Pregabalin

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For drug-resistant focal epilepsy, pregabalin is useful as an add-on therapy to other treatments.{{cite journal |vauthors=Panebianco M, Bresnahan R, Marson AG |title=Pregabalin add-on for drug-resistant focal epilepsy |journal=The Cochrane Database of Systematic Reviews |volume=3 |issue=3 |pages=CD005612 |date=March 2022 |doi=10.1002/14651858.CD005612.pub5 |pmc=8962962 |pmid=35349176}} Its use alone is less effective than some other seizure medications.{{cite journal |vauthors=Zhou Q, Zheng J, Yu L, Jia X |title=Pregabalin monotherapy for epilepsy |journal=The Cochrane Database of Systematic Reviews |volume=2012 |pages=CD009429 |date=October 2012 |issue=10 |doi=10.1002/14651858.CD009429.pub2 |pmid=23076957|pmc=11942706 }} It is unclear how it compares to gabapentin for this use.

The European Federation of Neurological Societies recommends pregabalin as a first-line agent for the treatment of pain associated with diabetic neuropathy, post-herpetic neuralgia, and central neuropathic pain.{{cite journal |vauthors=Attal N, Cruccu G, Baron R, Haanpää M, Hansson P, Jensen TS, Nurmikko T |title=EFNS guidelines on the pharmacological treatment of neuropathic pain: 2010 revision |journal=European Journal of Neurology |volume=17 |issue=9 |pages=1113–1e88 |date=September 2010 |title-link=doi |doi=10.1111/j.1468-1331.2010.02999.x |doi-access=free |pmid=20402746 |s2cid=14236933}} A minority obtain substantial benefit, and a larger number obtain moderate benefit.{{cite journal |vauthors=Derry S, Bell RF, Straube S, Wiffen PJ, Aldington D, Moore RA |title=Pregabalin for neuropathic pain in adults |journal=The Cochrane Database of Systematic Reviews |volume=1 |pages=CD007076 |date=January 2019 |issue=1 |doi=10.1002/14651858.CD007076.pub3 |pmc=6353204 |pmid=30673120}} It is given equal weight as gabapentin and tricyclic antidepressants as a first-line agent, however, the latter are less expensive as of 2010.{{cite journal |vauthors=Finnerup NB, Sindrup SH, Jensen TS |title=The evidence for pharmacological treatment of neuropathic pain |journal=Pain |volume=150 |issue=3 |pages=573–581 |date=September 2010 |doi=10.1016/j.pain.2010.06.019 |pmid=20705215 |s2cid=29830155}} Pregabalin is as effective at relieving pain as duloxetine and amitriptyline. Combination treatment of pregabalin and amitriptyline or duloxetine offers additional pain relief for people whose pain is not adequately controlled with one medication and is safe.{{cite journal |date=April 6, 2023 |title=Combination therapy for painful diabetic neuropathy is safe and effective |journal=NIHR Evidence |language=en |doi=10.3310/nihrevidence_57470 |s2cid=258013544 |url=https://evidence.nihr.ac.uk/alert/combination-therapy-for-painful-diabetic-neuropathy-is-safe-and-effective/ |url-access=subscription |access-date=April 28, 2023 |url-status=live |archive-url=https://web.archive.org/web/20230428104720/https://evidence.nihr.ac.uk/alert/combination-therapy-for-painful-diabetic-neuropathy-is-safe-and-effective/ |archive-date=April 28, 2023}}{{cite journal |vauthors=Tesfaye S, Sloan G, Petrie J, White D, Bradburn M, Julious S, Rajbhandari S, Sharma S, Rayman G, Gouni R, Alam U, Cooper C, Loban A, Sutherland K, Glover R, Waterhouse S, Turton E, Horspool M, Gandhi R, Maguire D, Jude EB, Ahmed SH, Vas P, Hariman C, McDougall C, Devers M, Tsatlidis V, Johnson M, Rice AS, Bouhassira D, Bennett DL, Selvarajah D |title=Comparison of amitriptyline supplemented with pregabalin, pregabalin supplemented with amitriptyline, and duloxetine supplemented with pregabalin for the treatment of diabetic peripheral neuropathic pain (OPTION-DM): a multicentre, double-blind, randomised crossover trial |journal=Lancet |volume=400 |issue=10353 |pages=680–690 |date=August 2022 |doi=10.1016/s0140-6736(22)01472-6 |pmc=9418415 |pmid=36007534}}

Studies have shown that higher doses of pregabalin are associated with greater efficacy.{{cite journal |vauthors=Freynhagen R, Baron R, Kawaguchi Y, Malik RA, Martire DL, Parsons B, Rey RD, Schug SA, Jensen TS, Tölle TR, Ushida T, Whalen E |title=Pregabalin for neuropathic pain in primary care settings: recommendations for dosing and titration |journal=Postgraduate Medicine |volume=133 |issue=1 |pages=1–9 |date=January 2021 |publisher=Informa UK Limited |doi=10.1080/00325481.2020.1857992 |doi-access=free |pmid=33423590 |s2cid=231574963 |url=https://pure.au.dk/portal/files/274258964/00325481.2020.pdf |access-date=February 19, 2024 |url-status=live |archive-url=https://web.archive.org/web/20240227025752/https://pure.au.dk/ws/portalfiles/portal/274258964/00325481.2020.pdf |archive-date=February 27, 2024}}

Pregabalin's use in cancer-associated neuropathic pain is controversial,{{cite journal |vauthors=Bennett MI, Laird B, van Litsenburg C, Nimour M |title=Pregabalin for the management of neuropathic pain in adults with cancer: a systematic review of the literature |journal=Pain Medicine |volume=14 |issue=11 |pages=1681–1688 |date=November 2013 |title-link=doi |doi=10.1111/pme.12212 |doi-access=free |pmid=23915361}} though such use is common.{{cite book |vauthors=Howard P |title=Palliative care formulary. |date=2017 |publisher=Pharmaceutical press |isbn=978-0-85711-348-1 |edition=6 |page=Chapter 4 Central Nervous System}} It has been examined for the prevention of post-surgical chronic pain, but its utility for this purpose is controversial.{{cite journal |vauthors=Clarke H, Bonin RP, Orser BA, Englesakis M, Wijeysundera DN, Katz J |title=The prevention of chronic postsurgical pain using gabapentin and pregabalin: a combined systematic review and meta-analysis |journal=Anesthesia and Analgesia |volume=115 |issue=2 |pages=428–442 |date=August 2012 |doi=10.1213/ANE.0b013e318249d36e |hdl=10315/27968 |hdl-access=free |pmid=22415535 |s2cid=18933131}}{{cite journal |vauthors=Chaparro LE, Smith SA, Moore RA, Wiffen PJ, Gilron I |title=Pharmacotherapy for the prevention of chronic pain after surgery in adults |journal=The Cochrane Database of Systematic Reviews |volume=2021 |issue=7 |pages=CD008307 |date=July 2013 |doi=10.1002/14651858.CD008307.pub2 |pmc=6481826 |pmid=23881791}}

Pregabalin is generally not regarded as efficacious in the treatment of acute pain. In trials examining the utility of pregabalin for the treatment of acute post-surgical pain, no effect on overall pain levels was observed, but people did require less morphine and had fewer opioid-related side effects.{{cite journal |vauthors=Hamilton TW, Strickland LH, Pandit HG |title=A Meta-Analysis on the Use of Gabapentinoids for the Treatment of Acute Postoperative Pain Following Total Knee Arthroplasty |journal=The Journal of Bone and Joint Surgery. American Volume |volume=98 |issue=16 |pages=1340–1350 |date=August 2016 |doi=10.2106/jbjs.15.01202 |pmid=27535436 |url=https://ora.ox.ac.uk/objects/uuid:cbe29197-14a9-47dc-b961-2ad3e24fd1c0 |url-access=subscription |access-date=August 24, 2020 |url-status=live |archive-url=https://web.archive.org/web/20200929012600/https://ora.ox.ac.uk/objects/uuid:cbe29197-14a9-47dc-b961-2ad3e24fd1c0 |archive-date=September 29, 2020}} Several possible mechanisms for pain improvement have been discussed.{{cite journal |vauthors=Patel R, Dickenson AH |title=Mechanisms of the gabapentinoids and α 2 δ-1 calcium channel subunit in neuropathic pain |journal=Pharmacology Research & Perspectives |volume=4 |issue=2 |pages=e00205 |date=April 2016 |doi=10.1002/prp2.205 |pmc=4804325 |pmid=27069626}}

Pregabalin is effective for treatment of generalized anxiety disorder.{{cite journal |vauthors=Slee A, Nazareth I, Bondaronek P, Liu Y, Cheng Z, Freemantle N |title=Pharmacological treatments for generalised anxiety disorder: a systematic review and network meta-analysis |journal=Lancet |volume=393 |issue=10173 |pages=768–777 |date=February 2019 |doi=10.1016/S0140-6736(18)31793-8 |pmid=30712879 |s2cid=72332967 |url=https://discovery.ucl.ac.uk/id/eprint/10070219/1/Freemantle_Slee_GAD_Meta_Text%20R1_20180627%20clean.pdf |access-date=September 8, 2020 |url-status=live |archive-url=https://web.archive.org/web/20200313031825/https://discovery.ucl.ac.uk/id/eprint/10070219/1/Freemantle_Slee_GAD_Meta_Text%20R1_20180627%20clean.pdf |archive-date=March 13, 2020}}; {{cite web |title=Supplemental Appendices |date=June 5, 2018 |url=https://discovery.ucl.ac.uk/id/eprint/10070219/7/Freemantle_Slee_GAD_Web_Appendix%20R1_20180627.pdf |archive-url=https://web.archive.org/web/20200309183455/https://discovery.ucl.ac.uk/id/eprint/10070219/7/Freemantle_Slee_GAD_Web_Appendix%20R1_20180627.pdf |archive-date=March 9, 2020}}; {{cite web |title=Authors' Reply |date=June 5, 2018 |url=https://discovery.ucl.ac.uk/id/eprint/10084194/3/Nazareth_Lancet%20Correspondence051019.pdf |archive-url=https://web.archive.org/web/20201017231136/https://discovery.ucl.ac.uk/id/eprint/10084194/3/Nazareth_Lancet%20Correspondence051019.pdf |archive-date=October 17, 2020}} It is also effective for the short- and long-term treatment of social anxiety disorder and in reducing preoperative anxiety.{{cite journal |date=October 17, 2022 |title=Review finds little evidence to support gabapentinoid use in bipolar disorder or insomnia |journal=NIHR Evidence |type=Plain English summary |language=en |publisher=National Institute for Health and Care Research |doi=10.3310/nihrevidence_54173 |s2cid=252983016 |url=https://evidence.nihr.ac.uk/alert/review-finds-little-evidence-support-gabapentinoid-use-bipolar-disorder-or-insomnia/ |url-access=subscription |access-date=October 27, 2022 |url-status=live |archive-url=https://web.archive.org/web/20221127080508/https://evidence.nihr.ac.uk/alert/review-finds-little-evidence-support-gabapentinoid-use-bipolar-disorder-or-insomnia/ |archive-date=November 27, 2022}}{{cite journal |vauthors=Hong JS, Atkinson LZ, Al-Juffali N, Awad A, Geddes JR, Tunbridge EM, Harrison PJ, Cipriani A |title=Gabapentin and pregabalin in bipolar disorder, anxiety states, and insomnia: Systematic review, meta-analysis, and rationale |journal=Molecular Psychiatry |volume=27 |issue=3 |pages=1339–1349 |date=March 2022 |doi=10.1038/s41380-021-01386-6 |pmc=9095464 |pmid=34819636}} However, there is concern regarding pregabalin's off-label use due to the lack of strong scientific evidence for its efficacy in multiple conditions and its proven side effects.{{cite journal |vauthors=Hong JS, Atkinson LZ, Al-Juffali N, Awad A, Geddes JR, Tunbridge EM, Harrison PJ, Cipriani A |date=March 2022 |title=Gabapentin and pregabalin in bipolar disorder, anxiety states, and insomnia: Systematic review, meta-analysis, and rationale |journal=Molecular Psychiatry |volume=27 |issue=3 |pages=1339–1349 |doi=10.1038/s41380-021-01386-6 |pmc=9095464 |pmid=34819636}}

The World Federation of Biological Psychiatry recommends pregabalin as one of several first line agents for the treatment of generalized anxiety disorder, but recommends other agents such as those of the selective serotonin reuptake inhibitor (SSRI) class as first line treatment for obsessive–compulsive disorder (OCD) and post-traumatic stress disorder (PTSD).{{cite journal |vauthors=Bandelow B, Sher L, Bunevicius R, Hollander E, Kasper S, Zohar J, Möller HJ |date=June 2012 |title=Guidelines for the pharmacological treatment of anxiety disorders, obsessive-compulsive disorder and posttraumatic stress disorder in primary care |journal=International Journal of Psychiatry in Clinical Practice |volume=16 |issue=2 |pages=77–84 |doi=10.3109/13651501.2012.667114 |pmid=22540422 |s2cid=16253034 |url=https://www.wfsbp.org/fileadmin/user_upload/Treatment_Guidelines/Bandelow_et_al_01.pdf |access-date=October 16, 2020 |url-status=live |archive-url=https://web.archive.org/web/20180403134713/http://www.wfsbp.org/fileadmin/user_upload/Treatment_Guidelines/Bandelow_et_al_01.pdf |archive-date=April 3, 2018}}{{cite journal |vauthors=Wensel TM, Powe KW, Cates ME |date=March 2012 |title=Pregabalin for the treatment of generalized anxiety disorder |journal=The Annals of Pharmacotherapy |volume=46 |issue=3 |pages=424–429 |doi=10.1345/aph.1Q405 |pmid=22395254 |s2cid=26320851}} For PTSD, pregabalin as complementary treatment seems to be effective.

Pregabalin has anxiolytic effects similar to benzodiazepines with less risk of dependence. The effects of pregabalin appear within one week of use,{{cite web |title=How long does it take for Lyrica to work? |website=Drugs.com |date=May 25, 2021 |url=https://www.drugs.com/medical-answers/long-lyrica-work-3558304/ |access-date=February 18, 2022 |url-status=live |archive-url=https://web.archive.org/web/20220218195925/https://www.drugs.com/medical-answers/long-lyrica-work-3558304/ |archive-date=February 18, 2022}} and are similar in effectiveness to lorazepam, alprazolam, and bromazepam, but pregabalin has demonstrated superiority by producing more consistent therapeutic effects for psychosomatic anxiety symptoms. Long-term trials have shown continued effectiveness without the development of tolerance, and, in addition, unlike benzodiazepines, it has a beneficial effect on sleep and sleep architecture, characterized by the enhancement of slow-wave sleep. It produces less severe cognitive and psychomotor impairment compared to benzodiazepines.{{cite journal |vauthors=Bandelow B, Wedekind D, Leon T |title=Pregabalin for the treatment of generalized anxiety disorder: a novel pharmacologic intervention |journal=Expert Review of Neurotherapeutics |volume=7 |issue=7 |pages=769–781 |date=July 2007 |doi=10.1586/14737175.7.7.769 |pmid=17610384 |s2cid=6229344}}{{cite journal |vauthors=Owen RT |title=Pregabalin: its efficacy, safety and tolerability profile in generalized anxiety |journal=Drugs of Today |volume=43 |issue=9 |pages=601–610 |date=September 2007 |doi=10.1358/dot.2007.43.9.1133188 |pmid=17940637}}

A 2019 review found that pregabalin reduces symptoms, and was generally well tolerated.

Although pregabalin is sometimes prescribed for people with bipolar disorder, there is no evidence showing that it is effective.{{cite journal |vauthors=Ng QX, Han MX, Teoh SE, Yaow CY, Lim YL, Chee KT |title=A Systematic Review of the Clinical Use of Gabapentin and Pregabalin in Bipolar Disorder |journal=Pharmaceuticals |volume=14 |issue=9 |pages=834 |date=August 2021 |doi=10.3390/ph14090834 |doi-access=free |pmc=8469561 |pmid=34577534}}

There is no evidence and significant risk in using pregabalin for sciatica and low back pain.{{cite journal |vauthors=Giménez-Campos MS, Pimenta-Fermisson-Ramos P, Díaz-Cambronero JI, Carbonell-Sanchís R, López-Briz E, Ruíz-García V |title=A systematic review and meta-analysis of the effectiveness and adverse events of gabapentin and pregabalin for sciatica pain |journal=Atencion Primaria |volume=54 |issue=1 |pages=102144 |date=January 2022 |publisher=Elsevier BV |doi=10.1016/j.aprim.2021.102144 |pmc=8515246 |pmid=34637958}}{{cite journal |vauthors=Shanthanna H, Gilron I, Rajarathinam M, AlAmri R, Kamath S, Thabane L, Devereaux PJ, Bhandari M |title=Benefits and safety of gabapentinoids in chronic low back pain: A systematic review and meta-analysis of randomized controlled trials |journal=PLOS Medicine |volume=14 |issue=8 |pages=e1002369 |date=August 2017 |doi=10.1371/journal.pmed.1002369 |doi-access=free |pmc=5557428 |pmid=28809936}}{{cite news |vauthors=Mannix L |date=December 18, 2018 |title=This popular drug is linked to addiction and suicide. Why do doctors keep prescribing it? |work=The Canberra Times |url=https://www.canberratimes.com.au/national/victoria/this-popular-drug-is-linked-to-addiction-and-suicide-why-do-doctors-keep-prescribing-it-20181129-p50j1x.html |access-date=December 18, 2018 |archive-url=https://web.archive.org/web/20181218193541/https://www.canberratimes.com.au/national/victoria/this-popular-drug-is-linked-to-addiction-and-suicide-why-do-doctors-keep-prescribing-it-20181129-p50j1x.html |archive-date=December 18, 2018}} Evidence of benefit in alcohol withdrawal as well as withdrawal from certain other drugs is limited as of 2016.{{cite journal |vauthors=Freynhagen R, Backonja M, Schug S, Lyndon G, Parsons B, Watt S, Behar R |title=Pregabalin for the Treatment of Drug and Alcohol Withdrawal Symptoms: A Comprehensive Review |journal=CNS Drugs |volume=30 |issue=12 |pages=1191–1200 |date=December 2016 |doi=10.1007/s40263-016-0390-z |pmc=5124051 |pmid=27848217}}

There is no evidence for its use in the prevention of migraines and gabapentin has also been found not to be useful.{{cite journal |vauthors=Linde M, Mulleners WM, Chronicle EP, McCrory DC |title=Gabapentin or pregabalin for the prophylaxis of episodic migraine in adults |journal=The Cochrane Database of Systematic Reviews |volume=6 |issue=6 |pages=CD010609 |date=June 2013 |doi=10.1002/14651858.CD010609 |pmc=6599858 |pmid=23797675}}

A 2025 review found possible benefits in sleep quality in fibromyalgia.{{cite journal | vauthors = Pathak A, Kelleher EM, Brennan I, Amarnani R, Wall A, Murphy R, Lee H, Fordham B, Irani A | title = Treatments for enhancing sleep quality in fibromyalgia: a systematic review and meta-analysis | journal = Rheumatology | pages = keaf147 | date = March 2025 | pmid = 40084994 | doi = 10.1093/rheumatology/keaf147 | doi-access = free }}

Exposure to pregabalin is associated with weight gain, drowsiness, fatigue, dizziness, vertigo, leg swelling, disturbed vision, loss of coordination, and euphoria.{{cite journal |vauthors=Onakpoya IJ, Thomas ET, Lee JJ, Goldacre B, Heneghan CJ |title=Benefits and harms of pregabalin in the management of neuropathic pain: a rapid review and meta-analysis of randomised clinical trials |journal=BMJ Open |volume=9 |issue=1 |pages=e023600 |date=January 2019 |doi=10.1136/bmjopen-2018-023600 |pmc=6347863 |pmid=30670513}} It has an adverse effect profile similar to other central nervous system (CNS) depressants. Even though pregabalin is a depressant and anticonvulsant, it can sometimes paradoxically induce seizures, particularly in large overdoses.{{cite journal |vauthors=Slocum GW, Schult RF, Gorodetsky RM, Wiegand TJ, Kamali M, Acquisto NM |date=January 1, 2018 |title=Pregabalin and paradoxical reaction of seizures in a large overdose |journal=Toxicology Communications |volume=2 |issue=1 |pages=19–20 |doi=10.1080/24734306.2018.1458465 |doi-access=free |s2cid=79760296}} Adverse drug reactions associated with the use of pregabalin include:{{cite journal | vauthors = Semel D, Murphy TK, Zlateva G, Cheung R, Emir B | title = Evaluation of the safety and efficacy of pregabalin in older patients with neuropathic pain: results from a pooled analysis of 11 clinical studies | journal = BMC Family Practice | volume = 11 | issue = 1 | pages = 85 | date = November 2010 | pmid = 21054853 | pmc = 2988717 | doi = 10.1186/1471-2296-11-85 | doi-access = free }}{{citation |publisher=Pfizer Australia Pty Ltd. |title=Lyrica (Australian Approved Product Information) |newspaper=Pfizer: The World's Largest Research-Based Pharmaceutical Company |year=2006|archive-url=https://web.archive.org/web/20180313141049/https://www.pfizer.com.au/products/lyrica |url=https://www.pfizer.com.au/products/lyrica |archive-date=March 13, 2018}}{{cite book |title=Australian Medicines Handbook, 2006 |publisher=Australian Medicines Handbook |year=2006 |isbn=978-0-9757919-2-9 |veditors=Rossi S}}{{page needed|date=August 2016}}

• Very common (>10% of people with pregabalin): dizziness, drowsiness.
• Common (1–10% of people with pregabalin): peripheral edema, blurred vision, diplopia, increased appetite and subsequent weight gain, euphoria, confusion, vivid dreams, changes in libido (increase or decrease), irritability, ataxia, attention changes, feeling high, memory impairment, tremor, dysarthria, paresthesia, vertigo, dry mouth, constipation, nausea, vomiting, flatulence, erectile dysfunction, fatigue, feelings of drunkenness, abnormal walking, asthenia, nasopharyngitis, increased creatine kinase level.
• Infrequent (0.1–1% of people with pregabalin): depression, lethargy, agitation, anorgasmia, hallucinations, myoclonus, hypoaesthesia, hyperaesthesia, tachycardia, hypersalivation, hypoglycaemia, excessive sweating, flushing, rash, muscle cramp, myalgia, arthralgia, urinary incontinence, dysuria, thrombocytopenia, kidney calculus.
• Rare (<0.1% of people with pregabalin): neutropenia, first-degree heart block, hypotension, hypertension, pancreatitis, dysphagia, oliguria, rhabdomyolysis, suicidal thoughts or behavior.{{cite web |date=June 2011 |title=Medication Guide (Pfizer Inc.) |publisher=U.S. Food and Drug Administration (FDA) |url=https://www.fda.gov/downloads/Drugs/DrugSafety/UCM152825.pdf |access-date=November 6, 2011 |archive-url=https://web.archive.org/web/20110908154358/http://www.fda.gov/downloads/Drugs/DrugSafety/UCM152825.pdf |archive-date=September 8, 2011}}

Cases of recreational use, with associated adverse effects, have been reported.{{cite journal |vauthors=Millar J, Sadasivan S, Weatherup N, Lutton S |date=September 7, 2013 |title=Lyrica Nights–Recreational Pregabalin Abuse in an Urban Emergency Department |journal=Emergency Medicine Journal |volume=30 |issue=10 |pages=874.2–874 |doi=10.1136/emermed-2013-203113.20 |s2cid=73986091}}

Following abrupt or rapid discontinuation of pregabalin, some people reported symptoms suggestive of physical dependence. The FDA determined that the substance dependence profile of pregabalin, as measured by a personal physical withdrawal checklist, was quantitatively less than benzodiazepines.

Even people who have discontinued short-term use of pregabalin have experienced withdrawal symptoms including insomnia, headache, heart palpitations, nausea, anxiety, diarrhea, flu-like symptoms, major depression, pain, seizures, excessive sweating, muscle twitching, and dizziness.{{cite web |title=Lyrica Capsules |website=medicines.org.uk |url=https://www.medicines.org.uk/EMC/medicine/14651/SPC/Lyrica+Capsules/ |access-date=October 19, 2020 |url-status=live |archive-url=https://web.archive.org/web/20201020191035/https://www.medicines.org.uk/EMC/medicine/14651/SPC/Lyrica+Capsules/ |archive-date=October 20, 2020}}

A tapered discontinuation is recommended to reduce the chances of withdrawal symptoms. Lyrica's US package insert recommends a taper period of at least one week.{{cite web |title=LYRICA (pregabalin) Capsules & Oral Solution, CV |url=https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021446s035,022488s013lbl.pdf |archive-url=https://web.archive.org/web/20200212033514/https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021446s035,022488s013lbl.pdf |url-status=dead |archive-date=February 12, 2020 |website=accessdata.fda.gov |access-date=February 26, 2025 |date=2018}} Best Practice Advocacy Centre New Zealand{{cite web |title=Deprescribing gabapentinoids - bpacnz |url=https://bpac.org.nz/2024/deprescribing-gabapentin.aspx |website=bpac.org.nz}} and NHS Somerset{{cite web | author = NHS Somerset Integrated Care Board |title=Gabapentinoid suggested tapering regimes |url=https://nhssomerset.nhs.uk/wp-content/uploads/sites/2/ICB-tapering-gabapentinoid-v1approved-2.docx}} recommend a much slower withdrawal.

It is unclear if it is safe for use in pregnancy with some studies showing potential harm.{{cite web |title=Pregabalin Pregnancy and Breastfeeding Warnings |url=https://www.drugs.com/pregnancy/pregabalin.html |access-date=August 29, 2016 |url-status=live |archive-url=https://web.archive.org/web/20190321033634/https://www.drugs.com/pregnancy/pregabalin.html |archive-date=March 21, 2019}}

In December 2019, the US Food and Drug Administration (FDA) warned about serious breathing issues for those taking gabapentin or pregabalin when used with central nervous system (CNS) depressants or for those with lung problems.{{cite web |date=December 19, 2019 |title=FDA warns about serious breathing problems with seizure and nerve pain medicines gabapentin (Neurontin, Gralise, Horizant) and pregabalin (Lyrica, Lyrica CR) When used with CNS depressants or in patients with lung problems |website=U.S. Food and Drug Administration (FDA) |url=https://www.fda.gov/drugs/drug-safety-and-availability/fda-warns-about-serious-breathing-problems-seizure-and-nerve-pain-medicines-gabapentin-neurontin |access-date=December 21, 2019 |url-status=dead |archive-url=https://web.archive.org/web/20191222091828/https://www.fda.gov/drugs/drug-safety-and-availability/fda-warns-about-serious-breathing-problems-seizure-and-nerve-pain-medicines-gabapentin-neurontin |archive-date=December 22, 2019}} {{Source-attribution}}{{cite web |date=December 19, 2019 |title=FDA warns about serious breathing problems with seizure and nerve pain medicines gabapentin (Neurontin, Gralise, Horizant) and pregabalin (Lyrica, Lyrica CR) When used with CNS depressants or in patients with lung problems |website=U.S. Food and Drug Administration (FDA) |format=PDF |url=https://www.fda.gov/media/133681/download |url-status=live |archive-url=https://web.archive.org/web/20191222091828/https://www.fda.gov/media/133681/download |archive-date=December 22, 2019}} {{Source-attribution}}

The FDA required new warnings about the risk of respiratory depression to be added to the prescribing information of the gabapentinoids. The FDA also required the drug manufacturers to conduct clinical trials to further evaluate their abuse potential, particularly in combination with opioids, because misuse and abuse of these products together is increasing, and co-use may increase the risk of respiratory depression.

Among 49 case reports submitted to the FDA over the five-year period from 2012 to 2017, twelve people died from respiratory depression with gabapentinoids, all of whom had at least one risk factor.

The FDA reviewed the results of two randomized, double-blind, placebo-controlled clinical trials in healthy people, three observational studies, and several studies in animals. One trial showed that using pregabalin alone and using it with an opioid pain reliever can depress breathing function. The other trial showed gabapentin alone increased pauses in breathing during sleep. The three observational studies at one academic medical center showed a relationship between gabapentinoids given before surgery and respiratory depression occurring after different kinds of surgeries. The FDA also reviewed several animal studies that showed pregabalin alone and pregabalin plus opioids can depress respiratory function.

Pregabalin has potential for recreational use and abuse. It possesses a relatively wide therapeutic index and margin of safety compared to other central nervous system (CNS) depressants, and its effects may include euphoria, anxiolysis, and sedation.

Although generally considered to have low abuse potential, reports describe pregabalin inducing sensations of euphoria, calmness, excitement, and a "high" comparable to that of marijuana. These effects may contribute to the development of substance dependence, and withdrawal symptoms can occur if the medication is stopped abruptly.{{cite web |title=Is Lyrica a controlled substance / Narcotic? |url=https://www.drugs.com/medical-answers/lyrica-controlled-substance-narcotic-3571636/ |access-date=May 6, 2024 |url-status=live |archive-url=https://web.archive.org/web/20240204164725/https://www.drugs.com/medical-answers/lyrica-controlled-substance-narcotic-3571636/ |archive-date=February 4, 2024}}{{cite book |date=2024 |title=Prescription of Controlled Substances: Benefits and Risks |vauthors=Preuss CV, Kalava A, King KC |pmid=30726003}}

While pregabalin and marijuana share certain effects, such as CNS depressant and orexigenic (appetite-stimulating) properties, they differ significantly in their pharmacodynamics. Marijuana is primarily an anxiogenic substance with mild psychedelic effects, whereas pregabalin is an anxiolytic agent associated with mild euphoria.{{cite journal | vauthors = Sharpe L, Sinclair J, Kramer A, de Manincor M, Sarris J | title = Cannabis, a cause for anxiety? A critical appraisal of the anxiogenic and anxiolytic properties | journal = Journal of Translational Medicine | volume = 18 | issue = 1 | pages = 374 | date = October 2020 | pmid = 33008420 | pmc = 7531079 | doi = 10.1186/s12967-020-02518-2| doi-access = free }}{{cite journal | vauthors = Schjerning O, Rosenzweig M, Pottegård A, Damkier P, Nielsen J | title = Abuse Potential of Pregabalin: A Systematic Review | journal = CNS Drugs | volume = 30 | issue = 1 | pages = 9–25 | date = January 2016 | pmid = 26767525 | doi = 10.1007/s40263-015-0303-6 }}

An overdose of pregabalin usually consists of severe drowsiness, severe ataxia, blurred vision, slurred speech, uncontrollable jerking motions (myoclonus), and anxiety.{{cite journal |vauthors=Desai A, Kherallah Y, Szabo C, Marawar R |title=Gabapentin or pregabalin induced myoclonus: A case series and literature review |journal=Journal of Clinical Neuroscience |volume=61 |pages=225–234 |date=March 2019 |doi=10.1016/j.jocn.2018.09.019 |pmid=30381161 |s2cid=53165515}} In one case study, macular detachment was reported with overdose{{cite journal |vauthors=Tanyıldız B, Kandemir B, Mangan MS, Tangılntız A, Göktaş E, Şimşek S |date=October 2018 |title=Bilateral Serous Macular Detachment After Attempted Suicide with Pregabalin |journal=Turkish Journal of Ophthalmology |volume=48 |issue=5 |pages=254–257 |doi=10.4274/tjo.70923 |pmc=6216534 |pmid=30405948}} Despite these symptoms an overdose is not usually fatal unless mixed with another CNS depressant. Several people with kidney failure developed myoclonus while receiving pregabalin, apparently as a result of the gradual accumulation of the drug. Acute overdosage may be manifested by drowsiness, tachycardia, and hypertonia. Plasma, serum, or blood concentrations of pregabalin may be measured to monitor therapy or to confirm a diagnosis of poisoning in hospitalized people.{{cite journal |vauthors=Murphy NG, Mosher L |year=2008 |title=79. Severe myoclonus from pregabalin (Lyrica) due to chronic renal insufficiency |journal=Clinical Toxicology |volume=46 |issue=7 |page=604 |title-link=doi |doi=10.1080/15563650802255033 |doi-access=free |s2cid=218857181}}{{cite journal |vauthors=Yoo L, Matalon D, Hoffman RS, Goldfarb DS |title=Treatment of pregabalin toxicity by hemodialysis in a patient with kidney failure |journal=American Journal of Kidney Diseases |volume=54 |issue=6 |pages=1127–1130 |date=December 2009 |format=PDF |citeseerx=10.1.1.955.4223 |doi=10.1053/j.ajkd.2009.04.014 |pmid=19493601 |url=http://citeseerx.ist.psu.edu/viewdoc/download?doi=10.1.1.955.4223&rep=rep1&type=pdf |access-date=October 19, 2020 |url-status=live |archive-url=https://web.archive.org/web/20220412003441/http://citeseerx.ist.psu.edu/viewdoc/download?doi=10.1.1.955.4223&rep=rep1&type=pdf |archive-date=April 12, 2022}}{{cite book |vauthors=Baselt RC |title=Disposition of Toxic Drugs and Chemicals in Man |publisher=Biomedical Publications |year=2008 |isbn=978-0-9626523-7-0 |edition=8th |pages=1296–1297}}

No drug interactions have been demonstrated in vivo. However, the manufacturer notes potential pharmacological interactions with opioids, benzodiazepines, barbiturates, ethanol (alcohol), and other central nervous system depressants. Concurrent use of ACE inhibitors and pregabalin may increase the risk of angioedema. Pregabalin may also enhance the fluid-retaining effects of certain antidiabetic agents, such as thiazolidinediones.{{cite web |title=Pregabalin |work=Lexi-Drugs [database on the Internet |location=Hudson (OH) |publisher=Lexi-Comp, Inc. |date=2007 |url=https://www.localhealthrx.com/drugs/pregabalin/ |access-date=October 29, 2015 |url-status=dead |archive-url=https://web.archive.org/web/20201019225603/https://www.localhealthrx.com/drugs/pregabalin/ |archive-date=October 19, 2020}}.

Pregabalin may independently increase the risk of angioedema, and this risk is further elevated when used in combination with other drugs known to increase the likelihood of angioedema. These include, but are not limited to, certain L-type calcium channel blockers, ACE inhibitors, angiotensin II receptor blockers, and other agents that inhibit the renin–angiotensin–aldosterone system.{{cite web | work = MedCentral. | title = Pregabalin oral | access-date = January 31, 2025 | url = https://www.medcentral.com/drugs/monograph/93954-305048/pregabalin-oral }}

Pregabalin can also cause rare but serious adverse effects,{{cite journal | vauthors = Zhang M, Du K, Lu Y, Wu W, Yan H, Jiang Q, Liu L, Feng X | title = Pregabalin-induced delayed cutaneous hypersensitivity reaction occurring after 40 days of use: a case report | journal = The Journal of International Medical Research | volume = 52 | issue = 4 | pages = 3000605241245004 | date = April 2024 | pmid = 38635889 | pmc = 11032052 | doi = 10.1177/03000605241245004 }} particularly when used in combination with other CNS depressants.{{cite web |title=Control of pregabalin and gabapentin under the Misuse of Drugs Act 1971 |url=https://www.gov.uk/government/publications/circular-0192018-control-of-pregabalin-and-gabapentin-under-the-misuse-of-drugs-act-1971/control-of-pregabalin-and-gabapentin-under-the-misuse-of-drugs-act-1971 |url-status=live |archive-url=https://web.archive.org/web/20240221044657/https://www.gov.uk/government/publications/circular-0192018-control-of-pregabalin-and-gabapentin-under-the-misuse-of-drugs-act-1971/control-of-pregabalin-and-gabapentin-under-the-misuse-of-drugs-act-1971 |archive-date=February 21, 2024 |access-date=February 21, 2024}}{{cite web |title=Pregabalin and gabapentin to be controlled as class C drugs |url=https://www.gov.uk/government/news/pregabalin-and-gabapentin-to-be-controlled-as-class-c-drugs |access-date=April 2, 2020 |url-status=live |archive-url=https://web.archive.org/web/20201112034051/https://www.gov.uk/government/news/pregabalin-and-gabapentin-to-be-controlled-as-class-c-drugs |archive-date=November 12, 2020}}

{{Main article|Gabapentinoid}}

Pregabalin is a gabapentinoid medication, meaning drugs that chemically are derivatives of γ-aminobutyric acid (GABA), an inhibitory neurotransmitter. However, pregabalin, like other gabapentinoids, does not mimic GABA or influence GABA receptors. Instead, its action requires binding to a specific site on the α₂δ-1 protein and secondarily to reduce the release of excitatory neurotransmitters.

Pregabalin does not directly block calcium channels (it is not a calcium channel blocker), as it does not bind to the ion conducting channel protein, called α1. However, in vitro studies show that pregabalin can reduce the normal traffic of calcium channels from intracellular sites (where they do not function) to membrane sites where they are functional.

While the mechanism of action of pregabalin is not definitively characterized, its action in animal models of pain, seizures and anxiety requires binding to the α₂δ-1 protein.{{cite journal | vauthors = Taylor CP, Harris EW | title = Analgesia with Gabapentin and Pregabalin May Involve N-Methyl-d-Aspartate Receptors, Neurexins, and Thrombospondins | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 374 | issue = 1 | pages = 161–174 | date = July 2020 | pmid = 32321743 | doi = 10.1124/jpet.120.266056 }} It has been found that this binding inhibits several actions of α2δ-1 and also inhibits the release of excitatory neurotransmitters. These excitatory neurotransmitters include glutamate, norepinephrine (noradrenaline), serotonin, dopamine, substance P, and calcitonin gene-related peptide.{{cite journal | vauthors = Dooley DJ, Taylor CP, Donevan S, Feltner D | title = Ca2+ channel alpha2delta ligands: novel modulators of neurotransmission | journal = Trends in Pharmacological Sciences | volume = 28 | issue = 2 | pages = 75–82 | date = February 2007 | pmid = 17222465 | doi = 10.1016/j.tips.2006.12.006 }} By inhibiting the release of these neurotransmitters, pregabalin reduces excess activity of neuron networks, which helps alleviate symptoms and provides relief for patients experiencing pain, seizures, or other related symptoms.{{cite journal | vauthors = Holsboer-Trachsler E, Prieto R | title = Effects of pregabalin on sleep in generalized anxiety disorder | journal = The International Journal of Neuropsychopharmacology | volume = 16 | issue = 4 | pages = 925–936 | date = May 2013 | pmid = 23009881 | doi = 10.1017/S1461145712000922 }}

File:Gabapentinoids.png

File:Voltage gated calcium channel.jpg]]

There are two drug-binding α₂δ subunits, α₂δ-1 and α₂δ-2, and pregabalin shows similar affinity for (and hence lack of selectivity between) these two sites. Pregabalin is selective in its binding to the α₂δ VGCC subunits and does not bind significantly to other known drug receptors.{{cite journal |vauthors=Sills GJ |date=February 2006 |title=The mechanisms of action of gabapentin and pregabalin |journal=Current Opinion in Pharmacology |volume=6 |issue=1 |pages=108–113 |doi=10.1016/j.coph.2005.11.003 |pmid=16376147}}

Despite the fact that pregabalin is a GABA analogue,{{cite journal |vauthors=Bryans JS, Wustrow DJ |title=3-substituted GABA analogs with central nervous system activity: a review |journal=Medicinal Research Reviews |volume=19 |issue=2 |pages=149–177 |date=March 1999 |doi=10.1002/(SICI)1098-1128(199903)19:2<149::AID-MED3>3.0.CO;2-B |pmid=10189176 |s2cid=38496241}} it does not bind to GABA receptors, does not convert into {{abbrlink|GABA|γ-aminobutyric acid}} or another GABA receptor agonist in vivo, and does not directly modulate GABA transport or metabolism. There is currently no evidence that the effects of pregabalin are mediated by any mechanism other than binding to the α₂δ-1 protein.{{cite journal |vauthors=Stahl SM, Porreca F, Taylor CP, Cheung R, Thorpe AJ, Clair A |title=The diverse therapeutic actions of pregabalin: is a single mechanism responsible for several pharmacological activities? |journal=Trends in Pharmacological Sciences |volume=34 |issue=6 |pages=332–339 |date=June 2013 |doi=10.1016/j.tips.2013.04.001 |pmid=23642658}} In accordance, inhibition of α₂δ-1 proteins by pregabalin appears to be responsible for its anticonvulsant, analgesic, and anxiolytic effects in animal models.

Recently, the α₂δ-1 protein has been found (independent of calcium channels) to associate directly with certain NMDA-type glutamate receptors, some AMPA-type glutamate receptors and also with the extracellular matrix protein, thrombospondin, and to modulate the function of these proteins. This has been proposed to contribute to the analgesic action of pregabalin animal models and in clinical use.

The endogenous α-amino acids L-leucine and L-isoleucine, which closely resemble pregabalin and the other gabapentinoids in chemical structure, are apparent ligands of the α₂δ VGCC subunit with similar affinity as the gabapentinoids (e.g., IC₅₀=71 nM for L-isoleucine), and are present in human cerebrospinal fluid at micromolar concentrations (e.g., 12.9 μM for L-leucine, 4.8 μM for L-isoleucine). It has been theorized that they may be the endogenous ligands of the subunit and that they may competitively antagonize the effects of gabapentinoids.{{cite journal |vauthors=Davies A, Hendrich J, Van Minh AT, Wratten J, Douglas L, Dolphin AC |title=Functional biology of the alpha(2)delta subunits of voltage-gated calcium channels |journal=Trends in Pharmacological Sciences |volume=28 |issue=5 |pages=220–228 |date=May 2007 |doi=10.1016/j.tips.2007.03.005 |pmid=17403543 |url=https://scholar.google.com/scholar?hl=en&as_sdt=0%2C5&q=Functional+biology+of+the+%CE%B12%CE%B4+subunits+of+voltage-gated+calcium+channels&btnG= |url-access=subscription |access-date=October 19, 2020 |url-status=live |archive-url=https://web.archive.org/web/20201021072722/https://scholar.google.com/scholar?hl=en&as_sdt=0,5&q=Functional+biology+of+the+%CE%B12%CE%B4+subunits+of+voltage-gated+calcium+channels&btnG= |archive-date=October 21, 2020}} In accordance, while gabapentinoids like pregabalin and gabapentin have nanomolar affinities for the α₂δ subunit, their potencies in vivo are in the low micromolar range, and competition for binding by endogenous L-amino acids has been said to likely be responsible for this discrepancy.

Pregabalin was found to possess 6-fold higher affinity than gabapentin for α₂δ subunit-containing VGCCs in one study.{{cite journal |vauthors=Baidya DK, Agarwal A, Khanna P, Arora MK |title=Pregabalin in acute and chronic pain |journal=Journal of Anaesthesiology Clinical Pharmacology |volume=27 |issue=3 |pages=307–314 |date=July 2011 |doi=10.4103/0970-9185.83672 |doi-access=free |pmc=3161452 |pmid=21897498}}{{cite book |vauthors=McMahon SB |title=Wall and Melzack's textbook of pain |date=2013 |publisher=Elsevier/Saunders |isbn=9780702040597 |edition=6th |location=Philadelphia, PA |page=515 |url=https://books.google.com/books?id=bNlvQJSqrB8C&pg=PA515}} However, another study found that pregabalin and gabapentin had similar affinities for the human recombinant α₂δ-1 subunit (K_i=32 nM and 40 nM, respectively).{{cite journal |vauthors=Taylor CP, Angelotti T, Fauman E |title=Pharmacology and mechanism of action of pregabalin: the calcium channel alpha2-delta (alpha2-delta) subunit as a target for antiepileptic drug discovery |journal=Epilepsy Research |volume=73 |issue=2 |pages=137–150 |date=February 2007 |doi=10.1016/j.eplepsyres.2006.09.008 |pmid=17126531 |s2cid=54254671 |url=https://scholar.google.com/scholar?hl=en&as_sdt=0%2C5&q=Pharmacology+and+mechanism+of+action+of+pregabalin%3A+The+calcium+channel+%CE%B12%E2%80%93%CE%B4+%28alpha2%E2%80%93delta%29+subunit+as+a+target+for+antiepileptic+drug+discovery&btnG= |url-access=subscription |access-date=October 19, 2020 |url-status=live |archive-url=https://web.archive.org/web/20201023083313/https://scholar.google.com/scholar?hl=en&as_sdt=0,5&q=Pharmacology+and+mechanism+of+action+of+pregabalin:+The+calcium+channel+%CE%B12%E2%80%93%CE%B4+(alpha2%E2%80%93delta)+subunit+as+a+target+for+antiepileptic+drug+discovery&btnG= |archive-date=October 23, 2020}} In any case, pregabalin is 2 to 4 times more potent than gabapentin as an analgesic and, in animals, appears to be 3 to 10 times more potent than gabapentin as an anticonvulsant.{{cite journal |vauthors=Lauria-Horner BA, Pohl RB |title=Pregabalin: a new anxiolytic |journal=Expert Opinion on Investigational Drugs |volume=12 |issue=4 |pages=663–672 |date=April 2003 |doi=10.1517/13543784.12.4.663 |pmid=12665421 |s2cid=36137322}}

Pregabalin is absorbed from the intestines by an active transport process mediated via the large neutral amino acid transporter 1 (LAT1, SLC7A5), a transporter for amino acids such as L-leucine and L-phenylalanine.{{cite journal |vauthors=Dickens D, Webb SD, Antonyuk S, Giannoudis A, Owen A, Rädisch S, Hasnain SS, Pirmohamed M |title=Transport of gabapentin by LAT1 (SLC7A5) |journal=Biochemical Pharmacology |volume=85 |issue=11 |pages=1672–1683 |date=June 2013 |doi=10.1016/j.bcp.2013.03.022 |pmid=23567998 |url=https://scholar.google.com/scholar?hl=en&as_sdt=0%2C5&q=+Transport+of+gabapentin+by+LAT1+%28SLC7A5%29+&btnG= |url-access=subscription |access-date=October 19, 2020 |url-status=live |archive-url=https://web.archive.org/web/20201021020947/https://scholar.google.com/scholar?hl=en&as_sdt=0,5&q=+Transport+of+gabapentin+by+LAT1+(SLC7A5)+&btnG= |archive-date=October 21, 2020}} Very few (less than 10 drugs) are known to be transported by this transporter.{{cite journal |vauthors=del Amo EM, Urtti A, Yliperttula M |title=Pharmacokinetic role of L-type amino acid transporters LAT1 and LAT2 |journal=European Journal of Pharmaceutical Sciences |volume=35 |issue=3 |pages=161–174 |date=October 2008 |doi=10.1016/j.ejps.2008.06.015 |pmid=18656534}} Unlike gabapentin, which is transported solely by the LAT1,{{cite journal |vauthors=Bockbrader HN, Radulovic LL, Posvar EL, Strand JC, Alvey CW, Busch JA, Randinitis EJ, Corrigan BW, Haig GM, Boyd RA, Wesche DL |title=Clinical pharmacokinetics of pregabalin in healthy volunteers |journal=Journal of Clinical Pharmacology |volume=50 |issue=8 |pages=941–950 |date=August 2010 |doi=10.1177/0091270009352087 |pmid=20147618 |s2cid=9905501}} pregabalin seems to be transported not only by the LAT1 but also by other carriers. The LAT1 is easily saturable, so the pharmacokinetics of gabapentin are dose-dependent, with diminished bioavailability and delayed peak levels at higher doses. In contrast, this is not the case for pregabalin, which shows linear pharmacokinetics and no saturation of absorption.

The oral bioavailability of pregabalin is greater than or equal to 90% across and beyond its entire clinical dose range (75 to 600 mg/day). Food does not significantly influence the oral bioavailability of pregabalin. Pregabalin is rapidly absorbed when administered on an empty stomach, with a T_max (time to peak levels) of generally less than or equal to 1 hour at doses of 300 mg or less.{{cite web |date=March 6, 2013 |title=Summary of product characteristics |publisher=European Medicines Agency (EMA) |url=http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/000546/WC500046602.pdf |access-date=May 6, 2013 |url-status=live |archive-url=https://web.archive.org/web/20180916023926/http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/000546/WC500046602.pdf |archive-date=September 16, 2018}} However, food has been found to substantially delay the absorption of pregabalin and to significantly reduce peak levels without affecting the bioavailability of the drug; T_max values for pregabalin of 0.6 hours in a fasted state and 3.2 hours in a fed state (5-fold difference), and the C_max is reduced by 25–31% in a fed versus fasted state.

Pregabalin crosses the blood–brain barrier and enters the central nervous system. However, due to its low lipophilicity, pregabalin requires active transport across the blood–brain barrier.{{cite journal |vauthors=Geldenhuys WJ, Mohammad AS, Adkins CE, Lockman PR |title=Molecular determinants of blood-brain barrier permeation |journal=Therapeutic Delivery |volume=6 |issue=8 |pages=961–971 |year=2015 |doi=10.4155/tde.15.32 |pmc=4675962 |pmid=26305616}}{{cite journal |vauthors=Müller CE |title=Prodrug approaches for enhancing the bioavailability of drugs with low solubility |journal=Chemistry & Biodiversity |volume=6 |issue=11 |pages=2071–2083 |date=November 2009 |doi=10.1002/cbdv.200900114 |pmid=19937841 |s2cid=32513471}} The LAT1 is highly expressed at the blood–brain barrier{{cite journal |vauthors=Boado RJ, Li JY, Nagaya M, Zhang C, Pardridge WM |title=Selective expression of the large neutral amino acid transporter at the blood-brain barrier |journal=Proceedings of the National Academy of Sciences of the United States of America |volume=96 |issue=21 |pages=12079–12084 |date=October 1999 |bibcode=1999PNAS...9612079B |title-link=doi |doi=10.1073/pnas.96.21.12079 |doi-access=free |pmc=18415 |pmid=10518579}} and transports pregabalin across into the brain. Pregabalin has been shown to cross the placenta in rats and is present in the milk of lactating rats. In humans, the volume of distribution of an orally administered dose of pregabalin is approximately 0.56 L/kg. Pregabalin is not significantly bound to plasma proteins (<1%).

Pregabalin undergoes little or no metabolism.{{cite book |title=Antiepileptic Drugs to Treat Psychiatric Disorders |publisher=INFRMA-HC |year=2008 |isbn=978-0-8493-8259-8 |veditors=McElroy SL, Keck PE, Post RM |editor-link1=Susan McElroy |page=370}} In experiments using nuclear medicine techniques, it was revealed that approximately 98% of the radioactivity recovered in the urine was unchanged pregabalin. The main metabolite is N-methylpregabalin.

Pregabalin is generally safe in patients with liver cirrhosis.{{cite journal |vauthors=Ma J, Björnsson ES, Chalasani N |title=The Safe Use of Analgesics in Patients with Cirrhosis: A Narrative Review |journal=Am J Med |volume=137 |issue=2 |pages=99–106 |date=February 2024 |doi=10.1016/j.amjmed.2023.10.022 |pmid=37918778 |s2cid=264888110}}

Pregabalin is eliminated by the kidneys in the urine, mainly in its unchanged form. It has a relatively short elimination half-life, with a reported value of 6.3 hours. Because of its short elimination half-life, pregabalin is administered 2 to 3 times per day to maintain therapeutic levels. The kidney clearance of pregabalin is 73 mL/minute.{{cite web |title=Lyrica- pregabalin capsule Lyrica- pregabalin solution |website=DailyMed |date=June 15, 2020 |url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=60185c88-ecfd-46f9-adb9-b97c6b00a553 |access-date=August 27, 2022 |url-status=live |archive-url=https://web.archive.org/web/20210925211707/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=60185c88-ecfd-46f9-adb9-b97c6b00a553 |archive-date=September 25, 2021}}

Pregabalin is a GABA analogue that is a 3-substituted derivative as well as a γ-amino acid. Because of its chemical and pharmacological similarities to gabapentin, it is sometimes called a gabapentinoid drug. Specifically, pregabalin is (S)-(+)-3-isobutyl-GABA.{{cite journal |vauthors=Yogeeswari P, Ragavendran JV, Sriram D |title=An update on GABA analogs for CNS drug discovery |journal=Recent Patents on CNS Drug Discovery |volume=1 |issue=1 |pages=113–118 |date=January 2006 |title-link=doi |doi=10.2174/157488906775245291 |pmid=18221197}}{{cite journal |vauthors=Rose MA, Kam PC |title=Gabapentin: pharmacology and its use in pain management |journal=Anaesthesia |volume=57 |issue=5 |pages=451–462 |date=May 2002 |title-link=doi |doi=10.1046/j.0003-2409.2001.02399.x |pmid=11966555 |s2cid=27431734}}{{cite book |vauthors=Wheless JW, Willmore J, Brumback RA |title=Advanced Therapy in Epilepsy |publisher=PMPH-USA |year=2009 |isbn=978-1-60795-004-2 |pages=302 |url=https://books.google.com/books?id=4W7UI-FPZmoC&pg=PA302}} Pregabalin also closely resembles the α-amino acids L-leucine and L-isoleucine, and this may be of greater relevance in relation to its pharmacodynamics than its structural similarity to GABA.

Chemical syntheses of pregabalin have been described.{{cite book |vauthors=Vardanyan R, Hruby V |title=Synthesis of Best-Seller Drugs |date=January 7, 2016 |publisher=Elsevier Science |isbn=978-0-12-411524-8 |pages=158 |url=https://books.google.com/books?id=A8oHBgAAQBAJ&pg=PA158 |access-date=June 22, 2018 |url-status=live |archive-url=https://web.archive.org/web/20210829003809/https://books.google.com/books?id=A8oHBgAAQBAJ&pg=PA158 |archive-date=August 29, 2021}}{{cite book |vauthors=Andrushko V, Andrushko N |title=Stereoselective Synthesis of Drugs and Natural Products |date=August 16, 2013 |publisher=John Wiley & Sons |isbn=978-1-118-62833-1 |pages=869 |url=https://books.google.com/books?id=jXFwAAAAQBAJ&pg=PA869 |access-date=June 22, 2018 |url-status=live |archive-url=https://web.archive.org/web/20210829205931/https://books.google.com/books?id=jXFwAAAAQBAJ&pg=PA869 |archive-date=August 29, 2021}}

Pregabalin was synthesized in 1990 as an anticonvulsant that was developed as a successor to the related gabapentin.{{cite book |vauthors=Kaye AD, Vadivelu N, Urman RD |title=Substance Abuse: Inpatient and Outpatient Management for Every Clinician |date=2014 |publisher=Springer |isbn=9781493919512 |page=324 |url=https://books.google.com/books?id=ms2lBQAAQBAJ&pg=PA324 |access-date=August 24, 2020 |url-status=live |archive-url=https://web.archive.org/web/20220301084046/https://books.google.com/books?id=ms2lBQAAQBAJ&pg=PA324 |archive-date=March 1, 2022}} It was first synthesized by medicinal chemist Richard Bruce Silverman at Northwestern University in Evanston, Illinois.{{cite web |vauthors=Lowe D |author-link=Derek Lowe (chemist) |date=March 25, 2008 |title=Getting to Lyrica |website=In the Pipeline |publisher=Science |url=https://www.science.org/content/blog-post/getting-lyrica |access-date=November 21, 2015 |url-status=live |archive-url=https://web.archive.org/web/20220827061356/https://www.science.org/content/blog-post/getting-lyrica |archive-date=August 27, 2022}} During 1988 to 1990, Ryszard Andruszkiewicz, a visiting research fellow, synthesized a series of molecules requested by Silverman.{{cite journal | vauthors = Andruszkiewicz R, Silverman RB | title = 4-Amino-3-alkylbutanoic acids as substrates for gamma-aminobutyric acid aminotransferase | journal = The Journal of Biological Chemistry | volume = 265 | issue = 36 | pages = 22288–22291 | date = December 1990 | pmid = 2266125 | doi = 10.1016/S0021-9258(18)45702-X | title-link = doi | doi-access = free }} Upon testing in mouse seizure models by collaborators at Parke-Davis Pharmaceuticals,{{cite journal | vauthors = Silverman RB, Andruszkiewicz R, Nanavati SM, Taylor CP, Vartanian MG | title = 3-Alkyl-4-aminobutyric acids: the first class of anticonvulsant agents that activates L-glutamic acid decarboxylase | journal = Journal of Medicinal Chemistry | volume = 34 | issue = 7 | pages = 2295–2298 | date = July 1991 | pmid = 2067001 | doi = 10.1021/jm00111a053 }} one looked particularly promising. In vitro, it activated L-glutamic acid decarboxylase, an enzyme, but this later proved to be unimportant to prevention of seizures. Silverman had originally hoped that the enzyme would increase the production of the inhibitory neurotransmitter GABA and block convulsions.{{cite news |date=February 25, 2010 |title=Silverman's golden drug makes him NU's golden ticket |url=http://www.northbynorthwestern.com/story/silvermans-golden-drug-makes-him-nus-golden-ticket/ |url-status=dead |archive-url=https://web.archive.org/web/20160601194802/http://www.northbynorthwestern.com/story/silvermans-golden-drug-makes-him-nus-golden-ticket/ |archive-date=June 1, 2016 |access-date=May 19, 2016 |work=North by Northwestern |vauthors=Merrill N}} After extensive development studies and clinical trials by Parke-Davis the drug was approved in the European Union in 2004. The US received FDA approval for use in treating epilepsy, diabetic neuropathic pain, and postherpetic neuralgia in December 2004. Pregabalin then appeared on the US market under the brand name Lyrica in the fall of 2005.{{cite journal | vauthors = Dworkin RH, Kirkpatrick P | title = Pregabalin | journal = Nature Reviews. Drug Discovery | volume = 4 | issue = 6 | pages = 455–456 | date = June 2005 | pmid = 15959952 | doi = 10.1038/nrd1756 | url = https://scholar.google.com/scholar?hl=en&as_sdt=0%2C5&q=Fresh+from+the+pipeline%3A+Pregabalin+2005&btnG= | access-date = October 26, 2020 | url-access = subscription | url-status = live | s2cid = 265702200 | archive-url = https://web.archive.org/web/20201029175208/https://scholar.google.com/scholar?hl=en&as_sdt=0,5&q=Fresh+from+the+pipeline:+Pregabalin+2005&btnG= | archive-date = October 29, 2020 }} In 2017, the FDA approved pregabalin extended-release Lyrica CR for the management of neuropathic pain associated with diabetic peripheral neuropathy, and postherpetic neuralgia.{{cite news |title=FDA approves LYRICA CR extended-release tablets CV |newspaper=Seeking Alpha |date=October 12, 2017 |url=https://seekingalpha.com/news/3300636-fda-approves-lyrica-cr-extended-release-tablets-cv |access-date=September 16, 2022 |url-status=live |archive-url=https://web.archive.org/web/20220920163128/https://seekingalpha.com/news/3300636-fda-approves-lyrica-cr-extended-release-tablets-cv |archive-date=September 20, 2022}} However, unlike the immediate release formulation, Lyrica CR was not approved for the management of fibromyalgia or as add-on therapy for adults with partial onset seizures.{{cite news |work=Reuters |title=BRIEF-FDA approves Pfizer's Lyrica CR extended-release tablets CV |url=https://www.reuters.com/article/brief-fda-approves-pfizers-lyrica-cr-ext/brief-fda-approves-pfizers-lyrica-cr-extended-release-tablets-cv-idUSASB0BMUS |access-date=October 3, 2018 |url-status=live |archive-url=https://web.archive.org/web/20181004021252/https://www.reuters.com/article/brief-fda-approves-pfizers-lyrica-cr-ext/brief-fda-approves-pfizers-lyrica-cr-extended-release-tablets-cv-idUSASB0BMUS |archive-date=October 4, 2018}}

• United States: During clinical trials a small number of users (~4%) reported euphoria after use, which led to its control in the US.{{cite web |title=Lyrica: Package Insert & Prescribing Information |website=Drugs.com |url=https://www.drugs.com/pro/lyrica.html |access-date=August 18, 2016 |url-status=live |archive-url=https://web.archive.org/web/20170813014258/https://www.drugs.com/pro/lyrica.html |archive-date=August 13, 2017}} The Drug Enforcement Administration (DEA) classified pregabalin as a depressant and placed pregabalin, including its salts, and all products containing pregabalin into Schedule V of the Controlled Substances Act.{{cite web |title=2005 - Placement of Pregabalin Into Schedule V |website=DEA Diversion Control Division |date=July 28, 2005 |url=https://www.deadiversion.usdoj.gov/fed_regs/rules/2005/fr0728.htm |access-date=August 27, 2022 |url-status=live |archive-url=https://web.archive.org/web/20220528181200/https://www.deadiversion.usdoj.gov/fed_regs/rules/2005/fr0728.htm |archive-date=May 28, 2022}}{{cite web |title=Schedules of Controlled Substances: Placement of Pregabalin Into Schedule V |website=Federal Register |date=July 28, 2005 |url=https://www.federalregister.gov/documents/2005/07/28/05-15036/schedules-of-controlled-substances-placement-of-pregabalin-into-schedule-v |access-date=August 27, 2022 |url-status=live |archive-url=https://web.archive.org/web/20210802131217/https://www.federalregister.gov/documents/2005/07/28/05-15036/schedules-of-controlled-substances-placement-of-pregabalin-into-schedule-v |archive-date=August 2, 2021}}{{cite web |title=Title 21 CFR – PART 1308 – Section 1308.15 Schedule V |website=usdoj.gov |url=http://www.deadiversion.usdoj.gov/21cfr/cfr/1308/1308_15.htm |access-date=September 27, 2015 |url-status=dead |archive-url=https://web.archive.org/web/20200903190235/https://www.deadiversion.usdoj.gov/21cfr/cfr/1308/1308_15.htm |archive-date=September 3, 2020}}
• Norway: Pregabalin is in prescription Schedule B, alongside benzodiazepines.{{cite web |work=Felleskatalogen |date=May 7, 2015 |title=Lyrica |language=no |url=https://www.felleskatalogen.no/medisin/lyrica-pfizer-561166 |access-date=October 26, 2020 |url-status=dead |archive-url=https://web.archive.org/web/20161223153207/https://www.felleskatalogen.no/medisin/lyrica-pfizer-561166 |archive-date=December 23, 2016}}{{cite journal |vauthors=Chalabianloo F, Schjøtt J |title=Pregabalin og misbrukspotensial |trans-title=Pregabalin and its potential for abuse |language=no |journal=Tidsskrift for den Norske Laegeforening |volume=129 |issue=3 |pages=186–187 |date=January 2009 |title-link=doi |doi=10.4045/tidsskr.08.0047 |doi-access=free |pmid=19180163 |url=https://tidsskriftet.no/2009/01/legemidler-i-praksis/pregabalin-og-misbrukspotensial |access-date=October 26, 2020 |url-status=live |archive-url=https://web.archive.org/web/20201029162224/https://tidsskriftet.no/2009/01/legemidler-i-praksis/pregabalin-og-misbrukspotensial |archive-date=October 29, 2020}}
• United Kingdom: On January 14, 2016, the Advisory Council on the Misuse of Drugs (ACMD) recommended that pregabalin, along with gabapentin, be controlled under the Misuse of Drugs Act 1971.{{cite web |date=January 14, 2016 |title=Re: Pregabalin and Gabapentin advice |website=GOV.UK |url=https://assets.publishing.service.gov.uk/government/uploads/system/uploads/attachment_data/file/491854/ACMD_Advice_-_Pregabalin_and_gabapentin.pdf |access-date=February 6, 2019 |url-status=live |archive-url=https://web.archive.org/web/20201108101040/https://assets.publishing.service.gov.uk/government/uploads/system/uploads/attachment_data/file/491854/ACMD_Advice_-_Pregabalin_and_gabapentin.pdf |archive-date=November 8, 2020}}{{cite web |date=November 10, 2017 |title=Pregabalin and gabapentin: proposal to schedule under the Misuse of Drugs Regulations 2001 |website=GOV.UK |url=https://www.gov.uk/government/consultations/pregabalin-and-gabapentin-proposal-to-schedule-under-the-misuse-of-drugs-regulations-2001 |access-date=April 2, 2020 |url-status=live |archive-url=https://web.archive.org/web/20200103103115/https://www.gov.uk/government/consultations/pregabalin-and-gabapentin-proposal-to-schedule-under-the-misuse-of-drugs-regulations-2001 |archive-date=January 3, 2020}} In October 2018, it was announced that pregabalin would be reclassified as a Class C controlled substance, effective April 2019.{{cite journal |vauthors=Mayor S |title=Pregabalin and gabapentin become controlled drugs to cut deaths from misuse |journal=BMJ |volume=363 |pages=k4364 |date=October 2018 |doi=10.1136/bmj.k4364 |pmid=30327316 |s2cid=53520780 |url=https://www.bmj.com/content/363/bmj.k4364 |url-access=subscription |access-date=February 6, 2019 |url-status=live |archive-url=https://web.archive.org/web/20190809170709/https://www.bmj.com/content/363/bmj.k4364 |archive-date=August 9, 2019}}{{cite web |date=October 15, 2018 |title=Pregabalin and gabapentin to be controlled as Class C drugs |website=GOV.UK |url=https://www.gov.uk/government/news/pregabalin-and-gabapentin-to-be-controlled-as-class-c-drugs |access-date=April 2, 2020 |url-status=live |archive-url=https://web.archive.org/web/20201112034051/https://www.gov.uk/government/news/pregabalin-and-gabapentin-to-be-controlled-as-class-c-drugs |archive-date=November 12, 2020}}{{cite web |title=Control of pregabalin and gabapentin under the Misuse of Drugs Act 1971 |website=GOV.UK |date=March 29, 2019 |url=https://www.gov.uk/government/publications/circular-0192018-control-of-pregabalin-and-gabapentin-under-the-misuse-of-drugs-act-1971/control-of-pregabalin-and-gabapentin-under-the-misuse-of-drugs-act-1971 |access-date=February 21, 2024 |url-status=live |archive-url=https://web.archive.org/web/20240221044657/https://www.gov.uk/government/publications/circular-0192018-control-of-pregabalin-and-gabapentin-under-the-misuse-of-drugs-act-1971/control-of-pregabalin-and-gabapentin-under-the-misuse-of-drugs-act-1971 |archive-date=February 21, 2024}} As a Class C drug, pregabalin now requires a prescription in the UK,{{cite web |date=August 12, 2013 |title=Controlled Drug Classes |url=https://www.release.org.uk/law/classes |url-status=live |archive-url=https://web.archive.org/web/20240328102114/https://www.release.org.uk/law/classes |archive-date=March 28, 2024 |access-date=May 6, 2024}}{{cite web |date=October 31, 2022 |title=What are Class C Drugs? |url=https://cpdonline.co.uk/knowledge-base/mental-health/what-are-class-c-drugs/ |url-status=live |archive-url=https://web.archive.org/web/20240506185542/https://cpdonline.co.uk/knowledge-base/mental-health/what-are-class-c-drugs/ |archive-date=May 6, 2024 |access-date=May 6, 2024}} and the prescription must clearly specify the dose.

In the United States, the FDA has approved pregabalin for adjunctive therapy for adults with partial onset seizures, management of postherpetic neuralgia and neuropathic pain associated with spinal cord injury and diabetic peripheral neuropathy, and the treatment of fibromyalgia.{{cite web |title=Pfizer to pay $2.3 billion to resolve criminal and civil health care liability relating to fraudulent marketing and the payment of kickbacks |publisher=Stop Medicare Fraud, U.S. Departments of Health & Human Services, and of Justice |url=http://www.stopmedicarefraud.gov/pfizerfactsheet.html |access-date=July 4, 2012 |url-status=dead |archive-url=https://web.archive.org/web/20120830023954/http://www.stopmedicarefraud.gov/pfizerfactsheet.html |archive-date=August 30, 2012}} Pregabalin has also been approved in the European Union, the United Kingdom, and Russia for treatment of generalized anxiety disorder.{{cite press release |title=Pfizer's Lyrica Approved for the Treatment of Generalized Anxiety Disorder (GAD) in Europe |url=http://www.prnewswire.com/cgi-bin/stories.pl?ACCT=104&STORY=/www/story/03-27-2006/0004327379 |access-date=November 6, 2011 |url-status=dead |archive-url=https://web.archive.org/web/20070929121837/http://www.prnewswire.com/cgi-bin/stories.pl?ACCT=104&STORY=%2Fwww%2Fstory%2F03-27-2006%2F0004327379 |archive-date=September 29, 2007}}

Pregabalin is available as a generic medication in a number of countries, including the United States as of July 2019.{{citation |vauthors=Levy S |title=Nine generic firms get FDA approval for generic Lyrica. |work=Drug Store News |date=July 22, 2019 |url=https://www.drugstorenews.com/pharmacy/nine-generic-firms-get-fda-approval-for-generic-lyrica/ |archive-url=https://web.archive.org/web/20200805105514/https://drugstorenews.com/pharmacy/nine-generic-firms-get-fda-approval-for-generic-lyrica |archive-date=August 5, 2020}} In the United States as of July 2019 the wholesale/pharmacy cost for generic pregabalin is US$0.17–0.22 per 150 mg capsule.{{cite web |title=Generic Lyrica launches at 97% discount to brand version |website=46brooklyn Research |date=July 23, 2019 |url=https://www.46brooklyn.com/news/2019/7/23/lyrica-goes-generic |access-date=December 25, 2019 |url-status=live |archive-url=https://web.archive.org/web/20200716075241/https://www.46brooklyn.com/news/2019/7/23/lyrica-goes-generic |archive-date=July 16, 2020}}

From 2008 until 2018, Pfizer engaged in extensive direct-to-consumer advertising campaigns to promote its branded product Lyrica for fibromyalgia and diabetic nerve pain indications. In January 2016, the company spent a record amount, $24.6 million for a single drug on TV ads, reaching global revenues of $14 billion, more than half in the United States.{{cite news |vauthors=Bulik BS |date=March 2016 |title=AbbVie's Humira, Pfizer's Lyrica kick off 2016 with hefty TV ad spend |work=FiercePharma |url=https://www.fiercepharma.com/marketing/abbvie-s-humira-pfizer-s-lyrica-kick-off-2016-hefty-tv-ad-spend |access-date=March 5, 2017 |archive-url=https://web.archive.org/web/20201029161332/https://www.fiercepharma.com/marketing/abbvie-s-humira-pfizer-s-lyrica-kick-off-2016-hefty-tv-ad-spend |archive-date=October 29, 2020}}

Up until 2009, Pfizer promoted Lyrica for other uses that had not been approved by medical regulators. For Lyrica and three other drugs, Pfizer was fined a record amount of US$2.3 billion by the Department of Justice,{{cite news |vauthors=Harris G |date=September 2, 2009 |title=Pfizer Pays $2.3 Billion to Settle Marketing Case |work=The New York Times |url=https://www.nytimes.com/2009/09/03/business/03health.html |access-date=December 21, 2017 |url-status=live |archive-url=https://web.archive.org/web/20200926003914/https://www.nytimes.com/2009/09/03/business/03health.html |archive-date=September 26, 2020}}{{cite web |date=September 2, 2009 |title=Pfizer agrees record fraud fine |website=BBC News |url=http://news.bbc.co.uk/2/hi/business/8234533.stm |access-date=December 21, 2017 |url-status=live |archive-url=https://web.archive.org/web/20090908011344/http://news.bbc.co.uk/2/hi/business/8234533.stm |archive-date=September 8, 2009}}{{cite web |date=2010 |title=Portions of the Pfizer Inc. 2010 Financial Report |website=U.S. Securities and Exchange Commission |url=https://www.sec.gov/Archives/edgar/data/78003/000119312511048877/dex13.htm |access-date=December 21, 2017 |url-status=live |archive-url=https://web.archive.org/web/20190610193252/https://www.sec.gov/Archives/edgar/data/78003/000119312511048877/dex13.htm |archive-date=June 10, 2019}} after pleading guilty to advertising and branding "with the intent to defraud or mislead". Pfizer illegally promoted the drugs, with doctors "invited to consultant meetings, many in resort locations; attendees expenses were paid; they received a fee just for being there", according to prosecutor Michael Loucks.

Professor Richard "Rick" Silverman of Northwestern University developed pregabalin there. The university holds a patent on it, exclusively licensed to Pfizer.{{cite journal |vauthors=Jacoby M |year=2008 |title=Financial Windfall from Lyrica |journal=Chemical & Engineering News |volume=86 |issue=10 |pages=56–61 |doi=10.1021/cen-v086n010.p056 |url=https://cen.acs.org/articles/86/i10/Financial-Windfall-Lyrica.html |url-access=subscription |access-date=October 26, 2020 |url-status=live |archive-url=https://web.archive.org/web/20201026170423/https://cen.acs.org/articles/86/i10/Financial-Windfall-Lyrica.html |archive-date=October 26, 2020}}{{cite patent |country=US |number=6197819B1 |inventor=Silverman RB, Andruszkiewicz R |assign1=Northwestern University |gdate=March 6, 2001 |title=Gamma amino butyric acid analogs and optical isomers |url=https://patents.google.com/patent/US6197819B1/en}} {{Webarchive|url=https://web.archive.org/web/20190321033355/https://patents.google.com/patent/US6197819B1/en |date=March 21, 2019}} That patent, along with others, was challenged by generic manufacturers and was upheld in 2014, giving Pfizer exclusivity for Lyrica in the US until 2018.{{cite news |vauthors=Decker S |date=February 6, 2014 |title=Pfizer Wins Ruling to Block Generic Lyrica Until 2018 |work=Bloomberg |url=https://www.bloomberg.com/news/2014-02-06/pfizer-wins-ruling-to-block-generic-lyrica-until-2018.html |access-date=October 26, 2020 |url-status=live |archive-url=https://web.archive.org/web/20140208151103/https://www.bloomberg.com/news/2014-02-06/pfizer-wins-ruling-to-block-generic-lyrica-until-2018.html |archive-date=February 8, 2014}}{{cite web |title=Decision: Pfizer Inc. (PFE) v. Teva Pharmaceuticals USA Inc., 12-1576, U.S. Court of Appeals for the Federal Circuit (Washington) |url=https://www.finnegan.com/files/Publication/48de9f25-b22f-4d07-9c56-151fa117073b/Presentation/PublicationAttachment/67b8c48d-5c6b-48ef-b29d-160d7303d9fa/12-1576%202-6-14.pdf |access-date=October 26, 2020 |url-status=live |archive-url=https://web.archive.org/web/20201029163458/https://www.finnegan.com/files/Publication/48de9f25-b22f-4d07-9c56-151fa117073b/Presentation/PublicationAttachment/67b8c48d-5c6b-48ef-b29d-160d7303d9fa/12-1576%202-6-14.pdf |archive-date=October 29, 2020}}

Pfizer's main patent for Lyrica, for seizure disorders, in the UK expired in 2013. In November 2018, the Supreme Court of the United Kingdom ruled that Pfizer's second patent on the drug, for the treatment of pain, was invalid because there was a lack of evidence for the conditions it covered – central and peripheral neuropathic pain. From October 2015, GPs were forced to change people from generic pregabalin to branded until the second patent ran out in July 2017. This cost the NHS £502 million.{{cite news |date=November 14, 2018 |title=Pfizer's failed pregabalin patent appeal means NHS could reclaim £502m |publisher=Pulse |url=https://www.pulsetoday.co.uk/news/politics/pfizers-failed-pregabalin-patent-appeal-means-nhs-could-reclaim-502m/ |access-date=May 17, 2024 |archive-url=https://web.archive.org/web/20181115195322/http://www.pulsetoday.co.uk/clinical/clinical-specialties/prescribing/pfizers-failed-pregabalin-patent-appeal-means-nhs-could-reclaim-502m/20037790.article |archive-date=November 15, 2018}}

As of October 2017, pregabalin is marketed under many brand names: Algerika, Alivax, Alyse, Alzain, Andogablin, Aprion, Averopreg, Axual, Balifibro, Brieka, Clasica, Convugabalin, Dapapalin, Dismedox, Dolgenal, Dolica, Dragonor, Ecubalin, Epica, Epiron, Gaba-P, Gabanext, Gabarol, Gabica, Gablin, Gablovac, Gabrika, Gavin, Gialtyn, Glonervya, Helimon, Hexgabalin, Irenypathic, Kabian, Kemirica, Kineptia, Lecaent, Lingabat, Linprel, Lyribastad, Lyric, Lyrica, Lyrineur, Lyrolin, Lyzalon, Martesia, Maxgalin, Mystika, Neuragabalin, Neugaba, Neurega, Neurica, Neuristan, Neurolin, Neurovan, Neurum, Newrica, Nuramed, Paden, Pagadin, Pagamax, Painica, Pevesca, PG, Plenica, Pragiola, Prebalin, Prebanal, Prebel, Prebictal, Prebien, Prefaxil, Pregaba, Pregabalin, Pregabalina, Pregabaline, Prégabaline, Pregabalinum, Pregabateg, Pregaben, Pregabid, Pregabin, Pregacent, Pregadel, Pregagamma, Pregalex, Pregalin, Pregalodos, Pregamid, Pregan, Preganerve, Pregastar, Pregatrend, Pregavalex, Pregdin Apex, Pregeb, Pregobin, Prejunate, Prelin, Preludyo, Prelyx, Premilin, Preneurolin, Prestat, Pretor, Priga, Provelyn, Regapen, Resenz, Rewisca, Serigabtin, Symra, Vronogabic, Xablin, and Xil.{{cite web |title=Pregabalin international brands |website=Drugs.com |url=https://www.drugs.com/international/pregabalin.html |access-date=October 27, 2017 |url-status=live |archive-url=https://web.archive.org/web/20190828172817/https://www.drugs.com/international/pregabalin.html |archive-date=August 28, 2019}}

It is marketed as a combination drug with mecobalamin under the brand names Agemax-P, Alphamix-PG, Freenerve-P, Gaben, Macraberin-P, Mecoblend-P, Mecozen-PG, Meex-PG, Methylnuron-P, Nervolin, Nervopreg, Neurica-M, Neuroprime-PG, Neutron-OD, Nuroday-P, Nurodon-PG, Nuwin-P, Pecomin-PG, Prebel-M, Predic-GM, Pregacent-M, Pregamet, Preganerv-M, Pregeb-M OD, Pregmic, Prejunate Plus, Preneurolin Plus, Pretek-GM, Rejusite, Renerve-P, Safyvit-PR, Vitcobin-P, and Voltanerv with Methylcobalamin and ALA by Cogentrix Pharma.

In the US, Lyrica is marketed by Viatris after Upjohn was spun off from Pfizer.{{cite web | title=Pfizer Completes Transaction to Combine Its Upjohn Business with Mylan | publisher=Pfizer | via=Business Wire | date=November 16, 2020 | url=https://www.businesswire.com/news/home/20201116005378/en/ | access-date=June 17, 2024}}{{cite web | title=Lyrica | website=Pfizer | url=https://www.pfizer.com/products/product-detail/lyrica | access-date=June 17, 2024}}{{cite web | title=Brands | website=Viatris | date=November 16, 2020 | url=https://www.viatris.com/en/products/brands | access-date=June 17, 2024}}

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