Department of Clinical, Social, and Administrative Sciences, Department of Pharmacy Services, University of Michigan Health System and College of Pharmacy, Ann Arbor, MI, USA.
Ann Pharmacother. 2011 Nov;45(11):1384-98. doi: 10.1345/aph.1Q225. Epub 2011 Oct 18.
To review the pharmacology, microbiology, chemistry, in vitro activity, pharmacokinetics, clinical efficacy, safety, dosage, and administration of ceftaroline fosamil (Teflaro, Forest Laboratories, Inc.), a novel parenteral broad-spectrum cephalosporin approved by the Food and Drug Administration (FDA) on October 29, 2010, for the treatment of adults with acute bacterial skin and skin structure infections (ABSSSI) and community-acquired bacterial pneumonia (CABP).
A search of MEDLINE (1966-July 2011) using the search terms ceftaroline fosamil, ceftaroline, TAK-599, PPI-0903, PPI-0903M, and T-91825 was performed. Supplementary sources included program abstracts from the Interscience Conference on Antimicrobial Agents and Chemotherapy, American Society of Microbiology, European Congress on Clinical Microbiology and Infectious Diseases, and the Infectious Diseases Society of America from 2005 to 2010, as well as information available from the manufacturer's Web site.
All English-language articles identified from the data sources were evaluated. In vitro, preclinical, and Phase 1, 2, and 3 clinical trials were included.
Clinical trials have been conducted evaluating use of ceftaroline for treatment of ABSSSI and CABP. Safety data from Phase 1, 2, and 3 clinical trials suggest that it is well tolerated and has a safety and tolerability profile common to the cephalosporin class. Ceftaroline has excellent in vitro activity against gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA), which makes it an attractive monotherapy for the treatment of ABSSSI. However, it lacks activity against problem gram-negative bacteria (eg, Pseudomonas spp.), which will likely limit its use for serious health care-associated infections. While its role in treating CABP is supported by excellent in vitro activity against Streptococcus pneumoniae and clinical efficacy data, currently available comparators may offer some advantages over ceftaroline. Finally, data are lacking to assess its role in the treatment of serious infections due to MRSA (eg, pneumonia, bacteremia).
These considerations should be part of the formulary review process; however, when considering the significant role MRSA plays in ABSSSI in both the community and hospital settings, we believe that ceftaroline will provide clinicians with a welcome option in addition to currently available anti-MRSA therapies for the treatment of ABSSSI.
回顾法唑培南（头孢洛林酯，福来斯特实验室，Inc.）的药理学、微生物学、化学、体外活性、药代动力学、临床疗效、安全性、剂量和给药，该药是一种新型的注射用广谱头孢菌素，于 2010 年 10 月 29 日获得美国食品和药物管理局（FDA）批准，用于治疗成人急性细菌性皮肤和皮肤结构感染（ABSSSI）和社区获得性细菌性肺炎（CABP）。
使用搜索词头孢洛林酯、头孢洛林、TAK-599、PPI-0903、PPI-0903M 和 T-91825，在 MEDLINE（1966 年-2011 年 7 月）进行了一次搜索。补充资料包括 2005 年至 2010 年在抗菌药物化学疗法协会国际会议、美国微生物学会、欧洲临床微生物学和传染病大会和传染病学会上的会议摘要，以及从制造商网站获得的信息。
从数据来源中评估了所有英文文章。包括了体外、临床前和 1、2、3 期临床试验。
已经进行了临床试验，评估了头孢洛林治疗 ABSSSI 和 CABP 的效果。1、2、3 期临床试验的安全性数据表明，它具有良好的耐受性，并且具有与头孢菌素类药物相同的安全性和耐受性特征。头孢洛林对革兰氏阳性病原体具有极好的体外活性，包括耐甲氧西林金黄色葡萄球菌（MRSA），这使其成为治疗 ABSSSI 的一种有吸引力的单一疗法。然而，它对革兰氏阴性问题菌（如铜绿假单胞菌）没有活性，这可能限制其用于严重的医疗保健相关感染。虽然其治疗 CABP 的作用得到了对肺炎链球菌具有极好的体外活性和临床疗效数据的支持，但目前可用的比较药物可能在某些方面优于头孢洛林。最后，由于缺乏数据来评估其在治疗由 MRSA（如肺炎、菌血症）引起的严重感染中的作用。
这些考虑因素应该是配方审查过程的一部分；然而，当考虑到社区和医院环境中 MRSA 在 ABSSSI 中所起的重要作用时，我们认为头孢洛林将为临床医生提供一种除目前可用的抗 MRSA 疗法之外的治疗 ABSSSI 的另一种治疗选择。
