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美罗培南:一种新型碳青霉烯类抗菌药物。

Meropenem: a new carbapenem antimicrobial.

作者信息

Pryka R D, Haig G M

机构信息

Department of Pharmacy Practice, College of Pharmacy, University of Toledo, OH 43606.

出版信息

Ann Pharmacother. 1994 Sep;28(9):1045-54. doi: 10.1177/106002809402800910.

Abstract

OBJECTIVE

To describe and then compare an investigational carbapenem antibiotic, meropenem, with the only currently available antibiotic in this class, imipenem/cilastatin.

DATA IDENTIFICATION

An English language search using MEDLINE (1988-1993); Abstracts of the 31st Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC), 1991; and Abstracts of the 32nd ICAAC, 1992.

STUDY SELECTION

All current scientific publications were reviewed for study design and quality. Emphasis was placed on susceptibility and pharmacokinetic analysis. Phase 3 clinical trials are now being completed and have only been published in abstract form. Hence, conclusions derived regarding efficacy were tempered.

RESULTS

Meropenem is active against a broad spectrum of gram-positive and -negative pathogens including beta-lactamase producers. Meropenem appears to be two- to fourfold less active than imipenem against gram-positive organisms. Meropenem is two- to fivefold more active against enterobacteriaceae. The two compounds appear to be equally active against Pseudomonas aeruginosa. Pharmacokinetic disposition is also similar for imipenem and meropenem. Meropenem may exhibit greater tissue penetration. Meropenem is not labile to renal hydrolysis and can be administered without a competitive antagonist of dihydropeptidase, such as cilastatin. In clinical trials, meropenem appears to be as safe and effective as imipenem/cilastatin or ceftazidime in the treatment of infections involving soft tissue, urinary tract, upper respiratory tract, abdominal processes, and febrile neutropenic episodes.

CONCLUSIONS

Meropenem is comparable to imipenem in terms of in vitro susceptibility pattern and pharmacokinetic disposition. Overall, meropenem seems to offer promise as the second of the carbapenem class of antibiotics. Clinical data are preliminary, and further data are needed.

摘要

目的

描述并比较一种研究性碳青霉烯类抗生素美罗培南与该类目前唯一可用的抗生素亚胺培南/西司他丁。

资料识别

使用MEDLINE(1988 - 1993年)进行英文文献检索;1991年第31届抗微生物药物和化疗跨学科会议(ICAAC)摘要;以及1992年第32届ICAAC摘要。

研究选择

对所有当前科学出版物的研究设计和质量进行了审查。重点在于敏感性和药代动力学分析。3期临床试验目前正在完成,且仅以摘要形式发表。因此,关于疗效得出的结论较为谨慎。

结果

美罗培南对包括产β-内酰胺酶菌在内的广泛革兰氏阳性和阴性病原体具有活性。美罗培南对革兰氏阳性菌的活性似乎比亚胺培南低两到四倍。美罗培南对肠杆菌科细菌的活性高两到五倍。这两种化合物对铜绿假单胞菌的活性似乎相当。亚胺培南和美罗培南的药代动力学分布也相似。美罗培南可能具有更强的组织穿透力。美罗培南对肾脏水解不稳定,且无需二肽酶竞争性拮抗剂(如西司他丁)即可给药。在临床试验中,美罗培南在治疗涉及软组织、泌尿道、上呼吸道、腹部疾病和发热性中性粒细胞减少症的感染方面似乎与亚胺培南/西司他丁或头孢他啶一样安全有效。

结论

美罗培南在体外敏感性模式和药代动力学分布方面与亚胺培南相当。总体而言,美罗培南作为碳青霉烯类抗生素中的第二种似乎有前景。临床数据是初步的,还需要进一步的数据。

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