Pefloxacin

Pefloxacin (Pefloxacinium) is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC₅₀ of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC₉₀s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies^{[1][2][3][4][5][6][7][8][9]}. In Vitro:Pefloxacin inhibits 90% of strains such as Escherichia coli and Klebsiella pneumoniae at ≤0.5 mg/L, 90% of Pseudomonas aeruginosa at 4 mg/L, and 90% of the Bacteroides fragilis group at 16 mg/L^[1].
Pefloxacin (0.06-64 mg/L) shows good activity against many bacteria such as staphylococci and E. coli, but poor activity against bacteria like Gardnerella vaginalis and Mobiluncus spp.^[2].
Pefloxacin (5-60 μg/mL; 30 min) can inhibit the DNA relaxation reaction catalyzed by E. coli topoisomerase I, with an IC₅₀ of 45 μg/mL^[3].
In Vivo:Pefloxacin (cumulative total dose: 1.25-1280 mg/kg; s.c.; divided injection, every 6 h) shows a high maximal antibacterial effect (E_max) against 15 gram-negative bacilli infections in a neutropenic mouse thigh infection model, and can reduce the bacterial load in infected mice^[4].
Pefloxacin (200 mg/kg; s.c.; 2 h before and 5 h after UVA irradiation) can increase UVA-induced back skin swelling, the number of sunburn cells, reduce the number of epidermal Langerhans cells, and inhibit local contact hypersensitivity in mice^[5].
Pefloxacin (up to 150 mg/kg; p.o.; daily) is ineffective against Mycobacterium tuberculosis infection in mice^[6].
Pefloxacin (40-240 mg/kg; s.c.; every 8-12 h; 3 days) can significantly reduce parasitemia and increase the survival rate of Swiss albino mice infected with Plasmodium yoelii, with superior efficacy to Ciprofloxacin (HY-B0356)^[7].