterial hypertension. In many centers, they are used as first-line treatment. Since impaired renal function can be a complication of long-standing blood pressure elevation, the usefulness of dihydropyridine calcium antagonists in hypertensive patients with reduced glomerular filtration rate is an important clinical issue. Several studies of the pharmacokinetics of calcium antagonists, such as nifedipine and related compounds, clearly show that the important pharmacokinetic variables are not affected by impaired renal function. Moreover, the antihypertensive efficacy is not reduced in patients with reduced glomerular filtration rate. A matter of potentially great clinical importance is the fact that several studies have shown that treatment with dihydropyridine calcium antagonists in patients with impaired renal function has reduced the rate of deterioration in filtration rate, leading to a preservation of renal function. It can therefore be concluded that dihydropyridine calcium antagonists are useful in the treatment of hypertensive patients with impaired renal function, that the major pharmacokinetic and pharmacodynamic variables are not negatively affected, in particular that the antihypertensive effect is maintained in such patients, and that there is no retention of metabolites. Finally, the observation that the decline in renal function can be slowed down suggests that dihydropyridine calcium antagonists may be the preferential treatment in hypertensive patients with reduced renal function.
二氢吡啶类钙拮抗剂在动脉高血压的治疗中发挥着重要作用。在许多医疗中心,它们被用作一线治疗药物。由于肾功能损害可能是长期血压升高的并发症,二氢吡啶类钙拮抗剂在肾小球滤过率降低的高血压患者中的有效性是一个重要的临床问题。几项关于钙拮抗剂(如硝苯地平和相关化合物)药代动力学的研究清楚地表明,重要的药代动力学变量不受肾功能损害的影响。此外,肾小球滤过率降低的患者其降压疗效并未降低。具有潜在重大临床意义的是,几项研究表明,肾功能受损患者使用二氢吡啶类钙拮抗剂治疗可降低滤过率的恶化速度,从而保护肾功能。因此可以得出结论,二氢吡啶类钙拮抗剂对肾功能受损的高血压患者有效,主要的药代动力学和药效学变量不会受到负面影响,特别是此类患者的降压作用得以维持,且无代谢产物潴留。最后,肾功能下降可被减缓这一观察结果表明,二氢吡啶类钙拮抗剂可能是肾功能降低的高血压患者的优先治疗药物。