Pharmacokinetics of flumequine and in vitro activity against bacterial pathogens of gilthead sea bream Sparus aurata

Diseases of Aquatic Organisms

Gera M. Troisi¹  Maria Alexis¹  Maria Koutsodimou¹  Ioannis Nengas¹  Athanassios E. Tyrpenou¹  Maria Yiagnisis¹  George Rigos¹ 

关键词: Flumequine;    Gilthead sea bream;    Pharmacokinetics;    Bioavailability;    Minimum inhibitory concentration;    Mediterranean mariculture;   

DOI  :  10.3354/dao054035

学科分类：生物科学（综合）

来源: Inter-Research

【 摘 要 】

ABSTRACT: The present study investigated the kinetic profile of flumequine (FLU) in gilthead sea bream Sparus aurata (170 g) held at 19°C and evaluated its in vitro efficacy against important bacterial diseases in Mediterranean mariculture.Following a single intravascular injection (10 mg kg^-1 fish), the distribution half-life (t_x1/2α) and the half-life of the terminal phase of elimination (t_1/2γ) of the drug were 0.2 and 30 h respectively. Tissue penetration of FLU was low, since both the apparent distribution volume of the drug at steady-state (V_d(ss)) and the apparent volume of the centralcompartment (V_c) were small (0.57 and 0.15 l kg^-1). The mean residence time (MRT) was short (11 h) and the total clearance (CL_T) of the drug was slow (0.05 l kg^-1 h^-1). Following oraladministration (20 mg kg¹), the bioavailability (F %) of FLU was 29% and the maximum plasma concentration was 1.7 µg ml^-1. The minimum inhibitory concentration (MIC) of the drug in distilled water supplemented with 2% NaClagainst Vibrio anguillarum Serotype 1b, Photobacterium damsela ssp. piscicida, V. alginolyticus, V. damsela and V. fluvialis was 0.15, 0.3, 1.2, 0.019 and 0.15 µg ml^-1 respectively. The addition however of 10mM Ca²⁺ and 55 mM Mg²⁺ to the medium resulted in an 8- to >120-fold reduction in FLU activity. The results indicate that FLU has an adequate kinetic profile in gilthead sea bream and that marine cations induce a significant impacton the activity of FLU, rendering its use against bacterial pathogens questionable.

【 授权许可】

Unknown