How Do GABA Analogs Work?

Gamma-aminobutyric acid (GABA) analogs are derived from GABA, an essential inhibitory neurotransmitter in the central nervous system, which maintains overall balance and inhibits unnecessary neuronal excitation. These drugs block the brain signals and are used in the treatment of seizures, anxiety, neuropathic/non-neuropathic pain, and alcohol withdrawal symptoms.

There are different GABA analogs each with its own mechanism of action and uses.

Acamprosate works by stimulating the inhibitory neurotransmitter GABA signaling at its receptors and stabilizes the chemical signaling of the brain. Alcohol withdrawal induces the excess release of excitatory neurotransmitters such as glutamate, and this condition of excitotoxicity causes nerve cell death. Acamprosate works as an antagonist of glutamate by blocking its receptors. This maintains abstinence in an alcohol-dependent patient. These drugs are to be used along with psychotherapy.

Gabapentin is an alkylated GABA analog. The exact mechanism of action is unknown. Gabapentin acts as an antagonist on presynaptic voltage-gated channels. It binds to the alpha-2 delta subunit of voltage-gated calcium channels, which inhibit inward calcium currents and decrease neurotransmitter release. Evidence also supports that gabapentin affects the GABAergic system and releases inhibitory neurotransmitter GABA.

Gabapentin enacarbil is a prodrug of gabapentin used for the treatment of seizures, and postherpetic neuralgia (PHN), a painful complication that occurs after a shingles infection.

GABA analogs are used to treat:

• Seizures
• Neuropathic or non-neuropathic pain
• Anxiety
• PHN
• Alcohol withdrawal symptoms
• Restless leg syndrome

Side effects of GABA analogs include:

• Nausea and vomiting
• Diarrhea
• Dizziness
• Constipation
• Headache
• Syncope
• Stomach pain
• Fatigue
• Weight loss
• High blood pressure
• Increased heartbeat
• Insomnia
• Muscle and joint pain
• Mood changes
• Suicidal thoughts
• Change in the amount of urine
• Blurred vision
• Anaphylaxis (life-threatening allergic reactions)
• Swelling of face, tongue, or throat
• Trouble breathing
• Skin rash and itching
• Severe dizziness
• Fever

The information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

Generic and brand names of GABA analogs include:

• Acamprosate (Campral)
• Gabapentin (Gralise, Neurontin)
• Gabapentin enacarbil (Horizant)