sparkk51, on 07 June 2012 - 12:40 AM, said:
Considering Phenibut is, as I said earlier, a very simple derivative of GABA itself, wouldnt that imply that the noted tolerance it produces be an effect of down-regulation of GABA receptors instead of some other mechanism which inhibits (specifically) Phenibut's mode of action? May we assume that finding a proper long-term GABA agonist is futile?
Does the tolerance that arises from using Phenibut only occur when more than a certain dose is taken per day?
I have this intuitive sense that all the ill-remarks directed at phenibut are really, deservedly, for the GABA system itself. Otherwise, wouldn't it be implied that there is some substance out there which effectively agonizes GABA receptors while not producing tolerance for an appropriate amount of time?
Now, as for the effects of the neurotransmitter itself; does GABA have a strong connection with temporal lobe functions? I believe I read somewhere that GABA is produced in this area of the brain, although I wouldnt be surprised if I was mistaken. The reason I ask is because I believe I have weak temporal lobes considering my poor recollective memory and auditory processing.
Whether it's futile to find a long-term GABA agonist or not depends on what you want to do with it. Phenibut and baclofen can be effective long-term anti-spasticity agents for use in spinal injuries, multiple sclerosis, cerebral palsy... But long term anxiolytic effects are harder to sustain.
It's not impossible to use it for long-term anxiety relief, but some people can do it and others can't. It depends on what type of anxiety you have, and what the triggers are, and how well you're using coping skills... that sort of thing.
What is clearly not sustainable is using phenibut (or baclofen) as a sleeping aid. That does not work. In fact, no GABA agonist sleeping pill works well over the long term. They give you amnesia so you forget lying in bed awake, then you assume you got good sleep. But you didn't get better sleep -- all current sleeping pills only add 5-20 minutes of sleep to your nights in the short term. Over the long term, some of them continue to give you an extra 5-10 minutes, but some of them quit working entirely. That's why I always recommend CBT-I over sleeping pills; it's the only truly effective option. Sure, it's harder to modify your behavior than to pop a relaxation-and-forgetfulness pill every night, but CBT-I cures the insomnia and the pill doesn't. That's the only thing that really matters if you suffer from insomnia.
Anyway, back to GABA agonists. The GABA system is pretty plastic, so yeah, tolerance does develop to any GABA-A or -B agonist if you're using it daily. Simple fact. But when using a benzo (or phenibut) responsibly, the tolerance often stops at some point where you're still getting effective help for anxiety. As long as you DO NOT escalate the dose further (chasing euphoria or sleep), you can probably stay on that same dose for years at a time. I know plenty of people on long term treatment with daily clonazepam, and it works fine. In the past, I've used MRM Relax-All with Phenibut safely. It contains a very low dose of phenibut -- I believe it's 500mg per 4 capsules. I'd take 1-2 capsules before social events that caused anxiety, and the anxiety would be significantly reduced. I only did this about 6-10 days out of the month, and I never had a problem with tolerance or withdrawal.
People who use phenibut to get high DO have tolerance and withdrawal. They escalate their dose, sometimes taking tens of grams per day. Not milligrams, but grams. That's very unhealthy. But using phenibut as I described, a few hundred milligrams 1-3 times a week, is perfectly safe. In fact, I'd still be using phenibut before social events if I hadn't cured my anxiety with psychotherapy.