Pharmacokinetics and safety of trovafloxacin (CP-99, 219), a new quinolone antibiotic, following adminstration of single oral doses to healthy male volunteers

Renli Teng, Stephen C. Harris, David E. Nix, Jerome J. Schentag, George Foulds, Theodore E. Liston

Research output: Contribution to journalArticle

86 Scopus citations

Abstract

Trovafloxacin (CP-99, 219) is a new fluoroquinolone antibacterial agent with a broad spectrum of activity against Gram-positive and Gram-negative bacteria. The pharmacokinetics and safety of trovafloxacin were characterised in healthy male volunteers after administration of single oral doses of 30, 100, 300, 600 and 1000 mg. trovafloxacin was rapidly absorbed and serum concentrations reached a maximum approximately 1 h after dosing. The corresponding mean Cmax values (mean ± SD) were 0.3 ± 0.0, 1.5 ± 0.5, 4.4 ± 11, 6.6 ± 1.4 and 10.1 ± 0.5 mg/L. Terminal-phase half-life was independent of dose, with an overall mean of 9.9 ± 2.5 h. Generally, Cmax and AUC0∞ increased linearly with dose. Less than 10% of the administered dose was recovered unchanged in urine. Over the dosing range, trovafloxacin renal clearance was fairly constant, averaging 0.67 ± 0.36 L/h. Trovafloxacin binding to serum proteins was moderate (70%). Trovafloxacin was well tolerated at doses of 300 mg or below. There were no significant changes in the clinical chemistry or haematology parameters evaluated over the entire dosing range.

Original languageEnglish (US)
Pages (from-to)385-394
Number of pages10
JournalJournal of Antimicrobial Chemotherapy
Volume36
Issue number2
DOIs
StatePublished - Aug 1 1995
Externally publishedYes

ASJC Scopus subject areas

  • Pharmacology
  • Microbiology (medical)
  • Infectious Diseases
  • Pharmacology (medical)

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