Pharmacokinetics and penetration into inflammatory fluid of trovafloxacin (CP-99,219).
A single 200-mg oral dose of trovafloxacin (CP-99,219) was given to each of eight healthy male volunteers, and the concentrations of the drug were measured in plasma, cantharides-induced inflammatory fluid, and urine over the subsequent 36 h. The mean maximum concentration observed in plasma was 2.9 micrograms/ml at a mean time of 0.75 h postdose. The mean maximum concentration observed in inflammatory fluid was 1.2 micrograms/ml at 4.0 h postdose. The mean elimination half-life in plasma was 7.8 h. The overall penetration into inflammatory fluid was 64%, as assessed by determining the ratio of the area under the concentration-time curves. Recovery of the dose in urine within the first 36 h postdose was 5.0% of the administered dose. Our results indicate that trovafloxacin, at a dosage of 200 mg once or twice daily, should be adequate for the treatment of systemic infections caused by most common bacterial pathogens.
Wise
R
R
Department of Medical Microbiology, City Hospital National Health Service Trust, Birmingham, United Kingdom.
Mortiboy
D
D
Child
J
J
Andrews
J M
JM
D000293:Adolescent; D000328:Adult; D000890:Anti-Infective Agents / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D001768:Blister / Q000139:chemically induced / Q000188:drug therapy / Q000378:metabolism*; D004334:Drug Administration Schedule; D005122:Exudates and Transudates / Q000378:metabolism; D024841:Fluoroquinolones; D006207:Half-Life; D006801:Humans; D008297:Male; D009287:Naphthyridines / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine
D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D009287:Naphthyridines; C080163:trovafloxacin