Murakawa T, Sabath L D
Antimicrob Agents Chemother. 1977 Jan;11(1):1-6. doi: 10.1128/AAC.11.1.1.
Pirbenicillin, a semisynthetic penicillin, showed greater in vitro activity against 68 recent isolates of Pseudomonas aeruginosa than did ticarcillin or carbenicillin. The median minimum inhibitory concentration of each of these three compounds, respectively, was 3.1, 12.5, and 25 mug/ml when a 10(-4) dilution of an overnight culture (about 10(5) colony-forming units [CFU]/ml) was used as inoculum, but these differences were less striking when larger inocula were used: at 10(7) CFU/ml these values were 6.25, 12.5, and 50 mug/ml, and at 10(8) to 10(9) CFU/ml these values were 50, 50, and 100 mug/ml. All three compounds showed greater inhibitory activity at pH 6 than at pH 8. This pH effect was greatest with pirbenicillin, for 6.25 mug of pirbenicillin per ml inhibited 7, 11, and 57% of the strains at pH 6, 7, and 8, respectively; these values were 4, 4, and 11% with ticarcillin and 0, 0, and 7% with carbenicillin. At sufficient inhibitory concentrations, the rates of bacterial killing of the three compounds were similar. The observed differences in anti-pseudomonad activity were not due to differences in stability to pseudomonad beta-lactamases, but all three compounds were more stable than were cefazolin, cephaloridine, and benzylpenicillin.
匹氨西林是一种半合成青霉素,与替卡西林或羧苄西林相比,它对68株近期分离出的铜绿假单胞菌显示出更强的体外活性。当使用过夜培养物的10⁻⁴稀释液(约10⁵菌落形成单位[CFU]/ml)作为接种物时,这三种化合物各自的最低抑菌浓度中位数分别为3.1、12.5和25μg/ml,但当使用更大接种量时,这些差异就不那么明显了:在10⁷CFU/ml时,这些值分别为6.25、12.5和50μg/ml,在10⁸至10⁹CFU/ml时,这些值分别为50、50和100μg/ml。所有三种化合物在pH 6时的抑制活性均高于pH 8时。这种pH效应在匹氨西林中最为显著,因为每毫升6.25μg的匹氨西林在pH 6、7和8时分别抑制7%、11%和57%的菌株;替卡西林的这些值分别为4%、4%和11%,羧苄西林的这些值分别为0%、0%和7%。在足够的抑制浓度下,这三种化合物的细菌杀灭率相似。观察到的抗假单胞菌活性差异并非由于对假单胞菌β-内酰胺酶的稳定性不同,但这三种化合物都比头孢唑林、头孢噻啶和苄青霉素更稳定。