Gabapentin: a Ca2+ channel alpha 2-delta ligand far beyond epilepsy therapy.
Gabapentin is an antiepileptic drug (AED) by design expected to mimic the action of the neurotransmitter gamma-aminobutyric acid (GABA). However, its principal proposed mechanism of action is the interaction with the alpha 2-delta subunit of L-type voltage-regulated calcium channels. Gabapentin possesses several desirable pharmacokinetic properties, along with few drug interactions, particularly with other AEDs. These properties make it a well-tolerated drug, with the most commonly reported adverse events being somnolence and dizziness. Gabapentin is one of the new first-generation AEDs that expanded its use into a broad range of neurologic and psychiatric disorders shortly after it was licensed in 1993 for use in drug-resistant partial epilepsy with or without secondary generalization. Nowadays, most worldwide prescriptions for gabapentin are for conditions other than epilepsy, especially the treatment of chronic pain of different etiologies. This article will review the pharmacology, mechanism of action, drug interactions and adverse effects of gabapentin. In addition, the clinical trial data, cost analysis and recommended schedule of administration, are also reviewed.
Striano
Pasquale
P
Epilepsy Center, Federico II University, Naples, Muscular and Neurodegenerative Diseases Unit, G. Gaslini Institute, Genoa, Italy. pstriano@email.it
Striano
Salvatore
S
D000588:Amines / Q000009:adverse effects / Q000627:therapeutic use*; D000818:Animals; D000927:Anticonvulsants / Q000627:therapeutic use*; D020746:Calcium Channels, L-Type / Q000187:drug effects*; D002986:Clinical Trials as Topic; D003071:Cognition / Q000187:drug effects; D003509:Cyclohexanecarboxylic Acids / Q000009:adverse effects / Q000627:therapeutic use*; D003929:Diabetic Neuropathies / Q000188:drug therapy; D016903:Drug Monitoring; D004827:Epilepsy / Q000188:drug therapy*; D000077206:Gabapentin; D006801:Humans; D008024:Ligands; D051474:Neuralgia, Postherpetic / Q000188:drug therapy; D005680:gamma-Aminobutyric Acid / Q000009:adverse effects / Q000627:therapeutic use*
D000588:Amines; D000927:Anticonvulsants; D020746:Calcium Channels, L-Type; D003509:Cyclohexanecarboxylic Acids; D008024:Ligands; D005680:gamma-Aminobutyric Acid; D000077206:Gabapentin