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Medical research is pretty clear that there is little chance that GABA taken orally will penetrate the blood-brain barrier. Supplements and preparations containing “GABA” itself are misleading.
There are over-the-counter supplements that are derivatives of GABA such as Phenibut and Picamilon.
GABA injections are being tested as a cure for Type 1 diabetes, but have not been tried for SPS.
1. Awad R, Crump K, Mullally M, Sardana RK, Arnason JT, Trudeau VL. An Improved Method for Production of Recombinant Human Glutamic Acid Decarboxylase 65 for Use in Phytopharmaceutical Assessment.
Pharmaceutical Biology 2008;46:1-2, 72-81
2. Johnstone AP. Nussey SS. Direct evidence for limited clonality of antibodies to glutamic acid decarboxylase (GAD) in stiff man syndrome using baculovirus expressed GAD. J Neurol Neurosurg Psychiatry. May 1994; 57(5): 659 Link to article
Picamilon (also known as nicotinoyl-GABA, pycamilon, and pikamilon) is a dietary supplement formed by combining niacin with GABA. Picamilon is sold in the United States as a dietary supplement, while in Russia it is sold as a prescription drug. Picamilon is able to cross the blood–brain barrier and is then hydrolyzed into GABA and niacin. The released GABA in theory would activate GABA receptors potentially producing an anxiolytic response. The second released component, niacin acts as a strong vasodilator, which might be useful for the treatment of migraine headaches. However, excessive niacin can cause cardiovascular symptoms such as flushing and fast pulse. Wikipedia.
2. Phenibut, Fenibut, Noofen, Fenigam, Phenigam, Phenybut, Phenygam, Phenylgamma, PHG, PhGABA
β-Phenyl-γ-aminobutyric acid is a derivative of the naturally occurring inhibitory neurotransmitter γ-aminobutyric acid (GABA). The addition of a phenyl ring allows phenibut to cross the blood brain barrier.
Phenibut is sold as a nutritional supplement, and is not approved as a pharmaceutical in the United States or Europe, but in Russia it is sold as a psychotropic drug. It has been reported by some to possess nootropic actions for its ability to improve neurological functions, but other researchers have not observed these effects. It is generally accepted that phenibut has anxiolytic effects.
Phenibut was discovered in the Soviet Union in the 1960s, and has since been used there to treat a wide range of ailments including post-traumatic stress disorder, anxiety, and insomnia. The effects are similar to baclofen, but less potent per milligram of dosage. Phenibut exerts its effects by being an agonist at the metabotropic GABA-β receptor, and at higher doses also at the ionotropic GABA-β receptor. It has been shown to enhance levels of dopamine.
The literature reports that phenibut has almost no negative side effects, with only an increase in sleepiness observed, however this effect is not nearly as pronounced as with benzodiazepine usage. Tolerance has been reported with extended use of high doses (e.g. 5–10 grams). There are numerous reports of withdrawal symptoms mainly due to misuse or excess. There is one reported case of withdrawal involving nervousness and shakiness, psychomotor agitation, feeling easily annoyed and irritated, fatigue, poor appetite, heart pounding and racing, nausea, insomnia, and feeling tense and keyed up. Drugs.com.