Eperezolid

对消化链球菌\痤疮丙酸杆菌\产气荚膜梭菌\艰难梭菌\脆弱拟杆菌和梭杆菌属的MIC50值为0.5\1.0\2.0\1.0\16.0和2.0 mg/L.

厌氧菌是严重感染的普遍成因.临床感染的主要厌氧菌包括脆弱拟杆菌群\梭状芽孢杆菌和消化链球菌属.恶唑烷酮类是一类新型的合成抗菌剂,抑制蛋白合成的起始.此类的两种化合物,Eperezolid和linezolid能够抑制粪肠球菌和屎肠球菌.

体外实验:小于2 mg/L的Eperezolid能够抑制90%的测试株,有痤疮丙酸杆菌(30株)\消化链球菌属(50株)\产气荚膜梭菌(50株)和艰难梭菌(50株).相比于Eperezolid(MIC90值为16 mg/L),Linezolid具有更高(MIC90值为4.0 mg/L)的抗脆弱拟杆菌(100株)活性[1].

体内试验:在大鼠腹腔内脓肿模型中测定Eperezolid和Linezolid抗粪肠球菌和万古霉素耐受性屎肠球菌的活性.Eperezolid按25 mg/kg剂量每天两次给药,对降低粪肠球菌的脓肿细菌密度是无效的.静脉注射Eperezolid能够降低脓肿细菌密度将近2 log10 CFU/g [2].

临床试验:健康志愿者口服Eperezolid(1000 mg PO),血浆峰值浓度为6.28 mg/L,峰底浓度为1.62 mg/L [3].

参考文献：
[1] Edlund C, Oh H, Nord CE.  In vitro activity of linezolid and eperezolid against anaerobic bacteria. Clin Microbiol Infect. 1999;5(1):51-53.
[2] Schülin T, Thauvin-Eliopoulos C, Moellering RC Jr, Eliopoulos GM.  Activities of the oxazolidinones linezolid and eperezolid in experimental intra-abdominal abscess due to Enterococcus faecalis or vancomycin-resistant Enterococcus faecium. Antimicrob Agents Chemother. 1999;43(12):2873-6.
[3] Schaadt RD, Batts DH, Daley-Yates PT, Pawsey SD, Stalker DJ, Zurenko GE.  Serum inhibitory titers and serum bactericidal titers for human subjects receiving multiple doses of the antibacterial oxazolidinones eperezolid and linezolid. Diagn Microbiol Infect Dis. 1997;28(4):201-
4.  B3395