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Calcium α2δ Binding Drugs

Charles Ferdinand

Charles Ferdinand

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Joined
Apr 29, 2009
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323
Location
Rocky Point, México
Hi!
Does anyone knows drugs that bind to the α2δ subunit of the calcium channels, aside from Pregabalin and Gabapentin.
Metabolites are valid.
The root of my question is that Pregabalin doesn't work anymore on me, and I don't want to raise the dose, and Gabapentin has never worked, ever.
I have a disabling Anxiety Disorder, I can't tell which type because 5 pdocs and 3 therapists haven't been able to pin a diagnosis.

Regards!
 
tolerance to this new drug would develop as well to the point where side-effects are same or worse as pregabalin. what then ?

try ssris, nassas and other booster medications
 
5 pdocs have tried everything on me: SSRIs, an SNRI, Tryciclics, Tetracycilics, antipsychotics (typical and atypical), benzos (even exotic rare ones), Gabapentin (felt nothing), etc.
As I've said in other posts the only thing this treatments left me where an extra 40 pounds, from which I still have 20 that can't take off me. Just like a scar.
The only med that worked was Lyrica (combined with a benzo: in their own they did nothing) and at high doses (1200mgs).
So I'm looking for a drug that acts on the same subunits of the calcium channel, so maybe, perhaps, I can forget this disabling anxiety for a while.

Regards.
 
Did you mention selectivity in your original post? :p

Sorry for being asshole.

Edit: But actually, they all specifically target the subunit you mentioned.
 
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Think you're right, but I put the α2δ subunit only.
And yes you're right again, they target that subunit, but, are they anxiolytic? I'm just looking for a pregabalin or gabapentin analogue, I tried to be specific mentioning the subunit they bind to.

Regards.
 
Gabapentin was an accident. It was intended to bind to GABA receptors. Of course, it doesn't. But it has that weird calcium-channel blocking effect, which was unexpected. And then so you have pregabalin also having the same effect. These are relatively simple molecules, both GABA analogues with a lypophilic substituent on the beta carbon. I'm sure there's an SAR study somewhere of GABA analogues with other beta-alkyl substituents. Maybe an isopropyl, a tertbutyl, a propynyl, a cyclopentyl or whatever. I'm sure this info is already out there.

Then again, maybe the isobutyl (pregabalin) is the best it's gonna get.
 
Thanks guys. Thanks Seep.
I took a 4 days break from lyrica and benzos, so I was in hell and couldn't post.
Anyways, I took a lower dose, and it worked!, never like the first time of course, but at least I got more than 4 hours of sleep today.
Interesting info Seep. I'll talk to a friend of mine who just came out of med school, he is also a chemical laboratorist (don't know the right translation, sorry) so I'll talk to him
Thanks!

Rergards!
 
Good luck Charles.

Remember to push behavioral strategies for as much ground against your issues as you can -- the more you do this, the less trouble you'll have to deal with on the pharmacological end.

One thing you did not mention trying is some sort of opioid maintenance -- that is, a stable dose (an attempt at a stable dose) of buprenorphine.
 
Hi! I've thiking about an opoid (will try anyway and need advice, hence it's harm reduction), so, what would you recommend (don't wanna have anoher addiction), I've hearing a lot about tramadol here in BDD.

Regards!
 
Buprenorphine in relatively low doses is described by many to have a nice antidepressant/ anxiolytic effect that doesn't fade much over time. This consistent property is what makes it such a good opiate maintenance drug for so many.

For what it's worth, I was on 2mg/ day or less for around a year and got the same antidepressant/ anxiolytic effect that I was getting when I first started the drug when I came off of it. It really impressed me in it's ability to work in such a fashion for such an expended period, as I have tried various drugs without similar results (including many that you have)... Your results of course may vary, but seeing as you are looking for helpful substances in various categories and now opiates, I certainly recommend giving buprenorphine a try.
 
low dose (50-200mg/day) tramadol could be very useful for you. Along its opioid effect it affects the noradrenergic and serotonergic system as well

combined with pregabalin maybe you can finally find some long lasting relief
 
i think its OTC in mexico? but its definetly sold there that i know. possibly with some other name tho
 
Charles: I have the exact same problem that you do, except that for me, Gabapentin works better than Pregabalin.

The only other thing that worked for me were very low doses of Ketamine. .

Tramadol DID work for me, but it produced one of the most tortuous withdrawals I have experienced when I stopped taking it. My advise is not to mess with tramadol.

Do a search with my name in this forum along with the word "gabapentin". I'm sure you'll find a lot of threads of interest that I started on the same subject in the past.
 
It's now pretty well known that Tramadol has about as much abuse potential as other opiates, depending on the individual (for instance, opiates and Tramadol have no abuse potential for me since they don't seem to cause euphoria).
 
Neurontin is the only other commonly available calcium channel drug I know of. Lyrica and Neurontin have cross-tolerance though.

I would take a tolerance break. Tolerance raises SO quick with these drugs. The first time is intense and sometimes uncontrollable, then after it is just a good mood-stabilizer and anxiolytic. Really good IMO.

Neurontin is more "dirty". Think of it as comparing morphine and heroin. They do the same thing, just one works better and more directly. Lyrica would be the heroin...

-lenses
 
Somewhere in my documents collection I have an SAR study of pregabalin analogues, as I recall most of the simple alkyl groups they tried out do work instead of isobutyl, but I think isobutyl was the most potent...
 
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