Picamilon is a synthetic compound made of GABA and vitamin B3 (niacin). It crosses the blood-brain barrier more easily than GABA alone, and has been claimed to potentially improve cognitive function and reduce anxiety. But what does the science actually say, and how much do we really know about this compound? Read on to learn more about picamilon, how it might work, and what we know about its efficacy and safety.<\/p>\n
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Disclaimer:<\/em><\/strong> This post is not a recommendation or endorsement for the use of picamilon. The FDA has not approved this compound for any specific medical or other use, and the available research on it is still in a very early stage. We have written this post for informational purposes only, and our goal is solely to inform people about what science currently says about picamilon\u2019s potential effects, mechanisms, and side-effects.<\/em><\/p>\n Picamilon (nicotinoyl-gamma-aminobutyric acid<\/em>) is a synthetic combination of GABA<\/a> and niacin<\/a> (vitamin B3) that has been used by some in the past for the treatment of anxiety<\/a> disorders, among other potential applications [R<\/a>].<\/p>\n GABA is one of the major inhibitory neurotransmitters in the brain. Although its range of mechanisms and functions are complex, it has been generally associated with relaxing and anti-anxiety effects when its levels are increased [R<\/a>, R<\/a>].<\/p>\n Niacin is a vitamin involved in DNA repair, fat and cholesterol<\/a> synthesis, and the widening (dilation<\/em>) of blood vessels.<\/p>\n 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 [R<\/a>, R<\/a>].<\/p>\n Picamilon is not approved as a prescription drug in the United States.<\/strong> In 2015, the FDA ruled that picamilon can\u2019t be sold as a dietary supplement because not enough is known about its effects or its safety, and subsequently ordered five different supplement companies to remove it from their products. However, there are still some companies based in the United States that sell it illegally. Additionally, a review of the available consumer versions of picamilon reported that the dosages can vary wildly from product to product – ranging from as little as 2.7 mg all the way up to over 700mg – and users cannot always be sure exactly what these supplements contain, which raises many major questions related to consumer safety [R<\/a>].<\/p>\n When taken as an oral supplement by itself, GABA is generally not able to cross the blood-brain barrier<\/a> (only a small amount does). However, picamilon (i.e. a compound formulation in which GABA is bound to niacin) is believed to be able to cross the blood-brain barrier, which reportedly allows this particular formulation to affect the brain more readily and directly [R<\/a>, R<\/a>, R<\/a>].<\/p>\n Picamilon\u2019s reported ability to more readily cross the blood-brain barrier (BBB) is believed to be mostly due to the ability of niacin to widen blood vessels. Once picamilon enters the brain, the combined molecule is then broken down into its simpler components, GABA and niacin [R<\/a>].<\/p>\n Once in the brain, GABA activates GABA receptors (both GABAA<\/sub><\/a> and GABAB<\/sub> types), while niacin may increase blood flow throughout the brain (by dilating blood vessels). By bringing fresh oxygen and other essential nutrients that nourish brain cells, this additional blood flow to the brain is believed to account for at least some of the purported neuroprotective and \u201cnootropic<\/em>\u201d (\u201ccognitive-enhancing\u201d) benefits of picamilon – although more research will be needed to fully confirm this, as very little hard evidence regarding its effectiveness in human users is currently available [R<\/a>].<\/p>\n While some preliminary studies have investigated the potential use of picamilon in certain specific medical contexts, much of this research is still in a very early stage, and in most cases, it is not yet possible to come to any firm conclusions about its relative efficacy and safety in human users.<\/p>\n Therefore, the potential effects listed below are still considered to have insufficient evidence<\/strong>, and these findings should be taken with a grain of salt until further research work – including large-scale clinical trials in healthy human users – is performed.<\/p>\n Two very preliminary studies in patients with vision disorders have suggested that picamilon may have potential future use in helping treat certain types of eye disease.<\/p>\n The macula is the center of the retina of the eye, where vision is sharpest. According to one prospective cohort study of 60 patients with macular degeneration<\/em>, three months of picamilon supplementation was reported to improve visual acuity in some patients [R<\/a>].<\/p>\n Central chorioretinal dystrophy<\/em> is a hereditary retinal disorder that results in a progressive visual loss. One prospective cohort study of 48 patients with central chorioretinal dystrophy reported that picamilon improved the ability to distinguish shapes and colors (contrast sensitivity<\/em>), increased peripheral vision, and reduced glaucoma severity [R<\/a>].<\/p>\n While these early findings are promising, much larger-scale clinical trials in human users would be needed to confirm the potential application of picamilon in vision disorders, as well as to determine just how effective and safe it may be.<\/p>\n The following potential uses of picamilon are based solely on animal- or cell-based studies, and are lacking evidence<\/strong> from any appropriate human trials so far. Therefore, these are only potential \u201claunching-points\u201d for future clinical studies in humans, and no solid conclusions can be made about these effects in human users until much more additional research is done.<\/p>\n GABA is the brain\u2019s primary inhibitory neurotransmitter, and greater levels of this molecule have been generally associated with decreased levels of anxiety [R<\/a>].<\/p>\n GABA\u2019s main role in the brain is to slow down excitatory communication between neurons. Too little GABA can cause restless thinking, anxiety, and insomnia [R<\/a>, R<\/a>].<\/p>\n When released, GABA reduces the firing rate of neurons by blocking the activity of glutamate<\/a>, the brain\u2019s primary excitatory neurotransmitter. Too much glutamate<\/a> can contribute to feelings of anxiety, muscular tension, and even increased the risk of seizures. One of the (many) functions of GABA is to counteract these effects, which may account for its reported \u201canti-anxiety\u201d or \u201ccalming\u201d effects [R<\/a>].<\/p>\n People with relatively lower levels of GABA have been reported to have a relatively higher likelihood of developing anxiety disorders, which has led some researchers to suggest that increasing GABA could offer a potentially effective approach for treating anxiety [R<\/a>].<\/p>\n However, actual hard data on this use in humans is so far lacking, and what little evidence there is comes only from animal studies.<\/p>\n For example, according to one animal study, picamilon was reported to reduce anxiety- and depression<\/a>-related behaviors in rats – supposedly by activating GABA receptors [R<\/a>].<\/p>\n In other animal studies, picamilon was reported to suppress aggressive responses to startling stimuli and slowed down the animals\u2019 orientation to such stimuli. This may suggest a diminished anxiety response, although this evidence is very indirect, and would need to be confirmed by a lot more studies [R<\/a>].<\/p>\n<\/a>What is Picamilon?<\/strong><\/span><\/h2>\n
<\/a>Mechanism of Action<\/span><\/h2>\n
<\/a>Purported Uses of Picamilon<\/span><\/h2>\n
<\/a>INSUFFICIENT EVIDENCE:<\/span><\/h2>\n
<\/a>1) May Treat Certain Vision <\/strong>Disorders<\/span><\/h3>\n
<\/a>Animal And Cell Research (LACKING EVIDENCE):<\/span><\/h2>\n
<\/a>2) May Affect Anxiety and Depression<\/strong><\/span><\/h3>\n