Akaniro J C, Stutman H R, Arguedas A G, Vargas O M
Department of Pediatrics, Memorial Miller Children's Hospital, Long Beach, California 90801-1428.
Antimicrob Agents Chemother. 1992 Feb;36(2):255-61. doi: 10.1128/AAC.36.2.255.
Sparfloxacin is a new oral fluoroquinolone agent with putative activity against common pediatric pathogens. Using the broth microdilution method, we evaluated sparfloxacin activity in comparison with those of other antimicrobial agents against 383 pediatric isolates derived from cultures of blood and other normally sterile body fluids. MICs were assessed in Mueller-Hinton broth, serum, and urine, as well as at inoculum sizes of 10(4) to 10(8) CFU/ml. The emergence and stability of resistance and cross-resistance of Pseudomonas aeruginosa (mucoid and nonmucoid) and Staphylococcus aureus to sparfloxacin and ciprofloxacin were evaluated. Inhibitory activity of sparfloxacin against most test organisms was within achievable serum levels. Sparfloxacin was greater than or equal to 2- to 4-fold more active than other quinolones against gram-positive pathogens and 2- to 4-fold less active than ciprofloxacin against P. aeruginosa. Sparfloxacin activity was unaffected by urine and was enhanced by two- to eightfold in human serum. Its potency was not affected by inocula of less than or equal to 10(7) CFU/ml. The frequency of development of spontaneous resistance was similar to that found for other new quinolone agents, and stable resistance emerged only in P. aeruginosa. Sparfloxacin merits additional study against invasive pediatric pathogens.
司帕沙星是一种新型口服氟喹诺酮类药物，对常见儿科病原体具有假定活性。我们采用肉汤微量稀释法，将司帕沙星与其他抗菌药物的活性进行比较，评估其对383株来自血液及其他通常无菌的体液培养物的儿科分离菌株的活性。在 Mueller-Hinton 肉汤、血清和尿液中，以及接种量为10⁴至10⁸CFU/ml 时评估最低抑菌浓度（MIC）。评估了铜绿假单胞菌（黏液型和非黏液型）和金黄色葡萄球菌对司帕沙星和环丙沙星的耐药性、交叉耐药性的出现及稳定性。司帕沙星对大多数测试菌的抑制活性在可达到的血清水平范围内。司帕沙星对革兰氏阳性病原体的活性比其他喹诺酮类药物高2至4倍，对铜绿假单胞菌的活性比环丙沙星低2至4倍。司帕沙星的活性不受尿液影响，在人血清中活性增强2至8倍。其效力不受接种量小于或等于10⁷CFU/ml 的影响。自发耐药性的发生频率与其他新型喹诺酮类药物相似，且仅在铜绿假单胞菌中出现稳定耐药性。司帕沙星值得针对侵袭性儿科病原体进行进一步研究。
