值得期待的新β内酰胺酶抑制剂阿维巴坦及其复合制剂.docVIP

值得期待的新β内酰胺酶抑制剂阿维巴坦及其复合制剂 杨 帆，王明华 （200040上海，复旦大学附属华山医院抗生素研究所） [关键词] 阿维巴坦；β内酰胺酶抑制剂；丝氨酸β内酰胺酶 [中图法分类号] [文献标志码] A Avibactam, Aan anticipated new β-lactamase inhibitor avibactam and its combination Yang Fan, Wang Minghua (Institute of Antibiotics, Huashan Hospital, Fudan University, Shanghai, 200040, China) [Abstract] Avibactam is a synthetic non-β-lactam, β-lactamase inhibitor that inhibits the activities of Ambler class A and C β-lactamases and some class D enzymes. The addition of avibactam enhances the antimicrobial activity of cephalosporins against β-lactamase-producing Enterobacteriaceae, Pseudomonas aeruginosa, and some anaerobic bacteria. The pharmacokinetics of avibactam followed a two-compartment model and was not affected by the co-administration of ceftazidime. The maximum plasma drug concentration (Cmax) and area under the plasma concentration-time curve (AUC) of avibactam were increased linearly with the doses ranging from 50 mg to 2 000 mg. The mean volume of distribution and half-life of avibactam are 22 L and 2 hours respectively. Like ceftazidime, avibactamis primarily renally excreted excreted, and its clearance was correlatesd with creatinine clearance. Clinical trials to date have showed that ceftazidime/avibactam was well tolerated and as effective as carbapenem in the treatment of complicated intra-abdominal infection and complicated urinary tract infection. [Key words] avibactam; beta-lactam inhibitor; serine beta-lactamses Corresponding author: Yang Fan, Tel: 86-21E-mail：fanyang9@ [通信作者] 杨 帆，男，博士，副教授，硕士生导师。上海市医学会感染与化疗学会委员兼秘书。获国家重大科技专项重大新药创制子课题及上海市自然科学基金等课题资助。以第一作者或通讯作者发表论文10余篇。参加《抗菌药物临床应用指导原则》及10余部专注编写。主要从事感染性疾病诊治、抗感染药物临床评价、细菌耐药性研究和抗菌药物管理工作。E-mail： HYPERLINK mailto:fanyang9@ fanyang9@ [优先出版] β内酰胺类抗生素是临床最为常用的抗菌药物。近10年内世界范围内分离的肠杆菌科细菌、非发酵革兰阴性菌由于产超广谱β内酰胺酶（ESBLs）、AmpC酶和碳青霉烯酶（KPC），对青霉素类、头孢菌素类、β内酰胺酶抑制剂复方制剂乃至碳青霉烯类抗生素耐药现象严重。产KPC酶是目前肠杆菌科细菌对碳青霉烯类耐药的最主要原因。产β内酰胺酶的细菌对如喹诺酮类、氨基糖苷类、多粘菌素、替加环素等其他类别抗菌药物亦可耐药，给治疗带来重大挑战 ADDIN EN.CITE AD