title: [Therapeutic potential of sparfloxacin for preventing mycobacterial infections].
abstract: We studied the therapeutic potential of utilizing sparfloxacin (SPFX), a newly developed quinolone, to prevent various mycobacterial infections. The in vitro activity of SPFX as a preventive agent for various mycobacteria was determined using the actual count method on Ogawa egg medium. The minimal inhibitory concentrations (MICs) of SPFX were as follows: ofloxacin-sensitive M. tuberculosis, 0.16-0.32 microgram/ml; ofloxacin-resistant M. tuberculosis, 0.63-2.5 micrograms/ml; M. avium; 0.63-10 micrograms/ml (MICs were equal or less than 1.25 micrograms/ml in seven out of 11 strains); M. intracellulare, 2.5-10 micrograms/ml (MICs were equal or more than 10 micrograms/ml in 17 out of 23 strains); M. kansasii, < or = 0.08-0.16 microgram/ml; M. fortuitum, < or = 0.08 microgram/ml; M. chelonae subsp. abscessus, > 10 micrograms/ml; M. chelonae subsp. chelonae, 0.63 microgram/ml; M. scrofulaceum, < or = 0.08 microgram/ml; M. nonchromogenicum, 1.25 micrograms/ml; M. xenopi, < or = 0.08 microgram/ml; M. gordonae, < or = 0.08 microgram/ml. The average serum concentrations of SPFX during the period of multiple oral administration (200 mg once a day) were 0.35 +/- 0.16 microgram/ml before administration, 0.67 +/- 0.32 microgram/ml after one hour, 1.13 +/- 0.21 microgram/ml after two hours, 1.27 +/- 0.32 microgram/ml after four hours and 1.31 +/- 0.34 micrograms/ml after six hours. These results indicate that SPFX has a strong therapeutic potential to prevent infections due to M. tuberculosis, M. kansasii, M. fortuitum, M. chelonae subsp. chelonae, M. scrofulaceum, M. xenopi and M. gordonae. Moreover, it may be expected to be a promising agent against infections due to ofloxacin-resistant M. tuberculosis, M. avium and M. nonchromogenicum.
authors.affiliation: Department of Internal Medicine, National Sanatorium Minami Okayama Hospital, Japan.
authors.forename: S
authors.initials: S
authors.lastname: Kawahara
authors.forename: A
authors.initials: A
authors.lastname: Tada
authors.forename: M
authors.initials: M
authors.lastname: Takeuchi
authors.forename: K
authors.initials: K
authors.lastname: Kamisaka
authors.forename: C
authors.initials: C
authors.lastname: Okada
authors.forename: Y
authors.initials: Y
authors.lastname: Mishima
authors.forename: R
authors.initials: R
authors.lastname: Soda
authors.forename: K
authors.initials: K
authors.lastname: Takahashi
authors.forename: M
authors.initials: M
authors.lastname: Kibata
authors.forename: H
authors.initials: H
authors.lastname: Nagare
mesh_terms: D000890:Anti-Infective Agents / Q000493:pharmacokinetics / Q000494:pharmacology*; D000995:Antitubercular Agents / Q000493:pharmacokinetics / Q000494:pharmacology*; D024841:Fluoroquinolones; D006801:Humans; D008826:Microbial Sensitivity Tests; D009164:Mycobacterium Infections / Q000517:prevention & control*; D015363:Quinolones / Q000493:pharmacokinetics / Q000494:pharmacology*
chemical_list: D000890:Anti-Infective Agents; D000995:Antitubercular Agents; D024841:Fluoroquinolones; D015363:Quinolones; C061363:sparfloxacin