title: [Pharmacological properties and expected clinical role of an injectable new quinolone antibiotic, pazufloxacin mesilate].
abstract: Pazufloxacin mesilate (PZFX: Pasil INJECTION, Pazucross INJECTION) is a novel injectable quinolone antibiotic that was discovered by Toyama Chemical Co., Ltd. and codeveloped by Toyama Chemical Co. Ltd. and Mitsubishi Pharma Corporation. Laboratory studies indicated that PZFX reached high plasma levels quickly after intravenous administration, and it exhibited weak convulsion inducing activity, low local irritant effect, and less hypotensive activity, all of which are generally recognized as side effects associated with other injectable quinolones. PZFX has potent antibacterial and bactericidal activities against cephalosporin-, carbapenem-, and aminoglycoside-resistant strains. These favorable antibacterial and bactericidal activities gave PZFX superior therapeutic effects, compared to injectable cephalosporin antibiotics, on experimental animal infection models caused by those resistant strains. Clinical studies also revealed PZFX was as safe and effective as the injectable cephalosporin, ceftazidime, against various moderate to severe infections. Furthermore, PZFX showed good clinical effects on the infections resistant to chemotherapy by the other antimicrobial agents. These results indicate that PZFX is a viable choice for various bacterial infections. In this review, results of laboratory and clinical studies are summarized and the clinical role of PZFX among the injectable antimicrobials is discussed.
authors.affiliation: Research Laboratories, Toyama Chemical Co. Ltd., Japan.
authors.forename: Shinzaburo
authors.initials: S
authors.lastname: Minami
authors.forename: Rikizou
authors.initials: R
authors.lastname: Hattori
authors.forename: Akira
authors.initials: A
authors.lastname: Matsuda
mesh_terms: D042462:4-Quinolones; D000818:Animals; D000890:Anti-Infective Agents / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D001419:Bacteria / Q000187:drug effects*; D001424:Bacterial Infections / Q000188:drug therapy*; D002199:Capillary Permeability / Q000187:drug effects; D027081:DNA Gyrase / Q000187:drug effects; D004261:DNA Replication / Q000187:drug effects; D004269:DNA, Bacterial; D024881:Drug Resistance, Bacterial; D024841:Fluoroquinolones; D006439:Hemodynamics / Q000187:drug effects; D006636:Histamine Release / Q000187:drug effects; D006801:Humans; D007262:Infusions, Intravenous; D010078:Oxazines / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D012640:Seizures / Q000139:chemically induced
chemical_list: D042462:4-Quinolones; D000890:Anti-Infective Agents; D004269:DNA, Bacterial; D024841:Fluoroquinolones; D010078:Oxazines; C078052:pazufloxacin; D027081:DNA Gyrase