Pregabalin

Pregabalin
Clinical data
Pronunciation/priˈɡæbəlɪn/
Trade namesLyrica, others
Other names3-Isobutyl-GABA; (S)-3-Isobutyl-γ-aminobutyric acid; Isobutylgaba; CI-1008; PD-144723
AHFS/Drugs.comMonograph
MedlinePlusa605045
License data
Pregnancy
category
  • AU: D
Dependence
liability
Physical: High
Psychological: Moderate
Addiction
liability
Low (but varying with dosage and route of administration)
Routes of
administration
By mouth
Drug class
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • BR: Class C1 (Other controlled substances)
  • CA: ℞-only
  • NZ: Rx-only
  • UK: POM (Prescription only) / Class C
  • US: Schedule V
  • EU: Rx-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
BioavailabilityOral: ≥90%
Protein binding<1%
MetabolitesN-methylpregabalin
Onset of actionMay occur within a week (pain)
Elimination half-life4.5–7 hours (mean 6.3 hours)
Duration of action8–12 hours
ExcretionKidney
Identifiers
  • (3S)-3-(aminomethyl)-5-methylhexanoic acid
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.119.513
Chemical and physical data
FormulaC8H17NO2
Molar mass159.229 g·mol−1
3D model (JSmol)
  • CC(C)CC(CC(=O)O)CN
  • InChI=1S/C8H17NO2/c1-6(2)3-7(5-9)4-8(10)11/h6-7H,3-5,9H2,1-2H3,(H,10,11)/t7-/m0/s1 Y
  • Key:AYXYPKUFHZROOJ-ZETCQYMHSA-N Y
  (verify)

Pregabalin, sold under the brand name Lyrica among others, is an anticonvulsant, analgesic, and anxiolytic amino acid medication used to treat epilepsy, neuropathic pain, fibromyalgia, restless legs syndrome, opioid withdrawal, generalized anxiety disorder (GAD), and shingles. Pregabalin also has antiallodynic properties. Its use in epilepsy is as an add-on therapy for partial seizures. When used before surgery, it reduces pain but results in greater sedation and visual disturbances. It is taken by mouth.

Common side effects can include headache, dizziness, sleepiness, euphoria, confusion, trouble with memory, poor coordination, dry mouth, problems with vision, and weight gain. Serious side effects may include angioedema, kidney damage and drug misuse. As with all other drugs approved by the FDA for treating epilepsy, the pregabalin labeling warns of an increased suicide risk when combined with other drugs. When pregabalin is taken at high doses over a long period of time, addiction may occur, but if taken at usual doses the risk is low. Use during pregnancy or breastfeeding is of unclear safety.

It is a gabapentinoid medication which is a class of drugs within the derivatives of γ-aminobutyric acid (GABA analogues), an inhibitory neurotransmitter. Although pregabalin is inactive at GABA receptors and GABA synapses, it acts by binding specifically to the α2δ-1 protein that was first described as an auxiliary subunit of voltage-gated calcium channels.

Pregabalin was approved for medical use in the United States in 2004. In the US, pregabalin is a Schedule V controlled substance under the Controlled Substances Act of 1970, which means that the drug has low abuse potential compared to substances in Schedules I-IV, however, there is still a potential for misuse. It is available as a generic medication. In 2022, it was the 91st most commonly prescribed medication in the United States, with more than 7 million prescriptions.