title: Review of the treatment of restless legs syndrome: focus on gabapentin enacarbil.
abstract: The FDA approved gabapentin enacarbil in 2011 as the first non-dopaminergic agent for the treatment of restless legs syndrome (RLS) symptoms. Although gabapentin enacarbil is a pro-drug of gabapentin, its pharmacokinetics differ. Absorption of gabapentin enacarbil is more predictable, and inter-patient variability in bioavailability is lower than that of gabapentin. Studies have demonstrated superiority of gabapentin enacarbil compared to placebo. Comparisons to currently available RLS treatments are lacking, but clinical trials demonstrate comparable improvement in RLS symptoms to the dopamine agonists ropinirole and pramipexole, which are usually considered first-line therapy for daily RLS symptoms. Gabapentin enacarbil was well tolerated in clinical trials. The role of the drug in RLS treatment remains undefined, although it will likely be used as an alternative for refractory RLS when other treatments have failed. Additionally, gabapentin enacarbil may be recommended for patients with daily RLS symptoms that are less intense or are associated with pain as an alternative to dopamine agonists.
authors: Creighton University School of Pharmacy and Health Professions, Omaha, Nebraska, USA.
authors: Rachel A
authors: RA
authors: Burke
authors: Michele A
authors: MA
authors: Faulkner
keywords: Horizant; RLS; dopamine agonists; gabapentin enacarbil; restless legs syndrome
references: Curr Drug Saf. 2010 Apr;5(2):129-31
references: 20406161
references: Sleep Med. 2003 Mar;4(2):101-19
references: 14592341
references: CNS Drugs. 2009;23(4):281-92
references: 19374458
references: Neurology. 2007 May 8;68(19):1631-3
references: 17485653
references: Sleep Med. 2008 Jul;9(5):537-41
references: 18276187
references: Neurology. 2009 Feb 3;72(5):439-46
references: 19188575
references: Home Healthc Nurse. 2005 Apr;23(4):207-9
references: 15824606
references: Sleep Med. 2011 Aug;12(7):623-34
references: 21752711
references: Int J Clin Pharmacol Ther. 2010 Feb;48(2):120-8
references: 20137764
references: Neurology. 2002 Nov 26;59(10):1573-9
references: 12451200
references: Eur J Clin Pharmacol. 2011 May;67(5):539-40
references: 21104073
references: Mayo Clin Proc. 2010 Jun;85(6):512-21
references: 20511481
references: Sleep. 2004 Aug 1;27(5):907-14
references: 15453549
references: Sleep Med. 2010 Jan;11(1):31-7
references: 19464949
references: Neurology. 2006 Sep 26;67(6):1034-9
references: 16931507
references: Sleep. 1996 Dec;19(10):801-10
references: 9085489
references: Mayo Clin Proc. 2004 Jul;79(7):916-22
references: 15244390
references: Mov Disord. 2011 Sep;26(11):2065-72
references: 21611981
references: J Neurol Sci. 2009 Apr 15;279(1-2):62-5
references: 19167016
references: Sleep Med. 2001 Jan;2(1):57-61
references: 11152983
references: Cochrane Database Syst Rev. 2011 Mar 16;(3):CD006009
references: 21412893
references: Sleep Med. 2006 Oct;7(7):592-3
references: 16926116
references: Sleep Med. 2002 Jul;3(4):301-4
references: 14592191
references: Annu Rev Nutr. 2003;23:41-58
references: 12704220
references: Arch Intern Med. 2005 Jun 13;165(11):1286-92
references: 15956009
references: BMC Neurol. 2011 Sep 28;11:117
references: 21955669
references: Pain Med. 2011 Jul;12(7):1098-108
references: 21627766
references: Mov Disord. 2004 Dec;19(12):1414-23
references: 15390050
references: Clin Ther. 2009 Aug;31(8):1776-86
references: 19808136
references: J Neurol Neurosurg Psychiatry. 2004 Jan;75(1):92-7
references: 14707315
references: Lancet Neurol. 2011 Aug;10(8):710-20
references: 21705273
references: Sleep. 1999 Nov 1;22(7):970-99
references: 10566916
references: Curr Neurol Neurosci Rep. 2008 May;8(3):211-6
references: 18541116
references: Arch Neurol. 2004 Sep;61(9):1393-7
references: 15364685
references: Clin Neuropharmacol. 2009 Nov-Dec;32(6):311-20
references: 19667976
references: J Clin Sleep Med. 2011 Jun 15;7(3):282-92
references: 21677899
references: Sleep. 1998 Jun 15;21(4):371-7
references: 9646381
references: J Clin Sleep Med. 2010 Feb 15;6(1):79-83
references: 20191944
references: Neurology. 2000 Nov 14;55(9):1404-6
references: 11087794
references: Clin Neuropharmacol. 2011 Jan-Feb;34(1):8-16
references: 21242741
references: CNS Drugs. 2008;22(6):497-518
references: 18484792
references: J Neural Transm (Vienna). 2010 Apr;117(4):463-73
references: 20049491
references: Clin Neuropharmacol. 2007 Sep-Oct;30(5):249-55
references: 17909302
references: Sleep Med. 2007 Nov;8(7-8):742-52
references: 17512789
references: Neurology. 1999 Mar 23;52(5):938-43
references: 10102409
references: Cochrane Database Syst Rev. 2011 Feb 16;(2):CD005504
references: 21328278
references: Ren Fail. 2004 Jul;26(4):393-7
references: 15462107
references: J Clin Neurophysiol. 2001 Mar;18(2):128-47
references: 11435804
references: Neurology. 2007 Jan 23;68(4):301-3
references: 17242339
references: Mov Disord. 2008 Dec 15;23(16):2267-302
references: 18925578
references: Neuropsychobiology. 2003;48(2):82-6
references: 14504416
references: J Clin Pharmacol. 2008 Dec;48(12):1378-88
references: 18827074
references: Pharmacopsychiatry. 2002 May;35(3):109-11
references: 12107855
references: Sleep Med. 2006 Aug;7(5):407-17
references: 16815748
references: Pharm Res. 1993 Feb;10(2):276-81
references: 8456077
references: J Pharmacol Exp Ther. 2004 Oct;311(1):315-23
references: 15146028
references: Sleep Med. 2004 May;5(3):237-46
references: 15165529
references: Mov Disord. 2007 Apr 15;22(5):627-31
references: 17285614
references: Neurology. 1993 Feb;43(2):445
references: 8094897
references: Sleep. 2009 Feb;32(2):159-68
references: 19238802
references: BMC Neurol. 2011 Feb 27;11:28
references: 21352569
references: J Postgrad Med. 2010 Apr-Jun;56(2):157-62
references: 20622400