GABAergics

GABAergics are drugs that produce their central nervous system depressant effects by enhancing the effects of the neurotransmitter gamma-aminobutyric acid (GABA). This class of drugs includes both pharmaceutical and natural compounds.

Mechanism of action

GABAergics act by increasing the efficiency of GABA, the chief inhibitory neurotransmitter in the mammalian central nervous system. This is achieved either by increasing the amount of GABA, enhancing its binding to its receptor, or inhibiting its reuptake or degradation.

Types of GABAergics

There are several types of GABAergic drugs, classified based on their mechanism of action. These include:

• GABA receptor agonists: These drugs bind directly to GABA receptors and enhance their activity. Examples include barbiturates and benzodiazepines.
• GABA reuptake inhibitors: These drugs inhibit the reuptake of GABA into the presynaptic neuron, thereby increasing the amount of GABA available in the synaptic cleft. Examples include tiagabine.
• GABA transaminase inhibitors: These drugs inhibit the enzyme GABA transaminase, which is responsible for the breakdown of GABA. This results in an increase in the amount of GABA in the brain. Examples include vigabatrin.

Uses

GABAergic drugs are used in the treatment of various conditions, including anxiety disorders, insomnia, and certain types of epilepsy. They are also used as anesthetics and muscle relaxants.

Side effects

Common side effects of GABAergic drugs include drowsiness, dizziness, and impaired coordination. Long-term use can lead to physical dependence and withdrawal symptoms upon cessation.

See also

• Neurotransmitter
• GABA receptor
• GABA reuptake inhibitor
• GABA transaminase inhibitor