Journal of Antimicrobial Chemotherapy, Vol 39, 75-80, Copyright © 1997 by The British Society for Antimicrobial Chemotherapy
J Vincent, J Venitz, R Teng, BA Baris, SA Willavize, RJ Polzer and HL Friedman
Fifteen healthy male volunteers (in four groups) received single 1 h i.v.
infusions of alatrofloxacin (CP-116,517) equivalent to 30, 100, 200 or 300
mg of its active metabolite, trovafloxacin (CP-99,219). Blood and urine
were sampled over 73 and 72 h, respectively, and plasma levels of
alatrofloxacin and serum concentrations of trovafloxacin were determined by
HPLC with UV detection. Alatrofloxacin was not detectable in plasma samples
collected after the end of infusion, indicating rapid conversion to
trovafloxacin. Maximum serum concentrations of trovafloxacin were achieved
at the end of the infusions. Mean maximum plasma trovafloxacin
concentrations for the four alatrofloxacin doses were 0.4, 1.8, 2.3 and 4.3
mg/L. The mean area under the concentration- time curve increased
proportionally with the dose. The elimination half- life (T(1/2)) for
trovafloxacin was independent of the dose and the mean T(1/2)s for the 100,
200 and 300 mg equivalent doses of alatrofloxacin were 10.4, 12.3 and 10.8
h. Approximately 10% of the equivalent dose was recovered as unchanged
trovafloxacin in the urine. No clinical adverse or laboratory reactions
were associated with i.v. administration of alatrofloxacin and its
conversion to trovafloxacin. These results indicate that alatrofloxacin is
rapidly converted to trovafloxacin and that the pharmacokinetic parameters
for this new fluoroquinolone after i.v. administration of its parent
compound are similar to those reported after oral administration of
equivalent trovafloxacin doses.
ORIGINAL ARTICLES
Pharmacokinetics and safety of trovafloxacin in healthy male volunteers following administration of single intravenous doses of the prodrug, alatrofloxacin
Central Research Division, Pfizer Inc., Groton, CT 06340, USA.
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