Title: Pefloxacin
CAS Registry Number: 70458-92-3
CAS Name: 1-Ethyl-6-fluoro-1,4-dihydro-7-(4-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid
Additional Names: pefloxacine
Manufacturers' Codes: EU-5306; 1589RB; AM-725
Molecular Formula: C17H20FN3O3
Molecular Weight: 333.36
Percent Composition: C 61.25%, H 6.05%, F 5.70%, N 12.61%, O 14.40%
Literature References: Fluorinated quinolone antibacterial; analog of norfloxacin, q.v. Prepn: M. Pesson, DE 2840910; idem, US 4292317 (1979, 1981 to Roger Bellon/Dainippon). Pharmacology and antibacterial spectrum: Y. Goueffon et al., C.R. Seances Acad. Sci. Ser. 3 292, 37 (1981). Pharmacokinetics: J. Barre et al., J. Pharm. Sci. 73, 1379 (1984). Bioavailability and metabolism: A. Contrepois et al., J. Antimicrob. Chemother. 14, 51 (1984); G. Montay et al., Antimicrob. Agents Chemother. 25, 463 (1984). HPLC determn in urine and plasma: eidem, J. Chromatogr. 272, 359 (1983). Adsorptive stripping voltammetry determn in bulk form, tablets and serum: A. M. Beltagi, J. Pharm. Biomed. Anal. 31, 1079 (2003). Symposium on pharmacokinetics, clinical efficacy and safety: J. Antimicrob. Chemother. 26, Suppl. B, 1-229 (1990).
Properties: Crystals from DMF, mp 270-272° (dec). Slightly sol in water; sol in alkaline and acidic solutions. LD50 in mice (mg/kg): 225 i.v., 1000 orally; in rats (g/kg): 1.5 i.p., 2.5 orally (Goueffon).
Melting point: mp 270-272° (dec)
Toxicity data: LD50 in mice (mg/kg): 225 i.v., 1000 orally; in rats (g/kg): 1.5 i.p., 2.5 orally (Goueffon)
Derivative Type: Methanesulfonate dihydrate
CAS Registry Number: 149676-40-4; 70458-95-6 (methanesulfonate)
Additional Names: Pefloxacin mesylate
Manufacturers' Codes: 1589mRB
Trademarks: Peflacine (Bellon); Peflox (Formenti)
Molecular Formula: C17H20FN3O3.CH3SO3H.2H2O
Molecular Weight: 465.49
Percent Composition: C 46.44%, H 6.06%, F 4.08%, N 9.03%, O 27.50%, S 6.89%
Therap-Cat: Antibacterial.
Keywords: Antibacterial (Synthetic); Quinolones and Analogs.

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