Role of gabapentin enacarbil XR in restless legs syndrome.

Therapeutics and Clinical Risk Management
Sheila Sivam, Brendon J Yee

Abstract

Gabapentin enacarbil XR is a new extended-release formulation which attempts to overcome the reduced efficacy of shorter-acting gabapentin, with sustained delivery over a 24-hour period. It is a gabapentin prodrug which is efficiently and rapidly converted to gabapentin during active transport throughout the length of the intestine via high-capacity monocarboxylate type 1 nutrient transporters unlike its predecessor, which is absorbed via low-capacity transporters largely confined to the upper intestinal region. Its lack of saturable absorption allows for dose-proportional absorption and hence increased bioavailability. Several clinical trials addressing its efficacy in moderate to severe restless legs syndrome (RLS) demonstrate improvements in the International RLS Rating Scale after a 2-week to 3-month period. Open-label studies of 52 weeks' duration showed maintenance of symptom reduction with once-daily administration of the extended-release formulation. The most commonly reported treatment-emergent adverse effects were somnolence and dizziness. Although the incidence of emergent adverse effects is high, it is comparable with that of gabapentin. No studies thus far have documented augmentation as an issue, unlike that obser...Continue Reading

References

Sep 22, 1977·The New England Journal of Medicine·M I Botez, B Lambert
Jan 1, 1967·Experimental Brain Research·K Krnjević, S Schwartz
May 1, 1994·Age and Ageing·S T O'KeeffeJ N Lavan
Apr 21, 2001·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·M SaletuB Saletu
Jul 11, 2001·Journal of Women's Health & Gender-based Medicine·K A LeeK Baratte-Beebe
Jul 20, 2002·Journal of Psychosomatic Research·Maurice M Ohayon, Thomas Roth
Sep 21, 2002·European Archives of Psychiatry and Clinical Neuroscience·M SaletuB Saletu
Sep 25, 2003·Neuropsychobiology·Svenja HappeJosef Zeitlhofer
Nov 1, 2003·Sleep Medicine·Arthur S WaltersUNKNOWN International Restless Legs Syndrome Study Group
Jul 21, 2004·Clinical Therapeutics·Linda AbetzHelen Knight
Sep 29, 2004·Neurology·M ManconiE Granieri
Sep 5, 2006·Journal of the American Board of Family Medicine : JABFM·Melissa McManama AukermanBeth Bailey
Nov 14, 2006·Chest·Charlene E Gamaldo, Christopher J Earley
May 23, 2007·Movement Disorders : Official Journal of the Movement Disorder Society·Wolfgang H OertelKarin Stiasny-Kolster
Jun 15, 2007·Movement Disorders : Official Journal of the Movement Disorder Society·Heike BenesRalf Kohnen
Nov 16, 2007·Medicine·Arn H Eliasson, Christopher J Lettieri
Sep 5, 2008·European Journal of Obstetrics, Gynecology, and Reproductive Biology·Ingerid Herstad NygaardThomas Bøhmer
Oct 2, 2008·Journal of Clinical Pharmacology·Kenneth C CundyDaniel M Canafax
Aug 12, 2009·Clinical Neuropharmacology·Arthur S WaltersUNKNOWN XP045 Study Group
Oct 13, 2009·Journal of Internal Medicine·Karl Ekbom, J Ulfberg
Jun 1, 2010·Mayo Clinic Proceedings·Richard K BoganUNKNOWN XP060 Study Group
Jan 19, 2011·Clinical Neuropharmacology·Aaron L EllenbogenDan Chen
Jan 25, 2011·International Journal of Clinical Pharmacology and Therapeutics·R LalK C Cundy
Mar 1, 2011·BMC Neurology·Diego Garcia-BorregueroMarco Zucconi
Jun 17, 2011·Journal of Clinical Sleep Medicine : JCSM : Official Publication of the American Academy of Sleep Medicine·Daniel O LeeUNKNOWN XP053 Study Group
Nov 1, 2011·Progress in Neuro-psychopharmacology & Biological Psychiatry·Yuichi InoueNobutaka Hattori
Nov 15, 2011·Expert Opinion on Pharmacotherapy·Rachel A Burke, Michele A Faulkner
Sep 5, 2013·Mayo Clinic Proceedings·Michael H SilberUNKNOWN Medical Advisory Board of the Willis-Ekbom Disease Foundation

❮ Previous
Next ❯

Citations

Aug 21, 2013·Sleep Medicine·John W WinkelmanAndrew G Clair
Dec 5, 2012·Acta Neurologica Scandinavica. Supplementum·H M B LundeL Bø
Jun 15, 2013·Epilepsy & Behavior : E&B·Amos D KorczynIvan Rektor
Mar 26, 2015·Arquivos de neuro-psiquiatria·Alan Christmann FröhlichWalter André dos Santos Moraes

❮ Previous
Next ❯

Methods Mentioned

BETA
pharmacotherapy
sedation

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.