Tomioka H, Sato K, Saito H
Department of Microbiology and Immunology, Shimane Medical University, Japan.
Kekkaku. 1991 Oct;66(10):643-9.
Sparfloxacin (SPFX), a new quinolone, was studied its in vitro and in vivo activities against various mycobacteria, especially Mycobacterium intracellulare. SPFX exhibited a potent in vitro activity against M. tuberculosis, M.kansasii and M.fortuitum with MIC90 values of 0.2, 6.25 and 1.6 micrograms/ml, respectively, and the potency of SPFX was higher than that of ofloxacin (OFLX). M.marinum, M.scrofulaceum, M.avium, M.intracellulare, M.chelonae (subsp. abscessus and chelonae) were resistant to SPFX. SPFX inhibited the growth of M. intracellulare in 7H9 broth when added at the concentration of 0.2 microgram/ml and rapidly killed the organisms at the dose of 1 microgram/ml. The activity of SPFX was higher than that of OFLX. SPFX exhibited a greater antimicrobial activity against M.intracellulare phagocytosed by murine peritoneal macrophages than did OFLX. SPFX exhibited a weak therapeutic activity against M.intracellulare infection induced in mice, on the basis of the rate of bacterial elimination in the host lungs and spleen, but such an efficacy was not noted for OFLX. SPFX combined with rifampicin (RFP), or in combination with RFP and kanamycin yielded a slightly increased therapeutic efficacy, based on the degree of pulmonary gross lesions in host animals or CFU of organisms in the lungs and spleen.
司帕沙星（SPFX）是一种新型喹诺酮类药物，对各种分枝杆菌，尤其是胞内分枝杆菌进行了体内外活性研究。SPFX对结核分枝杆菌、堪萨斯分枝杆菌和偶然分枝杆菌表现出强大的体外活性，其MIC90值分别为0.2、6.25和1.6微克/毫升，且SPFX的活性高于氧氟沙星（OFLX）。海分枝杆菌、瘰疬分枝杆菌、鸟分枝杆菌、胞内分枝杆菌、龟分枝杆菌（脓肿亚种和龟亚种）对SPFX耐药。当以0.2微克/毫升的浓度添加时，SPFX可抑制7H9肉汤中胞内分枝杆菌的生长，并在1微克/毫升的剂量下迅速杀灭该菌。SPFX的活性高于OFLX。与OFLX相比，SPFX对小鼠腹腔巨噬细胞吞噬的胞内分枝杆菌具有更强的抗菌活性。基于宿主肺和脾中细菌清除率，SPFX对小鼠体内诱导的胞内分枝杆菌感染表现出较弱的治疗活性，但OFLX未观察到这种疗效。基于宿主动物肺部大体病变程度或肺和脾中细菌的CFU，SPFX与利福平（RFP）联合使用，或与RFP和卡那霉素联合使用，治疗效果略有提高。
