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[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]
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Contributors: Prab R. Tumpati, MD