Gabapentinoids are a class of drugs that are derivatives of the inhibitory neurotransmitter γ-aminobutyric acid (GABA) which block α2δ subunit-containing voltage-dependent calcium channels. This site has been referred to as the gabapentin receptor (α2δ subunit), as it is the target of the drugs gabapentin and pregabalin. Clinically-used gabapentinoids include gabapentin (Neurontin) and pregabalin (Lyrica) as well as a gabapentin prodrug, gabapentin enacarbil (Horizant). In addition, phenibut (Noofen) has been found to act as a gabapentinoid in addition to its primary mechanism of action. Another analogue mirogabalin is in clinical trials but has not yet been approved. Other compounds from this family used in research but not developed for medical use include atagabalin, 4-methylpregabalin and PD-217,014.
Gabapentinoids are used clinically in the treatment of conditions including epilepsy, neuropathic pain, fibromyalgia, generalized anxiety disorder, and restless legs syndrome. Some off-label uses include migraine, social phobia, panic disorder, mania, bipolar disorder, and alcohol withdrawal.