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Benzos High vs. Low receptor binding?

speedballs_over

Bluelighter
Joined
Sep 13, 2010
Messages
651
I'm not well versed in benzo pharmacology, beyond what most bluelighters understand from repetitive, accurate posts.

Does it's receptor affinity act like opioid binding where one cmpd binds in a way that prevents other benzos from binding significantly thus blocking them from being (fully) effective?

Beyond the obvious stupidity of mixing benzos, I'd like to know if there's benzos that block others. So i can avoid wasting any.

HR content: trying to understand which benzo might dominate in a combo, hopefully coming directly from clinical data, but i doubt that exists, esp., with RC benzos. Reduce misuse, be smarter about use.

Of course, this is for others, I'm in the beginning of an Ashton taper! Maybe in five years I'll be able to enjoy an occasional benzo, but kinda doubt it, like with dope once dependent is hard to "chip"

Thanks!
 
It's really hard to answer this.

Generally combining most benzos has an additive effect. The only compound I know of that's like suboxone or whatever is flumazenil (used as an antidote for BZD overdose).
 
Maybe it's the subinding site (a1, a2....ax) that sets the rules, and there are so many, each with unique functions.... it's an ignorant guess, at best. Bupe was probably a poor comparison since it is a partial agonist, and I know of no such benzos. Nonetheless, I suspected it is a difficult question - or maybe it's the answer that would scramble my brain?

I was aware of the antagonist, it's good that's available. I wonder if it needs some naloxone type publicity? I say,"No", b/c benzo ods cannot be afforded to deal with by agencies like needle exchanges that focus on opioid / amp pills, meth and heroin and whatever else can be injected (yes, i know how to prepare an IV shot of flubromazolam, but it's meh... Unless you just straight up knock out or kill yourself. Bad,, bad, bad idea.
 
to be honest i was a little confused about what you're really looking for.. is it that you have a bunch of different types of benzos and you don't want to potentially waste them by taking ones that would cancel each other out? - i don't think that's possible with benzos because benzo receptors & GABA(A) receptors are positive allosteric effectors to each other


when the neurotransmitter gamma-aminobutyric acid (GABA) is naturally produced by your cells the binding of GABA to its receptor, GABA(A), causes an inhibitory response in neuronal cells (basically brain activity is decreased, and you are in general more relaxed, note: GABA does other things but I'm just focusing on this aspect). now, benzos work by enhancing the effects of GABA on the GABA(A) receptor so you are even more relaxed than usual. when GABA signals bind to GABA(A) receptors at the same time as benzo agonists are binding to their receptors, they enhance each others binding because a conformational change occurs (a change in the structure of the receptors induced by the binding of signals to the receptors). this conformation change is what causes the enhancement of GABA: it cause the GABA(A) receptor to stabilize causing Cl- ion channels to remain open further depolarizing the cell (i.e. you are now very relaxed) because with the Cl- channels remaining open, more negative ions can keep entering causing the nerve cell to have an even more negative voltage. with an increasingly negative voltage, it is harder to create an action potential. less action potentials occurring = sedative effects


now to discuss the actual benzo receptor...
just recently, scientists found out that there are two types of benzo receptors: central-type and peripheral-type. Central-type receptors are the ones responsible for the acute effects. Not much is known about peripheral-types at this point, but it is hypthosized that they are involved with the benzos that work more slowly. Diazepam is a benzo that binds to both types of receptors with a high affinity. This is why diazepam is the benzo of choice among doctors when they are detoxing patients off of alcohol or other benzos. As I'm sure you know, diazepam's half life is on the longer side, this is thought to be because it binds to the peripheral-type receptors, however its onset is pretty rapid because it also binds to the central receptor.


So... when you are choosing which benzos to mix (however, i don't recommend this because i think it would be better to simply take a higher dose of one type of benzo although i imagine this is why you want to mix because you have limited quantities of various types)... i would pick to mix a fast acting benzo with a slow acting benzo
(see chart: http://www.vhpharmsci.com/vhformulary/tools/benzodiazepines-comparison.htm)... this way you can have both types of your benzo receptors being acted on at once instead of just one type.. I read that diazepam acts on both, but I'm not sure what other benzos are able to do that as well (if I had to guess, I would guess Klonopin does as well). Anyway, I would mix it up slow acting with fast acting so you get all your GABA receptors enhanced for maximal effects.


So, while i don't think its possible for one benzo to block another benzo, to be sure of this you can pick benzos that act on different receptors that way they won't be signaling the same receptor. With all that being said, I've combined many types of benzos and it has always just caused stronger effects.... temazepam w/ valium w/ klonopin w/ ativan w/ xanax w/ etc. (I've never taken all 5 together, but u get the point...)

Well, i hope this was helpful and interesting? obviously don't overdo it!

Source: http://www.uic.edu/classes/phar/pha...ne Receptor-Chloride Ion channel Complex6.htm
 
It's okay to mix benzo's, just know your tolly. I've mixed Klonopin and xanax numerous times, sure I've mixed valium with some of those, it gets incredibly boring on Suboxone maintaince so ya try things,lol. There is something that is used to reverse benzo overdose, i can't think of what it's called and don't think it used alot.
 
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