Pharmer’s Review: Personal thoughts on PharmaGABA Experiment (and Why Basics Matter)
Back to Basics: The QQRT Approach
Before diving into supplements, it's crucial to focus on the fundamentals of sleep.
Here are the basics according to the Sleep Foundation, Dr. Walker, and the CDC—
Quantity
Our bodies thrive on 7-9 hours of sleep each night (Centers for Disease Control and Prevention, 2022).
Quality
High-quality sleep involves a quiet, dark, and cool environment (Walker, 2017).
Regularity
Maintaining a consistent sleep schedule is crucial for stability (Sleep Foundation, 2021).
Timing
Aligning sleep with natural rhythm (sleep chronotype) helps regulate our sleep cycle.
My Experience with PharmaGABA
As a light sleeper,
I knew my sleep would likely be disrupted on my upcoming trip to Florida.
My suggested solution was PharmaGABA—
A supplement with interesting research and mechanism of action.
The goal was to—
Reduce the anticipated sleep disruption
Monitor any changes in my mental and physical state.
Curiosity led me down a rabbit hole of research with this molecule.
Here's what I discovered—
The Science Behind PharmaGABA
GABA (gamma-aminobutyric acid) is the brain’s primary inhibitory neurotransmitter.
It works by binding to GABA receptors in the brain,
which are divided into two main types— GABA-A and GABA-B receptors.
GABA-A Receptors
Mechanism
These are receptors that function as chloride ion channels.
When GABA binds to these receptors, chloride ions flow into the neuron, “hyperpolarizing” it and making it less likely to fire an action potential, thus exerting a calming effect (Bettler et al., 2004).
Subunits
GABA-A receptors are composed of various Subunits (α, β, γ, δ, ε, θ, π, and ρ).
The specific combination of these subunits determines the receptor's pharmacological properties and regional distribution in the brain (Bettler et al., 2004).
GABA-B Receptors
Mechanism
Activation of GABA-B receptors leads to the opening of potassium channels and the closing of calcium channels, resulting in prolonged inhibitory effects.
This helps control neurotransmitter release and neuronal excitability over longer periods (Bowery & Smart, 2006).
Subunits
GABA-B receptors have GABA-B1 and GABA-B2 subunits, essential for the receptor's functionality and cell surface expression (Bowery & Smart, 2006).
PharmaGABA Receptor subunits
This table summarizes the findings based on research from Lehmann (2009), Storici et al. (2004), Evenseth et al. (2020), and Polsky-Fisher et al. (2006).
How PharmaGABA Works
PharmaGABA is a natural form of GABA produced via fermentation.
It works by binding to GABA receptors, enhancing calming mechanisms of the brain.
When PharmaGABA binds, it opens “gates”, allowing “calming” chloride ions to flow in.
Key points on PharmaGABAUsage
Take PharmaGABA as directed, typically 100-200 mg before bedtime or during stressful situations.
Onset of Action
Effects can generally be felt within 30 minutes to an hour after ingestion.
Pharmacokinetics
PharmaGABA is absorbed through the intestinal walls and exerts its effects on the nervous system without significant metabolism by the liver.
Mechanism of Action
It enhances GABAergic activity by binding to GABA-A receptors, promoting chloride ion influx and hyperpolarizing neurons.
Metabolism
PharmaGABA is naturally metabolized without significant liver enzyme involvement.
Safety
Generally well-tolerated with minimal side effects, such as mild drowsiness or headaches. Avoid exceeding recommended doses.
Interactions
No significant drug interactions have been reported; however, consult with a healthcare provider if you are taking other medications.
Real-World Impact
PharmaGABA is known to reduce stress markers and boost alpha waves (calming).
Personally, it made winding down easier,
though it wasn’t a miracle cure for my sleep issues.
Using PharmaGABA ONLY When Needed
While I no longer take PharmaGABA,
I keep it handy for particularly stressful days or travel.
It’s a helpful tool, never a daily necessity.
Lessons Learned
Start with Basics
Ensure your sleep habits (QQRT) are solid before turning to supplements.
Use Sparingly
Save PharmaGABA for specific situations rather than daily use.
Observe and Adjust
Monitor how your body responds and adjust accordingly.
Key Takeaways
Good sleep and stress management begin with the basics.
Focus on QQRT, then use supplements like PharmaGABA when necessary.
Stay mindful, stay curious, and remember – the path forward begins with the basics.
References:
Bettler, B., Kaupmann, K., Mosbacher, J., & Gassmann, M. (2004). Molecular structure and physiological functions of GABA(B) receptors. Physiological reviews, 84(3), 835–867. https://doi.org/10.1152/physrev.00036.2003
Bowery, N. G., & Smart, T. G. (2006). GABA and glycine as neurotransmitters: A brief history. British Journal of Pharmacology, 147(S1), S109-S119. https://doi.org/10.1038/sj.bjp.0706442
Centers for Disease Control and Prevention. (2022). How Much Sleep Do I Need? Retrieved from CDC website
Evenseth, L. S. M., Gabrielsen, M., & Sylte, I. (2020). The GABAB Receptor—Structure, Ligand Binding and Drug Development. Molecules, 25(13), 3093. https://doi.org/10.3390/molecules25133093
Lehmann, A. (2009). GABAB receptors as drug targets to treat gastroesophageal reflux disease. Neuropharmacology, 56(1), 115-121. https://doi.org/10.1016/j.neuropharm.2008.06.019
Polsky-Fisher, S. L., Vickers, S., Cui, D., Subramanian, R., Arison, B. H., Agrawal, N. G. B., ... & Rodrigues, A. D. (2006). Metabolism and Disposition of a Potent and Selective GABA-Aα2/3 Receptor Agonist in Healthy Male Volunteers. Drug Metabolism and Disposition, 34(6), 1004-1010. https://doi.org/10.1124/dmd.106.009043
Sleep Foundation. (2021). Sleep Guidelines and Help During the COVID-19 Pandemic. Retrieved from Sleep Foundation website
Storici, P., De Biase, D., Bossa, F., Bruno, S., Mozzarelli, A., Peneff, C., Silverman, R. B., & Schirmer, T. (2004). Structures of γ-Aminobutyric Acid (GABA) Aminotransferase, a Pyridoxal 5′-Phosphate, and [2Fe-2S] Cluster-containing Enzyme, Complexed with γ-Ethynyl-GABA and with the Antiepilepsy Drug Vigabatrin. Journal of Biological Chemistry, 279(1), 363-374. https://doi.org/10.1074/jbc.M305868200
Walker, M. (2017). Why We Sleep: Unlocking the Power of Sleep and Dreams. Scribner.