Gabapentin enacarbil for treatment of restless legs syndrome in adults;Enacarbilo de gabapentina para el tratamiento del síndrome de piernas inquietas en adultos

Annals of Pharmacotherapy

Volumn 46, Issue 2, 2012, Pages 229-239

  Hayes, William J ^a   Lemon, Michael D ^a   Farver, Debra K ^a  

^a SOUTH DAKOTA STATE UNIVERSITY   (United States)

Author keywords

Gabapentin enacarbil; Restless legs syndrome; XP13512 GSK1838262

Indexed keywords

DIPHENHYDRAMINE; GABAPENTIN ENACARBIL; PLACEBO;

ADULT DISEASE; APPETITE; AREA UNDER THE CURVE; BODY WEIGHT; DEPRESSION; DISEASE SEVERITY; DIZZINESS; DRESS SYNDROME; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG COST; DRUG EFFICACY; DRUG ELIMINATION; DRUG ERUPTION; DRUG FEVER; DRUG HALF LIFE; DRUG MECHANISM; DRUG PROTEIN BINDING; DRUG SAFETY; FATIGUE; FLATULENCE; HUMAN; LIBIDO; LYMPHADENOPATHY; NAUSEA; PATIENT COUNSELING; PERIPHERAL EDEMA; PRIORITY JOURNAL; RESTLESS LEGS SYNDROME; REVIEW; SIDE EFFECT; SOMNOLENCE; STEADY STATE; SUICIDE; THERAPY EFFECT; VERTIGO; XEROSTOMIA;

ADULT; ANIMALS; CALCIUM CHANNEL BLOCKERS; CARBAMATES; GAMMA-AMINOBUTYRIC ACID; HUMANS; PRODRUGS; RESTLESS LEGS SYNDROME;

EID: 84856997587     PISSN: 10600280     EISSN: None     Source Type: Journal    
DOI: 10.1345/aph.1Q578     Document Type: Review

References (44)

1. Allen RP, Bharmal M, Calloway M. Prevalence and disease burden of primary restless legs syndrome: results of a general population survey in the United States. Mov Disord 2011;26:114-20. DOI 10.1002/mds.23430
2. Allen RP, Stillman P, Myers AJ. Physician-diagnosed restless legs syndrome in a large sample of primary medical care patients in western Europe: prevalence and characteristics. Sleep Med 2010;11:31-7. DOI 10.1016/j.sleep.2009.03.007
3. Allen RP, Walters AS, Montplaisir J, et al. Restless legs syndrome prevalence and impact: REST general population study. Arch Intern Med 2005;165:1286-92. DOI 10.1001/archinte.165.11.1286
4. Allen RP, Picchietti D, Hening WA, Trenkwalder C, Walters AS, Montplaisi J. Restless legs syndrome: diagnostic criteria, special considerations, and epidemiology. A report from the restless legs syndrome diagnosis and epidemiology workshop at the National Institutes of Health. Sleep Med 2003;4:101-19.
5. Earley CJ, Silber MH. Restless legs syndrome: understanding its consequences and the need for better treatment. Sleep Med 2010;11:807-15. DOI 10.1016/j.sleep.2010.07.007
6. Abetz L, Allen R, Follet A, et al. Evaluating the quality of life of patients with restless legs syndrome. Clin Ther 2004;26:925-35.
7. Garcia-Borreguero D, Stillman P, Benes H, et al. Algorithms for the diagnosis and treatment of restless legs syndrome in primary care. BMC Neurol 2011;11:28. DOI 10.1186/1471-2377-11-28
8. Silber MH, Ehrenberg BL, Allen RP, et al. An algorithm for the management of restless legs syndrome. Mayo Clin Proc 2004;79:916-22.
9. Hening WA. Current guidelines and standards of practice for restless legs syndrome. Am J Med 2007;120:S22-7. DOI 10.1016/j.amjmed.2006.11.004
10. Vignatelli L, Billiard M, Clarenbach P, et al. EFNS guidelines on management of restless legs syndrome and periodic limb movement disorder in sleep. Eur J Neurol 2006;13:1049-65. DOI 10.1111/j.1468-1331.2006.01410.x
11. Trenkwalder C, Hening WA, Montagna P, et al. Treatment of restless legs syndrome: an evidence-based review and implications for clinical practice. Mov Disord 2008;23:2267-302. DOI 10.1002/mds.22254
12. Product information. Mirapex (pramipexole). Ridgefield, CT: Boehringer Ingelheim Pharmaceuticals, Inc., May 2011.
13. Product information. Requip (ropinirole). Research Triangle Park, NC: GlaxoSmithKline, May 2009.
14. Ferini-Strambi L, Manconi M. Treatment of restless legs syndrome. Parkinsonism Relat Disord 2009;15(suppl 4):S65-70. DOI 10.1016/s1353-8020(09)70838-7
15. Zintzaras E, Kitsios GD, Papathanasiou AA, et al. Randomized trials of dopamine agonists in restless legs syndrome: a systematic review, quality assessment, and meta-analysis. Clin Ther 2010;32:221-37. DOI 10.1016/j.clinthera.2010.01.028
16. Garcia-Borreguero D, Allen RP, Benes H, et al. Augmentation as a treatment complication of restless legs syndrome: concept and management. Mov Disord 2007;22(suppl 18):S476-84. DOI 10.1002/mds.21610
17. Garcia-Borreguero D, Williams AM. Dopaminergic augmentation of restless legs syndrome. Sleep Med Rev 2010;14:339-46. DOI 10.1016/j.smrv.2009.11.006
18. Garcia-Borreguero D, Larrosa O, de la Llave Y, Verger K, Masramon X, Hernandez G. Treatment of restless legs syndrome with gabapentin: a double-blind, cross-over study. Neurology 2002;59:1573-9.
19. Happe S, Klosch G, Saletu B, Zeitlhofer J. Treatment of idiopathic restless legs syndrome (RLS) with gabapentin. Neurology 2001;57:1717-9.
20. Happe S, Sauter C, Klosch G, Saletu B, Zeitlhofer J. Gabapentin versus ropinirole in the treatment of idiopathic restless legs syndrome. Neuropsychobiology 2003;48:82-6. DOI 10.1159/000072882
21. Merlino G, Serafini A, Lorenzut S, Sommaro M, Gigli GL, Valente M. Gabapentin enacarbil in restless legs syndrome. Drugs Today (Barc) 2010;46:3-11. DOI 10.1358/dot.2010.46.1.1424766
22. Kushida CA, Walters AS, Becker P, et al. A randomized, double-blind, placebo-controlled, crossover study of XP13512/GSK1838262 in the treatment of patients with primary restless legs syndrome. Sleep 2009;32:159-68.
23. Gidal BE, Radulovic LL, Kruger S, Rutecki P, Pitterle M, Bockbrader HN. Inter-and intra-subject variability in gabapentin absorption and absolute bioavailability. Epilepsy Res 2000;40:123-7.
24. Product information. Horizant (gabapentin enacarbil). Research Triangle Park, NC: GlaxoSmithKline, December 2011.
25. Cundy KC, Annamalai T, Bu L, et al. XP13512 [(+/-)-1-([(alpha-isobutanoyloxyethoxy) carbonyl] aminomethyl)-1-cyclohexane acetic acid], a novel gabapentin prodrug: II. Improved oral bioavailability, dose proportionality, and colonic absorption compared with gabapentin in rats and monkeys. J Pharmacol Exp Ther 2004;311:324-33. DOI 10.1124/jpet.104.067959
26. Cundy KC, Sastry S, Luo W, Zou J, Moors TL, Canafax DM. Clinical pharmacokinetics of XP13512, a novel transported prodrug of gabapentin. J Clin Pharmacol 2008;48:1378-88. DOI 10.1177/0091270008322909
27. Product information. Neurontin (gabapentin). New York, NY: Parke-Davis Division of Pfizer Inc., July 2010.
28. Lal R, Sukbuntherng J, Luo W, et al. Pharmacokinetics and tolerability of single escalating doses of gabapentin enacarbil: a randomized-sequence, double-blind, placebo-controlled crossover study in healthy volunteers. Clin Ther 2009;31:1776-86. DOI 10.1016/j.clinthera.2009.07.026
29. Stewart BH, Kugler AR, Thompson PR, Bockbrader HN. A saturable transport mechanism in the intestinal absorption of gabapentin is the underlying cause of the lack of proportionality between increasing dose and drug levels in plasma. Pharm Res 1993;10:276-81.
30. Stevenson CM, Kim J, Fleisher D. Colonic absorption of antiepileptic agents. Epilepsia 1997;38:63-7.
31. Kushida CA, Becker PM, Ellenbogen AL, Canafax DM, Barrett RW. Randomized, double-blind, placebo-controlled study of XP13512/ GSK1838262 in patients with RLS. Neurology 2009;72:439-46. DOI 10.1212/01.wnl.0000341770.91926.cc
32. Walters AS, Ondo WG, Kushida CA, et al. Gabapentin enacarbil in restless legs syndrome: a phase 2b, 2-week, randomized, double-blind, placebo-controlled trial. Clin Neuropharmacol 2009;32:311-20. DOI 10.1097/WNF.0b013e3181b3ab16
33. Lee DO, Ziman RB, Perkins AT, Poceta JS, Walters AS, Barrett RW. A randomized, double-blind, placebo-controlled study to assess the efficacy and tolerability of gabapentin enacarbil in subjects with restless legs syndrome. J Clin Sleep Med 2011;7:282-92. DOI 10.5664/jcsm.1074
34. Bogan RK, Bornemann MA, Kushida CA, Tran PV, Barrett RW. Longterm maintenance treatment of restless legs syndrome with gabapentin enacarbil: a randomized controlled study. Mayo Clin Proc 2010;85:512-21.
35. Ellenbogen AL, Thein SG, Winslow DH, et al. A 52-week study of gabapentin enacarbil in restless legs syndrome. Clin Neuropharmacol 2011;34:8-16. DOI 10.1097/WNF.0b013e3182087d48
36. Winkelman JW, Bogan RK, Schmidt MH, Hudson JD, Derossett SE, Hill-Zabala CE. Randomized polysomnography study of gabapentin enacarbil in subjects with restless legs syndrome. Mov Disord 2011;26: 2065-72. DOI 10.1002/mds.23771
37. Canafax DM, Bhanegaonkar A, Bharmal M, Calloway M. Validation of the Post Sleep Questionnaire for assessing subjects with restless legs syndrome: results from two double-blind, multicenter, placebo-controlled clinical trials. BMC Neurol 2011;11:48. DOI 10.1186/1471-2377-11-48
38. Zomorodi K, Lal R, Atluri H, et al. A randomized, double-blind, placebocontrolled, dose-response study to assess the pharmacokinetics and tolerability of gabapentin enacarbil in subjects with restless legs syndrome. J Clin Pharmacol 2009;49:1122.
39. Food and Drug Administration. Medical review of gabapentin enacarbil. www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022399Orig1s000 MedR.pdf (accessed 2011 Sept 2).
40. Center For Drug Evaluation And Research. Summary review document for gabapentin enacarbil. www.accessdata.fda.gov/drugsatfda_docs/nda/ 2011/022399Orig1s000SumR.pdf (accessed 2011 Sept 2).
41. Montplaisir J, Karrasch J, Haan J, Volc D. Ropinirole is effective in the long-term management of restless legs syndrome: a randomized controlled trial. Mov Disord 2006;21:1627-35. DOI 10.1002/mds.21050
42. Trenkwalder C, Stiasny-Kolster K, Kupsch A, Oertel WH, Koester J, Reess J. Controlled withdrawal of pramipexole after 6 months of openlabel treatment in patients with restless legs syndrome. Mov Disord 2006;21:1404-10. DOI 10.1002/mds.20983
43. McKesson Connect. 2012. https://connect.mckesson.com/portal/site/smo/ template.LOGIN/?cid=mckcom (accessed 2012 Jan 26).
44. GlaxoSmithKline. Quick Search for gabapentin enacarbil. August 2011. www.gsk-clinicalstudyregister.com/quick-search-list.jsp?tab=protocols &letterrange=G-K&type=Compound&item=gabapentin+enacarbil& studyType=All&phase=All&status=All&population=All&marketing=All &country=All&studyId= (accessed 2011 Sept 2).