Bioconcentration, metabolism and half-life time of the human therapeutic drug diltiazem in rainbow trout Oncorhynchus mykiss

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60076658%3A12520%2F16%3A43890367" target="_blank" >RIV/60076658:12520/16:43890367 - isvavai.cz</a>

Výsledek na webu

<a href="http://www.sciencedirect.com/science/article/pii/S0045653515300394" target="_blank" >http://www.sciencedirect.com/science/article/pii/S0045653515300394</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.chemosphere.2015.08.038" target="_blank" >10.1016/j.chemosphere.2015.08.038</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Bioconcentration, metabolism and half-life time of the human therapeutic drug diltiazem in rainbow trout Oncorhynchus mykiss

Popis výsledku v původním jazyce

Diltiazem is a human therapeutic drug and a member of the group of calcium channel blockers having widespread use in the treatment of angina pectoris and hypertension. The objective of the present study was to assess the bioconcentration, metabolism, and half-life time of diltiazem in rainbow trout Oncorhynchus mykiss. juvenile trout were exposed for 21 and 42 days to three nominal concentrations of diltiazem: 0.03 mu g L-1 (environmentally relevant concentration), 3 mu g L-1, and 30 mu g L-1 (sub-lethal concentrations). The bioconcentration factor (BCF) of diltiazem was relatively low (0.5-194) in analysed tissues, following the order kidney > liver > muscle > blood plasma. The half-life Of diltiazem in liver, kidney, and muscle was 1.5 h, 6.2 h, and 49 h, respectively. The rate of metabolism for diltiazem in liver, kidney, muscle, and blood plasma was estimated to be 85 +/- 9%, 64 +/- 14%, 46 +/- 6%, and 41 +/- 8%, respectively. Eight diltiazem metabolites were detected. The presence of desmethyl diltiazem (M1), desacetyl diltiazem (M2), and desacetyl desmethyl diltiazem (M3) suggests that rainbow trout metabolize diltiazem mainly via desmethylation and desacetylation, similar to mammals. In addition, diltiazem undergoes hydroxylation in fish. At environmentally relevant concentrations, diltiazem and its metabolites were identified in liver and kidney, indicating the potential for uptake and metabolism in non-target organisms in the aquatic environment.

Název v anglickém jazyce

Bioconcentration, metabolism and half-life time of the human therapeutic drug diltiazem in rainbow trout Oncorhynchus mykiss

Popis výsledku anglicky

Diltiazem is a human therapeutic drug and a member of the group of calcium channel blockers having widespread use in the treatment of angina pectoris and hypertension. The objective of the present study was to assess the bioconcentration, metabolism, and half-life time of diltiazem in rainbow trout Oncorhynchus mykiss. juvenile trout were exposed for 21 and 42 days to three nominal concentrations of diltiazem: 0.03 mu g L-1 (environmentally relevant concentration), 3 mu g L-1, and 30 mu g L-1 (sub-lethal concentrations). The bioconcentration factor (BCF) of diltiazem was relatively low (0.5-194) in analysed tissues, following the order kidney > liver > muscle > blood plasma. The half-life Of diltiazem in liver, kidney, and muscle was 1.5 h, 6.2 h, and 49 h, respectively. The rate of metabolism for diltiazem in liver, kidney, muscle, and blood plasma was estimated to be 85 +/- 9%, 64 +/- 14%, 46 +/- 6%, and 41 +/- 8%, respectively. Eight diltiazem metabolites were detected. The presence of desmethyl diltiazem (M1), desacetyl diltiazem (M2), and desacetyl desmethyl diltiazem (M3) suggests that rainbow trout metabolize diltiazem mainly via desmethylation and desacetylation, similar to mammals. In addition, diltiazem undergoes hydroxylation in fish. At environmentally relevant concentrations, diltiazem and its metabolites were identified in liver and kidney, indicating the potential for uptake and metabolism in non-target organisms in the aquatic environment.

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

DN - Vliv životního prostředí na zdraví

OECD FORD obor

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Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Rok uplatnění

2016

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Chemosphere

ISSN

0045-6535

e-ISSN

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Svazek periodika

144

Číslo periodika v rámci svazku

Neuveden

Stát vydavatele periodika

GB - Spojené království Velké Británie a Severního Irska

Počet stran výsledku

6

Strana od-do

154-159

Kód UT WoS článku

000367774400021

EID výsledku v databázi Scopus

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