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Talk:Tilidine: Difference between revisions
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{{SummarySheet}} | {{SummarySheet}} | ||
Tilidine is a synthetic [[opioid]] analgesic, | '''Tilidine''' (known under brand names including '''Valoron''', '''Valtran''', '''Tilicomp''') is a synthetic [[opioid]] analgesic. Tilidine is mainly used in some European countries such as Germany, Belgium, Luxembourg, Switzerland and also South Africa. As is the case with other opioids, it is also commonly used as a recreational drug.{{citation needed}} | ||
==Pharmacology== | |||
Tilidine itself is only a weak µ-opioid agonist. Its pharmacological activity when administered is mediated by its active major metabolite nortilidine, which is further metabolised to the also active bisnortilidine. Tilidine is therefore a prodrug. The demethylation of tilidine to nortilidine and bisnortilidine occures in the liver and is catalysed by the Cytochrome P450 family of enzymes, mainly by CYP3A4 CYP2D6 and CYP2C19. <ref>J. Weiss, E. Sawa, K.-D. Riedel, W. E. Haefeli, G. Mikus: In vitro metabolism of the opioid tilidine and interaction of tilidine and nortilidine with CYP3A4, CYP2C19, and CYP2D6. In: Naunyn-Schmiedeberg’s Arch. Pharmacol. 378, 2008, S. 275–282, doi:10.1007/s00210-008-0294-7.</ref> | |||
==Subjective effects== | ==Subjective effects== | ||