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2000
Volume 17, Issue 1
  • ISSN: 2589-9775
  • E-ISSN: 2589-9783

Abstract

Background

Gabapentin and pregabalin were developed for epilepsy and neuropathic pain. They work voltage-gated calcium channels and are used for broad-spectrum diagnoses, ., epilepsy, neuropathic pain, other chronic pain syndromes, anxiety disorders, alcohol-drug withdrawal syndromes, agitation, insomnia, . Especially in a world dealing with the opioid crisis, gabapentinoids were considered safer alternatives to opioid analgesics.

Methods

This review aims to comprehensively search and summarize recent studies concerning the abuse of gabapentinoids published between 2021 and 2022 from various regions around the world.

Results

Studies have highlighted that a history of substance use disorder is a significant risk factor for gabapentinoid abuse. Concurrent abuse of gabapentinoids with illicit drugs can exacerbate drug-related damages. Drug screening and postmortem toxicology tests have revealed an increase in gabapentinoid consumption. In response to the abuse potential, several countries have classified gabapentinoids as controlled substances.

Conclusion

Gabapentinoids are highly abused molecules worldwide. Physicians should be aware of their abuse potential.

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2023-11-28
2025-05-05
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References

  1. MorrisonE.E. SandilandsE.A. WebbD.J. Gabapentin and pregabalin: Do the benefits outweigh the harms?J. R. Coll. Phys. Edinb.201747431031310.4997/jrcpe.2017.40229537399
    [Google Scholar]
  2. EvoyKE PeckhamAM CovveyJR TidgewellKJ . Gabapentinoid pharmacology in the context of emerging misuse liability. J Clin Pharmacol 202161S2)(2S899910.1002/jcph.183334396549
    [Google Scholar]
  3. EvoyK.E. SadrameliS. ContrerasJ. CovveyJ.R. PeckhamA.M. MorrisonM.D. Abuse and misuse of pregabalin and gabapentin: A systematic review update.Drugs202181112515610.1007/s40265‑020‑01432‑733215352
    [Google Scholar]
  4. IbiloyeE.A. BarnerJ.C. LawsonK.A. RascatiK.L. EvoyK.E. PeckhamA.M. Prevalence of and factors associated with gabapentinoid use and misuse among Texas Medicaid recipients.Clin. Drug Investig.202141324525310.1007/s40261‑021‑01009‑633580482
    [Google Scholar]
  5. PelesE. SasonA. SchreiberS. AdelsonM. Pregabalin misuse: Motives, pattern, and knowledge about its risks among patients in methadone maintenance treatment.J. Psychoactive Drugs202153323824610.1080/02791072.2020.186139233357129
    [Google Scholar]
  6. GuglielmoR. MartinottiG. ClericiM. JaniriL. Pregabalin for alcohol dependence: A critical review of the literature.Adv. Ther.2012291194795710.1007/s12325‑012‑0061‑523132700
    [Google Scholar]
  7. BiermannT. BleichS. KornhuberJ. HillemacherT. Pregabalin in benzodiazepine withdrawal.Pharmacopsychiatry200740629229310.1055/s‑2007‑99214618030656
    [Google Scholar]
  8. KämmererN. LemenagerT. GrosshansM. KieferF. HermannD. Pregabalin for the reduction of opiate withdrawal symptoms.Psychiatr. Prax.201239735135222689280
    [Google Scholar]
  9. HasaneinP. ShakeriS. Pregabalin role in inhibition of morphine analgesic tolerance and physical dependency in rats.Eur. J. Pharmacol.201474211311710.1016/j.ejphar.2014.08.03025220244
    [Google Scholar]
  10. ScanlonA. Pregabalin for detoxification from opioids: A single case study.Ment. Health Subst. Use20147426328510.1080/17523281.2014.924549
    [Google Scholar]
  11. FreynhagenR. BackonjaM. SchugS. Pregabalin for the treatment of drug and alcohol withdrawal symptoms: A comprehensive review.CNS Drugs201630121191120010.1007/s40263‑016‑0390‑z27848217
    [Google Scholar]
  12. AhmedS. BachuR. KotapatiP. Use of gabapentin in the treatment of substance use and psychiatric disorders: A systematic review.Front. Psychiatry20191022810.3389/fpsyt.2019.0022831133886
    [Google Scholar]
  13. FluyauD. CookS.C. ChimaA. KailasamV.K. RevadigarN. Pharmacological management of psychoactive substance withdrawal syndrome.Drugs Ther. Perspect.2021371151953510.1007/s40267‑021‑00874‑7
    [Google Scholar]
  14. Zengin İspirG. DanışmanM. TulacıR.G. ÖzdelK. Emotion dysregulation and affective temperaments in opioid use disorder: The preliminary results of a prospective study.J. Addict. Dis.202341319620310.1080/10550887.2022.208744935713278
    [Google Scholar]
  15. SchifanoF. ChiappiniS. Pregabalin: A range of misuse‐related unanswered questions.CNS Neurosci. Ther.201925565966010.1111/cns.1311530834646
    [Google Scholar]
  16. EvoyK.E. CovveyJ.R. PeckhamA.M. RevelesK.R. Gabapentinoid misuse, abuse and non-prescribed obtainment in a United States general population sample.Int. J. Clin. Pharm.20214341055106410.1007/s11096‑020‑01217‑833387188
    [Google Scholar]
  17. KuehnB.M. Growing role of gabapentin in opioid-related overdoses highlights misuse potential and off-label prescribing practices.JAMA2022328131283128510.1001/jama.2022.1365936069924
    [Google Scholar]
  18. Turkish drug report.2021Available from: https://www.narkotik.pol.tr/kurumlar/narkotik.pol.tr/TUB%C4%B0M/2021-TURKISH-DRUG-REPORT.pdf
    [Google Scholar]
  19. ÖztürkY.E. YeterO. AteşI. Changes in the frequency and pattern of drugs detected among suspected drug users during the COVID-19 pandemic in Turkey.Int. J. Legal Med.202213651273127910.1007/s00414‑022‑02794‑135147732
    [Google Scholar]
  20. PesceA. SundyhanataR. RitzD. ThomasR. AckermanG. BollmanK. Effects of a pandemic and isolation on alcohol and psychoactive medication use in a population of rehabilitation and pain patients.Ann. Clin. Lab. Sci.202151569469734686512
    [Google Scholar]
  21. PaulyN.J. DelcherC. SlavovaS. LindahlE. TalbertJ. FreemanP.R. Trends in gabapentin prescribing in a commercially insured US adult population, 2009-2016.J. Manag. Care Spec. Pharm.202026324625210.18553/jmcp.2020.26.3.24632105169
    [Google Scholar]
  22. EsechieA. KuoY.F. GoodwinJ.S. WestraJ. RajiM.A. Trends in prescribing pattern of opioid and benzodiazepine substitutes among medicare part D beneficiaries from 2013 to 2018: A retrospective study.BMJ Open20211111e05348710.1136/bmjopen‑2021‑05348734794996
    [Google Scholar]
  23. PapazisisG. SpachosD. SiafisS. Assessment of the safety signal for the abuse potential of pregabalin and gabapentin using the FAERS database and big data search analytics.Front. Psychiatry20211264026410.3389/fpsyt.2021.64026434093263
    [Google Scholar]
  24. AindowS. CrossinR. ToopL. HudsonB. Managing the misuse potential and risk of psychological harm from gabapentinoids in primary care in New Zealand.J. Prim. Health Care202113430230710.1071/HC2101134937640
    [Google Scholar]
  25. MoriartyF. BennettK. FaheyT. Opioid and analgesic utilization in Ireland in 2000 and 2015: A repeated cross‐sectional study.Pharmacol. Res. Perspect.2022101e0089910.1002/prp2.89934913613
    [Google Scholar]
  26. DufayetL. CareW. DeheulS. Increase in pregabalin recreational use in adolescents in France.Clin. Toxicol. 202159111027103010.1080/15563650.2021.189271933733968
    [Google Scholar]
  27. FonsecaF. LenahanW. DartR.C. Non-medical use of prescription gabapentinoids (Gabapentin and Pregabalin) in five European countries.Front. Psychiatry20211267622410.3389/fpsyt.2021.67622433995154
    [Google Scholar]
  28. XiaY. ForgetP. Opioid and gabapentinoid prescriptions in England from 2015 to 2020.PLoS One20221711e027686710.1371/journal.pone.027686736441772
    [Google Scholar]
  29. ChappuyM. NourredineM. ClercB. Gabapentinoid use in French most precarious populations: Insight from lyon permanent access to healthcare (PASS) units, 2016—1Q2021.Fundam. Clin. Pharmacol.202236244845210.1111/fcp.1272634498306
    [Google Scholar]
  30. AntunovicM. VucinicS. Kotur-StevuljevicJ. Rise of pregabalin poisoning and abuse cases in Serbia: A ten-year retrospective study.Int. J. Gen. Med.2023161239125010.2147/IJGM.S40561637065979
    [Google Scholar]
  31. BonnetU. McAnallyH.B. How prevalent and severe is addiction on GABAmimetic drugs in an elderly German general hospital population? Focus on gabapentinoids, benzodiazepines, and z‐hypnotic drugs.Hum. Psychopharmacol.2022373e282210.1002/hup.282234687489
    [Google Scholar]
  32. FlemmingR. Patterns of pregabalin prescribing in four German federal states: Analysis of routine data to investigate potential misuse of pregabalin.BMJ Open2022127e06010410.1136/bmjopen‑2021‑06010435879005
    [Google Scholar]
  33. PolatC.S. KonakH.E. AkıncıM.G. OnatS.S. AltasE.U. Misuse of gabapentinoids (pregabalin and gabapentin) in patients with neuropathic pain related to spinal cord injury.J. Spinal Cord Med.20221635108174
    [Google Scholar]
  34. ZhaoD. NunesA.P. BaekJ. LapaneK.L. An algorithm to identify gabapentin misuse and/or abuse in administrative claims data.Drug Alcohol Depend.202223510942910.1016/j.drugalcdep.2022.10942935427982
    [Google Scholar]
  35. ZhangY. CastracaneA.R. WinstanleyE.L. Assessment of gabapentin misuse using prescription drug monitoring program data.Subst. Abus.202142445445910.1080/08897077.2021.189160233689673
    [Google Scholar]
  36. PeltokorpiJ. HakkoH. RiipinenP. RialaK. Profile of substance misuse among adolescent and young adult gabapentinoid users: A register-based follow-up study of former adolescent psychiatric inpatients.Subst. Use Misuse202156559860510.1080/10826084.2021.188366233663338
    [Google Scholar]
  37. SasonA. AdelsonM. SchreiberS. PelesE. Pregabalin misuse in methadone maintenance treatment patients in Israel: Prevalence and risk factors.Drug Alcohol Depend.201818981110.1016/j.drugalcdep.2018.04.02529857329
    [Google Scholar]
  38. EllisM.S. ButtramM.E. KasperZ.A. Nonmedical use of gabapentin and opioid agonist medications in treatment-seeking individuals with opioid use disorder.Drug Alcohol Depend.202223410940010.1016/j.drugalcdep.2022.10940035290917
    [Google Scholar]
  39. OldfieldB.J. LiY. Vickers-SmithR. Sociodemographic and clinical correlates of gabapentin receipt with and without opioids among a national cohort of patients with HIV.AIDS Care20223481053106310.1080/09540121.2021.193985134114904
    [Google Scholar]
  40. ButtramM.E. KurtzS.P. Descriptions of gabapentin misuse and associated behaviors among a sample of opioid (Mis) users in South Florida.J. Psychoactive Drugs2021531475410.1080/02791072.2020.180208732748701
    [Google Scholar]
  41. AlanB.E. KızılkanM.P. AkgülS. Pregabalin abuse in adolescence: A case series.Turk. J. Pediatr.202264235736310.24953/turkjped.2020.3035611425
    [Google Scholar]
  42. SutherlandR. DietzeP.M. GisevN. Patterns and correlates of prescribed and non‐prescribed pregabalin use among a sample of people who inject drugs in Australia.Drug Alcohol Rev.202039556857410.1111/dar.1308332557912
    [Google Scholar]
  43. ButtramM.E. SurrattH.L. Factors associated with gabapentin misuse among people who inject drugs in Appalachian Kentucky.Subst. Use Misuse202055142364237010.1080/10826084.2020.181708232917119
    [Google Scholar]
  44. ZhouL. BhattacharjeeS. KwohC.K. Dual‐trajectories of opioid and gabapentinoid use and risk of subsequent drug overdose among Medicare beneficiaries in the United States: A retrospective cohort study.Addiction2021116481983010.1111/add.1518932648951
    [Google Scholar]
  45. KhanN.F. BykovK. GlynnR.J. BarnettM.L. GagneJ.J. Coprescription of opioids with other medications and risk of opioid overdose.Clin. Pharmacol. Ther.202111041011101710.1002/cpt.231434048030
    [Google Scholar]
  46. OlopoeniaA. Camelo-CastilloW. QatoD.M. Adverse outcomes associated with concurrent gabapentin, opioid, and benzodiazepine utilization: A nested case-control study.Lancet Reg Health Am202213100302
    [Google Scholar]
  47. OkoyeN.C. McMillinG.A. Patterns of neonatal co-exposure to gabapentin and commonly abused drugs observed in umbilical cord tissue.J. Anal. Toxicol.202145550651210.1093/jat/bkaa11832860706
    [Google Scholar]
  48. ChatterjeeA. LopezD. RamkellawanS. “That’s what we call the cocktail”: Non-opioid medication and supplement misuse among opioid users.Subst. Abus.202142217518210.1080/08897077.2019.167194331638874
    [Google Scholar]
  49. MattsonC.L. ChowdhuryF. GilsonT.P. Notes from the Field: trends in gabapentin detection and involvement in drug overdose deaths: 23 States and the District of Columbia, 2019–2020.MMWR Morb. Mortal. Wkly. Rep.2022711966466610.15585/mmwr.mm7119a335552367
    [Google Scholar]
  50. RileyS.B. GarbuttK. CrowC. IsbellT.S. ScalzoA.J. Gabapentin prevalence: Clinical and forensic experience in St. Louis, Missouri, USA.Forensic Sci. Res.20216321822310.1080/20961790.2021.199107534868714
    [Google Scholar]
  51. KalkN.J. ChiuC.T. SadoughiR. Fatalities associated with gabapentinoids in England (2004–2020).Br. J. Clin. Pharmacol.20228883911391710.1111/bcp.1535235435281
    [Google Scholar]
  52. DarkeS. DuflouJ. PeacockA. FarrellM. LappinJ. Characteristics of fatal gabapentinoid-related poisoning in Australia, 2000–2020.Clin. Toxicol. 202260330431010.1080/15563650.2021.196515934402696
    [Google Scholar]
  53. NaharL.K. MurphyK. PatersonS. Toxicological relevance of pregabalin in heroin users: A two-year postmortem population study.J. Anal. Toxicol.202246547147810.1093/jat/bkab07034114622
    [Google Scholar]
  54. LynnE. CousinsG. LyonsS. BennettK.E. Comparing characteristics of suicide to non-suicide drug poisoning deaths, by sex, in Ireland.J. Affect. Disord.2022306808910.1016/j.jad.2022.03.03035306124
    [Google Scholar]
  55. ShiueK.Y. AustinA.E. ProescholdbellS. CoxM.E. AureliusM. NaumannR.B. Literal text analysis of poly-class and polydrug overdose deaths in North Carolina, 2015–2019.Drug Alcohol Depend.202122810904810.1016/j.drugalcdep.2021.10904834601275
    [Google Scholar]
  56. KriikkuP. OjanperäI. Pregabalin and gabapentin in non-opioid poisoning deaths.Forensic Sci. Int.202132411083010.1016/j.forsciint.2021.11083034000615
    [Google Scholar]
  57. KetenciS. GölboyuB.E. SalbaşE. UzunerB. ÇiftçiB. The attitudes of Turkish physicians in the treatment of fibromyalgia; is ‘Pregabalinophobia’ the new reality of pain medicine?Agri202234320020935792696
    [Google Scholar]
  58. KaravolisZ.A. SuA.B. PeckhamA.M. State-level response to gabapentin misuse in the United States: Implications and future direction.Am. J. Health Syst. Pharm.2022799e143e14810.1093/ajhp/zxab48634951456
    [Google Scholar]
  59. AlthunianT.A. AlomranM.I. AlsagriG.M. AlrasheedM.M. AlshammariT.M. The impact of regulatory restrictions on pregabalin use in Saudi Arabia: An interrupted time series analysis.Pharmacoepidemiol. Drug Saf.202231557758210.1002/pds.540835049110
    [Google Scholar]
  60. AlkhalafA.A. BukhariR.A. AlshehriE.A. AlshehriS.O. BadrA.F. Abuse liability of gabapentin in the Saudi population after the pregabalin restriction: A cross-sectional study.J. Taibah Univ. Med. Sci.202116570070510.1016/j.jtumed.2021.04.00934690650
    [Google Scholar]
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