4 replies to this topic

[moleface]

I've seen lots of people talking about taking larger daily doses of picamilon, but after a couple hours online I still can't find much information on the risks associated with exceeding the recommended daily dosage of 300mg.

Is the 300mg daily limit based on any sort of risk factor? Could larger doses increase the MAOI effect or the risk for withdrawal syndrome from downregulation of GABA-A? Or is the 300mg limit just the threshold dose required to get effective but not overly psychoactive effects from the substance? I'm wondering this because I feel like the effects of picamilon only become pronounced to me when I'm taking 200-300mg in a single dose several times a day.

Don't get me wrong - picamilon definitely works for me, even at small 50mg doses. I'm constantly high strung, so it's conspicuous to me whenever something blocks some of my anxiety and irritability. But I actually find that the anxiety relief gets stronger if I take larger doses. After 300mg or so the effects seem to plateau, so I don't think this is placebo.

Edited by moleface, 10 April 2011 - 12:52 AM.

[moleface]

After giving this some thought, I'm now wondering if the recommended maximum dosage for picamilon is overly cautious. It seems plausible that it's entirely based on the premise that too much niacin can be hepatoxic.

If phenibut's therapeutic effects begin around 500-1000mg, why is so much less picamilon supposedly required to elevate GABA levels sufficiently to alleviate anxiety? If phenibut and picamilon are both just GABA bound to a carrier molecule, shouldn't around the same amount of each substance be required to produce comparable GABAergic effects?

The way I'd heard it explained was that once picamilon crosses the blood brain barrier, it splits into niacin and GABA. So shouldn't the dosage required to produce anti-anxiety effects be similar to that of phenibut? Why would a 50mg dosage of picamilon be effective?

Could most of the nootropic properties of picamilon be attributed to the niacin? Isn't GABA just GABA once it crosses the blood brain barrier, regardless of the carrier molecule it was bonded to? I'd assume that 25mg or so of GABA wouldn't make a massive difference in the GABA system's functioning - unless being bound to niacin somehow massively potentiates the GABA or changes its properties in other ways.

Edited by moleface, 14 April 2011 - 12:16 AM.

[The Human Meteorite]

After giving this some thought, I'm now wondering if the recommended maximum dosage for picamilon is overly cautious. It seems plausible that it's entirely based on the premise that too much niacin can be hepatoxic.

If phenibut's therapeutic effects begin around 500-1000mg, why is so much less picamilon supposedly required to elevate GABA levels sufficiently to alleviate anxiety? If phenibut and picamilon are both just GABA bound to a carrier molecule, shouldn't around the same amount of each substance be required to produce comparable GABAergic effects?

The way I'd heard it explained was that once picamilon crosses the blood brain barrier, it splits into niacin and GABA. So shouldn't the dosage required to produce anti-anxiety effects be similar to that of phenibut? Why would a 50mg dosage of picamilon be effective?

Could most of the nootropic properties of picamilon be attributed to the niacin? Isn't GABA just GABA once it crosses the blood brain barrier, regardless of the carrier molecule it was bonded to? I'd assume that 25mg or so of GABA wouldn't make a massive difference in the GABA system's functioning - unless being bound to niacin somehow massively potentiates the GABA or changes its properties in other ways.

The primary difference between picamilon and phenibut is that picamilon will actually break apart into niacinamide (not niacin, despite common belief), and GABA in the brain. Phenibut, being a phenethylamine derivative of GABA appears to bind more selectively to GABA-B while exerting dopaminergic effects too. Potency is always dynamic regardless of specific pharmacology and chemical similarity because every molecule has a unique affinity for the transports across the blood brain barrier, or ability to passively bypass it due to chemical polarity, and once in the brain the binding affinity is generally different even for very similar compounds.
However, I do believe most of picamilon's effects are attributed to niacinamide rather than GABA. Niacin has been found to be a powerful anxiolytic on it's own, anyway.

[moleface]

After giving this some thought, I'm now wondering if the recommended maximum dosage for picamilon is overly cautious. It seems plausible that it's entirely based on the premise that too much niacin can be hepatoxic.

If phenibut's therapeutic effects begin around 500-1000mg, why is so much less picamilon supposedly required to elevate GABA levels sufficiently to alleviate anxiety? If phenibut and picamilon are both just GABA bound to a carrier molecule, shouldn't around the same amount of each substance be required to produce comparable GABAergic effects?

The way I'd heard it explained was that once picamilon crosses the blood brain barrier, it splits into niacin and GABA. So shouldn't the dosage required to produce anti-anxiety effects be similar to that of phenibut? Why would a 50mg dosage of picamilon be effective?

Could most of the nootropic properties of picamilon be attributed to the niacin? Isn't GABA just GABA once it crosses the blood brain barrier, regardless of the carrier molecule it was bonded to? I'd assume that 25mg or so of GABA wouldn't make a massive difference in the GABA system's functioning - unless being bound to niacin somehow massively potentiates the GABA or changes its properties in other ways.

The primary difference between picamilon and phenibut is that picamilon will actually break apart into niacinamide (not niacin, despite common belief), and GABA in the brain. Phenibut, being a phenethylamine derivative of GABA appears to bind more selectively to GABA-B while exerting dopaminergic effects too. Potency is always dynamic regardless of specific pharmacology and chemical similarity because every molecule has a unique affinity for the transports across the blood brain barrier, or ability to passively bypass it due to chemical polarity, and once in the brain the binding affinity is generally different even for very similar compounds.
However, I do believe most of picamilon's effects are attributed to niacinamide rather than GABA. Niacin has been found to be a powerful anxiolytic on it's own, anyway.

Thanks for the reply. That definitely makes sense - I'd assumed that phenibut broke down as well, though I didn't quite understand how simple GABA seemed to be affecting other neurotransmitters.

So picamilon exerts its effects by increasing the amount of available GABA, while phenibut binds to actual receptors to inhibit reuptake? I'm assuming that this is why higher doses of picamilon are considered to be more energizing, since I've heard of paradoxical anxiety from higher doses of GABA supplements.

I just started niacinamide and I'm taking it alongside the picamilon, and picamilon seems to have the slight edge. I've been going through phenibut withdrawal, so it's really obvious when something has a physical effect on my GABA levels because the physical symptoms of withdrawal slightly recede. I'm not sure how much of a difference I'd notice between the two if my brain's GABA system wasn't messed up.

As far as dosing goes - if the effective threshold dose for niacinamide and GABA is 500mg, wouldn't 1g of picamilon make more sense as a dose? Unless combining niacin and GABA into one molecule somehow greatly increases the potency of both, there doesn't seem to be any reason to stick with such low doses.

Edited by moleface, 14 April 2011 - 03:39 AM.

[moleface]

It's confusing- I keep finding varying claims about picamilon online. Some claim that picamilon is a unique molecule that doesn't break down once it crosses the blood brain barrier, and that it exhibits stronger effects than either niacin or gaba and has a longer half life. Others say that it breaks off into niacin and GABA once it crosses the blood brain barrier.

If picamilon is a unique compound that exhibits similar but stronger properties than either niacin or GABA on their own, I'm wondering if there would be any problem with taking niacinamide at the same time. If picamilon isn't exactly niacin but it acts on the brain via the same pathways, would there be issues with receptor competition while taking both simultaneously?