Pregabalin: Latest safety evidence and clinical implications for the management of neuropathic pain

Therapeutic Advances in Drug Safety

Volumn 5, Issue 1, 2014, Pages 38-56

  Toth, Cory ^a  

^a UNIVERSITY OF CALGARY   (Canada)

Author keywords

adverse effects; anticonvulsant drugs; epilepsy; neuropathic pain; pregabalin; review; safety

Indexed keywords

PLACEBO; PREGABALIN; TIAGABINE;

ANGIONEUROTIC EDEMA; BLISTER; BLURRED VISION; BRAIN DISEASE; BRAIN EDEMA; CARCINOGENICITY; CONGESTIVE HEART FAILURE; CONSTIPATION; DIZZINESS; DOSE RESPONSE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG HALF LIFE; DRUG HYPERSENSITIVITY; DRUG MECHANISM; DRUG METABOLISM; DRUG POTENCY; DRUG SAFETY; DRUG TOLERABILITY; DYSPNEA; ERYTHEMA; HUMAN; HYPERTENSION; INCREASED APPETITE; INFECTION; NEUROPATHIC PAIN; NEUROPHARMACOLOGY; NONHUMAN; OBESITY; PERIPHERAL EDEMA; PLASMA PROTEIN BINDING; PRIORITY JOURNAL; RASH; REVIEW; SEDATION; SOMNOLENCE; TERATOGENICITY; TIME TO MAXIMUM PLASMA CONCENTRATION; URTICARIA; WEIGHT GAIN; WHEEZING; XEROSTOMIA;

EID: 84898906370     PISSN: 20420986     EISSN: 20420994     Source Type: Journal    
DOI: 10.1177/2042098613505614     Document Type: Review

References (135)

1. Achar A. Chatterjee G. Ray T. Naskar B. (2010) Comparative study of clinical efficacy with amitriptyline, pregabalin, and amitriptyline plus pregabalin combination in postherpetic neuralgia. Indian J Dermatol Venereol Leprol 76: 63–65.
2. Anonymous (2005) Pregabalin: new drug. Very similar to gabapentin. Prescrire Int 14: 203–206.
3. Arezzo J. Rosenstock J. Lamoreaux L. Pauer L. (2008) Efficacy and safety of pregabalin 600 mg/d for treating painful diabetic peripheral neuropathy: a double-blind placebo-controlled trial. BMC Neurol 8: 33.
4. Arif H. Buchsbaum R. Weintraub D. Koyfman S. Salas-Humara C. Bazil C. (2007) Comparison and predictors of rash associated with 15 antiepileptic drugs. Neurology 68: 1701–1709.
5. Arnold L. Russell I. Diri E. Duan W. Young J. Jr Sharma U. (2008) A 14-week, randomized, double-blinded, placebo-controlled monotherapy trial of pregabalin in patients with fibromyalgia. J Pain 9: 792–805.
6. Backonja M. (1999) Gabapentin monotherapy for the symptomatic treatment of painful neuropathy: a multicenter, double-blind, placebo-controlled trial in patients with diabetes mellitus. Epilepsia 40(Suppl. 6): S57–S59; discussion S73–S74.
7. Bansal D. Bhansali A. Hota D. Chakrabarti A. Dutta P. (2009) Amitriptyline vs. pregabalin in painful diabetic neuropathy: a randomized double blind clinical trial. Diabet Med 26: 1019–1026.
8. Barbarisi M. Pace M. Passavanti M. Maisto M. Mazzariello L. Pota V. (2010) Pregabalin and transcutaneous electrical nerve stimulation for postherpetic neuralgia treatment. Clin J Pain 26: 567–572.
9. Baron R. Freynhagen R. Tolle T. Cloutier C. Leon T. Murphy T. (2010) The efficacy and safety of pregabalin in the treatment of neuropathic pain associated with chronic lumbosacral radiculopathy. Pain 150: 420–427.
10. Baron R. Mayoral V. Leijon G. Binder A. Steigerwald I. Serpell M. (2009a) 5% lidocaine medicated plaster versus pregabalin in post-herpetic neuralgia and diabetic polyneuropathy: an open-label, non-inferiority two-stage RCT study. Curr Med Res Opin 25: 1663–1676.
11. Baron R. Mayoral V. Leijon G. Binder A. Steigerwald I. Serpell M. (2009b) Efficacy and safety of combination therapy with 5% lidocaine medicated plaster and pregabalin in post-herpetic neuralgia and diabetic polyneuropathy. Curr Med Res Opin 25: 1677–1687.
12. Bauer C. Nieto-Rostro M. Rahman W. Tran-Van-Minh A. Ferron L. Douglas L. (2009) The increased trafficking of the calcium channel subunit alpha2delta-1 to presynaptic terminals in neuropathic pain is inhibited by the alpha2delta ligand pregabalin. J Neurosci 29: 4076–4088.
13. Bockbrader H. Burger P. Knapp L. (2011) Pregabalin effect on steady-state pharmacokinetics of carbamazepine, lamotrigine, phenobarbital, phenytoin, topiramate, valproate, and tiagabine. Epilepsia 52: 405–409.
14. Bockbrader H. Wesche D. Miller R. Chapel S. Janiczek N. Burger P. (2010) A comparison of the pharmacokinetics and pharmacodynamics of pregabalin and gabapentin. Clin Pharmacokinet 49: 661–669.
15. Bouhassira D. Lanteri-Minet M. Attal N. Laurent B. Touboul C. (2008) Prevalence of chronic pain with neuropathic characteristics in the general population. Pain 136: 380–387.
16. Boyle J. Eriksson M. Gribble L. Gouni R. Johnsen S. Coppini D. (2012) Randomized, placebo-controlled comparison of amitriptyline, duloxetine, and pregabalin in patients with chronic diabetic peripheral neuropathic pain: impact on pain, polysomnographic sleep, daytime functioning, and quality of life. Diabetes Care 35: 2451–2458.
17. Bramness J. Sandvik P. Engeland A. Skurtveit S. (2010) Does pregabalin (Lyrica(R)) help patients reduce their use of benzodiazepines? A comparison with gabapentin using the Norwegian Prescription Database. Basic Clin Pharmacol Toxicol 107: 883–886.
18. Brawek B. Loffler M. Weyerbrock A. Feuerstein T. (2009) Effects of gabapentin and pregabalin on K+-evoked 3H-GABA and 3H-glutamate release from human neocortical synaptosomes. Naunyn Schmiedebergs Arch Pharmacol 379: 361–369.
19. Cabrera J. Emir B. Dills D. Murphy T. Whalen E. Clair A. (2012) Characterizing and understanding body weight patterns in patients treated with pregabalin. Curr Med Res Opin 28: 1027–1037.
20. Cada D. Levien D. Baker D. (2006) Pregabalin. Hospital Pharmacy 41: 157–172.
21. Cardenas D. Nieshoff E. Suda K. Goto S. Sanin L. Kaneko T. (2013) A randomized trial of pregabalin in patients with neuropathic pain due to spinal cord injury. Neurology 80: 533–539.
22. Chalabianloo F. Schjott J. (2009) [Pregabalin and its potential for abuse]. Tidsskr Nor Laegeforen 129: 186–187.
23. Chiechio S. Zammataro M. Caraci F. Rampello L. Copani A. Sabato A. (2009) Pregabalin in the treatment of chronic pain: an overview. Clin Drug Investig 29: 203–213.
24. Crofford L. Mease P. Simpson S. Young J. Jr Martin S. Haig G. (2008) Fibromyalgia relapse evaluation and efficacy for durability of meaningful relief (FREEDOM): a 6-month, double-blind, placebo-controlled trial with pregabalin. Pain 136: 419–431.
25. Delahoy P. Thompson S. Marschner I. (2010) Pregabalin versus gabapentin in partial epilepsy: a meta-analysis of dose-response relationships. BMC Neurol 10: 104.
26. Dogan S. Ozberk S. Yurci A. (2011) Pregabalin-induced hepatotoxicity. Eur J Gastroenterol Hepatol 23: 628.
27. Dworkin R. Corbin A. Young J. Jr Sharma U. LaMoreaux L. Bockbrader H. (2003) Pregabalin for the treatment of postherpetic neuralgia: a randomized, placebo-controlled trial. Neurology 60: 1274–1283.
28. Dworkin R. O–Connor A. Audette J. Baron R. Gourlay G. Haanpaa M. (2010) Recommendations for the pharmacological management of neuropathic pain: an overview and literature update. Mayo Clin Proc 85(3 Suppl.): S3–S14.
29. Einarsdottir S. Bjornsson E. (2008) Pregabalin as a probable cause of acute liver injury. Eur J Gastroenterol Hepatol 20: 1049.
30. Eipe N. Penning J. (2011) Postoperative respiratory depression with pregabalin: a case series and a preoperative decision algorithm. Pain Res Manag 16: 353–356.
31. Elliott A. Smith B. Penny K. Smith W. Chambers W. (1999) The epidemiology of chronic pain in the community. Lancet 354: 1248–1252.
32. Eroglu C. Allen N. Susman M. O–Rourke N. Park C. Ozkan E. (2009) Gabapentin receptor alpha2delta-1 is a neuronal thrombospondin receptor responsible for excitatory CNS synaptogenesis. Cell 139: 380–392.
33. Feltner D. Crockatt J. Dubovsky S. Cohn C. Shrivastava R. Targum S. (2003) A randomized, double-blind, placebo-controlled, fixed-dose, multicenter study of pregabalin in patients with generalized anxiety disorder. J Clin Psychopharmacol 23: 240–249.
34. Field M. Cox P. Stott E. Melrose H. Offord J. Su T. (2006) Identification of the alpha2-delta-1 subunit of voltage-dependent calcium channels as a molecular target for pain mediating the analgesic actions of pregabalin. Proc Natl Acad Sci U S A 103: 17537–17542.
35. Field M. Oles R. Singh L. (2001) Pregabalin may represent a novel class of anxiolytic agents with a broad spectrum of activity. Br J Pharmacol 132: 1–4.
36. Fink K. Dooley D. Meder W. Suman-Chauhan N. Duffy S. Clusmann H. (2002) Inhibition of neuronal Ca(2+) influx by gabapentin and pregabalin in the human neocortex. Neuropharmacology 42: 229–236.
37. Finnerup N. (2008) A review of central neuropathic pain states. Curr Opin Anaesthesiol 21: 586–589.
38. Freeman R. Durso-Decruz E. Emir B. (2008) Efficacy, safety, and tolerability of pregabalin treatment for painful diabetic peripheral neuropathy: findings from seven randomized, controlled trials across a range of doses. Diabetes Care 31: 1448–1454.
39. Freynhagen R. Baron R. (2009) The evaluation of neuropathic components in low back pain. Curr Pain Headache Rep 13: 185–190.
40. Freynhagen R. Strojek K. Griesing T. Whalen E. Balkenohl M. (2005) Efficacy of pregabalin in neuropathic pain evaluated in a 12-week, randomised, double-blind, multicentre, placebo-controlled trial of flexible- and fixed-dose regimens. Pain 115: 254–263.
41. Gajraj N. (2007) Pregabalin: its pharmacology and use in pain management. Anesth Analg 105: 1805–1815.
42. Gore M. Sadosky A. Tai K. Stacey B. (2007) A retrospective evaluation of the use of gabapentin and pregabalin in patients with postherpetic neuralgia in usual-care settings. Clin Ther 29: 1655–1670.
43. Gotz E. Feuerstein T. Lais A. Meyer D. (1993) Effects of gabapentin on release of gamma-aminobutyric acid from slices of rat neostriatum. Arzneimittelforschung 43: 636–638.
44. Gray P. Kirby J. Smith M. Cabot P. Williams B. Doecke J. (2011) Pregabalin in severe burn injury pain: a double-blind, randomised placebo-controlled trial. Pain 152: 1279–1288.
45. Heckmann J. Ulrich K. Dutsch M. Neundorfer B. (2005) Pregabalin associated asterixis. Am J Phys Med Rehabil 84: 724.
46. Hindmarch I. Trick L. Ridout F. (2005) A double-blind, placebo- and positive-internal-controlled (alprazolam) investigation of the cognitive and psychomotor profile of pregabalin in healthy volunteers. Psychopharmacology (Berl) 183: 133–143.
47. Huppertz H. Feuerstein T. Schulze-Bonhage A. (2001) Myoclonus in epilepsy patients with anticonvulsive add-on therapy with pregabalin. Epilepsia 42: 790–792.
48. Hurley R. Lesley M. Adams M. Brummett C. Wu C. (2008) Pregabalin as a treatment for painful diabetic peripheral neuropathy: a meta-analysis. Reg Anesth Pain Med 33: 389–394.
49. Hutson S. Berkich D. Drown P. Xu B. Aschner M. LaNoue K. (1998) Role of branched-chain aminotransferase isoenzymes and gabapentin in neurotransmitter metabolism. J Neurochem 71: 863–874.
50. Ifuku M. Iseki M. Hidaka I. Morita Y. Komatus S. Inada E. (2011) Replacement of gabapentin with pregabalin in postherpetic neuralgia therapy. Pain Med 12: 1112–1116.
51. Jenkins T. Smart T. Hackman F. Cooke C. Tan K. (2012) Efficient assessment of efficacy in post-traumatic peripheral neuropathic pain patients: pregabalin in a randomized, placebo-controlled, crossover study. J Pain Res 5: 243–250.
52. Jokela R. Ahonen J. Tallgren M. Haanpaa M. Korttila K. (2008) A randomized controlled trial of perioperative administration of pregabalin for pain after laparoscopic hysterectomy. Pain 134: 106–112.
53. Kaufman M. Choy M. (2012) Pregabalin and simvastatin: first report of a case of rhabdomyolysis. P T 37: 579–595.
54. Kim J. Bashford G. Murphy T. Martin A. Dror V. Cheung R. (2011) Safety and efficacy of pregabalin in patients with central post-stroke pain. Pain 152: 1018–1023.
55. Lawrence R. Helmick C. Arnett F. Deyo R. Felson D. Giannini E. (1998) Estimates of the prevalence of arthritis and selected musculoskeletal disorders in the United States. Arthritis Rheum 41: 778–799.
56. Lee S. (2012) Pregabalin intoxication-induced encephalopathy with triphasic waves. Epilepsy Behav 25: 170–173.
57. Lesser H. Sharma U. LaMoreaux L. Poole R. (2004) Pregabalin relieves symptoms of painful diabetic neuropathy: a randomized controlled trial. Neurology 63: 2104–2110.
58. Lindh J. (2010) [Hepatic adverse effects of pregabalin (Lyrica)]. Lakartidningen 107: 194.
59. Lucke A. Musshoff U. Kohling R. Osterfeld M. Mayer T. Wolf P. (1998) Gabapentin potentiation of the antiepileptic efficacy of vigabatrin in an in vitro model of epilepsy. Br J Pharmacol 124: 370–376.
60. Malaga I. Sanmarti F. (2006) Two cases of painful gynecomastia and lower extremity pain in association with pregabalin therapy. Epilepsia 47: 1576–1579.
61. Mease P. Russell I. Arnold L. Florian H. Young J. Jr Martin S. (2008) A randomized, double-blind, placebo-controlled, phase III trial of pregabalin in the treatment of patients with fibromyalgia. J Rheumatol 35: 502–514.
62. Mellick G. Mellick L. (1997) Reflex sympathetic dystrophy treated with gabapentin. Arch Phys Med Rehabil 78: 98–105.
63. Mellick G. Mellicy L. Mellick L. (1995) Gabapentin in the management of reflex sympathetic dystrophy. J Pain Symptom Manage 10: 265–266.
64. Mellick L. Mellick G. (1995) Successful treatment of reflex sympathetic dystrophy with gabapentin. Am J Emerg Med 13: 96.
65. Micheva K. Taylor C. Smith S. (2006) Pregabalin reduces the release of synaptic vesicles from cultured hippocampal neurons. Mol Pharmacol 70: 467–476.
66. Mishra S. Bhatnagar S. Nirvani Goyal G. Pratap Singh Rana S. Upadhya S. (2012) A comparative efficacy of amitriptyline, gabapentin, and pregabalin in neuropathic cancer pain: a prospective randomized double-blind placebo-controlled study. Am J Hosp Palliat Care 29: 177–182.
67. Moon D. Lee D. Lee S. Song S. Yoon D. Yoon M. (2010) Efficacy and tolerability of pregabalin using a flexible, optimized dose schedule in Korean patients with peripheral neuropathic pain: a 10-week, randomized, double-blind, placebo-controlled, multicenter study. Clin Ther 32: 2370–2385.
68. Moore R. Straube S. Wiffen P. Derry S. McQuay H. (2009) Pregabalin for acute and chronic pain in adults. Cochrane Database Syst Rev (3): CD007076.
69. Moulin D. Clark A. Gilron I. Ware M. Watson C. Sessle B. (2007) Pharmacological management of chronic neuropathic pain - consensus statement and guidelines from the Canadian Pain Society. Pain Res Manag 12: 13–21.
70. Navarro A. Saldana M. Perez C. Torrades S. Rejas J. (2010) Patient-reported outcomes in subjects with neuropathic pain receiving pregabalin: evidence from medical practice in primary care settings. Pain Med 11: 719–731.
71. Navarro A. Saldana M. Perez C. Torrades S. Rejas J. (2011) A cost-consequences analysis of the effect of pregabalin in the treatment of peripheral neuropathic pain in routine medical practice in primary care settings. BMC Neurol 11: 7.
72. Norton J. (2001) Gabapentin withdrawal syndrome. Clin Neuropharmacol 24: 245–246.
73. O–Connor A. Dworkin R. (2009) Treatment of neuropathic pain: an overview of recent guidelines. Am J Med 122(10 Suppl.): S22–S32.
74. Oaklander A. Buchbinder B. (2005) Pregabalin-withdrawal encephalopathy and splenial edema: a link to high-altitude illness? Ann Neurol 58: 309–312.
75. Ohta H. Oka H. Usui C. Ohkura M. Suzuki M. Nishioka K. (2012) A randomized, double-blind, multicenter, placebo-controlled phase III trial to evaluate the efficacy and safety of pregabalin in Japanese patients with fibromyalgia. Arthritis Res Ther 14: R217.
76. Oteri A. Trifiro G. Gagliostro M. Tari D. Moretti S. Bramanti P. (2010) Prescribing pattern of anti-epileptic drugs in an Italian setting of elderly outpatients: a population-based study during 2004–07. Br J Clin Pharmacol 70: 514–522.
77. Pande A. Crockatt J. Feltner D. Janney C. Smith W. Weisler R. (2003) Pregabalin in generalized anxiety disorder: a placebo-controlled trial. Am J Psychiatry 160: 533–540.
78. Parke-Davis (2005) Neurontin (gabapentin) [package insert]. New York: Parke-Davis Inc.
79. Parker D. Ong J. Marino V. Kerr D. (2004) Gabapentin activates presynaptic GABAB heteroreceptors in rat cortical slices. Eur J Pharmacol 495: 137–143.
80. Pauer L. Atkinson G. Murphy T. Petersel D. Zeiher B. (2012) Long-term maintenance of response across multiple fibromyalgia symptom domains in a randomized withdrawal study of pregabalin. Clin J Pain 28: 609–614.
81. Pauer L. Winkelmann A. Arsenault P. Jespersen A. Whelan L. Atkinson G. (2011) An international, randomized, double-blind, placebo-controlled, phase III trial of pregabalin monotherapy in treatment of patients with fibromyalgia. J Rheumatol 38: 2643–2652.
82. Perez C. Navarro A. Saldana M. Masramon X. Rejas J. (2010) Pregabalin and gabapentin in matched patients with peripheral neuropathic pain in routine medical practice in a primary care setting: findings from a cost-consequences analysis in a nested case-control study. Clin Ther 32: 1357–1370.
83. Perez C. Saldana M. Navarro A. Martinez S. Rejas J. (2009) Trigeminal neuralgia treated with pregabalin in family medicine settings: its effect on pain alleviation and cost reduction. J Clin Pharmacol 49: 582–590.
84. Perret D. Luo Z. (2009) Targeting voltage-gated calcium channels for neuropathic pain management. Neurotherapeutics 6: 679–692.
85. Pfizer (2005) Lyrica® (pregabalin) [package insert]. New York: Pfizer Inc.
86. Piyapolrungroj N. Li C. Bockbrader H. Liu G. Fleisher D. (2001) Mucosal uptake of gabapentin (neurontin) vs. pregabalin in the small intestine. Pharm Res 18: 1126–1130.
87. Pohl R. Feltner D. Fieve R. Pande A. (2005) Efficacy of pregabalin in the treatment of generalized anxiety disorder: double-blind, placebo-controlled comparison of BID versus TID dosing. J Clin Psychopharmacol 25: 151–158.
88. Pontari M. Krieger J. Litwin M. White P. Anderson R. McNaughton-Collins M. (2010) Pregabalin for the treatment of men with chronic prostatitis/chronic pelvic pain syndrome: a randomized controlled trial. Arch Intern Med 170: 1586–1593.
89. Prilipko O. Delavelle J. Seeck M. (2006) Pregabalin-withdrawal encephalopathy and splenial edema. Ann Neurol 59: 214.
90. Quilici S. Chancellor J. Lothgren M. Simon D. Said G. Le T.K. (2009) Meta-analysis of duloxetine vs. pregabalin and gabapentin in the treatment of diabetic peripheral neuropathic pain. BMC Neurol 9: 6.
91. Randinitis E. Posvar E. Alvey C. Sedman A. Cook J. Bockbrader H. (2003) Pharmacokinetics of pregabalin in subjects with various degrees of renal function. J Clin Pharmacol 43: 277–283.
92. Rehm S. Binder A. Baron R. (2010) Post-herpetic neuralgia: 5% lidocaine medicated plaster, pregabalin, or a combination of both? A randomized, open, clinical effectiveness study. Curr Med Res Opin 26: 1607–1619.
93. Rice A. Maton S. (2001a) Gabapentin in postherpetic neuralgia: a randomised, double blind, placebo controlled study. Pain 94: 215–224.
94. Rice A. Maton S. (2001b) Gabapentin in postherpetic neuralgia: a randomised, double blind, placebo controlled study. Pain 94: 215–224.
95. Richter R. Portenoy R. Sharma U. Lamoreaux L. Bockbrader H. Knapp L. (2005) Relief of painful diabetic peripheral neuropathy with pregabalin: a randomized, placebo-controlled trial. J Pain 6: 253–260.
96. Romano C. Romano D. Bonora C. Mineo G. (2009) Pregabalin, celecoxib, and their combination for treatment of chronic low-back pain. J Orthop Traumatol 10: 185–191.
97. Rosenstock J. Cappelleri J. Bolinder B. Gerber R. (2004a) Patient satisfaction and glycemic control after 1 year with inhaled insulin (Exubera) in patients with type 1 or type 2 diabetes. Diabetes Care 27: 1318–1323.
98. Rosenstock J. Tuchman M. LaMoreaux L. Sharma U. (2004b) Pregabalin for the treatment of painful diabetic peripheral neuropathy: a double-blind, placebo-controlled trial. Pain 110: 628–638.
99. Rowan A. Ramsay R. Collins J. Pryor F. Boardman K. Uthman B. (2005) New onset geriatric epilepsy: a randomized study of gabapentin, lamotrigine, and carbamazepine. Neurology 64: 1868–1873.
100. Rowbotham M. Harden N. Stacey B. Bernstein P. Magnus-Miller L. (1998) Gabapentin for the treatment of postherpetic neuralgia: a randomized controlled trial. JAMA 280: 1837–1842.
101. Ryu J. Lee P. Kim J. Do S. Kim C. (2012) Effects of pregabalin on the activity of glutamate transporter type 3. Br J Anaesth 109: 234–239.
102. Sabatowski R. Galvez R. Cherry D. Jacquot F. Vincent E. Maisonobe P. (2004) Pregabalin reduces pain and improves sleep and mood disturbances in patients with post-herpetic neuralgia: results of a randomised, placebo-controlled clinical trial. Pain 109: 26–35.
103. Saldana M. Navarro A. Perez C. Masramon X. Rejas J. (2010) A cost-consequences analysis of the effect of pregabalin in the treatment of painful radiculopathy under medical practice conditions in primary care settings. Pain Pract 10: 31–41.
104. Saldana M. Perez C. Navarro A. Masramon X. Rejas J. (2012) Pain alleviation and patient-reported health outcomes following switching to pregabalin in individuals with gabapentin-refractory neuropathic pain in routine medical practice. Clin Drug Investig 32: 401–412.
105. Satoh J. Yagihashi S. Baba M. Suzuki M. Arakawa A. Yoshiyama T. (2011) Efficacy and safety of pregabalin for treating neuropathic pain associated with diabetic peripheral neuropathy: a 14 week, randomized, double-blind, placebo-controlled trial. Diabet Med 28: 109–116.
106. Satzinger G. Hartenstein J. Herrmann M. Heidt W. Goedecke A. (1976) Cyclic amino acids. Ger. Offen. DE 2460891.
107. Schifano F. D–Offizi S. Piccione M. Corazza O. Deluca P. Davey Z. (2011) Is there a recreational misuse potential for pregabalin? Analysis of anecdotal online reports in comparison with related gabapentin and clonazepam data. Psychother Psychosom 80: 118–122.
108. Schwan S. Sundstrom A. Stjernberg E. Hallberg E. Hallberg P. (2010) A signal for an abuse liability for pregabalin – results from the Swedish spontaneous adverse drug reaction reporting system. Eur J Clin Pharmacol 66: 947–953.
109. Semel D. Murphy T. Zlateva G. Cheung R. Emir B. (2010) Evaluation of the safety and efficacy of pregabalin in older patients with neuropathic pain: results from a pooled analysis of 11 clinical studies. BMC Fam Pract 11: 85.
110. Sendra J. Junyent T. Pellicer M. (2011) Pregabalin-induced hepatotoxicity. Ann Pharmacother 45: e32.
111. Sharma U. Griesing T. Emir B. Young J. Jr (2010) Time to onset of neuropathic pain reduction: a retrospective analysis of data from nine controlled trials of pregabalin for painful diabetic peripheral neuropathy and postherpetic neuralgia. Am J Ther 17: 577–585.
112. Siddall P. Cousins M. Otte A. Griesing T. Chambers R. Murphy T. (2006) Pregabalin in central neuropathic pain associated with spinal cord injury: a placebo-controlled trial. Neurology 67: 1792–1800.
113. Simpson D. Schifitto G. Clifford D. Murphy T. Durso-De Cruz E. Glue P. (2010) Pregabalin for painful HIV neuropathy: a randomized, double-blind, placebo-controlled trial. Neurology 74: 413–420.
114. Smith T. Baldwin A. Cunningham L. Jr Cook A. (2008) Rash associated with pregabalin use. Ann Pharmacother 42: 1899–1902.
115. Stacey B. Barrett J. Whalen E. Phillips K. Rowbotham M. (2008a) Pregabalin for postherpetic neuralgia: placebo-controlled trial of fixed and flexible dosing regimens on allodynia and time to onset of pain relief. J Pain 9: 1006–1017.
116. Stacey B. Dworkin R. Murphy K. Sharma U. Emir B. Griesing T. (2008b) Pregabalin in the treatment of refractory neuropathic pain: results of a 15-month open-label trial. Pain Med 9: 1202–1208.
117. Su T. Feng M. Weber M. (2005) Mediation of highly concentrative uptake of pregabalin by L-type amino acid transport in Chinese hamster ovary and Caco-2 cells. J Pharmacol Exp Ther 313: 1406–1415.
118. Tanenberg R. Irving G. Risser R. Ahl J. Robinson M. Skljarevski V. (2011) Duloxetine, pregabalin, and duloxetine plus gabapentin for diabetic peripheral neuropathic pain management in patients with inadequate pain response to gabapentin: an open-label, randomized, noninferiority comparison. Mayo Clin Proc 86: 615–626.
119. Tansey B. (2004) Huge penalty in drug fraud Pfizer settles felony case in Neurontin off-label promotion. San Franscisco Chronicle, http://www.sfgate.com/cgi-bin/article.cgi?f=/c/a/2004/05/14/BUGKK6L0LB1.DTL (accessed 2 September 2013).
120. Taylor C. Angelotti T. Fauman E. (2007) Pharmacology and mechanism of action of pregabalin: the calcium channel alpha2-delta (alpha2-delta) subunit as a target for antiepileptic drug discovery. Epilepsy Res 73: 137–150.
121. Tolle T. Freynhagen R. Versavel M. Trostmann U. Young J. Jr (2008) Pregabalin for relief of neuropathic pain associated with diabetic neuropathy: a randomized, double-blind study. Eur J Pain 12: 203–213.
122. Torrance N. Smith B. Bennett M. Lee A. (2006) The epidemiology of chronic pain of predominantly neuropathic origin. Results from a general population survey. J Pain 7: 281–289.
123. Toth C. (2010) Substitution of gabapentin therapy with pregabalin therapy in neuropathic pain due to peripheral neuropathy. Pain Med 11: 456–465.
124. Toth C. (2012) Drug safety evaluation of pregabalin. Expert Opin Drug Saf 11: 487–502.
125. Toth C. Lander J. Wiebe S. (2009) The prevalance and impact of chronic pain with neuropathic pain symptoms in the general population. Pain Med 10: 918–929.
126. Treede R. Jensen T. Campbell J. Cruccu G. Dostrovsky J. Griffin J. (2008) Neuropathic pain: redefinition and a grading system for clinical and research purposes. Neurology 70: 1630–1635.
127. van Seventer R. Bach F. Toth C. Serpell M. Temple J. Murphy T. (2010) Pregabalin in the treatment of post-traumatic peripheral neuropathic pain: a randomized double-blind trial. Eur J Neurol 17: 1082–1089.
128. van Seventer R. Feister H. Young J. Jr Stoker M. Versavel M. Rigaudy L. (2006) Efficacy and tolerability of twice-daily pregabalin for treating pain and related sleep interference in postherpetic neuralgia: a 13-week, randomized trial. Curr Med Res Opin 22: 375–384.
129. Vartanian M. Radulovic L. Kinsora J. Serpa K. Vergnes M. Bertram E. (2006) Activity profile of pregabalin in rodent models of epilepsy and ataxia. Epilepsy Res 68: 189–205.
130. Verhaak P. Kerssens J. Dekker J. Sorbi M. Bensing J. (1998) Prevalence of chronic benign pain disorder among adults: a review of the literature. Pain 77: 231–239.
131. Vranken J. Dijkgraaf M. Kruis M. van der Vegt M. Hollmann M. Heesen M. (2008) Pregabalin in patients with central neuropathic pain: a randomized, double-blind, placebo-controlled trial of a flexible-dose regimen. Pain 136: 150–157.
132. Weissmann C. Di Guilmi M. Urbano F. Uchitel O. (2013) Acute effects of pregabalin on the function and cellular distribution of Ca(V)2.1 in HEK293t cells. Brain Res Bull 90: 107–113.
133. Wilhelm S. Schacht A. Lledo A. Pamulapati S. Tesfaye S. Tölle T. (2012) Use of duloxetine or pregabalin in monotherapy versus combination therapy or both drugs in patients with painful diabetic neuropathy: the ‘COMBO-DN Study–, a randomized, double blind, parallel group trial. Milan, Italy: International Association for the Study of Pain.
134. Xu Y. Oz G. LaNoue K. Keiger C. Berkich D. Gruetter R. (2004) Whole-brain glutamate metabolism evaluated by steady-state kinetics using a double-isotope procedure: effects of gabapentin. J Neurochem 90: 1104–1116.
135. Zin C. Nissen L. O–Callaghan J. Moore B. Smith M. (2010) Preliminary study of the plasma and cerebrospinal fluid concentrations of IL-6 and IL-10 in patients with chronic pain receiving intrathecal opioid infusions by chronically implanted pump for pain management. Pain Med 11: 550–561.