Gabapentinoid

Gabapentinoid is a class of drugs that includes two FDA-approved medications, gabapentin and pregabalin. These drugs are primarily used to treat neuropathic pain and epilepsy.

Overview

Gabapentinoids are analogs of the neurotransmitter gamma-aminobutyric acid (GABA). Despite this, they do not bind to the GABA receptors, but instead modulate the release of excitatory neurotransmitters.

Medical Uses

Gabapentinoids are used in the treatment of several medical conditions:

• Neuropathic pain: Gabapentinoids are effective in reducing pain and improving sleep in patients with neuropathic pain.
• Epilepsy: Both gabapentin and pregabalin are approved for the treatment of partial seizures.
• Fibromyalgia: Pregabalin is approved for the treatment of fibromyalgia in the United States.

Side Effects

Common side effects of gabapentinoids include dizziness, drowsiness, and peripheral edema. Serious side effects may include an increased risk of suicide, respiratory depression, and drug misuse.

Mechanism of Action

Gabapentinoids bind to the α2δ (alpha-2-delta) subunit of voltage-dependent calcium channels in the central nervous system. This reduces calcium influx at nerve terminals and subsequently reduces the release of excitatory neurotransmitters.

See Also

• Neuropathic pain
• Epilepsy
• Fibromyalgia
• Gamma-aminobutyric acid
• Neurotransmitter

• 
  Gabapentin 2D structure
• 
  Gabapentinoid chemical structures
• 
  Calcium channel with gabapentin bound