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奎奴普丁/达福普汀(RP 59500):一种新型链阳菌素类抗生素。

Quinupristin/dalfopristin (RP 59500): a new streptogramin antibiotic.

作者信息

Chant C, Rybak M J

机构信息

Department of Pharmacy, Henry Ford Hospital, Detroit, MI, USA.

出版信息

Ann Pharmacother. 1995 Oct;29(10):1022-7. doi: 10.1177/106002809502901013.

Abstract

OBJECTIVE

To review the current knowledge on RP 59500 (quinupristin/dalfopristin, Synercid), a new streptogramin antibiotic, with respect to its pharmacology, pharmacokinetics, pharmacodynamics, mechanism of resistance, and in vitro inhibitory and bactericidal activity.

DATA SOURCES

A MEDLINE search using keywords RP 59500, pristinamycin, virginiamycin, and streptogramin was performed. Relevant abstracts presented at recent scientific conferences also were consulted.

STUDY SELECTION

Because RP 59500 is a relatively new investigational agent, relevant in vitro and animal studies were selected. All available human studies were included as well.

DATA EXTRACTION

Data from in vitro and in vivo studies were included, with particular emphasis on human studies.

DATA SYNTHESIS

RP 59500 is a new injectable streptogramin antibiotic consisting of a mixture o 2 synergistic pristinamycin compounds. RP 59500 possesses in vitro inhibitory and bactericidal activity against most isolates of gram-positive organisms including vancomycin-resistant Enterococcus faecium, selected gram-negative bacteria, and most anaerobic organisms. Based on preliminary data, the drug appears to be metabolized rapidly and extensively while exhibiting a significant postantibiotic effect. Data from ongoing clinical trials suggests that RP 59500 is well-tolerated except for mild injection site irritations. However, before the role of RP 59500 within the vast armamentarium of antimicrobials can be elucidated, additional studies need to be conducted to document its clinical efficacy.

CONCLUSIONS

Based on in vitro susceptibility testing, in vivo studies, and preliminary clinical data, RP 59500 may be an alternative to the glycopeptides, especially for inherently resistant organisms. Further studies are needed to confirm this agent's in vitro activity and to establish its clinical efficacy.

摘要

目的

综述新型链阳性菌素抗生素RP 59500(奎奴普丁/达福普汀,Synercid)在药理学、药代动力学、药效学、耐药机制以及体外抑制和杀菌活性方面的现有知识。

资料来源

使用关键词RP 59500、 pristinamycin、维吉尼亚霉素和链阳性菌素进行了MEDLINE检索。还查阅了近期科学会议上发表的相关摘要。

研究选择

由于RP 59500是一种相对较新的研究药物,因此选择了相关的体外和动物研究。所有可用的人体研究也包括在内。

资料提取

纳入了体外和体内研究的数据,尤其侧重于人体研究。

资料综合

RP 59500是一种新型注射用链阳性菌素抗生素,由2种具有协同作用的pristinamycin化合物组成。RP 59500对大多数革兰氏阳性菌分离株具有体外抑制和杀菌活性,包括耐万古霉素的粪肠球菌、某些革兰氏阴性菌以及大多数厌氧菌。根据初步数据,该药物似乎能快速且广泛地代谢,同时具有显著的抗生素后效应。正在进行的临床试验数据表明RP 59500耐受性良好,除了有轻微的注射部位刺激。然而,在阐明RP 59500在众多抗菌药物中的作用之前,需要进行更多研究以证明其临床疗效。

结论

基于体外药敏试验、体内研究和初步临床数据,RP 59500可能是糖肽类药物的替代选择,尤其是对于天然耐药菌。需要进一步研究以证实该药物的体外活性并确定其临床疗效。

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