vigabatrin and benzos and barbs

[5-HT2]

barbiturates, unlike benzos, are direct agonists at teh GABAa receptor, so do not need GABA to be present at the receptor to function, thus the overdose risk is far higher, even without potentiation, and also, tolerance develops, but the LD:50 does not increase with it.

Barbiturates are not direct agonists, but allosteric modulators like benzos. However, they act at a different modulatory site on the GABA-A receptor, which is almost certainly why they are more dangerous.

Would a reuptake inhibitor actually WORK at all, with a direct agonist, to enhance effectiveness? seeing as direct agonists don't require the presence of GABA to activate the GABAa receptor, does the prescence/lack thereof of GABA alter the activity of barbiturates?

Yes, see above. A reuptake inhibitor would indirectly enhance effectiveness of a subsaturating dose of a direct agonist.

 

[Limpet_Chicken]

Thanks, 5-HT2, I am not nearly as well versed as some here in biochemistry, but do have an intense interest in the subject, could you reccomend further reading perhaps, online?

 

[jasoncrest]

Yes, see above. A reuptake inhibitor would indirectly enhance effectiveness of a subsaturating dose of a direct agonist.

Tiagabine is a GABA reuptake inhibitor, right?

It is an amazing medication, similar to Pregabalin and Vigabatrin, but with less side-effects.
It is very under-estimated, it does wonders for anxiety.

 

[Slay]

^^ there already a thread started on ADD right here about tiagabine and benzos back in 2005