Pregabalin

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

Pregabalin
Clinical data
Pronunciation/priˈɡæbəlɪn/
Trade namesLyrica, others
Other names3-isobutyl GABA, (S)-3-isobutyl-γ-aminobutyric acid
AHFS/Drugs.comMonograph
MedlinePlusa605045
License data
Pregnancy
category
  • AU: D
Dependence
liability
Physical: High
Psychological: Moderate
Addiction
liability
Low
Routes of
administration
By mouth
Drug classGabapentinoid;

Anticonvulsant;

GABA analogue
ATC code
Legal status
Legal status
Pharmacokinetic data
BioavailabilityOral: High (≥90% rapidly absorbed; administration with food may reduce the rate of Pregabalin absorption, yet it’s highly absorbed)
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 actionUnknown
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)

Common side effects include headache, dizziness, sleepiness, confusion, trouble with memory, poor coordination, dry mouth, problems with vision, and weight gain. Serious side effects may include angioedema, drug misuse, and an increased suicide risk. 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.

Pregabalin was approved for medical use in the United States in 2004. It was developed as a successor to the related gabapentin. It is available as a generic medication. In 2021, it was the 73rd most commonly prescribed medication in the United States, with more than 8 million prescriptions. In the US, pregabalin is a Schedule V controlled substance under the Controlled Substances Act of 1970. It is a Class C controlled substance in the UK.

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