Single- and multiple-dose pharmacokinetics of oral moxifloxacin and clarithromycin, and concentrations in serum, saliva and faeces.

Publisher: Informa Healthcare Country of Publication: England NLM ID: 0215333 Publication Model: Print Cited Medium: Print ISSN: 0036-5548 (Print) Linking ISSN: 00365548 NLM ISO Abbreviation: Scand J Infect Dis Subsets: MEDLINE

Publication: 2007-2014 : London : Informa Healthcare
Original Publication: Stockholm, Society for the Publication of Acta medica Scandinavica.

Aza Compounds* ; Fluoroquinolones* ; Quinolines*; Anti-Infective Agents/*pharmacokinetics ; Clarithromycin/*analogs & derivatives ; Clarithromycin/*pharmacokinetics ; Feces/*chemistry ; Saliva/*metabolism; Administration, Oral ; Adult ; Anti-Infective Agents/administration & dosage ; Anti-Infective Agents/blood ; Clarithromycin/administration & dosage ; Clarithromycin/blood ; Cross-Over Studies ; Dose-Response Relationship, Drug ; Double-Blind Method ; Drug Administration Schedule ; Drug Tolerance ; Feces/microbiology ; Half-Life ; Humans ; Intestines/drug effects ; Intestines/microbiology ; Male ; Metabolic Clearance Rate ; Moxifloxacin ; Oropharynx/drug effects ; Oropharynx/microbiology ; Saliva/microbiology

Moxifloxacin and clarithromycin are important antibacterial drugs in the treatment of community-acquired respiratory tract infections. In a double-blind, randomized, 2-period cross-over study the pharmacokinetics of moxifloxacin versus clarithromycin were determined after single and multiple doses in 12 healthy male volunteers. The concentrations of the antibiotics in serum, saliva and faeces were measured by validated high-performance liquid chromatographic methods. In serum, moxifloxacin exhibited a mean peak concentration of 3.1 +/- 0.6 mg/l after a time to peak concentration of 1.67 +/- 0.96 h on day 1, with a significant increase to 3.98 +/- 1.10 mg/l on day 7 (p < 0.05). The area under the curve-12 revealed a highly significant increase from 28.2 + 4.1 mg*h/l on day 1 to 39.5 +/- 6.6 mg*h/l on day 7 (p < 0.01). There were also significant differences in terminal half-life between day 1 and day 7 [10.6 h (range 9.0-12.8) vs 14.9 h (range 12.6-28.1); p < 0.01] and in mean residence time (15.1 +/- 1.9 vs 18.2 +/- 2.4 h; p < 0.01). The concentrations of moxifloxacin in saliva were well equilibrated with serum at a relatively constant saliva-serum ratio of about 0.8. Pharmacokinetic parameters of clarithromycin and its metabolite, 14-hydroxy-clarithromycin, were similar to previously published data. Accumulation was found. No serious adverse events were observed with either study drug.

0 (Anti-Infective Agents)
0 (Aza Compounds)
0 (Fluoroquinolones)
0 (Quinolines)
110671-78-8 (14-hydroxyclarithromycin)
H1250JIK0A (Clarithromycin)
U188XYD42P (Moxifloxacin)

Date Created: 20030218 Date Completed: 20030331 Latest Revision: 20190826

20231215

10.1080/0036554021000026963

12587622