Pregabalin: An Antiepileptic Agent Useful for Neuropathic Pain

Matthew L. Blommel; Amy L. Blommel


Am J Health Syst Pharm. 2007;64(14):1475-1482. 

In This Article


Pregabalin has demonstrated anticonvulsant, analgesic, and anxiolytic properties in preclinical models.[7] The drug's exact mechanism of action is unclear, but it may reduce excitatory neurotransmitter release by binding to the α2-δ protein subunit of voltage-gated calcium channels (Figure 2).[8] Pregabalin is a structural analogue of GABA, like gabapentin, but does not interact with GABA A or B receptors or influence GABA uptake.[9,10] In animal studies, pregabalin has been shown to be effective against seizures in a wide range of experimental models, exhibiting potent activity against seizures induced by maximal electroshock, pentylenetetrazol, bicuculline, and picrotoxin.[11] Recent structure-activity studies using a mutant mouse model of neuropathic pain have found that binding to α2-δ protein is a prerequisite for the analgesic actions of pregabalin.[12]

Figure 2.

Proposed mechanism of action of pregabalin. Pregabalin binds to the α2-δ subunit of voltage-gated calcium channels in the central nervous system. Illustration by Marie Dauenheimer, CMI.


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