Description

Daniel Barulli, PhD (Psychology), last updated: September 19, 2019. “7 Potential Uses of Picamilon + Dosage & Side Effects”. Retrieved from https://selfhacked.com/blog/picamilon/

INTRODUCTION

Picamilon (N-nicotinoyl-GABA) is a synthetic combination of GABA and Niacin (vitamin B3) used in the treatment of anxiety disorders.

GABA is a neurotransmitter with relaxing and anti-anxiety effects.

Niacin is a vitamin involved in DNA repair, fat and cholesterol synthesis, and widening of blood vessels.

When taken as an oral supplement by itself GABA is not able to cross the blood-brain barrier (only a small amount does). However, Picamilon (GABA bound to Niacin) is able to cross the blood-brain barrier.

Picamilon was first developed in the Soviet Union in the late 1960s and has been sold as a prescription drug for anxiety in Russia since the 1980s.

Mechanism of Action

Picamilon’s ability to cross the blood-brain barrier (BBB) is mostly due to the ability of niacin to widen blood vessels. Once Picamilon enters the brain, the molecule is broken down by water into GABA and Niacin.

Once in the brain, GABA activates GABA (both GABA-A and GABA-B) receptors, while Niacin increases blood flow to the brain by dilating blood vessels. This additional blood flow to the brain is thought to provide the neuroprotective and nootropic benefits of Picamilon. New blood coming into the brain brings fresh oxygen and other essential nutrients that nourish brain cells.

BENEFITS OF PICAMILON (Daniel Barulli, PhD (Psychology), last updated: September 19, 2019. “7 Potential Uses of Picamilon + Dosage & Side Effects”. Retrieved from https://selfhacked.com/blog/picamilon/.)

— May Decrease Anxiety and Depression

GABA is the brain’s primary inhibitory neurotransmitter, and greater levels of this molecule are associated with decreased levels of anxiety.

When released, GABA slows the firing rate of neurons. Too much Glutamate can contribute to feelings of anxiety, muscular tension, and even increased the risk of seizures. GABA slows neuronal firing rates by blocking the activity of Glutamate, the brain’s primary excitatory neurotransmitter.

GABA’s main role in the brain is to slow down excitatory communication between neurons. Too little GABA can cause restless thinking, anxiety, and insomnia. Increasing GABA in the brain alleviates all of these symptoms.

People with excessively low levels of GABA tend to develop anxiety disorders, suggesting that increasing GABA could provide an effective treatment for anxiety.

Picamilon reversed both anxiety and depression and activated GABA receptors in rats.

In other animal studies, Picamilon blunts aggressive responses to startling stimuli and slows orientation to such stimuli. This indicates a diminished anxiety response.

— May Improve Vision

The macula is the center of the retina of the eye, where vision is sharpest. In a study of 60 patients with macular degeneration (prospective cohort), three months of Picamilon supplementation improved visual acuity.

Central chorioretinal dystrophy is a hereditary retinal disorder that results in a progressive visual loss. In a study of 48 patients with central chorioretinal dystrophy (prospective cohort), Picamilon improved the ability to distinguish shapes and colours (contrast sensitivity), increased peripheral vision, and reduced glaucoma severity.

— May Improve Memory

Picamilon improved both short- and long-term memory as well as navigation ability in rats. It also prevented electroshock-induced memory impairment.

— May Protect the Brain

Picamilon protects neurons from being over-activated to the point of death (excitotoxicity). It has also been shown to increase mitochondrial function in the brain cells of rats who have sustained brain trauma.

Picamilon protected the brain and immune cells of sleep-deprived rats by preventing cell membrane damage and oxidative stress.

— May Increase Blood Flow to the Brain

In one study, Picamilon increased blood flow in the brain more than both Piracetam and Vinpocetine, two nootropics that are known for their ability to increase blood flow to the brain.

Picamilon is often prescribed in Russia to treat migraine headaches and is thought to be effective for this condition due to its ability to open constricted blood vessels in the brain.

— May Help with Parkinson’s Disease

Picamilon brought Serotonin and Dopamine up to near normal levels and increased the uptake of Dopamine in the brain in a rat model of Parkinson’s disease.

— May Protect Against Nerve Inflammation (Neuropathy)

Picamilon reduced inflammation of the nerves (neuropathy) in diabetic rats.

Side Effects, Drug Interactions, Limitations

Picamilon is safe and has relatively low toxicity. Side effects include:

– Headache
– Dizziness
– Nausea
– Skin flushing

At high doses, Picamilon can lower blood pressure, which may be unsafe for those with already low blood pressure.

Drug Interactions

Any drug that modulates the GABA receptors has the potential to alter the effects of picamilon. These include:

Alcohol, Barbiturates, Benzodiazepines, Nonbenzodiazepines (or Z-drugs) like Ambien

Drug interactions for Niacin include:

– High-dose aspirin, Uricosuric agents, Alcohol

RESEARCH DOSAGE (Daniel Barulli, PhD (Psychology), last updated: September 19, 2019. “7 Potential Uses of Picamilon + Dosage & Side Effects”. Retrieved from https://selfhacked.com/blog/picamilon/.)

The dosage used in clinical trials ranges from 10 to 300 mg once daily. Users report greater efficacy when taken away from food to maximise absorption.

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