Interaction of rocuronium with human liver cytochromes P450

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15110%2F15%3A33154985" target="_blank" >RIV/61989592:15110/15:33154985 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/00098892:_____/15:#0000937

Výsledek na webu

<a href="http://www.sciencedirect.com/science/article/pii/S1347861314000279" target="_blank" >http://www.sciencedirect.com/science/article/pii/S1347861314000279</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.jphs.2014.12.006" target="_blank" >10.1016/j.jphs.2014.12.006</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Interaction of rocuronium with human liver cytochromes P450

Popis výsledku v původním jazyce

Rocuronium is a neuromuscular blocking agent acting as a competitive antagonist of acetylcholine. Results of an inhibition of eight individual liver microsomal cytochromes P450 (CYP) are presented. As the patients are routinely premedicated with diazepam, possible interaction of diazepam with rocuronium has been also studied. Results indicated that rocuronium interacts with human liver microsomal CYPs by binding to the substrate site. Next, concentration dependent inhibition of liver microsomal CYP3A4 down to 42% (at rocuronium concentration 189 ?M) was found. This effect has been confirmed with two CYP3A4 substrates, testosterone (formation of 6?-hydroxytestosterone) and diazepam (temazepam formation). CYP2C9 and CYP2C19 activities were inhibited downto 75-80% (at the same rocuronium concentration). Activities of other microsomal CYPs have not been inhibited by rocuronium. To prove the possibility of rocuronium interaction with other drugs (diazepam), the effect of rocuronium on form

Název v anglickém jazyce

Interaction of rocuronium with human liver cytochromes P450

Popis výsledku anglicky

Rocuronium is a neuromuscular blocking agent acting as a competitive antagonist of acetylcholine. Results of an inhibition of eight individual liver microsomal cytochromes P450 (CYP) are presented. As the patients are routinely premedicated with diazepam, possible interaction of diazepam with rocuronium has been also studied. Results indicated that rocuronium interacts with human liver microsomal CYPs by binding to the substrate site. Next, concentration dependent inhibition of liver microsomal CYP3A4 down to 42% (at rocuronium concentration 189 ?M) was found. This effect has been confirmed with two CYP3A4 substrates, testosterone (formation of 6?-hydroxytestosterone) and diazepam (temazepam formation). CYP2C9 and CYP2C19 activities were inhibited downto 75-80% (at the same rocuronium concentration). Activities of other microsomal CYPs have not been inhibited by rocuronium. To prove the possibility of rocuronium interaction with other drugs (diazepam), the effect of rocuronium on form

Druh

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

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

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Projekt

<a href="/cs/project/NT13591" target="_blank" >NT13591: Primární kultury lidských hepatocytů jako model pro toxikologické, farmakologické a biochemické studie v transplantační medicíně</a><br>

Návaznosti

S - Specificky vyzkum na vysokych skolach

Rok uplatnění

2015

Kód důvěrnosti údajů

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

Název periodika

Journal of Pharmacological Sciences

ISSN

1347-8613

e-ISSN

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Svazek periodika

127

Číslo periodika v rámci svazku

2

Stát vydavatele periodika

JP - Japonsko

Počet stran výsledku

6

Strana od-do

190-195

Kód UT WoS článku

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EID výsledku v databázi Scopus

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