If you are a Kavinace user, by now you realize that this product is nowhere to be found. This is not exactly true, as an enterprising eBay reseller is offering bottles for $510 each while supplies last. A dietary supplement made by NeuroScience Inc., Kavinace is said to increase GABA levels and has been widely used for insomnia and anxiety. I’ve heard many personal stories about what a game-changer this product has been, and I’ve used it myself when nothing else worked to help me get a good night’s sleep.
The label’s “Supplement Facts” show the primary ingredient as a “proprietary blend” of the amino acid taurine and 4-amino-3-phenylbutyric acid HCl with 2mg of vitamin B6. If you have ever taken vitamin B6 and taurine to help with sleep (as I do), you may have found that these ingredients, even when taken at identical dosing, are ineffective. It was the NeuroScience’s proprietary blend that made Kavinace almost magically effective, and now one of the ingredients is under attack by the FDA. The company states on its website that the Kavinace product is currently unavailable and is being “reformulated.”
According to the FDA, the molecular structure 4-amino-3-phenylbutyric acid, (figure a) is also known by these names:
- 4-Amino-3-phenylbutanoic acid
- β-(aminomethyl)benzenepropanoic acid
- beta-(Aminomethyl)hydrocinnamic acid
- β-phenyl-γ-aminobutyric acid
According to the FDA, products such as Kavinace are “misbranded” because 4-amino-3-phenylbutyric acid HCl is represented as a dietary ingredient when it does not meet the statutory definition. In the US, vitamins and dietary supplements are defined and regulated by the Dietary Supplement Health and Education Act of 1994. In a warning letter sent to NeuroScience on April 10, 2019 referencing Phenibut, the company was given fifteen days to respond. The substance is not on is not listed on the Food and Drug Administration’s Dietary Supplement Ingredient advisory list.
A synthetic amino acid, Phenibut does not occur naturally. Created in the 1960’s in the Soviet Union (figure b) by adding a phenyl group to the Gamma-aminobutyric acid (GABA) molecule, the resulting compound is called 4-amino-3-phenylbutyric acid HCl. This compound, an ingredient in Kavinace’s “proprietary blend,” is able to cross the blood-brain barrier together with the amino acid taurine. In this way, taurine is enabled to activate GABA receptors in the brain, possibly increase GABA synthesis, block GABA reuptake so that it can perform neural calming functions and prevent GABA breakdown.
4-amino-3-phenylbutyric acid HCl can cause dependence when taken regularly, which means that people who use it and then stop taking it may experience withdrawal symptoms. These symptoms can include trouble sleeping, decreased appetite, nausea, muscle aches, anxiety and agitation. New Zealand recently considered the classification of Phenibut as a matter of public health. It is reported to interact with and accentuate the effects of tranquilizers and narcotics, causing possibly dangerous results.
Vitamin B6 is another Kavinace key ingredient. This vitamin is involved in many functions in the body: helping to make the hormones serotonin, melatonin and dopamine, as well as supporting immune health and cognitive function. There’s evidence that B6 supports sleep and affects our dreams. Vitamin B6 has also been connected to lower risk for depression.
More is not better, so be careful with experimentation. High levels of Vitamin B6 can be toxic and excessive levels of B6 have been linked to insomnia. If you’re considering a B6 supplement, it’s important to determine the right dose.
What the FDA enforcement action against NeuroScience means for consumers is that while the ingredients in Kavinace worked for many, the product is no longer available, and consumers are left to seek out a replacement. A naturopath in my local pharmacy has told me that people are struggling as they seek a solution. Will Neuroscience’s reformulation work as well as the original? Could it be that the FDA action paving the way for drug approval of this substance and increased profitability by some drug company?
Unfortunately, without Phenibut, the Kavinace product will not be as effective. This product has been one of the mainstays in my dietary supplement toolkit to help me sleep soundly, and I’m sorry to lose access to it. Worried about losing my ability to get a full night’s sleep, I hunted for alternatives.
I was able to track down a replacement product containing the same ingredients as Kavinace (including phenibut), but found it to be much more potent, the result being an unpleasant “drugged” feeling for several hours in the morning.
Preparing for inevitable loss, I tapered my Kavinace doses while researching how to replace this favorite product. I tried a trusted brand’s neurotransmitter support product containing niacin, vitamin-B6, magnesium, GABA, glycine, taurine, inositol and valerian. To my disappointment, the formulation did absolutely nothing to help the quality or quantity of my sleep.
What seems to be working best for the moment has been to re-balance my circadian rhythm and take minerals along with a non-essential amino acid which has been studied for stress and sleep quality. I began using a LYS wearable device a few weeks ago and quickly observed the value of getting into direct sunlight within 30 minutes of waking.
Now I prepare for bed with a cup of camomile tea, 300 mg L-magnesium threonate, 1,500 mg L-Ornithine, and 30 mg zinc with 4 mg copper (as glycinate), keeping in mind (but sometimes failing) to avoid eating within 3 hours of bedtime and avoiding blue light from digital devices. The result is that my circadian pattern has returned to its natural 5:15 am wake up time after a night of uninterrupted sleep – success!
We’re all hearing about AI and machine learning these days. My personal sleep experimentation effort has reinforced a goal of enhancing Amlia to collect data about the uses and effects of supplement products for the larger good. If you choose to share data, the app would collect and anonymize information about you (age, height, weight, gender, health conditions, etc.) and the supplements you’re taking, along with observed results and side effects to facilitate predictive analysis. This represents an opportunity to leverage big data about vitamin and supplement use to answer the question: “is this supplement working for others like me?”
If you’ve found a routine or supplement works for your sleep, please share your experience here in the comments section.