Pregabalin is a highly effective gabapentinoid agent used to modulate central nervous system hyperexcitability. It functions as a ligand that binds selectively to the alpha-2-delta subunit of voltage-gated calcium channels in presynaptic neurons. By stabilizing these channels, it significantly reduces the influx of calcium ions, which downregulates the excessive release of excitatory neurotransmitters such as glutamate, norepinephrine, and substance P, thereby restoring physiological balance to overstimulated nerve pathways.