Pregabalin (Lyrica)

Primer

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

See also article: Introduction to Pharmacology

Pharmacokinetics of Pregabalin

Absorption	Tmax = 1-2 hours
Distribution
Metabolism
Elimination
Half-life	6 hours

See also article: Cytochrome (CYP) P450 Metabolism

Pregabalin: Cytochrome P450 Metabolism

Substrate of (Metabolized by)
Induces
Inhibits

Pharmacodynamics

Mechanism of Action

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.

Toxicity

Indications

Generalized anxiety disorder^[1]

Dosing

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]

Formulations

Pregabalin comes in oral formulation.

Monitoring

Contraindications

Absolute

Relative

Drug-Drug Interactions

Side Effects

Pregabalin can also cause myoclonus (especially in the setting of acute kidney injuries when pregabalin is not able to be cleared).^[3]

Adverse Events

Clinical Pearls

Pregabalin has greater abuse potential than gabapentin.^[4]

Special Populations

Geriatric

See main article: Geriatric Pharmacology

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]

Pediatric

See main article: Pediatric Pharmacology

Obstetric and Fetal

See main article: Obstetric and Fetal Pharmacology

Medically Ill

See main article: Psychotropic Dosing in the Medically Ill

Resources

¹⁾ Baldwin, D. S., Ajel, K., Masdrakis, V. G., Nowak, M., & Rafiq, R. (2013). Pregabalin for the treatment of generalized anxiety disorder: an update. Neuropsychiatric Disease and Treatment.

²⁾ Naveed, S., Faquih, A. E., & Chaudhary, A. M. D. (2018). Pregabalin-associated discontinuation symptoms: a case report. Cureus, 10(10).

³⁾ Desai, A., Kherallah, Y., Szabo, C., & Marawar, R. (2019). Gabapentin or pregabalin induced myoclonus: A case series and literature review. Journal of Clinical Neuroscience, 61, 225-234.

⁴⁾ Bonnet, U., & Scherbaum, N. (2017). How addictive are gabapentin and pregabalin? A systematic review. European neuropsychopharmacology, 27(12), 1185-1215.

⁵⁾ Montgomery, S., Chatamra, K., Pauer, L., Whalen, E., & Baldinetti, F. (2008). Efficacy and safety of pregabalin in elderly people with generalised anxiety disorder. The British journal of psychiatry, 193(5), 389-394.

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