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[健康肾脏受试者和肾功能受损患者单次口服β-1受体阻滞剂塞利洛尔后的比较药代动力学]

[Comparative pharmacokinetics of the beta-1 receptor blookader celiprolol after a single oral administration in subjects with health kidneys and in patients with impaired renal function].

作者信息

Schmidt P, Takacs F, Pittner H, Minar E, Balcke P, Zazgornik J, Deutsch E

出版信息

Wien Klin Wochenschr. 1985 Sep 27;97(18):729-32.

PMID:2866633
Abstract

Pharmacokinetic parameters were determined after the oral administration of a single tablet containing 200 mg celiprolol HCl to 8 healthy volunteers with normal kidney function and 6 patients with stable impaired renal function of different degrees of severity. The plasma levels and the urinary excretion of celiprolol were followed up for 48 hours after administration with the help of specific chemo-analytical methods. The substance was equally well absorbed both by healthy volunteers and patients with renal disease. While the cumulative renal excretion (0 to 48 hours after administration) was reduced from 18.2% in healthy volunteers to 2.3% of the applied dose in kidney patients, the global elimination constant k fell from 0.104 h-1 in healthy volunteers to 0.072 h-1 in the patients with renal disease. It can be assumed that in patients with impaired renal function at least a part of the lacking renal elimination of celiprolol can be taken over by "extrarenal elimination". According to the method of Dettli a reduction in dosage of the beta 1-blocker, celiprolol is not necessary in patients with more or less impaired kidney function.

摘要

对8名肾功能正常的健康志愿者和6名不同严重程度稳定肾功能受损的患者口服一片含200mg盐酸塞利洛尔的片剂后,测定了药代动力学参数。借助特定的化学分析方法,给药后对塞利洛尔的血浆水平和尿排泄进行了48小时的跟踪。健康志愿者和肾病患者对该物质的吸收情况相同。虽然累积肾排泄(给药后0至48小时)从健康志愿者的18.2%降至肾病患者的给药剂量的2.3%,但总体消除常数k从健康志愿者的0.104 h-1降至肾病患者的0.072 h-1。可以假设,在肾功能受损的患者中,塞利洛尔缺乏的肾排泄至少有一部分可以由“肾外消除”来代偿。根据Dettli的方法,对于或多或少肾功能受损的患者,β1受体阻滞剂塞利洛尔无需减量。

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