Pregabalin (Lyrica)

Pregabalin (Trade name: Lyrica) is anticonvulsant and anxiolytic medication used in the treatment of epilepsy, neuropathic pain, fibromyalgia, restless leg syndrome, and generalized anxiety disorder.

Pharmacokinetics of Pregabalin

Pregabalin: Cytochrome P450 Metabolism

Substrate of (Metabolized by)
Induces
Inhibits
  • Pregabalin (similar to gabapentin) is a α2δ ligand and binds to the α2δ subunit of voltage-sensitive calcium channels (VSCC).
  • This changes the VSCC conformation to reduce calcium influx and thus reduce excessive stimulation of postsynaptic receptors.

Dosing for Pregabalin

Starting
Titration
Maximum
Taper
  • Pregabalin comes in oral formulation.