Picamilon by Ray Sahelian, M.D.

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
[Gabaergic mechanism of cerebrovascular and neuroprotective effects of afobazole and picamilon]
Eksp Klin Farmakol. 2005 Jan-Feb;68(1):20-4.
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, and their combination with Eksp Klin Farmakol. 2000 Sep-Oct;63(5):72-5. 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 Nov-Dec;44(6):559-64. 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.

Piracetam emails
Q. Does your research group have more information about Picamilon and Piracetam? Do you think they will enhance cognition?
   A. It appears that piracetam does have a role to play in cognition.

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..