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首页> 外文期刊>Life sciences >Effects of water deprivation for 72 hours on the pharmacokinetics of a new carbapenem, DA-1131, in rats.
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Effects of water deprivation for 72 hours on the pharmacokinetics of a new carbapenem, DA-1131, in rats.

机译：缺水72小时对新碳青霉烯DA-1131在大鼠体内的药代动力学的影响。

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摘要

Hormonal, physiological, and biochemical changes occurring in dehydrated patients could alter the pharmacokinetics of the drugs; therefore, the pharmacokinetics of DA-1131, a new carbapenem antibiotic, were investigated after 1-min intravenous administration of the drug at 50 mg/kg to control and 72-hr water-deprived rats. The impaired kidney and liver functions were observed in water-deprived rats on the basis of tissue microscopic examination. After intravenous infusion of the drug to water-deprived rats, the plasma concentrations of DA-1131 were higher and this resulted in a significantly greater total area under the plasma concentration-time curve from time zero to time infinity than those in control rats (4520 versus 3760 &mgr;g min/ml). This could be due to significantly slower total body clearance (CL) of DA-1131 in water-deprived rats (9.81 versus 14.1 ml/min/kg). The significantly slower CL of DA-1131 in water-deprived rats was due to significant decrease in both renal clearance (2.87 versus 5.13 ml/min/kg because of a significant decrease in 8-hr urinary excretion of unchanged DA-1131 [28.4 versus 39.9% of the intravenous dose] due to impaired kidney function) and nonrenal clearance (6.82 versus 8.66 ml/min/kg because of a significant decrease in the metabolism of DA-1131 in the kidney, as proved by the significant decrease in total renal DHP-I enzyme activity [1900 versus 2130 mU/each kidney]) in water-deprived rats. Water-deprivation did not alter the affinity of rat tissues to DA-1131.
机译：脱水患者发生的激素，生理和生化变化可能会改变药物的药代动力学。因此，在对对照组和缺水72小时的大鼠静脉注射50 mg / kg的药物1分钟后，研究了一种新的碳青霉烯类抗生素DA-1131的药代动力学。根据组织显微镜检查，在缺水的大鼠中观察到肾和肝功能受损。向缺水的大鼠静脉输注药物后，DA-1131的血浆浓度更高，这导致从零时到无限时的血浆浓度-时间曲线下的总面积比对照大鼠大得多（4520）与3760 mg / min相比）。这可能是由于缺水大鼠DA-1131的整体清除率（CL）显着降低（9.81对14.1 ml / min / kg）。在缺水的大鼠中，DA-1131的CL显着降低是由于两个肾脏清除率均显着降低（2.87对5.13 ml / min / kg，因为未改变DA-1131的8小时尿液排泄显着降低[28.4 vs. 39.9％的静脉注射剂量]（由于肾功能受损）和非肾脏清除率（6.82比8.66 ml / min / kg，因为DA-1131在肾脏中的代谢显着下降，总肾脏显着下降证明了这一点）缺水大鼠的DHP-1酶活性（1900对2130 mU /每个肾脏）。缺水不会改变大鼠组织对DA-1131的亲和力。

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