Orbifloxacin is a synthetic fluoroquinolone with broad spectrum bactericidal activity [1]. Orbifloxacin exerts bactericidal activity by inhibiting bacterial DNA gyrase and topoisomerase IV, thereby disrupting DNA replication and bacterial proliferation [2]. Orbifloxacin accumulates in leukocytes, which allows it to act on intracellular bacteria and be transported to and liberated at the sites of infection [3]. Orbifloxacin is widely used for the treatment of gastrointestinal and respiratory infections in cattle and swine[4].
In vivo, Orbifloxacin treatment via intramuscular injection at a single dose of 20mg/kg can effectively inhibit the bacterial load of Staphylococcus aureus ATCC 29213 in a neutropenic murine thigh infection model within 24 hours[5].
References:
[1] Santos O M M, Freitas J T J, Bitencourt M, et al. Three new orbifloxacin multicomponent crystal forms towards pharmaceutical improvement[J]. Journal of Molecular Structure, 2020, 1217: 128371.
[2] D’Atanasio N, Capezzone de Joannon A, Di Sante L, et al. Antibacterial activity of novel dual bacterial DNA type II topoisomerase inhibitors[J]. PLoS One, 2020, 15(2): e0228509.
[3] Scott D W, Peters J, Miller Jr W H. Efficacy of orbifloxacin tablets for the treatment of superficial and deep pyoderma due to Staphylococcus intermedius infection in dogs[J]. The Canadian Veterinary Journal, 2006, 47(10): 999.
[4] Marín P, Fernandez‐Varon E, Escudero E, et al. Pharmacokinetic–pharmacodynamic integration of orbifloxacin in rabbits after intravenous, subcutaneous and intramuscular administration[J]. Journal of veterinary pharmacology and therapeutics, 2008, 31(1): 77-82.
[5] Zhong L G, Tang S J, Liang L Y, et al. In vivo pharmacokinetic and pharmacodynamic profiles of orbifloxacin against Staphylococcus aureus in a neutropenic murine thigh infection model[J]. BMC Veterinary Research, 2025, 21(1): 531.
Orbifloxacin是一种合成的氟喹诺酮类药物，具有广谱杀菌活性[1]。Orbifloxacin通过抑制细菌DNA旋转酶和拓扑异构酶IV，从而破坏DNA复制和细菌增殖，发挥杀菌活性[2]。Orbifloxacin可在白细胞中积聚，从而作用于细胞内细菌，并被转运至感染部位释放[3]。Orbifloxacin广泛用于治疗牛和猪的胃肠道及呼吸道感染[4]。
在体内，在嗜中性粒细胞减少小鼠大腿感染模型中，单次肌肉注射20mg/kg剂量的Orbifloxacin，可在24小时内有效抑制金黄色葡萄球菌ATCC 29213的细菌载量[5]。