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达托霉素:一种新型环脂肽类抗菌药物。

Daptomycin: a novel cyclic lipopeptide antimicrobial.

作者信息

Schriever Christopher A, Fernández Cristina, Rodvold Keith A, Danziger Larry H

机构信息

Loyal University Medical Center, Maywood, IL, USA.

出版信息

Am J Health Syst Pharm. 2005 Jun 1;62(11):1145-58. doi: 10.1093/ajhp/62.11.1145.

Abstract

PURPOSE

The development, activity, pharmacokinetics, pharmacodynamics, clinical efficacy, adverse effects, and dosage and administration of daptomycin are reviewed.

SUMMARY

Daptomycin, a novel cyclic lipopeptide antimicrobial, is bactericidal against a range of gram-positive bacteria, including many multiple-drug-resistant isolates. It has only minimal activity against anaerobic bacteria and no activity against gram-negative bacteria. Daptomycin exhibits linear pharmacokinetics, and the plasma concentration-versus-time relationship is best described by a two-compartment model with first-order elimination. The initial bactericidal activity is rapid, extensive, and concentration related. In clinical trials, daptomycin has shown efficacy in treating complicated skin and skin-structure infections (CSSSIs); the drug carries FDA-approved labeling for same. The adverse effects of daptomycin appear comparable to those of vancomycin and semisynthetic penicillins. The dosage for CSSSIs is 4 mg/kg by i.v. infusion every 24 hours.

CONCLUSION

Daptomycin is bactericidal against gram-positive organisms and offers an option in the treatment of CSSSIs.

摘要

目的

综述达托霉素的研发、活性、药代动力学、药效学、临床疗效、不良反应以及剂量与用法。

总结

达托霉素是一种新型环状脂肽类抗菌药物,对一系列革兰氏阳性菌具有杀菌作用,包括许多多重耐药菌株。它对厌氧菌的活性极小,对革兰氏阴性菌无活性。达托霉素呈现线性药代动力学,血浆浓度与时间的关系最好用具有一级消除的二室模型来描述。其初始杀菌活性迅速、广泛且与浓度相关。在临床试验中,达托霉素已显示出治疗复杂性皮肤及皮肤结构感染(CSSSI)的疗效;该药具有FDA批准的针对此适应证的标签说明。达托霉素的不良反应似乎与万古霉素和半合成青霉素相当。CSSSI的剂量为每24小时静脉输注4mg/kg。

结论

达托霉素对革兰氏阳性菌具有杀菌作用,为CSSSI的治疗提供了一种选择。

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