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Combining benzos: would they compete for receptor sites?

Jamshyd

Jamshyd

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This is just a personal observation, but I noticed that if I combine Temazepam and Nitrazepam, I actually get less of a hypnotic effect than I do from either on its own. This happens every time and at all doses.

Opinions?
 
^Is it really important? (I ask simply for clarification).

The idea I am getting is that perhaps certain benzos will act competetively (or antagonistically?) with others over certain sites of the receptor.

In any case, the doses in question for last time were 90mg Temazepam and 40mg Nitrazepam.
 
Well, it's not just the strengh of the binding, but what signal they send to the receptor. Although temazepam is weaker, it MAY be the case that it binds stronger...
 
Yeah, doses do matter. To get the results you're describing, I think you'd have to have an almost equi-sedative doses for each (meaning is 5mg of X produced A sedation, then by taking a dose of Y that also produces A sedation, you could possibly have them competing for the receptor sites they have in common- whichever one that produces the sedation- and could possibly block it out).

I think it'd take very careful dosing, no?
 
All benzos bind to the same site on the GABA-A receptor, so they will compete to some extent, especially at high doses. The degree of competition will depend on the GABA-A receptor subtype selectivity of each compound as well as how close you get to saturating concentrations in the brain.
 
I know that benzos bind to quite a few receptor sites (GABA A a1,a2,a3,a5) and I strongly suspect that each benzo has it's own profile. If only someone could give a set of figures for the affinity to each receptor for ALL the benzos.

I think alcohol hits a1 & a4...
 
i agree, if anyone has a list of which benzos effect which recepter sites, that could be most helpful in determining certain aspects of one benzo over another.
 
Very interesting!

So in layman's terms (for now), could that mean that combining different benzos does not always result in an additive effect??

A chart for binding affinity for different GABA subunits for different benzos would be sexual now...
 
Well, Ocinaplon is being tested. That mostly binds to the a2 subunit (for comparison, Zolpidem mostly binds to the a2 subunit) The idea is to remove anxiety without causing sedation. There are not enough of those Z drugs to see what structural features are important to each subunit.
 
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