Pharmacology Tilidine - Pharmacology and chemistry

[AlsoTapered]

In the book by Casey/parfait it was stated that the double bond is absolutely necessary for tilidines activity.

That is most likely where I read it. For a time I did wonder if the C=C bond with it's pi-bonding was part of the pharmacophore which is why I was pleased to find that later work in which a cyclopentane replaces the cyclohexene and from every study I've seen, the two compounds are equipotent. I know, it's a petty detail but I was just pleased to remove all doubt.

 

[Hexenstahl]

@izo
I assume you have tried Tilidine since you are german, so here is a question I always wanted to ask but never had the opportunity to: is there any significant difference in the quality of the high between the tabs and the oral solution? I always found the oral solution to be a tad more euphoric but that could be placebo.

Also, do you have any info on the BA of non-oral ROAs, specifically IV? I'm asking because the oral solution could technically be IVed but I haven't found any info on the BA. I assume it must be extremely low though, because I haven't seen, heard or read of anybody who ever IVed Tilis lol.

 

[someguyontheinternet]

I think bioavailability of IV is always going to be 100%

 

[izo]

I assume you have tried Tilidine since you are german, so here is a question I always wanted to ask but never had the opportunity to: is there any significant difference in the quality of the high between the tabs and the oral solution? I always found the oral solution to be a tad more euphoric but that could be placebo.

Also, do you have any info on the BA of non-oral ROAs, specifically IV? I'm asking because the oral solution could technically be IVed but I haven't found any info on the BA. I assume it must be extremely low though, because I haven't seen, heard or read of anybody who ever IVed Tilis lol.

ive had tilidine once around 2005, so it was a long time ago. it was in solution and i always thought of tilidine as a more lighter version of methadone which felt quite equal for for exept for stronger binding.
iv consumption of tilidine would be senseless i think as it has to be converted to nortilidine which is the active principle and this has to happen in the liver. what always puzzled me was valeron n to which naloxone was added to prevent iv consumption but this doesnt make sense as it isnt active iv.

 

[Hexenstahl]

ive had tilidine once around 2005, so it was a long time ago. it was in solution and i always thought of tilidine as a more lighter version of methadone which felt quite equal for for exept for stronger binding.
iv consumption of tilidine would be senseless i think as it has to be converted to nortilidine which is the active principle and this has to happen in the liver. what always puzzled me was valeron n to which naloxone was added to prevent iv consumption but this doesnt make sense as it isnt active iv.

Oh right, Tilidine is a PRODRUG. Stupid me forgot my own info I wrote in the thread LOL

Thanks anyway

 

[Hexenstahl]

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

To investigate in vivo the effect of the CYP2C19 genotype on the pharmacokinetics of tilidine and the contribution of CYP3A4 and CYP2C19 to the formation of nortilidine using potent CYP3A4 inhibition by ritonavir.Fourteen healthy volunteers (seven CYP2C19 ...

www.ncbi.nlm.nih.gov

Found an interesting paper explaining the formation of the active metabolite nortilidine from tilidine.