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正常志愿者中青霉素与苯唑西林广谱抗生素联合用药的药代动力学研究(作者译)

[Pharmacokinetic studies on broad spectrum antibiotic combinations of penicillin and oxacillin in normal volunteers (author's transl)].

作者信息

Adam D, Bauer W, Seitz B, Voigt I

出版信息

Arzneimittelforschung. 1979;29(11):1769-804.

PMID:543889
Abstract

After i.v. application of broad spectrum penicillins (ampicillin, mezlocillin, carbenicillin) alone or combined with oxacillin (concomitantly) in different dosages to normal volunteers, the course of serum levels and recovery from urine were assessed and pharmacokinetic data were calculated for a 1-compartment model, in some cases also for a 2-compartment model. The following penicillins were tested alone and combined with oxacillin; ampicillin 3 g, oxacillin 2 g and their combination; ampicillin 2 g, oxacillin 1 g and their combination; mezlocillin 3.75 g, oxacillin 1.25 g and their combination; mezlocillin 2 g, oxacillin 1 g and their combination; carbenicillin 7.5 g, oxacillin 2.5 g and their combination. Apart from one combination (oxacillin 2 g + ampicillin 3 g), all penicillin combinations exceeded the serum levels achieved after individual application at any time. In combinations, the elimination constants decreased, total clearance was lower, and half-lives increased. The distribution volumes varied. With one exception, oxacillin 2.5 g + carbenicillin 7.5 g, all the combinations yielded a higher recovery from urine than did individual administration. When administering i.v. two penicillins simultaneously, a process similar to that following administration of probenecid in association with caronamide must need be considered. It may be assumed that the prolongation and elevation of serum levels after combined administration likewise lead to higher tissue concentrations, which effect might be of clinical consequence.

摘要

对正常志愿者静脉注射不同剂量的广谱青霉素(氨苄西林、美洛西林、羧苄西林),单独使用或与苯唑西林同时联合使用,评估血清水平变化过程和尿液中的回收情况,并针对一室模型计算药代动力学数据,某些情况下也针对二室模型进行计算。对以下青霉素进行了单独测试以及与苯唑西林联合测试:氨苄西林3g、苯唑西林2g及其组合;氨苄西林2g、苯唑西林1g及其组合;美洛西林3.75g、苯唑西林1.25g及其组合;美洛西林2g、苯唑西林1g及其组合;羧苄西林7.5g、苯唑西林2.5g及其组合。除一种组合(苯唑西林2g + 氨苄西林3g)外,所有青霉素组合在任何时间的血清水平均超过单独给药后的水平。在组合用药时,消除常数降低,总清除率降低,半衰期延长。分布容积各不相同。除了一个例外,即苯唑西林2.5g + 羧苄西林7.5g,所有组合的尿液回收量均高于单独给药。静脉同时注射两种青霉素时,必须考虑到一个类似于丙磺舒与卡隆酰胺联合给药后的过程。可以假定联合给药后血清水平的延长和升高同样会导致更高的组织浓度,这种效应可能具有临床意义。

相似文献

1
[Pharmacokinetic studies on broad spectrum antibiotic combinations of penicillin and oxacillin in normal volunteers (author's transl)].正常志愿者中青霉素与苯唑西林广谱抗生素联合用药的药代动力学研究(作者译)
Arzneimittelforschung. 1979;29(11):1769-804.
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[Pharmacokinetic studies with a combination of mezlocillin-oxacillin].美洛西林-苯唑西林联合用药的药代动力学研究
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[Pharmacokinetics of mezlocillin. Comparison with ampicillin and influence of probenecid (author's transl)].美洛西林的药代动力学。与氨苄西林的比较及丙磺舒的影响(作者译)
Nouv Presse Med. 1982 Feb 4;11(5 Pt 2):347-52.
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Fixed combination mezlocillin/oxacillin injected intramuscularly. Comparative study of local tolerability compared with ampicillin and determination of effectiveness and tolerability in the treatment of surgical and urinary tract infections.肌内注射美洛西林/苯唑西林固定组合。与氨苄西林相比局部耐受性的比较研究以及在治疗外科和尿路感染中的有效性和耐受性测定。
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[Therapy with an antibiotic combination mezlocillin/oxacillin and clinical experience/First communication: Adults (author's transl)].[美洛西林/苯唑西林联合抗生素治疗及临床经验/首次交流:成人(作者译)]
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Antibiotiki. 1976 Nov;21(11):1000-2.
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Antibiotic concentrations in blood and tissue. Intraoperative ischemia as a model for the determination of tissue concentrations using mezlocillin and oxacillin as examples.血液和组织中的抗生素浓度。以美洛西林和苯唑西林为例,将术中局部缺血作为测定组织浓度的模型。
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[Penetration of ampicillin and oxacillin into the tissues of rats with aseptic inflammation].[氨苄西林和苯唑西林在无菌性炎症大鼠组织中的渗透情况]
Antibiotiki. 1984 May;29(5):370-3.

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Pharmacokinetics of amoxicillin and flucloxacillin following the simultaneous intravenous administration of 4 g and 1 g, respectively.分别静脉注射4克阿莫西林和1克氟氯西林后的药代动力学。
Infection. 1983 May-Jun;11(3):150-4. doi: 10.1007/BF01641294.
2
[Mezlocillin and oxacillin concentrations in the bile of the choledochus].[胆总管胆汁中 mezlocillin 和苯唑西林的浓度]
Infection. 1982;10 Suppl 3:S209-12. doi: 10.1007/BF01640674.