Temafloxacin (hydrochloride) (Synonyms: A-62254)

MIC90: less than or equal to 0.06 micrograms/mL respiratory pathogens

Temafloxacin is a fluoroquinolone antibiotic.

Fluoroquinolone antibiotic is an organonitrogen heterocyclic antibiotic with a quinolone or quinolone-like moiety and have a fluorine atom attached to the central ring system.

In vitro: The in-vitro activities of temafloxacin, ciprofloxacin, and ofloxacin against gram-negative bacteria were compared. The 90% minimal inhibitory concentrations (MIC90s) of temafloxacin for respiratory pathogens were less than or equal to 0.06 micrograms/mL. Temafloxacin was also active against bacterial agents of sexually transmitted diseases, such as Neisseria gonorrhoeae and Chlamydia trachomatis [1].

In vivo: Mixed aerobic-anaerobic infection was induced by i.p. implantation of gelatin capsules containing Bacteroides fragilis, Escherichia coli, and sterile rat faeces. Temafloxacin was found to be highly active with a 90.9% cure rate in comparison with no treatment, and as active as a combination of clindamycin and gentamicin. Temafloxacin at 12 mg/dose resulted in rise to serum concentrations exceeding the MIC values of both microorganisms for at least 8 h [2].

Clinical trial: Clinical studies showed that temafloxacin has improved activity against pneumococci. Eradication rates in acute exacerbations of chronic bronchitis collated from individual studies are 98% overall and 100% in pneumococcal infections. Moreover, eradication rates in smokers and the elderly illustrate significant advantages for temafloxacin. In pneumonia, a twice-daily temafloxacin regimen has given equivalent overall results to those of amoxycillin (84.6% vs 80%) [3].

References:
[1] Hardy DJ.  In vitro activity of temafloxacin against gram-negative bacteria: an overview. Am J Med. 1991 Dec 30;91(6A):19S-23S.
[2] Thadepalli H, Hajji M, Perumal VK, Chuah SK, Gollapudi S.  Evaluation of temafloxacin in a rat model of intra-abdominal abscess. J Antimicrob Chemother. 1992 Jun;29(6):687-92.
[3] Ball P. The role of temafloxacin in the community setting: an overview. J Antimicrob Chemother. 1991 Dec;28 Suppl C:121-30.