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[生物利用度及其在药物治疗中的意义]

[Bioavailability and its significance in pharmacotherapy].

作者信息

Wiela-Hojeńska Anna, Orzechowska-Juzwenko Krystyna

机构信息

Katedra i Zakład Farmakologii Klinicznej, Akademii Medycznej we Wrocławiu.

出版信息

Pol Merkur Lekarski. 2003 Jan;14(79):89-93.

Abstract

The paper provides an overview of information related to bioavailability, including the fundamental notions and the factors, which can change this parameter described in quantitative way drug absorption--one of the processes involved in fate of drug in the organism. Systemic bioavailability is best described by the measurement of the relative amount of an administered dose that reaches the general circulation (Area Under the Curve, AUC), the maximum concentration achieved (Cmax), and the time (tmax) at which this occurs. Liver diseases may substantially increase the oral bioavailability of drugs that are subject to extensive first-pass metabolism e.g. pro-pranolol, lidocaine, metoprolol, verapamil. To avoid toxicity, oral doses of these drugs need to be reduced in patients with severe liver diseases.

摘要

本文概述了与生物利用度相关的信息,包括基本概念以及可能以定量方式改变该参数的因素,药物吸收是药物在机体中命运所涉及的过程之一。全身生物利用度最好通过测量进入体循环的给药剂量的相对量(曲线下面积,AUC)、达到的最大浓度(Cmax)以及出现该浓度的时间(tmax)来描述。肝脏疾病可能会大幅增加那些经历广泛首过代谢的药物的口服生物利用度,例如普萘洛尔、利多卡因、美托洛尔、维拉帕米。为避免毒性,患有严重肝脏疾病的患者需要减少这些药物的口服剂量。

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