Pregabalin

Pregabalin
Clinical data
Pronunciation/priˈɡæbəlɪn/
Trade namesLyrica, others[1]
Other names3-isobutyl GABA, (S)-3-isobutyl-γ-aminobutyric acid
AHFS/Drugs.comMonograph
MedlinePlusa605045
License data
Pregnancy
category
Dependence
liability
Physical: High[4]
Psychological: Moderate[4]
Addiction
liability
Low[4] (but varying with dosage and route of administration)
Routes of
administration
By mouth
Drug class
ATC code
Legal status
Legal status
Pharmacokinetic data
BioavailabilityOral: High (≥90% rapidly absorbed; food has no significant effect on bioavailability)[11]
Protein binding<1%[12]
MetabolitesN-methylpregabalin[11]
Onset of actionMay occur within a week (pain)[13]
Elimination half-life4.5–7 hours[14] (mean 6.3 hours)[14][15]
Duration of actionUnknown[16]
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 Edit this at Wikidata
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 checkY
  • Key:AYXYPKUFHZROOJ-ZETCQYMHSA-N checkY
  (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 leg syndrome, opioid withdrawal, and generalized anxiety disorder (GAD).[13][17][18] Pregabalin also has antiallodynic properties.[19][20][21] Its use in epilepsy is as an add-on therapy for partial seizures.[13] It is a gabapentinoid medication (GABA analogue) which are drugs that are derivatives of γ-aminobutyric acid (GABA), an inhibitory neurotransmitter.[22][23][24][25] Pregabalin acts by inhibiting certain calcium channels.[13][26][27] When used before surgery, it reduces pain but results in greater sedation and visual disturbances.[28] It is taken by mouth.[13]

Common side effects include headache, dizziness, sleepiness, confusion, trouble with memory, poor coordination, dry mouth, problems with vision, and weight gain.[13][29] Serious side effects may include angioedema, drug misuse, and an increased suicide risk.[13] 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.[4] Use during pregnancy or breastfeeding is of unclear safety.[30]

Pregabalin was approved for medical use in the United States in 2004.[13] It was developed as a successor to the related gabapentin.[31] It is available as a generic medication.[29][32][33][34][35] In 2021, it was the 73rd most commonly prescribed medication in the United States, with more than 8 million prescriptions.[36][37] In the US, pregabalin is a Schedule V controlled substance under the Controlled Substances Act of 1970,[13] which means that the drug has low abuse potential compared to substances in Schedules I-IV, however, there is still a potential for misuse.[38] Despite the low abuse potential, there have been reports of euphoria, improved happiness, excitement, calmness, and a "high" similar to marijuana with the use of pregabalin; there is a potential for developing dependence on these substances, and withdrawal symptoms may occur if the medication is abruptly discontinued.[39][40] It is a Class C controlled substance in the UK.[41] This classification has specific implications in the UK: class C drugs are considered by the UK government to be the least harmful of the controlled substances,[42] but it is still illegal to possess, supply, or sell Class C drugs like pregabalin without a prescription;[43][44] additional requirements are needed on the prescription, for example, the dose must be clearly defined.[42] Despite being seen as the least harmful by the UK government, possession of Class C drugs still attracts long prison sentences if found guilty in court; and there is a potential for misuse: pregabalin can bring about an elevated mood in users but can also have serious side effects, particularly when used in combination with other drugs.[42][45]

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  3. ^ "Product Information safety updates - January 2023". Australian Department of Health and Aged Care. Archived from the original on February 13, 2023. Retrieved February 13, 2023.
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