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苄氟噻嗪在高血压患者中的药代动力学

Pharmacokinetics of bendroflumenthiazide in hypertensive patients.

作者信息

Beermann B, Groschinsky-Grind M, Lindström B, Wikland B

出版信息

Eur J Clin Pharmacol. 1978 May 17;13(2):119-24. doi: 10.1007/BF00609755.

Abstract

After four weeks on placebo treatment, 8 hypertensive patients (WHO stage I) were treated for 2 weeks with bendroflumethiazide (bft) 2.5 mg and KCl 1.5 g daily. Subsequently they received bft 5 mg and KCl 1.5 g daily for a further fortnight. At the end of each period of treatment blood pressure was recorded and blood samples and urine were collected for analysis of bft by GLC. Before taking the daily dose of bft, no trace of the drug was found in plasma. Peak levels of bft were seen after 2.3 h and averaged 23 and 50 ng . ml-1 after 2.5 and 5 mg, respectively. After bft 2.5 mg the plasma level was too low for kinetic analysis. The plasma half-life after 5 mg averaged 4.1 h. The mean apparent volume of distribution was 1.18 1 . kg-1. Non-renal clearance averaged 200 ml . min-1. The renal clearance of bft was significantly lower (p less than 0.05) after 5 mg (48 ml . min-1) than after 2.5 mg bft (93 ml . min-1), although the creatinine clearance remained unchanged. No correlation was found between the plasma level of bft and its effect on blood pressure.

摘要

在接受四周安慰剂治疗后,8名高血压患者(世界卫生组织I期)接受了为期2周的治疗,每日服用2.5毫克苄氟噻嗪(bft)和1.5克氯化钾。随后,他们又连续两周每日服用5毫克bft和1.5克氯化钾。在每个治疗阶段结束时,记录血压,并采集血样和尿液,通过气相色谱法分析bft。在服用每日剂量的bft之前,血浆中未发现该药物的痕迹。bft的峰值水平在2.3小时后出现,2.5毫克和5毫克剂量后的平均峰值水平分别为23和50纳克·毫升-1。服用2.5毫克bft后,血浆水平过低,无法进行动力学分析。5毫克剂量后的血浆半衰期平均为4.1小时。平均表观分布容积为1.18升·千克-1。非肾清除率平均为200毫升·分钟-1。5毫克bft后的bft肾清除率(48毫升·分钟-1)显著低于2.5毫克bft后的肾清除率(93毫升·分钟-1)(p小于0.05),尽管肌酐清除率保持不变。未发现bft的血浆水平与其对血压的影响之间存在相关性。

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