Drabu Y J, Mehtar S, Blakemore P H
Drugs Exp Clin Res. 1987;13(4):201-3.
The in vitro activity of roxithromycin (RU 28965), a new semisynthetic macrolide, was compared with that of amoxycillin, cephradine, doxycycline and erythromycin against 160 respiratory and skin isolates including 10 methicillin-resistant Staph. aureus, 10 beta-lactamase-producing Haemophilus influenzae and 30 anaerobes. The MIC determinations were performed by an agar dilution method using a final inoculum of 10(4)-10(5) c.f.u./ml and results were recorded as the lowest concentration of the drug that inhibited visible growth (MIC). All organisms were incubated aerobically at 37 degrees C for 18 h, except anaerobes which were incubated in an anaerobic chamber at 37 degrees C for 48 h. The MICs of roxithromycin against staphylococci (30 strains, 10 of which were erythromycin-resistant, MIC greater than or equal to 2 mg/l) ranged from 0.03 to greater than or equal to 16 mg/l. The MIC90 against erythromycin-sensitive staphylococci was 1.0 mg/l. The MICs of roxithromycin ranged from 0.03-4 mg/l (MIC90 0.25 mg/l) against streptococci (50 strains), from 1 to 32 mg/l (MIC90 8 mg/l) against Haemophilus spp. (40), and from 0.06 to 0.25 mg/l (MIC90 0.125 mg/l) against B. catarrhalis (10). Roxithromycin was less active than erythromycin against fusobacteria (MIC 0.05 to greater than or equal to 128 mg/l) and against Veillonella spp. (MIC greater than 128 mg/l). Roxithromycin was more active than cephradine, doxycycline and amoxycillin against the aerobic organisms (except for amoxycillin against streptococci, where the activity was similar) but less active against the anaerobes examined. Taken together with reported kinetic advantages, these results suggest that roxithromycin may be a useful antibiotic in selected circumstances and studies to determine its efficacy seem indicated.
将新型半合成大环内酯类药物罗红霉素(RU 28965)的体外活性与阿莫西林、头孢拉定、强力霉素和红霉素进行了比较,受试菌株为160株呼吸道和皮肤分离菌,包括10株耐甲氧西林金黄色葡萄球菌、10株产β-内酰胺酶的流感嗜血杆菌和30株厌氧菌。采用琼脂稀释法测定最低抑菌浓度(MIC),最终接种量为10⁴ - 10⁵ c.f.u./ml,结果记录为抑制可见生长的最低药物浓度(MIC)。除厌氧菌在37℃厌氧箱中培养48小时外,所有菌株均在37℃需氧条件下培养18小时。罗红霉素对葡萄球菌(30株,其中10株对红霉素耐药,MIC≥2mg/l)的MIC范围为0.03至≥16mg/l。对红霉素敏感葡萄球菌的MIC90为1.0mg/l。罗红霉素对链球菌(50株)的MIC范围为0.03 - 4mg/l(MIC90 0.25mg/l),对嗜血杆菌属(40株)的MIC范围为1至32mg/l(MIC90 8mg/l),对卡他莫拉菌(10株)的MIC范围为0.06至0.25mg/l(MIC90 0.125mg/l)。罗红霉素对梭杆菌属(MIC 0.05至≥128mg/l)和韦荣球菌属(MIC>128mg/l)的活性低于红霉素。罗红霉素对需氧菌的活性高于头孢拉定、强力霉素和阿莫西林(阿莫西林对链球菌的活性与之相似),但对所检测的厌氧菌活性较低。结合已报道的动力学优势,这些结果表明罗红霉素在某些特定情况下可能是一种有用的抗生素,似乎有必要开展研究以确定其疗效。