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新型H+/K(+)-ATP酶抑制剂泮托拉唑单次静脉给药后的药代动力学剂量线性关系

Dose linearity of the pharmacokinetics of the new H+/K(+)-ATPase inhibitor pantoprazole after single intravenous administration.

作者信息

Bliesath H, Huber R, Hartmann M, Lühmann R, Wurst W

机构信息

Research Division, Byk Gulden Pharmaceuticals, Konstanz, Germany.

出版信息

Int J Clin Pharmacol Ther. 1996 May;34(1 Suppl):S18-24.

PMID:8793600
Abstract

Pantoprazole is a specific inhibitor of the H+/K(+)-ATPase of the gastric parietal cell. The dose-dependency of a range of pantoprazole pharmacokinetic characteristics was studied. Twelve healthy male subjects were given 10, 20, 40 and 80 mg pantoprazole intravenously according to a randomized, single blind, 4-period change-over scheme. The area under the concentration vs time curve (AUC) and the maximum serum concentration (Cmax) showed a linear increase in line with the dose. Apparent volume of distribution (Vd area), clearance (Cl) and terminal half-life (t1/2) were independent of the dose. The dose-independent elimination of pantoprazole was attributed to the lack of interaction of the drug with cytochrome P450. In clinical practice, a good predictable response, as well as a low potential for interaction with other drugs might be expected.

摘要

泮托拉唑是胃壁细胞H⁺/K⁺-ATP酶的特异性抑制剂。研究了一系列泮托拉唑药代动力学特征的剂量依赖性。12名健康男性受试者按照随机、单盲、4期交叉方案静脉注射10、20、40和80mg泮托拉唑。浓度-时间曲线下面积(AUC)和血清最大浓度(Cmax)随剂量呈线性增加。表观分布容积(Vd area)、清除率(Cl)和末端半衰期(t1/2)与剂量无关。泮托拉唑的非剂量依赖性消除归因于该药物与细胞色素P450缺乏相互作用。在临床实践中,可以预期有良好的可预测反应以及与其他药物相互作用的可能性较低。

相似文献

1
Dose linearity of the pharmacokinetics of the new H+/K(+)-ATPase inhibitor pantoprazole after single intravenous administration.新型H+/K(+)-ATP酶抑制剂泮托拉唑单次静脉给药后的药代动力学剂量线性关系
Int J Clin Pharmacol Ther. 1996 May;34(1 Suppl):S18-24.
2
Dose linearity of the pharmacokinetics of the new H+/K(+)-ATPase inhibitor pantoprazole after single intravenous administration.
Int J Clin Pharmacol Ther. 1994 Jan;32(1):44-50.
3
Pharmacokinetics of pantoprazole in man.
Int J Clin Pharmacol Ther. 1996 May;34(1 Suppl):S7-16.
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Lack of influence of pantoprazole on the disposition kinetics of theophylline in man.泮托拉唑对人体中茶碱处置动力学无影响。
Int J Clin Pharmacol Ther. 1996 May;34(1 Suppl):S51-7.
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Lack of interaction between pantoprazole and digoxin at therapeutic doses in man.泮托拉唑与地高辛在人体治疗剂量下无相互作用。
Int J Clin Pharmacol Ther. 1996 May;34(1 Suppl):S67-71.
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Pharmacokinetics and tolerance of pantoprazole, a proton pump inhibitor after single and multiple oral doses in healthy Japanese volunteers.
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Lack of pharmacokinetic interaction between pantoprazole and diclofenac.泮托拉唑与双氯芬酸之间不存在药代动力学相互作用。
Int J Clin Pharmacol Ther. 1996 May;34(1 Suppl):S76-80.
8
No influence of pantoprazole on the pharmacokinetics of phenytoin.泮托拉唑对苯妥英钠的药代动力学无影响。
Int J Clin Pharmacol Ther. 1996 May;34(1 Suppl):S72-5.
9
Pantoprazole does not interact with nifedipine in man under steady-state conditions.在稳态条件下,泮托拉唑与人硝苯地平不发生相互作用。
Int J Clin Pharmacol Ther. 1996 May;34(1 Suppl):S81-5.
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Pantoprazole does not interact with the pharmacokinetics of carbamazepine.泮托拉唑与卡马西平的药代动力学无相互作用。
Int J Clin Pharmacol Ther. 1998 Oct;36(10):521-4.

引用本文的文献

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Pantoprazole for the treatment of peptic ulcer bleeding and prevention of rebleeding.泮托拉唑用于治疗消化性溃疡出血及预防再出血。
Clin Med Insights Gastroenterol. 2012 Sep 17;5:51-60. doi: 10.4137/CGast.S9893. eCollection 2012.
2
Pantoprazole does not affect performance in traffic-related safety tests: a double-blind, randomised, placebo-controlled, crossover study in healthy volunteers.泮托拉唑对交通相关安全性测试中的表现无影响:一项在健康志愿者中进行的双盲、随机、安慰剂对照、交叉研究。
Clin Drug Investig. 1998;16(1):63-70. doi: 10.2165/00044011-199816010-00008.
3
Pantoprazole: an update of its pharmacological properties and therapeutic use in the management of acid-related disorders.
泮托拉唑:其药理特性及在酸相关性疾病管理中的治疗应用的最新进展。
Drugs. 2003;63(1):101-33. doi: 10.2165/00003495-200363010-00006.