Wang R, Liu Y N, Zhao H Z, Sun X D
Department of Clinical Pharmacology, Chinese PLA General Hospital, Beijing.
Chin Med J (Engl). 1992 Jun;105(6):500-5.
In vitro antibacterial activities (MBCs) and serum bactericidal activities (SBAs) of fluoroquinolones were compared. The MBCs were measured by the agar disk dilution test. The 40 tested strains belonging to 8 species were isolated from hospitalized patients. Against Gram positive cocci, Ciprofloxacin (CPLX) and ofloxacin (OFLX) were the more active and nefloxacin (NFLX) was less potent than the others. Against Ps. aeruginosa, CPLX had the highest activity, enoxacin (ENX) as well as OFLX had powerful activity, whereas NFLX was less active. All the 4 agents showed high activity against Gram negative bacilli. In the self-controlled, randomized crossover study, 4 fluoroquinolones were given to 10 healthy volunteers and then SBAs were determined using microdilution method. The peak SBAs of CPLX and OFLX were significantly higher than NFLX, and those of ENX were comparatively low, but there was no difference between ENX and OFLX against most of the strains tested. The percentages of peak SBAs greater than 1:8 of the 4 fluoroquinolones suggest that in the treatment of serious infections, CPLX and OFLX are more effective and ENX can also achieve high cure rate. The trough SBAs of the 4 fluoroquinolones suggest that the time interval of administration of CPLX and OFLX should be more than 8 hours, but increase of the dosage or shortening of the time interval between the administrations is recommended for ENX and NFLX.
比较了氟喹诺酮类药物的体外抗菌活性(MBCs)和血清杀菌活性(SBAs)。MBCs通过琼脂纸片稀释试验测定。从住院患者中分离出属于8个菌种的40株受试菌株。对于革兰氏阳性球菌,环丙沙星(CPLX)和氧氟沙星(OFLX)活性更强,而萘氟沙星(NFLX)的效力低于其他药物。对于铜绿假单胞菌,CPLX活性最高,依诺沙星(ENX)和OFLX也有较强活性,而NFLX活性较低。所有这4种药物对革兰氏阴性杆菌均显示出高活性。在自身对照、随机交叉研究中,给10名健康志愿者服用4种氟喹诺酮类药物,然后采用微量稀释法测定SBAs。CPLX和OFLX的峰值SBAs显著高于NFLX,ENX的峰值SBAs相对较低,但ENX和OFLX对大多数受试菌株无差异。4种氟喹诺酮类药物峰值SBAs大于1:8的百分比表明,在治疗严重感染时,CPLX和OFLX更有效,ENX也能达到高治愈率。4种氟喹诺酮类药物的谷值SBAs表明,CPLX和OFLX的给药时间间隔应超过8小时,但对于ENX和NFLX,建议增加剂量或缩短给药间隔时间。