Pregabalin controlled release

Pregabalin controlled release (CR) is an extended-release formulation of pregabalin, designed to provide a longer duration of action with once-daily dosing. It's primarily used to treat neuropathic pain conditions including diabetic peripheral neuropathy and postherpetic neuralgia. Pregabalin CR works by binding to the α2δ-1 subunit of voltage-gated calcium channels in the central nervous system. This binding reduces calcium influx at nerve terminals and subsequently decreases the release of several excitatory neurotransmitters including glutamate, substance P, norepinephrine, and calcitonin gene-related peptide. Despite being structurally similar to gamma-aminobutyric acid (GABA), pregabalin does not directly bind to GABA receptors or affect GABA binding. The controlled release formulation achieves peak plasma concentrations within 8.0 hours (range: 5.0–12.0 hours), compared to immediate-release pregabalin which peaks at approximately 0.7 hours (range: 0.7–1.5 hours). It is minimally metabolized and approximately 98% is excreted unchanged in urine. The mean elimination half-life is approximately 6.3 hours. It is administered once daily after an evening meal and tablets should be swallowed whole. When converting from immediate-release pregabalin, specific dose conversions are recommended.

Brand names

Lyrica CR

Other names

Pregabalin CR