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)
  • 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.
  • Generalized anxiety disorder[1]

Dosing for Pregabalin

Starting 50 mg PO daily
Titration Increase by 50 mg PO q1 week
Maximum 150 to 600 mg range is a therapeutic dose
Taper Gradually taper at least over the course of 1 week, some discontinuation/withdrawal syndromes have been reported.[2]
  • Pregabalin comes in oral formulation.
  • Pregabalin can also cause myoclonus (especially in the setting of acute kidney injuries when pregabalin is not able to be cleared).[3]

Pregabalin been studied in the geriatric population for generalized anxiety. Anxiety, somnolence, falls, and infection are potential adverse events to be aware of in the geriatric population.[5]