Coppens L, Klastersky J
Antimicrob Agents Chemother. 1979 Mar;15(3):396-9. doi: 10.1128/AAC.15.3.396.
The anti-pseudomonas activities of azlocillin and mezlocillin were compared with that of ticarcillin. We measured the minimal inhibitory and minimal bactericidal concentrations of the three drugs against 20 different strains of Pseudomonas aeruginosa and found significantly lower values for azlocillin than for the other two drugs. We then infused 5 g of each drug into 10 volunteers on three consecutive days and determined the serum levels of the three antibiotics at 1-h intervals from 1 to 6 h after injection. The levels of azlocillin were significantly higher than those of mezlocillin and ticarcillin (at 1 h: 236.55 mug/ml +/- 12.9 for azlocillin, 192.45 mug/ml +/- 28.8 for mezlocillin, and 131.5 mug/ml +/- 10.9 for ticarcillin). The inhibitory and bactericidal activities of the sera obtained 1 and 6 h after the injection against the same 20 strains of P. aeruginosa demonstrated a significantly greater anti-pseudomonas activity of azlocillin when compared with mezlocillin and ticarcillin; mezlocillin and ticarcillin had approximately the same activity. The mean values for bactericidal activity against the strains tested were 1/32 for azlocillin, 1/8 for mezlocillin, and 1/8 for ticarcillin. Azlocillin thus appears to be a promising anti-pseudomonas drug and should be tested in clinical trials.
将阿洛西林和美洛西林的抗假单胞菌活性与替卡西林进行了比较。我们测定了这三种药物对20株不同铜绿假单胞菌菌株的最低抑菌浓度和最低杀菌浓度,发现阿洛西林的值明显低于其他两种药物。然后,我们连续三天给10名志愿者输注5克每种药物,并在注射后1至6小时每隔1小时测定这三种抗生素的血清水平。阿洛西林的水平明显高于美洛西林和替卡西林(1小时时:阿洛西林为236.55微克/毫升±12.9,美洛西林为192.45微克/毫升±28.8,替卡西林为131.5微克/毫升±10.9)。注射后1小时和6小时获得的血清对相同20株铜绿假单胞菌的抑菌和杀菌活性表明,与美洛西林和替卡西林相比,阿洛西林具有明显更强的抗假单胞菌活性;美洛西林和替卡西林的活性大致相同。对受试菌株的杀菌活性平均值,阿洛西林为1/32,美洛西林为1/8,替卡西林为1/8。因此,阿洛西林似乎是一种有前景的抗假单胞菌药物,应进行临床试验。