Gabapentinoid

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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[edit | edit source]

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[edit | edit source]

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[edit | edit source]

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[edit | edit source]

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[edit | edit source]


Gabapentinoid Resources

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