Pregabalin is an anticonvulsant drug used to treat neuropathic pain conditions and fibromyalgia, and for the treatment of partial onset seizures in combination with other anticonvulsants. Pregabalin is structurally similar to gamma-aminobutyric acid (GABA) - an inhibitory neurotransmitter.
- Mechanism
- Curator reviewed · 4 references
Although the mechanism of action has not been fully elucidated, studies involving structurally related drugs suggest that presynaptic binding of pregabalin to voltage-gated calcium channels is key to the antiseizure and antinociceptive effects observed in animal models.
By binding presynaptically to the alpha2-delta subunit of voltage-gated calcium channels in the central nervous system, pregabalin modulates the release of several excitatory neurotransmitters including glutamate, substance-P, norepinephrine, and calcitonin gene related peptide. In addition, pregabalin prevents the alpha2-delta subunit from being trafficked from the dorsal root ganglia to the spinal dorsal horn, which may also contribute to the mechanism of action.
Although pregabalin is a structural derivative of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), it does not bind directly to GABA or benzodiazepine receptors.
- Primary indication
- Pregabalin is indicated for the management of neuropathic pain associated with diabetic peripheral neuropathy, postherpetic neuralgia, fibromyalgia, neuropathic pain associated with spinal cord injury, and as adjunctive therapy for the treatment of partial-onset seizures in...Curator reviewed · 14 structured indications
- Formula / weight
- C8H17NO2 · 159.2261 g/mol (avg)
- First approval
- Canada, 2010 · United States, 2004 · European Union, 2016
- Also known as
- 3-Isobutyl GABA
- Code names
- CI-1008 · PD-144723 · YNP-1807
- Brand names
Resolves to
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Which drugs share a target with Pregabalin, and which of those have an active Phase 3 trial?
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