Smith C B, Finland M
Appl Microbiol. 1968 Nov;16(11):1753-60. doi: 10.1128/am.16.11.1753-1760.1968.
Carbenicillin is a new semisynthetic penicillin which differs from other penicillins in showing moderate antibacterial activity against Pseudomonas. Its activity in vitro is enhanced at low pH. Serum binding is of low order and does not appreciably alter activity. Strains of Pseudomonas exposed to subinhibitory concentrations of carbenicillin rapidly develop resistance by a mechanism that does not depend upon destruction of the drug. In normal subjects, high levels of anti-Pseudomonas activity are readily obtained in the urine after intramuscular injection. Levels of carbenicillin adequate to inhibit many strains of Pseudomonas can be achieved in serum only with an intravenous administration of a large dose. Carbenicillin appears to exhibit the same low degree of toxicity as do other penicillins.
羧苄青霉素是一种新型半合成青霉素,它与其他青霉素的不同之处在于对假单胞菌显示出中等抗菌活性。其体外活性在低pH值时增强。血清结合率低,不会明显改变活性。暴露于亚抑制浓度羧苄青霉素的假单胞菌菌株会通过一种不依赖于药物破坏的机制迅速产生耐药性。在正常受试者中,肌内注射后尿液中很容易获得高水平的抗假单胞菌活性。只有通过静脉注射大剂量药物,才能在血清中达到足以抑制许多假单胞菌菌株的羧苄青霉素水平。羧苄青霉素似乎与其他青霉素一样,毒性程度较低。