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A GABA reuptake inhibitor (GRI) is a type of drug which acts as a reuptake inhibitor for the neurotransmitter gamma-Aminobutyric acid (GABA) by blocking the action of the gamma-Aminobutyric acid transporters (GATs). This in turn leads to increased extracellular concentrations of GABA and therefore an increase in GABAergic neurotransmission. [1]
Tolerance to gabapentinoids is reported to develop very rapidly with repeated use, although to also dissipate quickly upon discontinuation, and withdrawal symptoms such as insomnia, nausea, headache, and diarrhea have been reported. [58] [21] More severe withdrawal symptoms, such as severe rebound anxiety, have been reported with phenibut. [30]
Gabapentin is recommended as a first-line treatment for chronic neuropathic pain by various medical authorities. [10] [11] [31] [32] This is a general recommendation applicable to all neuropathic pain syndromes except for trigeminal neuralgia, where it may be used as a second- or third-line agent. [11] [32]
Like other GABA-T inhibitors, γ-acetylenic GABA causes GABA levels in the brain to be elevated. This is due to 4-aminobutyrate transaminase being the enzyme that converts γ-aminobutyric acid to L-glutamate. Inhibiting the enzyme stops this conversion from happening.
Individuals who have had more withdrawal episodes are at an increased risk of very severe withdrawal symptoms, up to and including seizures and death. Long-term activation of the GABA receptor by sedative–hypnotic drugs causes chronic GABA receptor downregulation as well as glutamate overactivity, which can lead to drug and neurotransmitter ...
Chronic obstructive pulmonary disease (COPD) is a type of progressive lung disease characterized by chronic respiratory symptoms and airflow limitation. [8] GOLD 2024 defined COPD as a heterogeneous lung condition characterized by chronic respiratory symptoms (dyspnea or shortness of breath, cough, sputum production or exacerbations) due to abnormalities of the airways (bronchitis ...
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