Medical Department, Ferrer Internacional SA, Barcelona, Spain.
Charles River Laboratories Montreal ULC., Senneville, Canada.
Future Microbiol. 2018 May 1;13:31-40. doi: 10.2217/fmb-2017-0291.
Ozenoxacin is a nonfluorinated quinolone antibacterial approved for topical treatment of impetigo. Because quinolones have known chondrotoxic effects in juvenile animals, the potential toxicity of ozenoxacin was assessed in preclinical studies.
MATERIALS & METHODS: Ozenoxacin or ofloxacin (300 mg/kg/day for 5 days, for each compound) was orally administered to juvenile rats, and oral ozenoxacin (10-100 mg/kg/day for 14 days) was administered to juvenile dogs.
In juvenile rats, ozenoxacin showed no chondrotoxicity, whereas ofloxacin produced typical quinolone-induced lesions in articular cartilage in three of ten rats. Oral ozenoxacin administration to juvenile dogs showed no chondrotoxicity or toxicologically relevant findings in selected target organs.
Ozenoxacin was generally well-tolerated in juvenile rats and dogs, with no evidence of quinolone-induced arthropathy.
噁嗪酮是一种非氟喹诺酮类抗菌药物,已被批准用于治疗脓疱疮的局部治疗。由于喹诺酮类药物在幼年动物中有已知的软骨毒性作用,因此在临床前研究中评估了噁嗪酮的潜在毒性。
将噁嗪酮或氧氟沙星(每种化合物 300mg/kg/天,连续 5 天)口服给予幼年大鼠,将噁嗪酮(10-100mg/kg/天,连续 14 天)口服给予幼年犬。
在幼年大鼠中,噁嗪酮没有软骨毒性,而氧氟沙星在十只大鼠中的三只中产生了典型的喹诺酮诱导的关节软骨病变。噁嗪酮在幼年犬中的口服给药未显示软骨毒性或在选定的靶器官中出现毒理学相关发现。
噁嗪酮在幼年大鼠和犬中总体耐受性良好,没有证据表明噁嗪酮引起的关节病。