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比索洛尔的药代动力学及其对透析难治性高血压的影响。

Pharmacokinetics of bisoprolol and its effect on dialysis refractory hypertension.

作者信息

Kanegae K, Hiroshige K, Suda T, Iwamoto M, Ohta T, Nakashima Y, Ohtani A

机构信息

Second Department of Internal Medicine, School of Medicine, University of Occupational and Environmental Health, Fukuoka, Japan.

出版信息

Int J Artif Organs. 1999 Dec;22(12):798-804.

PMID:10654875
Abstract

The efficacy, safety, and pharmacokinetics of bisoprolol were investigated following oral administration once daily for 12 weeks in hyperreninemic patients with dialysis-refractory hypertension. Mean blood pressure rapidly fell from 132 to 112 mmHg in the 5.0-mg/day (n = 6) and from 142 to 128 mmHg in the 2.5-mg/day patients (n = 5), which were accompanied by a fall in plasma renin activity. On nondialysis days, Cmax and T1/2 were significantly higher in patients than in healthy control subjects. However, Cmax in the 2.5-mg/day patients was almost equal to that in healthy control subjects receiving 5.0 mg/day of bisoprolol. Plasma bisoprolol was dialyzable. During the course of the study, dialysis hypotension and bradycardia occurred in two patients receiving 5.0 mg/day of bisoprolol. In conclusion, a daily dose of 2.5 mg bisoprolol seems to be an adequate and relatively effective dose in our patients with dialysis-refractory hypertension.

摘要

在高肾素血症且透析难治性高血压患者中,每日口服一次比索洛尔,持续12周,对其疗效、安全性和药代动力学进行了研究。5.0毫克/天组(n = 6)患者的平均血压迅速从132毫米汞柱降至112毫米汞柱,2.5毫克/天组(n = 5)患者的平均血压从142毫米汞柱降至128毫米汞柱,同时伴有血浆肾素活性下降。在非透析日,患者的Cmax和T1/2显著高于健康对照受试者。然而,2.5毫克/天组患者的Cmax几乎与接受5.0毫克/天比索洛尔的健康对照受试者相等。血浆中的比索洛尔可被透析清除。在研究过程中,两名接受5.0毫克/天比索洛尔治疗的患者出现了透析性低血压和心动过缓。总之,对于我们的透析难治性高血压患者,每日2.5毫克比索洛尔似乎是一个合适且相对有效的剂量。

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