Picamilon supplement information and benefit by Ray Sahelian, M.D. Review of its uses

Picamilon, also spelled pikamilon was made in 1969 by the All-Union Scientific Research Institute. Picamilon is a derivative of gamma-amino-butyric acid (GABA) and nicotinic acid, a B vitamin. Clinical use of picamilon began in the mid 1980s.

Picamilon Research and studies
Gabaergic mechanism of cerebrovascular and neuroprotective effects of afobazole and picamilon
Eksp Klin Farmakol. 2005.
The role of GABAergic mechanisms in realization of the effects of afobazole and picamilon on the cerebral circulation was studied in rats. It is found that the cerebrovascular effect of afobazole significantly decreases on the background of the GABA receptor antagonists bicuculline and picrotoxin. This is evidence of an important role of the GABA system in the its cerebrovascular and neuroprotective activity of afobazole. The results of experiments with picamilon showed that the cerebrovascular effect of this drug is not affected by receptor blocking with bicucullin. However, the blocking of chloride channels of the GABA receptors by picrotoxin significantly decreased the effect of picamilon on the cerebral blood flow.

Effects of pikamilon on the brain water-electrolyte balance and in models of responses to the noise and vibration exposure
Eksp Klin Farmakol. 2000. Pharmacology Department, Simferopol State Medical University, Crimea, Ukraine.
Electric impedance measurements on awake rabbits with electrodes implanted into cortex, thalamus, and hypothalamus showed that modeling of the noise and general (wide-band) vibration, as well as their combination with sea-sickness action, leads to disturbances in the aqueous-electrolyte balance in brain. This is manifested by extracellular and (less pronounced) intracellular edema development. Picamilon administration (10 mg/kg, i.v.) completely prevented development of the vibration-induced intracellular edema and markedly reduced the development of damage in all other cases studied.

Correction of diabetic neuropathies using aldose reductase inhibitors and pikamilon
Vopr Med Khim. 1998. Institute of Biochemistry, Kiev.
Streptosotocin-induced diabetes in rats is accompanied by the development of diabetic complications such as neuropathies. [2-14C] serotonin and [U-14C] GABA release from the neurotransmitter pre-loaded synaptosomes showed significant elevation. Aldose reductase inhibitors (AL-1576, sorbinil) administration leads to partial restoration of serotonin and GABA release, while picamilon restored only GABA release. It was shown that Na+,K(+)-ATPase activities decreased in synaptosomes, synaptic membranes and sciatic nerve of diabetic rats compared to control. Administration of AL-1576 normalized Na+, K(+)-ATPase activity, while sorbinil and picamilon less effectively. Sorbitol level are increased in streptozotocin-diabetic rats as compared to control. The picamilon and aldose reductase inhibitors administration to diabetic rats is accompanied by the partial reduction of brain sorbitol level. The findings confirm the important role of picamilon and aldose reductase inhibitors in the prevention and treatment of diabetic neuropathy.

Picamilone
Comparative study of the effect of picamilone and piracetam on learning in rats in a radial maze
Farmakol Toksikol. 1989.
During four weeks rats were learned to visit consequently 4 baited arms in the 8-armed radial maze. Picamilone ( nicotinoyl- GABA ) in a dose of 10 mg/kg daily accelerated rats to reach 80% level of learning (to 20-28 trials). After picamilone injections rats obtained the maximal level of short-term memory as just 3-5 trials. Piracetam in a dose of 200 mg/kg daily exerted no effects on long-term and short-term memory of rats in the radial maze.

I have read what you have to say about the supplement GABA and am wondering why you don't speak of Picamilone (I believe this is GABA bonded together with niacin, in order to cross the blood-brain barrier). Is this not a natural supplement? I know very little about it except that it is said to be wonderful for reducing anxiety. I have tried all kinds of herbs and also GABA powder for my anxiety, but nothing has been too noticeable.
   I found one study on GABA and picamilone, besides this I know very little about it and have not had a chance to try it myself to see if it works.

Emails
Q. Have you looked into Picamilon and it's mood altering properties?
   A. Picalmilon appears to be a combination of GABA and nicotinic acid. We have not evaluated this medicine in terms of cognition or its effect on mood.

I am thankful for your extensive research and information on all supplements and ailments. I understand your concern with pure GABA because of its blood brain barrier issues, but what do you think of the niacin bonding that Picamilion utilizes? Is Picalmilion of benefit?
   I have not taken a Picamilon supplement so I don't know how well it works.

Q. like to know what is your opinion of picamilon and it's adverse side effects? I have read that it is a MAO-A inhibitor and dangerous because it can cause tyramine build up in the blood. Is there any truth to this information?

In doing some research on my own about 5-htp on google, I came across something called picamilon from a blog website and was wondering if you have heard of it and know anything about it? Needless to say it sounds very interesting. They say it is only niacin and GABA. A lot of people say how well it works and in doing research on the side effects there doesn't seem to really be any. I just thought I would pass this on to you so that you can do research on it if interested. I am interested and would like to get your opinion on it for someone who is dealing with GAD and depression associated with the anxiety. I also am taking levoxyl so I do my best to check what I'm taking. I don't want any adverse side effects. I would ask my doctor about these things but they are not into the herbal remedies. So I am curious as to your opinion on picamilon and look forward to hearing from you about it along with my first email to you about 5-htp. I'm also curious about the mind power Rx. If it might help with my anxiety problem.
   Mind Power Rx may not be the best herbal supplement for anxiety, there are other products and herbs that work better. I have not taken picamilon pills or used this supplement with patients so I don't know how well it works.

I am a Naturopathic Doc in LA. I was doing a little research on this new compound picamilon. I am just trying to get a little clinical context since I don't know anyone who has used it clinically. I am working with a largish drug rehab facility and we are considering its use for anxiety and sleep disorder in addictive patients. I wonder if it is possible to have a brief conversation about any clinical experience you may have with this compound, or if you have access to any clinical trial data in English that you can point me to.