Picamilon - a better GABA alternative ?

[Doc Sandoz]

Oh damn , I haven't read a review like that before, actually most people seem to have benefits or feel nothing.
How long were you taking it for?

Just checked my old stores of powders and there are two packages of picamalon unopened. I threw away the stuff that I was describing and now I'm pretty sure it was phenibut. After that experience, I was reticent to try picamlon, so there it sits.. Sorry about the confusion.

 

[dukesbobby777]

Just checked my old stores of powders and there are two packages of picamalon unopened. I threw away the stuff that I was describing and now I'm pretty sure you are correct. It was phenibut. After that experience, I was reticent to try picamlon, so there it sits.. Sorry about the confusion.

Haha oh ok. Yeah no worries. I’ve never tried phenibut and I don’t think I ever will. Too risky with tolerance and withdrawal issues.

 

[shine]

I've taken it on and off for years but only small amounts. It has incredible cognitive benefits and increases visual acuity. The only downside is that it increases vasodilation by such an extent that I feel like my vessels are gonna pop. I often get red eyes from it, probably from the dilation.

Edit: It is great to counteract the vasoconstriction from certain psychedelics and puts you in a calm mood. They mix very well.

Edit 2: I just realized it was one of the first supplements I ever took. That was in 2011, 10 years ago. Time flies.

 

[Mauritio]

Just checked my old stores of powders and there are two packages of picamalon unopened. I threw away the stuff that I was describing and now I'm pretty sure it was phenibut. After that experience, I was reticent to try picamlon, so there it sits.. Sorry about the confusion.

Ok got it . I used phnebibut for a long time 1-2 twice a week . It has phenomenal effects ,although it do try to stay away from it because of the things mentioned.

 

[Mauritio]

I've taken it on and off for years but only small amounts. It has incredible cognitive benefits and increases visual acuity. The only downside is that it increases vasodilation by such an extent that I feel like my vessels are gonna pop. I often get red eyes from it, probably from the dilation.

Edit: It is great to counteract the vasoconstriction from certain psychedelics and puts you in a calm mood. They mix very well.

Edit 2: I just realized it was one of the first supplements I ever took. That was in 2011, 10 years ago. Time flies.

You mind expanding on those cognitive benefits? Also any benefits on sleep ?

 

[shine]

You mind expanding on those cognitive benefits? Also any benefits on sleep ?

For me it increases verbal fluency, word recall, puts me in a relaxed state of attention (probably increases alpha brainwaves like theanine), is anti-depressive and makes me seek out novelty. Gets me out of routine. I'd say it is also great for socializing and completely makes you sober again when you had too many drinks.

But like I said, if I take too much the vasodilation is crazy and leads to headaches.

In terms of sleep I can't really say much. I always found it more stimulating/wakefulness-promoting, doesn't really make you sleepy.

 

[Mauritio]

For me it increases verbal fluency, word recall, puts me in a relaxed state of attention (probably increases alpha brainwaves like theanine), is anti-depressive and makes me seek out novelty. Gets me out of routine. I'd say it is also great for socializing and completely makes you sober again when you had too many drinks.

But like I said, if I take too much the vasodilation is crazy and leads to headaches.

In terms of sleep I can't really say much. I always found it more stimulating/wakefulness-promoting, doesn't really make you sleepy.

Ok thanks. I'll try it out.

 

[Coderr]

I've taken it on and off for years but only small amounts. It has incredible cognitive benefits and increases visual acuity. The only downside is that it increases vasodilation by such an extent that I feel like my vessels are gonna pop. I often get red eyes from it, probably from the dilation.

Edit: It is great to counteract the vasoconstriction from certain psychedelics and puts you in a calm mood. They mix very well.

Edit 2: I just realized it was one of the first supplements I ever took. That was in 2011, 10 years ago. Time flies.

Vasodilation effect does viagra effect?

 

[Mauritio]

For me it increases verbal fluency, word recall, puts me in a relaxed state of attention (probably increases alpha brainwaves like theanine), is anti-depressive and makes me seek out novelty. Gets me out of routine. I'd say it is also great for socializing and completely makes you sober again when you had too many drinks.

But like I said, if I take too much the vasodilation is crazy and leads to headaches.

In terms of sleep I can't really say much. I always found it more stimulating/wakefulness-promoting, doesn't really make you sleepy.

I've read that in russian circles 50mg is a good dose, whereas in the western world 100-200mg is advised.
I didn't have much luck with my recent GABAergics (fasoracetam and selank) ,but when I took 50mg of picamilon today my mood turned around quite a bit . I also noticed that for the first time I was able to completely play along a certain guitar solo ,which I've been practicing for weeks .

Did you find you're any significant tolerance to this ?
Most people say they don't notice any tolerance or only a little , so 5 days on 2 off , or 4 on 3 off ,might be enough for cycling ...

 

[shine]

I've read that in russian circles 50mg is a good dose, whereas in the western world 100-200mg is advised.
I didn't have much luck with my recent GABAergics (fasoracetam and selank) ,but when I took 50mg of picamilon today my mood turned around quite a bit . I also noticed that for the first time I was able to completely play along a certain guitar solo ,which I've been practicing for weeks .

Did you find you're any significant tolerance to this ?
Most people say they don't notice any tolerance or only a little , so 5 days on 2 off , or 4 on 3 off ,might be enough for cycling ...

Yes, I never take more than 50mg at once, most of the time I take half of that.
I do notice some tolerance after about 2 weeks of daily use. The 5/2 protocol should be sufficient.

Sounds like it is working for you, nice!

 

[Mauritio]

Yes, I never take more than 50mg at once, most of the time I take half of that.
I do notice some tolerance after about 2 weeks of daily use. The 5/2 protocol should be sufficient.

Sounds like it is working for you, nice!

I took another 50mg dose like an hour ago. And it seemed to lower my mood and make me more irritable. So it seems to depend on the dose a lot! I'll try just 25 or 30 mg tomorrow.

Many people report irritability on picamilon or nothing at all . Maybe they're just taking too much.

 

[Mauritio]

In anesthetized cats, pikamilon in a dose of 10 mg/kg, given by intravenous injection, in-
creased the blood flow by 28 +-3%, but when given internally -- by 18 +-1.7%; in conscious
animals it was increased by 63 +-10% and the effect lasted 120-150 min. The increase in the
blood flow in unanesthetized rabbits was 42 +- 7.3% by Intravenous injection and 24 +- 8% by
the peroral route.

In the strength and duration of its cerebrovascular effect, pikamilon is much superior
both to GABA and to nicotinic acid. Under the same experimental conditions GABA in a dose
of 10 mg/kg (intravenously) caused no change in the cerebral bloodflow, and only when given
in a dose of 300 mg/kg did it increase the blood flow into the brain by 20 • 2.9%, the effect
lasting 3-5 min. Nicotinic acid, also in large doses (50-100 mg/kg) increased the cerebral
blood flow temporally on average by 5-10%.
For instanc~ in a dose of i mg/kg pikamilon pre-
vents the negative consequences of emotional stress (in cats in normalizes the orienting
reaction and attention, when disturbed by the response to rage and fear); like diazepam it
has an inhibitory effect on motivated aggression, associated with fighting by rats for terri-
tory (EDs0 by internal administration is 0.42 mg/kg, for intraperitoneal injection 0.36
mg/kg).

Pikamilon has not only a tranquilizing effect without a sedative component, but also
elements of a stimulating action. Investigation of its effect on the threshold of "self-
stimulation" showed that in higher doses (80 and 160 mg/kg), by contrast with small doses
which have a tranquilizing effect, pikamilon lowered the "self-stimulation" threshold (like
amphetamine), but at the same time it reduced the number of self-stimulations, i.e., it has
an activating effect on positive reinforcement structures. The stimulating action of the
drug also has been shown in relation to the effects of sedative and general anesthetics. For
instance, in a dose of 100 mg/kg pikamilon reduced by 1.7 times the duration of the sedative
effect of hexobarbital sodium and reduced by half the duration of thiopental anesthesia.

A valuable property of pikamilon is the ability to restore the mental and physical working
capacity of rats, when lost due to overfatigue, within a short time. After administration
of pikamil0n in a dose of 5 mg/kg, defense conditioned reflexes (jumping onto a rod) were
restored after their disappearance due to fatigue (by 130% compared with 12% in the control).
In a dose of 50 mg/kg it restored physical working capacity during a rest period of 1 h
(rats swimming with a load) by 76% compared with 38% in the control; under similar conditions
sodium hydroxybutyrate had a positive effect on restoration of working capacity under minimal
rest conditions only in a dose of 100 mg/kg.
(Pikamilon-a new vasoactive and nootropic preparation)




@shine Here we go :

high doses =stimulating
low doses = calming, regenerating .
The 5mg/kg in rats would come pretty close to the 50mg for a human that's been talked about.

 

[golder]

Isn’t it paired with niacin rather than niacinamide? I know Ray is pro niacinamide but unsure if he is anti niacin?

 

[Mauritio]

There is evidence that activation of the GABA-ergic system in various kinds of stress
can play the role of a nonspecific mechanism preventing damage to the body when exposed to
various stimuli [13]. In confirmation of this hypothesis, Novikov and Yasnetsov [16], who
studied the effect of GABA derivatives (fenibut and pikamilon) on the development of toxic
(nicotinic) cerebral edema (as a universal nonspecific response of the CNS to the action of
unfavorable extrinsic or intrinsic factors), showed that pikamilon in a dose of 500 mg/kg,
injected 30 min before nicotine (40 ug/kg), prevented the development of edema. If the compound was given in a dose of 200-300 mg/kg the density of the brain tissue was increased, but
not up to the control level, and the total water content had no significant change. They sug-
gested that the mechanism of the antiedematous action of pikamilon is linked with a change in
energy metabolism in the neuroglial tissue.

...showed that the compound moder-
ately inhibits GABA uptake by synaptosomes, whereas nicotinic acid has no appreciable inhib-
itory action on this process [8].

Accumulation of the compound in muscle tissue 1-2 h after
injection was greater (I0 times) than that of GABA. Pikamilon is retained longer than GABA .

A toxicologic study of pikamilon showed that it possesses low toxicity. For instance,
LDs0 of pikamilon when given internally to albino mice is more than 10 g/kg, and when given intraperitoneally 10 g/kg, and intravenously, over 6 g/kg. A study of chronic toxicity (over
a period of 6 months) showed that pikamilon does not change general behavior or the general
condition of rats when administered over a long period in doses of 3 to 75 mg/kg and causes no
significant changes in the blood, urine, and internal organs of the animals. Some morphologi-
cal changes were found in the kidneys of rats receiving pikamilon in a dose of 75 mg/kg (15
times higher than the therapeutic dose). The character of changes discovered in a histo-
logical study of the kidneys indicated that they were manifestations of glomerulonephritis
and nephrosclerosis, and these subsequently led to the identification of renal pathology as
a contraindication to pikamilon. During the clinical study of the compound, even when ad ministered over a long period or in repeated courses, no disturbances were ever found affecting the kidneys or the urinary system.

In patients with an acute cerebrovascular disturbance an improvement occurred on the 4th-
5th day: the severity of the neurological symptoms was reduced. Later the headache, dizzines,
noise in the head, and memory disorders were reduced, the motor and speech disorders began to
regress rapidly, sleep improved, irritabilit~ emotional stress, and the anxiety state were
reduced. The velocity of the cerebral blood flow was increased. Administration of the
compound to patients with sequelae of cerebrovascular disturbances (more than a month later)
proved effective after the 2nd or 3rd day of treatment. The patients' emotional background,
speech, and memory were improved, and levels of enzyme activity (AS% ALT, LDH) and the lactate
concentration were restored to normal.

In patients with alcoholism pikamilon abolished many of the symptoms in the withdrawal
period, especially those such as apathy, weariness, and lethargy; the patients later become
more tranquil, less fussy and anxious, and their working capacity improved. The compound was
observed to reduce the severity and intensity of the withdrawal syndrome; but not to shorten
it.
When pikamilon was compared with other drugs of similar action (pyracetam, piriditol) it
was observed to have a stronger psychostimulant effect than pyracetam, its effect on the
withdrawal syndrome developed more rapidly than in the case of piriditol.


The clinical study of the preparation showed it to be well tolerated, and to give rise to
one or two side effects (an allergic rash, itching of the skin, mild nausea, and in some
eases, irritability, excitation, dizziness, headache), which disappeared if the dose was reduced or the drug discontinued.

 

[Mauritio]

Isn’t it paired with niacin rather than niacinamide? I know Ray is pro niacinamide but unsure if he is anti niacin?

Yeah that's a valid concern. I think he says it releases histamine.
When you're experimenting a calming effect and no rash/ flush you should be good . As those are clear histaminic symptoms (rash, adrenaline like stimulation)
And most people experience no flush unless they use very high doses . So another reason to go for lower doses of 25-50mg with picamilon.

 

[Frankdee20]

When we talk substrates for neurotransmitters, why doesn’t taking phenylalanine or tryptophan create problems, but taking Glutamine and GABA cause downregulation ?

 

[Mauritio]

When we talk substrates for neurotransmitters, why doesn’t taking phenylalanine or tryptophan create problems, but taking Glutamine and GABA cause downregulation ?

I mean phenylalanine must cause some sort of down regulation as it becomes ineffective for most after a few days of using .

 

[Frankdee20]

I mean phenylalanine must cause some sort of down regulation as it becomes ineffective for most after a few days of using .

I think those lose effectiveness over time due to transport being saturated

 

[Mauritio]

I think those lose effectiveness over time due to transport being saturated

True yeah , then I dont know.

 

[Mauritio]

The 100 mg yesterday was way too much. I became irritable and didnt sleep well .
I always notice with things that are very GABAergic that I get hypoglycemic(strong anti-cortisol response) , less empathy, androgenic feeling , and weight gain I gained 0,5 kg overnight and I can see it on my body .

When gaba is balanced I become social, mellow and relaxed .
10mg today gave me that feeling . I hope I can take that amount from time to time without weight gain . I dont think picamilon per se into blame for this ,its just a reaction I have to stroke anti-cortisol substances (6ketop4 , 11ketoT,...)