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β2肾上腺素能激动剂非诺特罗在健康女性体内的药代动力学。

The pharmacokinetics of the beta 2-adrenoceptor agonist fenoterol in healthy women.

作者信息

Warnke K, Hildebrandt R, Günther K, Langen U, Gundert-Remy U

机构信息

Abteilung für Experimentelle und Klinische Pharmakologie, Institut für Arzneimittel, Berlin, FRG.

出版信息

Eur J Clin Pharmacol. 1992;43(6):663-5. doi: 10.1007/BF02284970.

Abstract

We have studied the pharmacokinetics of fenoterol in healthy women during and after a 3 h intravenous infusion of different doses within the therapeutic range for tocolysis (0.5 microgram.min-1, 1.0 micrograms.min-1, and 2.0 micrograms.min-1). A specific and sensitive radioimmunoassay was used for the determination of fenoterol. For compartmental analysis the plasma concentration time data were fitted with the TOPFIT program, assuming two exponentials. The total clearance of fenoterol increased with dose (1299 ml.min-1 at 0.5 microgram.min-1, 1483 ml.min-1 at 1.0 micrograms.min-1, and 1924 ml.min-1 at 2.0 micrograms.min-1), as did the apparent volume of distribution (from 49 l at the lowest to 85 l at the highest dose). In contrast, the apparent half-lives were not dose-dependent, with t1/2.lambda 1 4.8 min and t1/2.lambda z 52 min.

摘要

我们研究了在健康女性中,静脉输注不同剂量(在治疗早产的治疗范围内,即0.5微克·分钟⁻¹、1.0微克·分钟⁻¹和2.0微克·分钟⁻¹)的非诺特罗3小时期间及之后的药代动力学。采用特异性和灵敏的放射免疫分析法测定非诺特罗。对于房室分析,假设为双指数函数,血浆浓度-时间数据用TOPFIT程序进行拟合。非诺特罗的总清除率随剂量增加(0.5微克·分钟⁻¹时为1299毫升·分钟⁻¹,1.0微克·分钟⁻¹时为1483毫升·分钟⁻¹,2.0微克·分钟⁻¹时为1924毫升·分钟⁻¹),分布容积也如此(最低剂量时为49升,最高剂量时为85升)。相比之下,表观半衰期不依赖于剂量,t1/2.λ1为4.8分钟,t1/2.λz为52分钟。

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