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拉贝洛尔在高血压患者中的药代动力学和药效学研究。

Pharmacokinetics and pharmacodynamic studies of labetalol in hypertensive subjects.

作者信息

McNeil J J, Anderson A E, Louis W J, Morgan D J

出版信息

Br J Clin Pharmacol. 1979;8(Suppl 2):157S-161S.

Abstract

1 The pharmacokinetics of labetalol were studied in twelve hypertensive patients, ten of whom were not receiving other therapy. 2 Following intravenous administration there was a three- to fourfold variation in terminal elimination half-life, volume of distribution and total plasma clearance. The mean elimination half-life was 3.25 hours. 3 Following oral administration the drug was absorbed rapidly. Systemic availability varied from 11-86% (mean 33%). 4 Plasma levels correlated poorly with the acute effect on BP, raising the possibility of labetalol acting in a deep tissue compartment or alternatively an active metabolite contributing to its effect.

摘要
  1. 对12名高血压患者进行了拉贝洛尔的药代动力学研究,其中10名未接受其他治疗。2. 静脉给药后,终末消除半衰期、分布容积和总血浆清除率有三到四倍的差异。平均消除半衰期为3.25小时。3. 口服给药后,药物吸收迅速。全身可用性在11%-86%之间变化(平均33%)。4. 血浆水平与对血压的急性作用相关性较差,这增加了拉贝洛尔在深部组织隔室起作用的可能性,或者有一种活性代谢物对其作用有贡献。

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