Retsema J A, English A R, Lynch J E
Antimicrob Agents Chemother. 1976 Jun;9(6):975-82. doi: 10.1128/AAC.9.6.975.
Pirbenicillin {6-[d-2-phenyl-2(N-4-pyridylformimidoylaminoacetamido) -acetamido]-penicillanic acid} showed broad-spectrum antibacterial activity in vitro and also in the treatment of experimental infections after parenteral administration to mice. Against Pseudomonas aeruginosa, a three- to fourfold potency advantage over carbenicillin was seen both in vitro and in vivo. The in vitro antibacterial spectrum of pirbenicillin includes Escherichia coli, Serratia, Citrobacter, and Enterobacter isolates, against which it exhibited minimal inhibitory concentration values comparable to those of carbenicillin. However, mice infected with E. coli and Serratia were protected at doses of pirbenicillin that were two to four times lower than those required of carbenicillin. Pirbenicillin was more active than carbenicillin against gram-positive bacteria, especially Streptococcus faecalis. It was less active than carbenicillin against Proteus spp. and was inactive against ampicillin-resistant E. coli strains. Pirbenicillin was bactericidal at concentrations generally equal to or only two-fold higher than the minimal inhibitory concentration. With appropriately buffered media, pirbenicillin demonstrated eight- and fourfold better minimal bactericidal concentration values towards Pseudomonas isolates than those of carbenicillin and ticarcillin, respectively.
匹氨西林{6 - [d - 2 - 苯基 - 2(N - 4 - 吡啶基甲脒基氨基乙酰氨基)-乙酰氨基]-青霉烷酸}在体外以及对小鼠进行肠胃外给药后的实验性感染治疗中均显示出广谱抗菌活性。在体外和体内,相对于羧苄西林,匹氨西林对铜绿假单胞菌的效价优势均达三至四倍。匹氨西林的体外抗菌谱包括大肠杆菌、沙雷氏菌属、枸橼酸杆菌属和肠杆菌属分离株,对这些菌株其显示出与羧苄西林相当的最低抑菌浓度值。然而,感染大肠杆菌和沙雷氏菌的小鼠,使用匹氨西林的剂量仅为羧苄西林所需剂量的二至四分之一即可得到保护。匹氨西林对革兰氏阳性菌,尤其是粪肠球菌,比羧苄西林更具活性。它对变形杆菌属的活性低于羧苄西林,并且对氨苄西林耐药的大肠杆菌菌株无活性。匹氨西林在通常等于或仅比最低抑菌浓度高两倍的浓度下具有杀菌作用。在适当缓冲的培养基中,匹氨西林对假单胞菌分离株的最低杀菌浓度值分别比羧苄西林和替卡西林好八倍和四倍。