Pazufloxacin Mesylate (T-3761), a new quinolone derivative, showed broad and potent antibacterial activity. Its MICs for 90% of the strains tested were 0.20 to 100 micrograms/ml against gram-positive bacteria, including members of the genera Staphylococcus, Streptococcus, and Enterococcus; 0.025 to 3.13 micrograms/ml against gram-negative bacteria, including members of the family Enterobacteriaceae and the genus Haemophilus; 0.05 to 50 micrograms/ml against glucose nonfermenters, including members of the genera Pseudomonas, Xanthomonas, Acinetobacter, Alcaligenes, and Moraxella; 0.025 micrograms/ml against Legionella spp.; and 6.25 to 25 micrograms/ml against anaerobes, including Bacteroides fragilis, Clostridium difficile, and Peptostreptococcus spp[3]. The 50% inhibitory concentrations of T-3761 for DNA gyrases isolated from E. coli and P. aeruginosa were 0.88 and 1.9 micrograms/ml, respectively[4]. All regimens of pazufloxacin administration were well tolerated. Pazufloxacin exhibits lack of dose proportionality over the dose range of 300 - 1,000 mg[5]. Pazufloxacin methanesulphonate at the dose of 300 mg and 500 mg have similar efficacy in treating acute bacterial infections. The dosage regimen of 300 mg Q12h intravenous infusion is recommended[6].
Pazufloxacin Mesylate/甲磺酸帕珠沙星 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Pseudomonas aeruginosa ATCC 27853
0.12, 0.25, 0.5, 0.75, or 1 µg/mL
16–20 h
To determine the minimum inhibitory concentration (MIC) of Pazufloxacin against Pseudomonas aeruginosa
Antibiotics (Basel). 2022 Jul 21;11(7):982.
E. coli UTI89
50 μM
7 days
Evaluate the killing effect of Pazufloxacin on E. coli UTI89 persisters, results showed complete eradication of persisters after 7 days of drug exposure
Antibiotics (Basel). 2015 May 12;4(2):179-87.
Pazufloxacin Mesylate/甲磺酸帕珠沙星 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Neutropenic thigh infection model
Subcutaneous injection
2.5, 10, and 40 mg/kg
Single dose
To evaluate the in vivo pharmacokinetic/pharmacodynamic (PK/PD) parameters of Pazufloxacin against Pseudomonas aeruginosa infection
Antibiotics (Basel). 2022 Jul 21;11(7):982.
Soviet Chinchilla rabbits
Healthy adult male rabbits
Oral
10 mg/kg
Every 12 hours for 21 days
To evaluate the effect of pazufloxacin and meloxicam on antioxidant status and oxidative stress in rabbits. Results showed that pazufloxacin and meloxicam, either alone or in combination, caused significant lipid peroxidation and alterations in antioxidant parameters.
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