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Article

Contribution of CYP2C19 and CYP3A4 to the formation of the active nortilidine from the prodrug tilidine.

British journal of clinical pharmacology - 1 Nov 2012

Grün Barbara, Merkel Ulrike, Riedel Klaus-Dieter, Weiss Johanna, Mikus Gerd

Abstract excerpt

WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT: The analgesic activity of tilidine is mediated by its active metabolite, nortilidine, which easily penetrates the blood-brain barrier and binds to the µ-opioid receptor as a potent agonist. Tilidine undergoes an extensive first-pass metabolism, which has been suggested to be mediated by CYP3A4 and CYP2C19; furthermore, strong inhibition of CYP3A4 and CYP2C19 by...

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Identifiers

PMID: 22381043
DOI: 10.1111/j.1365-2125.2012.04261.x
PMCID: PMC3495150

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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