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Clinical Trial
. 1999 May;43(5):1152-5.
doi: 10.1128/AAC.43.5.1152.

Lack of effect of zafirlukast on the pharmacokinetics of azithromycin, clarithromycin, and 14-hydroxyclarithromycin in healthy volunteers

K W Garey  1 , C A Peloquin, P G Godo, A N Nafziger, G W Amsden
Affiliations
Clinical Trial

Lack of effect of zafirlukast on the pharmacokinetics of azithromycin, clarithromycin, and 14-hydroxyclarithromycin in healthy volunteers

K W Garey et al. Antimicrob Agents Chemother. 1999 May.

Abstract

This randomized, open-label, crossover study was conducted to investigate whether the coadministration of zafirlukast would affect the pharmacokinetics of azithromycin, clarithromycin, or 14-hydroxyclarithromycin (14-OHC). Twelve healthy subjects (six males and six females) received single 500-mg doses of azithromycin and clarithromycin with and without zafirlukast given to a steady-state concentration. Blood was collected prior to all macrolide doses and for 3 and 10 days after each clarithromycin and azithromycin dose, respectively. Serum was assayed for azithromycin, clarithromycin, and 14-OHC concentrations by validated high-performance liquid chromatography assay systems. Data analyses were done by noncompartmental and nonparametric methods. Analysis of the patients indicated that the addition of steady-state concentrations of zafirlukast did not significantly alter the pharmacokinetic parameters of or overall exposure (based on the area under the concentration-time curve) to azithromycin, clarithromycin, and 14-OHC. While zafirlukast is a known inhibitor of CYP3A4, it does not appear to exert a clinically or statistically significant pharmacokinetic effect on azithromycin, clarithromycin, or 14-OHC.

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Figures

FIG. 1
FIG. 1
Individual azithromycin AUCT values during both the control (azithromycin [AZ]) and test (AZ plus zafirlukast [ZAF]) phases.
FIG. 2
FIG. 2
Individual clarithromycin AUC∞ values during both the control (clarithromycin [CL]) and test (CL plus zafirlukast [ZAF]) phases.
FIG. 3
FIG. 3
Individual 14-OHC AUC∞ values during both the control (14-OHC) and test (14-OHC plus zafirlukast [ZAF]) phases.
See this image and copyright information in PMC

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