Chen S X, Gu T H, Song D J, Guo J Z, Wang X M, Gong L S
Shanghai Institute of Hypertension, China.
Zhongguo Yao Li Xue Bao. 1994 May;15(3):263-6.
Twenty hypertensive patients were equally divided into 2 groups: A) with normal renal function (NRF) and B) with impaired renal function (IRF) according to creatinine clearance, blood urea nitrogen and creatinine levels. The pharmacokinetic and pharmacodynamic effects of diltiazem (Dil, 90 mg, bid x 7 d, p.o.) were studied. The pharmacokinetic parameters in IRF patients (Ka 0.7 +/- 0.2 h-1, T 1/2e 3.7 +/- 0.7 h, Cmax1 45 +/- 4 ng.ml-1, Tmax1 3.1 +/- 0.4 h) did not differ from those in NRF patients (0.7 +/- 0.5 h-1, 4.1 +/- 1.3 h, 41 +/- 5 ng.ml-1 and 3.4 +/- 0.4 h, P > 0.05). Antihypertensive efficacy of Dil in patients with IRF was similar to that in those with NRF, and the hypotensive effect lasted over 24 h. The plasma Dil concentrations were strongly correlated with a decrease in BP in both groups. It was concluded that IRF did not affect the disposition of slow release Dil tablet under a steady state. No dosage adjustment of Dil is necessary in hypertensive patients with IRF.
20例高血压患者根据肌酐清除率、血尿素氮和肌酐水平，被平均分为两组：A组肾功能正常（NRF），B组肾功能受损（IRF）。研究了地尔硫䓬（Dil，90mg，每日两次，口服，共7天）的药代动力学和药效学作用。IRF患者的药代动力学参数（Ka 0.7±0.2 h-1，T 1/2e 3.7±0.7 h，Cmax1 45±4 ng.ml-1，Tmax1 3.1±0.4 h）与NRF患者（0.7±0.5 h-1，4.1±1.3 h，41±5 ng.ml-1和3.4±0.4 h）相比无差异（P>0.05）。Dil对IRF患者的降压疗效与NRF患者相似，且降压作用持续超过24小时。两组患者血浆Dil浓度均与血压下降密切相关。得出结论：肾功能受损在稳态下不影响缓释Dil片的处置。肾功能受损的高血压患者无需调整Dil剂量。
