Global InformationPregabalin information
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| Pronunciation | /priˈɡæbəlɪn/ |
| Trade names | Lyrica, others[1] |
| Other names | 3-isobutyl GABA, (S)-3-isobutyl-γ-aminobutyric acid |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a605045 |
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| 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 |
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| Bioavailability | Oral: High (≥90% rapidly absorbed; food has no significant effect on bioavailability)[11] |
| Protein binding | <1%[12] |
| Metabolites | N-methylpregabalin[11] |
| Onset of action | May occur within a week (pain)[13] |
| Elimination half-life | 4.5–7 hours[14] (mean 6.3 hours)[14][15] |
| Duration of action | Unknown[16] |
| Excretion | Kidney |
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| ECHA InfoCard | 100.119.513 |
| Chemical and physical data | |
| Formula | C8H17NO2 |
| Molar mass | 159.229 g·mol−1 |
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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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- ^ "Avoid prescribing pregabalin in pregnancy if possible". Australian Government. Department of Health and Aged Care. Archived from the original on February 13, 2023. Retrieved February 13, 2023.
- ^ "Product Information safety updates - January 2023". Australian Government. Department of Health and Aged Care. Archived from the original on February 13, 2023. Retrieved February 13, 2023.
- ^ a b c d Schifano F (June 2014). "Misuse and abuse of pregabalin and gabapentin: cause for concern?". CNS Drugs. 28 (6): 491–496. doi:10.1007/s40263-014-0164-4. PMID 24760436.
- ^ "Prescription medicines: registration of new generic medicines and biosimilar medicines, 2017". Therapeutic Goods Administration (TGA). June 21, 2022. Archived from the original on July 6, 2023. Retrieved March 30, 2024.
- ^ Anvisa (March 31, 2023). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published April 4, 2023). Archived from the original on August 3, 2023. Retrieved August 16, 2023.
- ^ "Lyrica Consumer Medicine Information" (PDF). Archived (PDF) from the original on December 4, 2023. Retrieved December 4, 2023.
- ^ "Lyrica Summary of Product Characteristics (SmPC)". (emc). February 27, 2023. Archived from the original on December 21, 2023. Retrieved December 21, 2023.
- ^ Cite error: The named reference
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- ^ a b Cite error: The named reference
EMA2013was invoked but never defined (see the help page). - ^ Cite error: The named reference
Bock2010was invoked but never defined (see the help page). - ^ a b c d e f g h i "Pregabalin". The American Society of Health-System Pharmacists. Archived from the original on December 2, 2019. Retrieved February 3, 2019.
- ^ a b Expert Committee on Drug Dependence Forty-first Meeting (November 2018). Critical Review Report: Pregabalin (PDF) (Report). Geneva: World Health Organization. Archived from the original (PDF) on October 26, 2020.
- ^ Cross AL, Viswanath O, Sherman AI (July 19, 2022). "Pregabalin". StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing. PMID 29261857. Archived from the original on August 3, 2022. Retrieved August 27, 2022 – via NCBI Bookshelf.
- ^ Lilley LL, Collins SR, Snyder JS (2015). Pharmacology and the Nursing Process. Elsevier Health Sciences. p. 227. ISBN 9780323358286.
- ^ Frampton JE (September 2014). "Pregabalin: a review of its use in adults with generalized anxiety disorder". CNS Drugs. 28 (9): 835–854. doi:10.1007/s40263-014-0192-0. PMID 25149863. S2CID 5349255.
- ^ Iftikhar IH, Alghothani L, Trotti LM (December 2017). "Gabapentin enacarbil, pregabalin and rotigotine are equally effective in restless legs syndrome: a comparative meta-analysis". European Journal of Neurology. 24 (12): 1446–1456. doi:10.1111/ene.13449. PMID 28888061. S2CID 22262972.
- ^ Wyllie E, Cascino GD, Gidal BE, Goodkin HP (February 17, 2012). Wyllie's Treatment of Epilepsy: Principles and Practice. Lippincott Williams & Wilkins. p. 423. ISBN 978-1-4511-5348-4.
- ^ Kirsch D (October 10, 2013). Sleep Medicine in Neurology. John Wiley & Sons. p. 241. ISBN 978-1-118-76417-6.
- ^ Frye M, Moore K (2009). "Gabapentin and Pregabalin". In Schatzberg AF, Nemeroff CB (eds.). The American Psychiatric Publishing Textbook of Psychopharmacology. pp. 767–77. doi:10.1176/appi.books.9781585623860.as38. ISBN 978-1-58562-309-9. Archived from the original on February 27, 2024. Retrieved September 1, 2022.
- ^ Calandre EP, Rico-Villademoros F, Slim M (2016). "Alpha2delta ligands, gabapentin, pregabalin and mirogabalin: a review of their clinical pharmacology and therapeutic use". Expert Rev Neurother. 16 (11): 1263–1277. doi:10.1080/14737175.2016.1202764. PMID 27345098. S2CID 33200190.
- ^ Dooley DJ, Taylor CP, Donevan S, Feltner D (2007). "Ca2+ channel alpha2delta ligands: novel modulators of neurotransmission". Trends Pharmacol. Sci. 28 (2): 75–82. doi:10.1016/j.tips.2006.12.006. PMID 17222465.
- ^ Elaine Wyllie, Gregory D. Cascino, Barry E. Gidal, Howard P. Goodkin (February 17, 2012). Wyllie's Treatment of Epilepsy: Principles and Practice. Lippincott Williams & Wilkins. p. 423. ISBN 978-1-4511-5348-4.
- ^ Honorio Benzon, James P. Rathmell, Christopher L. Wu, Dennis C. Turk, Charles E. Argoff, Robert W Hurley (September 11, 2013). Practical Management of Pain. Elsevier Health Sciences. p. 1006. ISBN 978-0-323-17080-2.
- ^ Calandre EP, Rico-Villademoros F, Slim M (November 2016). "Alpha2delta ligands, gabapentin, pregabalin and mirogabalin: a review of their clinical pharmacology and therapeutic use". Expert Review of Neurotherapeutics. 16 (11): 1263–1277. doi:10.1080/14737175.2016.1202764. PMID 27345098. S2CID 33200190.
- ^ Uchitel OD, Di Guilmi MN, Urbano FJ, Gonzalez-Inchauspe C (2010). "Acute modulation of calcium currents and synaptic transmission by gabapentinoids". Channels. 4 (6): 490–496. doi:10.4161/chan.4.6.12864. hdl:11336/20897. PMID 21150315.
- ^ Mishriky BM, Waldron NH, Habib AS (January 2015). "Impact of pregabalin on acute and persistent postoperative pain: a systematic review and meta-analysis". British Journal of Anaesthesia. 114 (1): 10–31. doi:10.1093/bja/aeu293. PMID 25209095.
- ^ a b British National Formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 323. ISBN 9780857113382.
- ^ "Pregabalin Use During Pregnancy". Drugs.com. Archived from the original on March 21, 2019. Retrieved February 4, 2019.
- ^ Kaye AD, Vadivelu N, Urman RD (2014). Substance Abuse: Inpatient and Outpatient Management for Every Clinician. Springer. p. 324. ISBN 9781493919512. Archived from the original on March 1, 2022. Retrieved August 24, 2020.
- ^ "Generic Lyrica Availability". Drugs.com. Archived from the original on March 27, 2019. Retrieved February 4, 2019.
- ^ "FDA approves first generics of Lyrica". U.S. Food and Drug Administration (FDA) (Press release). September 11, 2019. Archived from the original on June 9, 2020. Retrieved October 27, 2019.
- ^ "Pregabalin ER: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Archived from the original on June 24, 2021. Retrieved June 19, 2021.
- ^ "Competitive Generic Therapy Approvals". U.S. Food and Drug Administration (FDA). June 29, 2023. Archived from the original on June 29, 2023. Retrieved June 29, 2023.
- ^ "The Top 300 of 2021". ClinCalc. Archived from the original on January 15, 2024. Retrieved January 14, 2024.
- ^ "Pregabalin - Drug Usage Statistics". ClinCalc. Archived from the original on July 8, 2020. Retrieved January 14, 2024.
- ^ "Is Lyrica a Controlled Substance?". Archived from the original on May 6, 2024. Retrieved May 6, 2024.
- ^ "Is Lyrica a controlled substance / Narcotic?". Archived from the original on February 4, 2024. Retrieved May 6, 2024.
- ^ Preuss CV, Kalava A, King KC (2024). Prescription of Controlled Substances: Benefits and Risks. PMID 30726003.
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- ^ "Controlled Drug Classes". August 12, 2013. Archived from the original on March 28, 2024. Retrieved May 6, 2024.
- ^ "What are Class C Drugs?". October 31, 2022. Archived from the original on May 6, 2024. Retrieved May 6, 2024.
- ^ "Pregabalin and gabapentin to be controlled as class C drugs". Archived from the original on November 12, 2020. Retrieved April 2, 2020.