Herbert D, Paramasivan C N, Venkatesan P, Kubendiran G, Prabhakar R, Mitchison D A
Tuberculosis Research Centre, Indian Council of Medical Research, Madras, India.
Antimicrob Agents Chemother. 1996 Oct;40(10):2296-9. doi: 10.1128/AAC.40.10.2296.
The bactericidal actions of ofloxacin and sulbactam-ampicillin, alone and in combination with rifampin and isoniazid, on exponential-phase and stationary-phase cultures of a drug-susceptible isolate of Mycobacterium tuberculosis were studied in vitro. In exponential-phase cultures, all drugs were bactericidal, with the higher concentrations of ofloxacin (5 micrograms/ml) and sulbactam-ampicillin (15 micrograms of ampicillin per ml) being as bactericidal as 1 microgram of isoniazid per ml or 1 microgram of rifampin per ml. In two-drug combinations, both drugs increased the levels of activity of isoniazid and rifampin and were almost as bactericidal as isoniazid-rifampin; they also appeared to increase the level of activity of isoniazid-rifampin in three-drug combinations. In contrast, ofloxacin and sulbactam-ampicillin had little bactericidal activity against stationary-phase cultures and were less active than isoniazid or rifampin alone. Furthermore, in two-drug or three-drug combinations, they did not increase the level of activity of isoniazid, rifampin, or isoniazid-rifampin. These findings suggest that ofloxacin and sulbactam-ampicillin are likely to be most useful in the early stages of treatment and in preventing the emergence of resistance to other drugs but are unlikely to be effective as sterilizing drugs helping to kill persisting lesional bacilli.
体外研究了氧氟沙星和舒巴坦-氨苄西林单独使用以及与利福平、异烟肼联合使用时,对结核分枝杆菌药物敏感株的对数生长期和稳定期培养物的杀菌作用。在对数生长期培养物中,所有药物均具有杀菌作用,较高浓度的氧氟沙星(5微克/毫升)和舒巴坦-氨苄西林(每毫升含15微克氨苄西林)与每毫升1微克异烟肼或1微克利福平的杀菌效果相当。在两药联合使用时,两种药物均提高了异烟肼和利福平的活性水平,且杀菌效果几乎与异烟肼-利福平相当;在三药联合使用时,它们似乎也提高了异烟肼-利福平的活性水平。相比之下,氧氟沙星和舒巴坦-氨苄西林对稳定期培养物的杀菌活性很小,且比单独使用异烟肼或利福平的活性更低。此外,在两药或三药联合使用时,它们并未提高异烟肼、利福平或异烟肼-利福平的活性水平。这些发现表明,氧氟沙星和舒巴坦-氨苄西林可能在治疗早期以及预防对其他药物产生耐药性方面最为有用,但作为有助于杀灭持续存在的病灶内细菌的灭菌药物可能无效。