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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.

DOI:10.1007/BF02284970
PMID:1493852
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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1
The pharmacokinetics of the beta 2-adrenoceptor agonist fenoterol in healthy women.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。
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引用本文的文献

1
Pharmacokinetics of fenoterol in pregnant and nonpregnant women.非诺特罗在孕妇和非孕妇中的药代动力学。
Eur J Clin Pharmacol. 1993;45(3):275-7. doi: 10.1007/BF00315396.

本文引用的文献

1
Interaction between oral hydralazine and propranolol. I. Changes in absorption, presystemic clearance and splanchnic blood flow.口服肼屈嗪与普萘洛尔的相互作用。I. 吸收、首过清除率和内脏血流量的变化。
J Pharmacol Exp Ther. 1984 May;229(2):509-14.
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[Comparative pharmacokinetic studies on fenoterol-hydrobromide in rat, dog and man].
Arzneimittelforschung. 1972 Jul;22(7):1190-6.
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Radioimmunological determination of fenoterol. Part I: Theoretical fundamentals.非诺特罗的放射免疫测定。第一部分:理论基础。
Arzneimittelforschung. 1985;35(1A):415-20.
4
Presystemic and systemic intestinal metabolism of fenoterol in the conscious rat.非诺特罗在清醒大鼠体内的肠前和全身肠道代谢
Drug Metab Dispos. 1985 Jul-Aug;13(4):464-70.
5
Radioimmunological determination of fenoterol. Part II: Antiserum and tracer for the determination of fenoterol.非诺特罗的放射免疫测定。第二部分:用于非诺特罗测定的抗血清和示踪剂。
Arzneimittelforschung. 1990 Aug;40(8):887-95.
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Fenoterol: a review of its pharmacological properties and therapeutic efficacy in asthma.非诺特罗:对其药理学特性及在哮喘治疗中的疗效的综述。
Drugs. 1978 Jan;15(1):3-32. doi: 10.2165/00003495-197815010-00002.