Pregabalin is a structural analogue of gamma-aminobutyric acid (GABA). It acts by presynaptic binding to the α -2-λ subunit of voltage-gated calcium channels that are widely distributed in the spinal cord and brain. This mechanism in pre and post-synaptic membranes leads to inhibition of excitatory neurotransmitters release. Compared with gabapentin, pregabalin due to its better fat solubility and transmission in blood-brain barrier is a more favorable replacement for this drug, with better pharmacokinetic properties and because of less hepatic metabolism, drug interactions are lower with pregabalin. Pregabalin in the treatment of neuropathic pain, incisional pain, aches and inflammatory pain induced by formalin has been used effectively.
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Last date updated on May, 2021