Role of gabapentin enacarbil XR in restless legs syndrome

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 throu...

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Main Authors:	Sivam, Sheila, Yee, Brendon J
Format:	Online
Language:	English
Published:	Dove Medical Press 2012
Online Access:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3346203/

id	pubmed-3346203
recordtype	oai_dc
spelling	pubmed-33462032012-05-08 Role of gabapentin enacarbil XR in restless legs syndrome Sivam, Sheila Yee, Brendon J Review 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 observed with most dopaminergic agents. In addition, both dopamine precursors and agonists have not been shown to increase slow wave sleep or improve overall sleep architecture consistently despite improvement in the periodic leg movement index, in contrast with gabapentin enacarbil. Presently, gabapentin enacarbil has not been approved by the Therapeutic Goods Administration or Medsafe for use in RLS. The cost of this medication may also be a potential barrier for many patients. Future comparative efficacy studies with gabapentin, first-line dopaminergic agents, rotigotine, being the other once daily RLS medication, and pregabalin, the structural analog of gabapentin, will be necessary. Dove Medical Press 2012 2012-05-01 /pmc/articles/PMC3346203/ /pubmed/22570552 http://dx.doi.org/10.2147/TCRM.S24436 Text en © 2012 Sivam and Yee, publisher and licensee Dove Medical Press Ltd. This is an Open Access article which permits unrestricted noncommercial use, provided the original work is properly cited.
repository_type	Open Access Journal
institution_category	Foreign Institution
institution	US National Center for Biotechnology Information
building	NCBI PubMed
collection	Online Access
language	English
format	Online
author	Sivam, Sheila Yee, Brendon J
spellingShingle	Sivam, Sheila Yee, Brendon J Role of gabapentin enacarbil XR in restless legs syndrome
author_facet	Sivam, Sheila Yee, Brendon J
author_sort	Sivam, Sheila
title	Role of gabapentin enacarbil XR in restless legs syndrome
title_short	Role of gabapentin enacarbil XR in restless legs syndrome
title_full	Role of gabapentin enacarbil XR in restless legs syndrome
title_fullStr	Role of gabapentin enacarbil XR in restless legs syndrome
title_full_unstemmed	Role of gabapentin enacarbil XR in restless legs syndrome
title_sort	role of gabapentin enacarbil xr in restless legs syndrome
description	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 observed with most dopaminergic agents. In addition, both dopamine precursors and agonists have not been shown to increase slow wave sleep or improve overall sleep architecture consistently despite improvement in the periodic leg movement index, in contrast with gabapentin enacarbil. Presently, gabapentin enacarbil has not been approved by the Therapeutic Goods Administration or Medsafe for use in RLS. The cost of this medication may also be a potential barrier for many patients. Future comparative efficacy studies with gabapentin, first-line dopaminergic agents, rotigotine, being the other once daily RLS medication, and pregabalin, the structural analog of gabapentin, will be necessary.
publisher	Dove Medical Press
publishDate	2012
url	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3346203/
_version_	1611527894028255232

Role of gabapentin enacarbil XR in restless legs syndrome

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