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[心肌梗死亚急性期并发心力衰竭患者开始使用哌唑嗪时的药代动力学及浓度-效应关系]

[The pharmacokinetics and the concentration-and-effect relationship of prazosin in patients at the beginning of the subacute period of myocardial infarct complicated by the development of heart failure].

作者信息

Ol'binskaia L I, Petrosian Iu R, Gofman A M

出版信息

Farmakol Toksikol. 1989 Sep-Oct;52(5):68-72.

PMID:2599083
Abstract

The pharmacokinetics of prazosin was studied in 16 patients in the early subacute period of myocardial infarction complicated with heart failure following a single and 10-day administration. The increase of the half-life of the drug (6.6 +/- 1.6 h) and the elevation of the blood plasma concentration 1-2.5 h after administration (87 +/- 33 ng/ml) were found. After 10-day administration the increase of the apparent total clearance of the drug was established. The blood plasma levels of prazosin significantly correlated with the change of the hemodynamic parameters measured invasively after a single administration of 2-5 mg of the drug. After 10 days of treatment the correlation weakened and the regression line angle reduced that reflected the development of tolerance to the drug. On the basis of the calculated effective concentrations, there were determined the optimal intervals of the drug dosage.

摘要

在16例心肌梗死并发心力衰竭的患者中,研究了哌唑嗪在急性心肌梗死早期亚急性期单次给药及连续10天给药后的药代动力学。发现给药后药物半衰期延长(6.6±1.6小时),给药后1 - 2.5小时血浆浓度升高(87±33纳克/毫升)。连续10天给药后,药物的表观总清除率增加。单次给予2 - 5毫克药物后,哌唑嗪的血浆水平与有创测量的血流动力学参数变化显著相关。治疗10天后,相关性减弱,回归线角度减小,这反映了对药物耐受性的发展。根据计算出的有效浓度,确定了药物给药的最佳间隔时间。

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