Does Wellbutrin affect GABA? (+3 factors)

In this concise article, we will explore the effects of Wellbutrin on GABA ( gamma-aminobutyric acid) neurotransmitter. We will also discuss the research results and how Wellbutrin affects GABA. We will also indicate the role of GABA in the central nervous system and mention other medications that act on GABA receptors.

Does Wellbutrin affect GABA?

Yes, Wellbutrin can affect GABA. Wellbutrin can impact GABA receptors or GABA neurotransmitter levels directly and indirectly. Wellbutrin primarily affects the levels of norepinephrine and dopamine in the brain. Therefore, it can mostly affect GABA indirectly.

Wellbutrin is used as an antidepressant and smoking cessation aid. Wellbutrin works by inhibiting the reuptake of norepinephrine and dopamine into the nerve cells. This causes an increase in the levels of these two neurotransmitters in the brain.

GABA, gamma-aminobutyric acid, is a neurotransmitter that plays a crucial role in the central nervous system by inhibiting or reducing the activity of the nerve cells. GABA has calming and relaxing effects on the nervous system.

 Wellbutrin modulation of these neurotransmitters causes interactions with other neurotransmitters like GABA. The exact nature of these interactions is still not fully understood.(1,2)

How does Wellbutrin affect GABA?

GABA receptors are abundant in the brain. Wellbutrin and several other drugs usually target these receptors. Wellbutrin can induce or inhibit the GABA flow of neurons by binding partially to the GABA receptors.(3)

Another mechanism by which Wellbutrin affects GABA is by acting directly on dopamine neurotransmitters. Wellbutrin tends to increase the levels of dopamine in the brain. Dopamine is a direct modulator of the GABA receptors. As a result, Wellbutrin can affect GABA by altering the dopamine levels. (4)

 

What does the research suggest?

While Wellbutrin’s primary action is on norepinephrine and dopamine, some studies suggest that it might have indirect effects on GABA. The mechanism through which Wellbutrin affects GABA is still under ongoing studies. Wellbutrin’s effects on GABA are not as well-established as its impact on norepinephrine and dopamine. 

 One research study suggests that Wellbutrin can act as a partial agonist on the GABA receptors. Wellbutrin’s effect on GABA is dose-related. Studies have shown that low concentrations of Wellbutrin inhibit the GABA currents while higher concentrations of Wellbutrin induce the GABA currents.(3)

Moreover, dopamine directly modulates the GABA neurotransmitters. This is important for maintaining cognitive functions. Dopamine interacts with GABA in a complex mechanism to sustain the stability of the prefrontal cortex. This interaction is essential in regulating thoughts, planning, decision-making and working memory. (4)

What are other medications that affect GABA?

Because GABA receptors are abundant in the brain, they are the site of action of several medications. GABA can be responsible for regulating neuronal excitability, anxiety, motor control, learning, planning, working memory and circadian rhythms. Therefore, GABA is the target of several drugs, including (5): 

  • Benzodiazepines: Benzodiazepines such as diazepam and alprazolam have calming and sedating effects as they increase GABA activity.

 

  • Barbiturates: Barbiturates such as phenobarbital and secobarbital can also increase GABA activity and have effects similar to benzodiazepines.

 

  • Anticonvulsants: Anticonvulsants have GABA-ergic effects. Examples of anticonvulsants include gabapentin and pregabalin are used to treat epilepsy, seizures and nerve pain.

 

  • Anesthetics: General anesthetics such as propofol increase the GABA-ergic effects to exert hypnotic and sedating effects.

 

  • Muscle relaxants: Baclofen is an example of a muscle relaxant that has a GABA-ergic effect to treat conditions such as muscle spasticity. (5)

Conclusion

To sum up, Wellbutrin can affect GABA. Studies have shown that Wellbutrin can affect GABA directly and indirectly. However, the research is not well-established about how Wellbutrin affects GABA directly. Studies are still ongoing in this area to understand the interaction between Wellbutrin and GABA receptors and neurotransmitters.

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References

1.-

Amirabadi S, Pakdel FG, Shahabi P, Naderi S, Osalou MA, Cankurt U. Microinfusion of bupropion inhibits putative GABAergic neuronal activity of the ventral tegmental area. Basic Clin Neurosci. 2014 Summer;5(3):182-90.

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4202543/

2.-

Jembrek MJ, Vlainic J. GABA Receptors: Pharmacological Potential and Pitfalls. Curr Pharm Des. 2015;21(34):4943-59.https://pubmed.ncbi.nlm.nih.gov/26365137/

4.-

Lew SE, Tseng KY. Dopamine modulation of GABAergic function enables network stability and input selectivity for sustaining working memory in a computational model of the prefrontal cortex. Neuropsychopharmacology. 2014 Dec;39(13):3067-76.https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4229578/

5.-

Sieghart W, Ramerstorfer J, Sarto-Jackson I, Varagic Z, Ernst M. A novel GABA(A) receptor pharmacology: drugs interacting with the α(+) β(-) interface. Br J Pharmacol. 2012 May;166(2):476-85. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3417481/#:~:text=GABAA%20receptors%20are%20the,neuroactive%20steroids%2C%20anaesthetics%20and%20convulsants.

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