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[埃瑞莫霉素在实验中的药代动力学研究]

[Pharmacokinetic study of eremomycin in an experiment].

作者信息

Filippos'iants S T, Malkova I V

出版信息

Antibiot Med Biotekhnol. 1987 Jul;32(7):511-6.

PMID:3118795
Abstract

Pharmacokinetics of eremomycin, a novel original glycopeptide antibiotic was studied. It was shown that after a single intravenous or subcutaneous administration to mice, rabbits and dogs eremomycin concentrations in blood and duration of the antibiotic circulation depended on the dose level and administration route. After subcutaneous or intramuscular administration eremomycin was rapidly absorbed and detected in serum even in 15-30 min. The maximum levels were observed in 2 hours. Absolute bioavailability after subcutaneous administration averaged to 85 per cent. Eremomycin penetrated into organs. The antibiotic concentrations in cerebrospinal fluid were low. The highest concentrations of eremomycin were detected in the kidneys, lungs and spleen. The antibiotic mainly excreted with urine. The renal clearance amounted to 85 per cent of the total clearance. 2-3-month exposure of dogs and rats to eremomycin in doses 4-10 times higher than the approximate single therapeutic doses for humans (250 mg) resulted in cumulation of the antibiotic.

摘要

对新型原创糖肽抗生素埃瑞霉素的药代动力学进行了研究。结果表明,对小鼠、兔子和狗单次静脉注射或皮下注射后,血液中的埃瑞霉素浓度以及抗生素的循环持续时间取决于剂量水平和给药途径。皮下或肌肉注射后,埃瑞霉素迅速吸收,甚至在15 - 30分钟内就能在血清中检测到。2小时后观察到最高水平。皮下给药后的绝对生物利用度平均为85%。埃瑞霉素可渗透到器官中。脑脊液中的抗生素浓度较低。在肾脏、肺和脾脏中检测到的埃瑞霉素浓度最高。抗生素主要通过尿液排泄。肾脏清除率占总清除率的85%。给狗和大鼠以高于人类近似单次治疗剂量(250毫克)4 - 10倍的剂量接触埃瑞霉素2 - 3个月,会导致抗生素蓄积。

相似文献

1
[Pharmacokinetic study of eremomycin in an experiment].[埃瑞莫霉素在实验中的药代动力学研究]
Antibiot Med Biotekhnol. 1987 Jul;32(7):511-6.
2
[Glycopeptide antibiotics: eremomycin, vancomycin, and teicoplanin. Comparison of several parameters of pharmacokinetics and antimicrobial activity].[糖肽类抗生素:埃瑞霉素、万古霉素和替考拉宁。药代动力学和抗菌活性若干参数的比较]
Antibiot Khimioter. 1989 Jul;34(7):523-6.
3
[Preclinical toxicological study of the new antibiotic eremomycin. Its acute toxicity for laboratory animals].新型抗生素埃瑞霉素的临床前毒理学研究。其对实验动物的急性毒性
Antibiot Med Biotekhnol. 1987 Dec;32(12):910-5.
4
[Pharmacokinetics of tobramycetin and gentamycin and the mechanism of their elimination by the kidneys].[妥布霉素和庆大霉素的药代动力学及其经肾脏消除的机制]
Antibiotiki. 1980 Aug;25(8):579-84.
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Pharmacokinetics of A40926 in rats after single intravenous and subcutaneous doses.单次静脉注射和皮下注射剂量后A40926在大鼠体内的药代动力学
Antimicrob Agents Chemother. 1988 Feb;32(2):246-9. doi: 10.1128/AAC.32.2.246.
6
[Preclinical toxicological study of the new antibiotic eremomycin. Chronic toxicity and effect on intrauterine development of rats].
Antibiot Khimioter. 1988 Apr;33(4):280-6.
7
[Action of antibiotic 1719 from a group of diazo compounds on hematopoiesis in laboratory animals and its pharmacokinetics].[一组重氮化合物中的抗生素1719对实验动物造血功能的作用及其药代动力学]
Antibiotiki. 1975 Jan;20(1):26-31.
8
[Eremomycin--a new antibiotic of the polycyclic glycopeptide group].埃瑞霉素——一种新型多环糖肽类抗生素
Antibiot Khimioter. 1989 May;34(5):348-52.
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[Experimental study of histamine-liberating properties of eremomycin].
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Clinical pharmacokinetics of teicoplanin.替考拉宁的临床药代动力学
Clin Pharmacokinet. 1990 Mar;18(3):184-209. doi: 10.2165/00003088-199018030-00002.