Publication: PHARMACOKINETICS OF DEFLAZACORT IN RABBITS AFTER INTRAVENOUS AND ORAL ADMINISTRATION AND ITS INTERACTION WITH ERYTHROMYCIN
Authors
Escudero, Ana I. ; Marín, Pedro ; Cárceles Rodríguez, Carlos ; Escudero, Elisa
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DOI
10.1111/jvp.12442
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info:eu-repo/semantics/article
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Abstract
The pharmacokinetic of deflazacort after intravenous and oral administration and the effect of erythromycin on the disposition of deflazacort in rabbits were investigated. A parallel study was carried out in twelve rabbits. The plasma concentration-time profiles of deflazacort were determined after intravenous and oral administration of single dosages of 5 mg/kg in the presence and absence (baseline) of multiple dose erythromycin regimens. Plasma levels of 21-desacetyldeflazacort were determined by HPLC. Plasma concentration-time curves were analysed by compartmental pharmacokinetic and non-compartmental methods.
The t½z values following intravenous and oral administration were 3.67 and 4.96 h, respectively. The apparent volume of distribution at steady state (Vss) was 4.08 ± 0.31 L/kg, this value indicates that deflazacort is widely distributed into the extravascular tissues. Moreover, bioavailability after oral administration of deflazacort (F = 87.48 %) was high.
Pharmacokinetic analysis after both routes of administration revealed a significant reduction in total body clearance, a significant increase in mean residence time, half-life and plasma concentrations of the steroid in the presence of multiple dose erythromycin. The results indicated the influence of the erythromycin on deflazacort disposition, which is consistent with a pharmacokinetic-type interaction in the elimination of the drug from the body. Moreover this interaction should be considered to avoid adverse effects when using both drugs concomitantly.
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