Mpenge Mbiye A, MacGowan Alasdair P
Department of Medical Microbiology, University Hospitals Bristol NHS Trust, Bristol Royal Infirmary, Bristol, England.
Department of Medical Microbiology, North Bristol NHS Trust, Southmead Hospital, Bristol, England.
Ther Clin Risk Manag. 2015 Apr 7;11:565-79. doi: 10.2147/TCRM.S75412. eCollection 2015.
Ceftaroline is a new parenteral cephalosporin approved by the European Medicines Agency (EMA) and the US Food and Drug Administration (FDA) for the treatment of complicated skin and soft tissue infections (cSSTIs) including those due to methicillin-resistant Staphylococcus aureus (MRSA), and community-acquired pneumonia (CAP). Ceftaroline has broad-spectrum activity against gram-positive and gram-negative bacteria and exerts its bactericidal effects by binding to penicillin-binding proteins (PBPs), resulting in inhibition of bacterial cell wall synthesis. It binds to PBP 2a of MRSA with high affinity and also binds to all six PBPs in Streptococcus pneumoniae. In in vitro studies, ceftaroline demonstrated potent activity against Staphylococcus aureus (including MRSA and vancomycin-intermediate isolates), Streptococcus pneumoniae (including multidrug resistant isolates), Haemophilus influenzae, Moraxella catarrhalis, and many common gram-negative pathogens, excluding extended spectrum beta-lactamase (ESBL)-producing Enterobacteriaceae and Pseudomonas aeruginosa. In Phase II and Phase III clinical trials, ceftaroline was noninferior to its comparator agents and demonstrated high clinical cure rates in the treatment of cSSTIs and CAP. It demonstrated favorable outcomes in patients treated for both regulatory-approved indications and unlicensed indications in a retrospective analysis. Ceftaroline is a safe and effective option for treatment in specific patient populations in which its efficacy and safety have been proven. This article reviews the challenges in the treatment of cSSTI and CAP, ceftaroline and its microbiology, pharmacology, efficacy, and safety data which support its use in treatment of cSSTIs and CAP.
头孢洛林是一种新型肠外头孢菌素，已获欧洲药品管理局（EMA）和美国食品药品监督管理局（FDA）批准，用于治疗包括耐甲氧西林金黄色葡萄球菌（MRSA）所致感染在内的复杂性皮肤及软组织感染（cSSTIs）以及社区获得性肺炎（CAP）。头孢洛林对革兰氏阳性菌和革兰氏阴性菌具有广谱活性，通过与青霉素结合蛋白（PBPs）结合发挥杀菌作用，从而抑制细菌细胞壁合成。它以高亲和力与MRSA的PBP 2a结合，也与肺炎链球菌的所有六种PBPs结合。在体外研究中，头孢洛林对金黄色葡萄球菌（包括MRSA和万古霉素中介菌株）、肺炎链球菌（包括多重耐药菌株）、流感嗜血杆菌、卡他莫拉菌以及许多常见革兰氏阴性病原体显示出强大活性，但不包括产超广谱β-内酰胺酶（ESBL）的肠杆菌科细菌和铜绿假单胞菌。在II期和III期临床试验中，头孢洛林不劣于其对照药物，在治疗cSSTIs和CAP方面显示出高临床治愈率。在一项回顾性分析中，它在治疗获批适应症和未获批适应症的患者中均显示出良好结果。对于已证实其疗效和安全性的特定患者群体，头孢洛林是一种安全有效的治疗选择。本文综述了cSSTI和CAP治疗中的挑战、头孢洛林及其微生物学、药理学、疗效和安全性数据，这些数据支持其用于治疗cSSTIs和CAP。
