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GABA-transaminase inhibitors are drugs which bind to enzymes and decreases their activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors.

1. Phenelzine, Nardil, Nardelzine

Phenelzine is a non-selective and irreversible monoamine oxidase inhibitor (MAOI) of the hydrazine class which is used as an antidepressant and anxiolytic. It is one of the few non-selective MAOIs still in widespread clinical use. It inhibits both of the respective isoforms of MAO, MAO-A and MAO-B, and does so almost equally, with slight preference for the former. By inhibiting MAO, phenelzine prevents the breakdown of the monoamine neurotransmitters serotonin, melatonin, norepinephrine, epinephrine, and dopamine, as well as the trace amine neuromodulators such as phenethylamine, tyramine, octopamine, and tryptamine. This leads to an increase in the extracellular concentrations of these neurochemicals and therefore an alteration in neurochemistry and neurotransmission. Phenelzine and its metabolites also inhibit alanine transaminase (ALA-T), and γ-Aminobutyric acid transaminase (GABA-T) and causes an increase in the alanine and GABA levels in the brain and body.

2. Vigabatrin, Sabril

Gamma-vinyl-GABA is an antiepileptic drug that inhibits the catabolism of gamma-aminobutyric acid (GABA) by irreversibly inhibiting GABA transaminase. It is an analog of GABA, but it is not a receptor agonist. Vigabatrin can cause permanent vision damage, including loss of peripheral vision and having blurry vision. Although vision loss is possible with any amount of vigabatrin, your risk may be greater with the more vigabatrin that you take daily and the longer you take it. Vision loss can happen at any time during treatment with vigabatrin. Vigabatrin is only available through a special program called SHARE. You and your doctor will need to be enrolled in this program before you can receive vigabatrin. You will need to get vigabatrin from a specialty pharmacy that is enrolled in the program.

1. Murinson B. Stiff-person syndrome. Johns Hopkins.School of Medicine.  Link to article

2. Ben-Menachem E, Person LI, Mumford J, et al. Effect of long-term vigabatrin therapy on selected neurotransmitter concentrations in cerebrospinal fluid. J Child Neurol. 1991;Suppl 2:S11-6. Link to article

3. Prevett MC, Brown P, Duncan JS. Improvement of stiffman syndrome with vigabatrin. Neurology 1997, 48:1133–1134.

Link to article

4. Sharoqi IA. Improvement of stiff-man syndrome with vigabatrin. Neurology. 1998 Mar;50(3):833-4. Link to article

5. Vermeij FH, van Doorn PA, Busch HF. Improvement of stiff-man syndrome with vigabatrin. Lancet 1996, 348:612.

Link to article

3. Lemon balm (Melissa officinalis)

Lemon balm (Melissa officinalis), also known as balm mint and not to be confused with bee balm (which is genus Monarda), is a perennial herb in the mint family Lamiaceae. High doses of purified lemon balm extracts were found to be effective in the amelioration of laboratory-induced stress in human subjects, producing "significantly increased self-ratings of calmness and reduced self-ratings of alertness and  a significant increase in the speed of mathematical processing, with no reduction in accuracy" following the administration of a 300 mg dose of extract. It is an inhibitor of GABA transaminase, which explains anxiolytic effects. The major compound responsible for GABA transaminase inhibition activity in lemon balm was then found to be rosmarinic acid. Caution: Lemon balm is believed to inhibit the absorption of the thyroid medication levothyroxine Synthroid). It is sold as a supplement and an ingredient in many over the counter preparations. It could interfere with the performance of your prescribed medications.


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