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What is the likely half-life of flubromidazolam?

D

donjel

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Sep 23, 2015
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I've checked the boards and got nada. Even an informed guess would be appreciated.

Thanks!
 
It has longer lasting after effects than Diclazepam, which already has a 42 hours half-life.
 
Subjectively that may be, but the biological activity and metabolism considered... flubromazolam is triazolam but the chloros replaced with a 7-bromo (less polar) and 2'-fluoro (more polar).

Since the halogens are not involved in the metabolism, I'd personally expect metabolism to be quite similar although lipophilicity may differ between them - but that much?? and with the two substitution modifications being contradictory in effect on polarity?..

On an order of magnitude, what I would find likely would be the order of triazolam which has a half-life of 1.5-5.5 hours according to wiki, and no active metabolites.
 
Who said it has longer lasting effects than diclazepam? As Sollipsis mentioned, the triazole ring system significantly decreased half life. Even the increase lipophilicity and metabolic stability gained from the halogen substitutes wouldn't be enough I don't think. If what you're saying is true, then I'd expect flubromazepam to have a half life of many 100s of hours, which I don't think it does.
 
aced126 said:
Who said it has longer lasting effects than diclazepam? As Sollipsis mentioned, the triazole ring system significantly decreased half life. Even the increase lipophilicity and metabolic stability gained from the halogen substitutes wouldn't be enough I don't think. If what you're saying is true, then I'd expect flubromazepam to have a half life of many 100s of hours, which I don't think it does.
Click to expand...
F-Pam has a HL of 106h.
 
Look at the drop in half life going from diclazepam to triazolam though. The triazole ring system reduces half life significantly.
 
Yes comparison with flubromazepam despite the 1 letter difference is not really valid since as aced says and is already suggested: the triazolo makes a huge difference - without it half-life may be longer but especially because of formation of the 3-hydroxy metabolite (and maybe avoidance of other metabolism routes?) in the pams such as the otherwise closely related phenazepam this does happen..

Not the case here.

The one or two active metabolites of triazolam are not truly relevant since they are apparently very short acting, at least the alpha hydroxy is.
 
Plasma T1/2 ≠ brain T1/2 as benzos are highly protein bound. Sol is spot on the money.
 
The half-life isn't determined yet. The peak effects from flubromazOLAM last about 10-16 hours. The after effects last at least 24 hours. People report overdoses having negative effects lasting days. Perhaps the drug has an active metabolite. FlubromazOLAM is dangerous. People have reported life ruining horror stories as bad as phenazepam on these multi day overdoses. Stay safe.
 
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