Picamilon, also known as isonicotinoyl gamma-aminobutyric and nicotinoyl-GABA, is a synthetic drug made from niacin (vitamin B3) and GABA.
Under normal circumstances, GABA supplements cannot cross the blood-brain barrier (BBB), so GABA can’t get from the bloodstream into the brain. However, because niacin increases blood flow, the combination of niacin and GABA means picamilon can cross the BBB and elicit various effects on brain health and mood, which we’ve discussed below.
Read more to learn about the uses, benefits, science, and safety of picamilon.
What Is Picamilon Used for?
Reasons people might use picamilon include:
Anti-Anxiety
Gamma-aminobutyric acid (GABA) is an inhibitory neurotransmitter. This means it can block the transmission of brain signals and reduce overall brain activity. In anxiety disorders, there is often overactivity in the brain; therefore, by reducing brain activity with GABA, picamilon can have a calming effect.
Although there are no published studies on humans demonstrating picamilon is helpful for anxiety, there is plenty of evidence supporting the anti-anxiety effects of other drugs that increase the action of GABA, such as benzodiazepines.
The calming effects of GABA mean picamilon could also help manage stress and improve sleep in those experiencing insomnia. However, there is no evidence to date investigating these claims.
Used as a Nootropic
As well as calming effects, there is some evidence to suggest that by increasing GABA, picamilon may improve cognitive function. For example, one study on people over the age of 40 demonstrated that 12 weeks of GABA supplementation improved the study participants’ non-verbal reasoning, memory, and attention. Furthermore, scientists have shown that other nootropics that increase GABA, such as phenibut, may have cognitive benefits.
We only have anecdotal reports to suggest picamilon has nootropic effects as there are no published human studies.
As well as GABA, the niacin component of picamilon may also improve mental function by increasing blood flow to the brain and increasing the supply of nutrients and energy to nerve cells. In line with this theory, scientists have found associations between levels of niacin in the diet and cognitive performance.
To date, we only have anecdotal reports to suggest picamilon has nootropic effects as there are no published human studies. However, one experiment on rats found that picamilon helped improve learning and short-term memory scores in a maze task.
Treatment of Eye Diseases
Russian doctors provide picamilon as a treatment for open-angle glaucoma – an eye disease caused by a build-up of fluid pressure, which damages the optic nerve and results in blurred vision.
Research has also found picamilon can improve vision in patients with chorioretinal dystrophy and age-related macular degeneration. These are both diseases caused by parts of the eye wearing away.
Improves Bladder and Bowel Control
One research experiment treated over 160 children experiencing bladder and bowel dysfunction with picamilon and found significant reductions in urinary and fecal incontinence.
Picamilon can also help treat benign prostatic hyperplasia (BPH). This is a condition that usually affects older men, whereby enlargement of the prostate gland blocks the flow of urine from the bladder.
Epilepsy
Some of the proposed causes of epilepsy include too little inhibition from GABA-producing nerves in the brain, which results in overactivity and seizures. There’s no direct evidence that picamilon is useful for epileptic patients. However, the antiepileptic drugs vigabatrin and tiagabine can effectively decrease seizures and share a similar brain mechanism to picamilon.
Picamilon Benefits
Antioxidant Properties
Some research suggests picamilon has antioxidant properties, meaning it can help counteract the effects of oxidative stress – the term for several harmful reactions involving oxygen. These reactions can cause nerve cell damage and are thought to be one of the primary causes of age-related brain deterioration.
To demonstrate the antioxidant properties of picamilon, researchers exposed mice to hypoxia (low oxygen conditions) known to increase oxidative stress, and showed that picamilon could help increase their life expectancy.
Furthermore, scientists have found that niacin can decrease oxidative stress reactions in rodents’ brain cells.
Benefits of long-term picamilon may therefore include helping to decrease brain deterioration for age-related oxidative stress.
Protects Mitochondria Function
The mitochondria are the “powerhouse” of a cell responsible for creating energy. In one experiment, researchers exposed rats to cerebral trauma and found that picamilon could protect against some of the damaging effects to the mitochondria.
Therefore, by protecting the mitochondria, picamilon could help increase energy production in the brain.
Edema Prevention
Edema refers to swelling caused by excess fluid trapped inside body tissues. Edema in the brain (cerebral edema) is particularly dangerous as it can stop blood flow to different parts of the brain, causing large portions of nerve cells to die off, resulting in subsequent brain damage.
Studies on rodents have found that picamilon can reduce the development of edema caused by loud noise exposure.
Picamilon (Pikatropin) Side Effects
Although there are no published studies about picamilon side effects in humans, online sources suggest Pikatropin (a brand name of picamilon) at a dose of less than 500 mg/day has no severe side effects.
Nonetheless, some reported side effects of picamilon include:
- Headache
- Nausea
- Flushing (caused by niacin)
- Dizziness
Because picamilon can decrease blood pressure, it may be potentially dangerous for people who have hypotension (low blood pressure).
By increasing GABA action, picamilon may also cause side effects related to GABA, such as drowsiness, memory loss, and sleepiness.
Picamilon Dosage
The limited human clinical research means it’s challenging to determine what dosage is most effective and safe and what doses are best suited to different picamilon uses.
In an identification of picamilon in dietary supplements sold in the United States, researchers found a vast range of recommended daily doses, from 2.7mg to 721.5mg.
However, most online retailers sell picamilon capsules at 150mg and 300mg for daily use.
As with all drugs, if you’re interested in trying picamilon, we recommend starting with a small dose and increasing the dose in small increments according to your needs after consulting with your physician.
Picamilon Supplements
In Russia, picamilon is provided by doctors as a prescription drug. In the United Kingdom, picamilon isn’t provided medically but is available as a dietary supplement or dietary ingredient. In the United States, picamilon isn’t FDA approved but can be found as an ingredient in nootropic supplements.
Because capsules contain set dosages, it’s easier to control picamilon intake than the powder form.
As a supplement, you can buy either picamilon capsules or picamilon powder. Because capsules contain set dosages, it’s easier to control picamilon intake with capsules than with the powder form.
Where to Buy Picamilon
You can buy picamilon online and in health food stores in the United Kingdom and most European countries.
However, because of its unapproved FDA status, picamilon does not fit into the category of dietary supplements and is more difficult to purchase in the United States. While there are a few online vendors selling picamilon, you need to be wary of online retailers selling these supplements because of the legal grey area.
Picamilon: Final Thoughts
By increasing the amount of GABA in the brain, picamilon can have both a calming and nootropic effect. Studies have also found that picamilon may be helpful in treating eye and bladder diseases.
Although experiments have suggested picamilon may have several health benefits in the brain, such as combating oxidative stress, there’s currently no human evidence to support these claims.
Because of the lack of human studies, we can’t draw any conclusions about the safety and recommended doses of picamilon. However, if you’re still interested in trying this supplement, your medical doctor may be able to offer specialist advice based on your individual needs.
