Gabapentin binds to the alpha-2-delta (α2δ) subunit of voltage-gated calcium channels on nerve cells. This reduces calcium flow into overactive neurons, decreasing the release of pain-signaling chemicals like glutamate. Gabapentin is a medication used in the treatment of various conditions such as epilepsy, post-herpetic neuralgia, neuropathic pain, and spasticity. It works by affecting calcium channels, leading to a decrease in excitatory neurotransmitters. Gabapentin is a valuable drug in seizure and neuropathic pain pharmacology. Its main action is binding to alpha-2-delta calcium-channel subunits, which reduces excitatory neurotransmitter release and neuronal hyperexcitability. Gabapentin binds to the α2δ-1 subunit of voltage-gated calcium channels in the CNS, particularly in presynaptic neurons. The inhibition of neurotransmitter release leads to dampened neuronal hyperexcitability, especially in epileptic foci and pain pathways. At very high concentrations, gabapentin can suppress the growth of cancer cells, presumably by affecting mitochondrial catabolism; however, the precise mechanism remains elusive. Understand the detailed mechanism of action of gabapentin including pharmacokinetics, uses, side effects, and FAQs. Gabapentin crosses several lipid membrane barriers via system L amino acid transporters. In vitro, gabapentin modulates the action of the GABA synthetic enzyme, glutamic acid decarboxylase (GAD) and the glutamate synthesizing enzyme, branched-chain amino acid transaminase.