Interaction of rocuronium with human liver cytochromes P450

Result code in 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>

Alternative codes found

RIV/00098892:_____/15:#0000937

Result on the web

<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>

Result language

angličtina

Original language name

Interaction of rocuronium with human liver cytochromes P450

Original language description

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

Czech name

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Czech description

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Type

J_x - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

CEP classification

FR - Pharmacology and apothecary chemistry

OECD FORD branch

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Project

<a href="/en/project/NT13591" target="_blank" >NT13591: Primary cultures of human hepatocytes as a model for toxicological, pharmacological and biochemical studies in transplantation medicine.</a><br>

Continuities

S - Specificky vyzkum na vysokych skolach

Publication year

2015

Confidentiality

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

Name of the periodical

Journal of Pharmacological Sciences

ISSN

1347-8613

e-ISSN

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Volume of the periodical

127

Issue of the periodical within the volume

2

Country of publishing house

JP - JAPAN

Number of pages

6

Pages from-to

190-195

UT code for WoS article

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EID of the result in the Scopus database

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