Pregabalin: A Review of its Use in Fibromyalgia
Abstract
Oral pregabalin, a calcium channel alpha(2)delta-subunit ligand with analgesic, anxiolytic and antiepileptic activity, has shown efficacy in the treatment of fibromyalgia. It has a multidimensional effect in the treatment of this complex condition, and is associated with rapid and clinically significant improvements in several outcome measures relating to core symptoms of the syndrome, including pain and sleep, in patients with long-standing fibromyalgia. Pregabalin treatment is also associated with improvements in the overall health status of these patients. The beneficial effects of pregabalin are durable in patients with an initial response to the drug. The most common adverse events associated with the drug are dizziness and somnolence, which are generally mild to moderate in intensity and are tolerated by many patients. Pregabalin is, therefore, a valuable option in the first-line treatment of patients with fibromyalgia.
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Pregabalin is a structural analog of the neurotransmitter gamma-aminobutyric acid (GABA).
“Pregabalin is a structural analog of the neurotransmitter γ-aminobutyric acid (GABA).”
From Comparative Efficacy and Harms of Duloxetine, Milnacipran, and Pregabalin in Fibromyalgia Syndrome (2010) · cites this paper as [42]
Pregabalin is a ligand to the alpha-2-delta subunit on voltage-gated calcium channels, which reduces calcium influx at nerve terminals and decreases the release of several neurotransmitters, including glutamate, norepinephrine, and substance P.
“This second-generation antiepileptic is a ligand to the alpha-2-delta subunit on voltage-gated calcium channels, which reduces calcium influx at nerve terminals resulting in a decreased release of several neurotransmitters, including glutamate, norepinephrine, and substance P.”
From Comparative Efficacy and Harms of Duloxetine, Milnacipran, and Pregabalin in Fibromyalgia Syndrome (2010) · cites this paper as [42]
Cites
EULAR evidence-based recommendations for the management of fibromyalgia syndrome
Carville, S. F., Arendt-Nielsen, S., Bliddal, H., Blotman, F., Branco, J. C., Buskila, D., Da Silva, J. A. P., Danneskiold-Samsøe, B., Dincer, F., Henriksson, C., et al. (2008) · Annals of the Rheumatic Diseases · doi:10.1136/ard.2007.071522 · Cited by 752 · see citing works
Arnold, L. M., Russell, I. J., Diri, E. W., Duan, W. R., Young, J. P., Sharma, U., Martin, S. A., Barrett, J. A., & Haig, G. (2008) · The Journal of Pain · doi:10.1016/j.jpain.2008.03.013 · Cited by 277 · see citing works
Employees With Fibromyalgia: Medical Comorbidity, Healthcare Costs, and Work Loss
White, L. A., Birnbaum, H. G., Kaltenboeck, A., Tang, J., Mallett, D., & Robinson, R. L. (2008) · Journal of Occupational & Environmental Medicine · doi:10.1097/jom.0b013e31815cff4b · Cited by 168 · see citing works
Novel pharmacotherapy for fibromyalgia
Wood, P. B., Holman, A. J., & Jones, K. D. (2007) · Expert Opinion on Investigational Drugs · doi:10.1517/13543784.16.6.829 · Cited by 30 · see citing works
Flagged first, then by citations
Cited by
Sorted by citations
Häuser, W., Bernardy, K., Üçeyler, N., & Sommer, C. (2009) · Pain · doi:10.1016/j.pain.2009.05.014 · Cited by 243 · see citing works
Calandre, E. P., Rico-Villademoros, F., & Slim, M. (2016) · Expert Review of Neurotherapeutics · doi:10.1080/14737175.2016.1202764 · Cited by 223 · see citing works
“Both in the treatment of fibromyalgia [27] and in the”
BackgroundComparative Efficacy and Harms of Duloxetine, Milnacipran, and Pregabalin in Fibromyalgia Syndrome
Häuser, W., Petzke, F., & Sommer, C. (2010) · The Journal of Pain · doi:10.1016/j.jpain.2010.01.002 · Cited by 216 · see citing works
Pregabalin in Neuropathic Pain: Evidences and Possible Mechanisms
Verma, V., Singh, N., & Jaggi, A. S. (2014) · Current Neuropharmacology · doi:10.2174/1570159x1201140117162802 · Cited by 205 · see citing works
“Pregabalin has shown efficacy in treating fibromyalgia with rapid and clinically significant improvements in several outcome measures related to core symptoms of the syndrome in patients with long-standing fibromyalgia [54].”
Background(2014) · Handbook of Clinical Neurology · doi:10.1016/b978-0-7020-4086-3.00033-3 · Cited by 86 · see citing works
Tuchman, M. M., Barrett, J. A., Donevan, S. D., Hedberg, T. G., & Taylor, C. P. (2010) · Journal of Pain · doi:10.1016/j.jpain.2010.02.024 · Cited by 73 · see citing works
Gender bias in diagnosing fibromyalgia.
Katz, J., Mamyrova, G., Guzhva, O., & Furmark, L. (2010) · Gender Medicine · doi:10.1016/j.genm.2010.01.003 · Cited by 52 · see citing works
Ahıskalıoğlu, A., Ince, I., Aksoy, M., Yalçin, E., Ahiskalioğlu, E., & Kılınç, A. (2016) · Journal of oral and maxillofacial surgery · doi:10.1016/j.joms.2015.09.008 · Cited by 44
Lee, Y. H., & Song, G. G. (2016) · Rheumatology International · doi:10.1007/s00296-016-3468-5 · Cited by 49 · see citing works
“Pregabalin modulates the influx of calcium ions into hyper-excited neurons and reduces the synaptic release of excitatory neurotransmitters including noradrenaline and dopamine [9].”
BackgroundAdjuvant analgesics in acute pain
Lui, F., & Ng, K. (2011) · Expert Opinion on Pharmacotherapy · doi:10.1517/14656566.2011.521743 · Cited by 40 · see citing works
“Pregabalin is beneficial in postherpetic neuralgia [67], fibromyalgia [68], painful diabetic neuropathy [69], and central pain in spinal cord injury [70].”
BackgroundYang, C. C., Ng, K., Sharma, A., Jafari, J., Surguy, S., Yazaki, E., Knowles, C. H., & Aziz, Q. (2012) · Alimentary Pharmacology and Therapeutics · doi:10.1111/j.1365-2036.2011.04955.x · Cited by 36
Peripheral nerve stimulation for fibromyalgia.
Plazier, M., Vanneste, S., Dekelver, I., Thimineur, M., & Ridder, D. D. (2011) · Progress in neurological surgery · doi:10.1159/000323046 · Cited by 34 · see citing works
Plazier, M., Dekelver, I., Vanneste, S., Stassijns, G., Menovsky, T., Thimineur, M., & Ridder, D. D. (2014) · Neuromodulation (Malden, Mass.) · doi:10.1111/ner.12121 · Cited by 30 · see citing works
Seidel, M. F., & Müller, W. (2011) · Expert Opinion on Pharmacotherapy · doi:10.1517/14656566.2011.557362 · Cited by 22 · see citing works
“It is chemically related to gabapentin and was initially developed for the treatment of epileptic disorders [78], thus belonging to the class of anticonvulsants.”
BackgroundPregabalin suppresses calcium-mediated proteolysis and improves stroke outcome
Yoon, J. S., Lee, J.-H., Son, T. G., Mughal, M. R., Greig, N. H., & Mattson, M. P. (2010) · Neurobiology of Disease · doi:10.1016/j.nbd.2010.11.011 · Cited by 21 · see citing works
“Pregabalin (S-3-(aminomethyl)-5methylhexanoic acid) is used to control neurogenic pain in various clinical conditions including fibromyalgia, diabetic neuropathy and complex regional pain syndrome (Lyseng-Williamson and Siddiqui, 2008).”
BackgroundA unified synthesis of all stereoisomers of 2-(aminomethyl)cyclobutane-1-carboxylic acid
André, V., Gras, M., Awada, H., Guillot, R., Robin, S., & Aitken, D. (2013) · doi:10.1016/j.tet.2013.02.063 · Cited by 18
Awada, H., Robin, S., Guillot, R., Yazbeck, O., Naoufal, D., Jaber, N., Hachem, A., & Aitken, D. (2014) · doi:10.1002/ejoc.201402676 · Cited by 16
[Questionable documentation of the effect of pregabalin in fibromyalgia].
Holtedahl, R. (2010) · Tidsskrift for Den Norske Laegeforening · doi:10.4045/tidsskr.09.0576 · Cited by 13 · see citing works
Pregabalin inhibits proinflammatory cytokine release in patients with fibromyalgia syndrome
Ellergezen, P. H., Alp, A., Çavun, S., Çelebi, M. C., & Macunluoğlu, A. C. (2023) · Archives of Rheumatology · doi:10.46497/archrheumatol.2023.9517 · Cited by 10 · see citing works
Filipe, A., Almeida, S., Pedroso, P., Neves, R., Marques, S., Sicard, É., Massicotte, J., & Ortuño, J. (2015) · Drugs in R&D · doi:10.1007/s40268-015-0094-8 · Cited by 8
“5 h) after oral administration and exposure to single (25–300 mg/day) or multiple dosages (75–900 mg/day) is dose proportional and oral bioavailability is high (C90 %) and independent of dose [1].”
BackgroundInfluentialSaid, A. M., Zubovic, E., Ha, A. Y., Skolnick, G., Naidoo, S. D., Aubuchon, J., & Patel, K. (2020) · The Journal of craniofacial surgery (Print) · doi:10.1097/scs.0000000000007109 · Cited by 6 · see citing works
“Its mechanism of action limits the release of neuroexcitatory transmitters, giving it antiallodynic and antihyperalgesic properties.(15) Several studies have shown that pregabalin is not only effective in treating persistent pain syndrome, but can also be used to treat acute postoperative pain.”
BackgroundThe mirogabalin ALDAY phase 3 program in pain associated with fibromyalgia: the lessons learned
Merante, D. (2020) · Current Medical Research and Opinion · doi:10.1080/03007995.2020.1725744 · Cited by 6 · see citing works
Chapman, S., Aladul, M. I., & Fitzpatrick, R. W. (2019) · BMJ Open · doi:10.1136/bmjopen-2018-026817 · Cited by 6
Cognitive behavior therapy for fibromyalgia: a meta analysis
Gritzner, S., Antick, J. R., Michael, P., & Cavanaugh, R. (2012) · Journal of Pain · doi:10.1016/j.jpain.2012.01.403 · Cited by 4 · see citing works
“Two medications have recently been approved by the US FDA for the pharmacological treatment of fibromyalgia (Lyseng-Williamson & Siddiqui, 2008).”
BackgroundRashid, M., Sarfraz, M., Arfat, M., Hussain, A., Abbas, N., Hussain, K., & Bukhari, N. (2021) · Journal of Drug Delivery Science and Technology · doi:10.1016/j.jddst.2021.102548 · Cited by 5
Urological and Gynaecological Chronic Pelvic Pain
Moldwin, R. (2017) · Cambridge International Law Journal · doi:10.1007/978-3-319-48464-8 · Cited by 5 · see citing works
“CP/CPPS and likely IC/BPS as well are associated with more direct medical costs than that incurred in managing patients with insulin-dependent diabetes [9].”
BackgroundMethodInfluentialMerante, D., & Patel, S. (2019) · Pain medicine (Malden, Mass.) · doi:10.1093/pm/pnz077 · Cited by 4
Diagnostik und Therapie des Fibromyalgiesyndroms
Köllner, V., Bernardy, K., Sommer, C., & Häuser, W. (2009) · DMW - Deutsche Medizinische Wochenschrift · doi:10.1055/s-0029-1222585 · Cited by 4 · see citing works
Suivi thérapeutique pharmacologique de la prégabaline.
Bentué-Ferrer, D., Tribut, O., & Verdier, M. (2010) · The´rapie (Paris) · doi:10.2515/therapie/2009064 · Cited by 4
Review of fibromyalgia treatment guidelines: part 2 – pharmacological treatment
Heymann, R., Rezende, M., Paiva, E. D. S., de Assis, M. D., Braz, A. D. S., Ranzolin, A., Reis, A. P. M. G., Golmia, A. P. F., Maia, A. B. A., Silva, D. S., et al. (2026) · Advances in Rheumatology · doi:10.1186/s42358-025-00483-2 · Cited by 3 · see citing works
Part 1: N-alkylated glycines as potent α2δ ligands.
Thompson, L. R., Blakemore, D., Brugier, D., Bryans, J., Chu, W.-L.-A., Maw, G., Poinsard, C., Rawson, D., & Warren, A. N. (2011) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2011.04.045 · Cited by 3
Bal, R., Legree, L., & Diwan, S. (2010) · Techniques in Regional Anesthesia and Pain Management · doi:10.1053/j.trap.2010.03.001 · Cited by 2 · see citing works
Fibromialgia: Un diagnóstico que debe ser oportuno
Berrocal-Kasay, A. (2014) · Revista Médica Herediana · doi:10.20453/rmh.v25i2.252 · Cited by 1 · see citing works
Brogan, S. E., Mandyam, S., & Odell, D. W. (2018) · Elsevier eBooks · doi:10.1016/b978-0-323-48110-6.00019-3 · Cited by 5 · see citing works
Liu, Q., 文传兵, Dai, Y., Ma, T., Liu, M. M., Jia, Z., Luo, F., & Wang, D. (2026) · Journal of Pain Research · doi:10.2147/jpr.s605429
Alkylsulfanyl analogs as potent α2δ ligands.
Shimada, K., Ohata, Y., Kobayashi, J., Onishi, Y., Kawamura, A., Domon, Y., Arakawa, N., Inoue, T., Kitano, Y., Matsuda, F., et al. (2018) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2018.05.006
Gut Hypersensitivity Related Symptoms
Farmer, A. D., Peiris, M., & Aziz, Q. (2013) · Wiley eBooks · doi:10.1002/9781118444689.ch12
Update von 10 Empfehlungen zur Therapie mit NSAR
Rintelen, B., Brezinschek, H., Sautner, J., Herold, M., & Leeb, B. (2010) · doi:10.1055/s-0029-1243231
Neuroleptic Agents for Chronic Pelvic Pain
Schnall, R. F., & Pontari, M. (2017) · doi:10.1007/978-3-319-48464-8_10
A Practitioner’s Guide to Prescribing Pregabalin for Adults with Intellectual Disabilities
de León, J. (2012) · Springer eBooks · doi:10.1007/978-1-4614-2012-5_16 · Cited by 1 · see citing works
- Authors
- Lyseng-Williamson, K. A., & Siddiqui, M. A. A.
- Affiliations
- Wolters Kluwer Health (NZ)
- Corresponding author
- Lyseng-Williamson, Katherine A
- Venue
- Drugs
- Published
- 2008
- Volume
- 68
- Issue
- 15
- Pages
- 2205-2223
- ISSN
- 0012-6667 (ISSN-L)
- OpenAlex
- W2033371164
- Cited by
- 50
- References
- 0
- Citations by year
- 2026: 2 · 2023: 1 · 2021: 1 · 2020: 2 · 2019: 2 · 2018: 2 · 2017: 1 · 2016: 2 · 2015: 2 · 2014: 2 · 2013: 7 · 2012: 3
- FWCI
- 5.37
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Drugs (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Psychiatry and Mental health › Fibromyalgia and Chronic Fatigue Syndrome Research
- Health Sciences › Medicine › Physiology › Pain Mechanisms and Treatments
- Health Sciences › Medicine › Gastroenterology › Gastrointestinal motility and disorders
- Keywords
- pregabalin, fibromyalgia, alpha2delta subunit, voltage-gated calcium channels, analgesic efficacy, sleep quality, anxiety, adverse events, dizziness, sleepiness, pharmacokinetics, first-line therapy, health-related quality of life, antiepileptic drugs, anxiolytics
- MeSH terms
- Pregabalin, Anti-Inflammatory Agents, Non-Steroidal, Clinical Trials as Topic, Drug Interactions, Fibromyalgia, gamma-Aminobutyric Acid, Humans, Endpoint Determination
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