9
views
0
recommends
+1 Recommend
1 collections
    0
    shares
      • Record: found
      • Abstract: found
      • Article: found
      Is Open Access

      Gabapentin enacarbil extended release for the treatment of postherpetic neuralgia in adults

      review-article

      Read this article at

      ScienceOpenPublisherPMC
      Bookmark
          There is no author summary for this article yet. Authors can add summaries to their articles on ScienceOpen to make them more accessible to a non-specialist audience.

          Abstract

          The development of biomedical technology is allowing refinement of drug therapies in order to improve medication profiles and benefit patients. Gabapentin (Gp) is a medication licensed globally for various indications, including postherpetic neuralgia. It has a pharmacokinetic profile which has been suggested may limit its clinical effects and reduce medication compliance. In 2012, the US Food and Drug Administration licensed a novel preparation which aims to circumvent these limitations. Gp enacarbil is a prodrug of Gp, which is additionally prepared in an extended release preparation. The resulting compound has an improved absorption profile and a reduced dosing frequency in comparison to immediate release Gp. An absence of comparative data, however, limits the direct evaluation of the medication to both immediate release and other extended release preparations available on the market. Additionally, no data are currently available addressing efficacy, tolerability, or side effects with other first line treatments of postherpetic neuralgia. Additional experimental data should be sought to clarify the position of Gp enacarbil, both within postherpetic neuralgia treatment protocols and in relation to the increasing numbers of gabapentinoids available.

          Video abstract

          Most cited references26

          • Record: found
          • Abstract: found
          • Article: not found

          Gabapentin receptor alpha2delta-1 is a neuronal thrombospondin receptor responsible for excitatory CNS synaptogenesis.

          Synapses are asymmetric cellular adhesions that are critical for nervous system development and function, but the mechanisms that induce their formation are not well understood. We have previously identified thrombospondin as an astrocyte-secreted protein that promotes central nervous system (CNS) synaptogenesis. Here, we identify the neuronal thrombospondin receptor involved in CNS synapse formation as alpha2delta-1, the receptor for the anti-epileptic and analgesic drug gabapentin. We show that the VWF-A domain of alpha2delta-1 interacts with the epidermal growth factor-like repeats common to all thrombospondins. alpha2delta-1 overexpression increases synaptogenesis in vitro and in vivo and is required postsynaptically for thrombospondin- and astrocyte-induced synapse formation in vitro. Gabapentin antagonizes thrombospondin binding to alpha2delta-1 and powerfully inhibits excitatory synapse formation in vitro and in vivo. These findings identify alpha2delta-1 as a receptor involved in excitatory synapse formation and suggest that gabapentin may function therapeutically by blocking new synapse formation.
            Bookmark
            • Record: found
            • Abstract: not found
            • Article: not found

            Practice guidelines for chronic pain management: an updated report by the American Society of Anesthesiologists Task Force on Chronic Pain Management and the American Society of Regional Anesthesia and Pain Medicine.

            , (2010)
              Bookmark
              • Record: found
              • Abstract: found
              • Article: not found

              The impact of reducing dose frequency on health outcomes.

              Dosing schedules may be one important factor determining whether patients take their prescribed medication. Schedules may influence whether a patient stays on the prescribed therapy and, if so, the degree to which the regimen is followed. Both factors are important determinants of health outcomes and health care costs. The goal of this study was to investigate the impact of reducing dose frequency on health outcomes and health care costs. Articles from peer-reviewed journals were identified from the medical literature databases MEDLINE, International Pharmaceutical Abstracts, and HealthSTAR for the years 1985 through 2002. The search included all references that reported on the impact of a change of dose frequency on chronic disease. Search terms used were combinations of dose frequency, dose schedule, and dosing and efficacy, safety, clinical effectiveness, preferences, adherence, compliance, persistence, health-related quality of life, patient satisfaction, resource use, and costs. Reducing the number of daily doses through extended-release formulations or newer drugs has frequently been shown to provide the patient with better symptom control in a number of disease states. Overall improvements were seen in adherence, patient quality of life, patient satisfaction, and costs. However, results of some studies indicate that not all patients, medications, or diseases may be candidates for reduced dosing due to the potential effects on symptom control, incidence of adverse events, and overcompensation for missed doses. Where feasible, reducing dose frequency may offer benefits for the patient in terms of health outcomes and for the health care budget holder in terms of costs.
                Bookmark

                Author and article information

                Journal
                Ther Clin Risk Manag
                Ther Clin Risk Manag
                Therapeutics and Clinical Risk Management
                Therapeutics and Clinical Risk Management
                Dove Medical Press
                1176-6336
                1178-203X
                2013
                2013
                25 November 2013
                : 9
                : 469-475
                Affiliations
                [1 ]Chelsea Westminster Hospital, London, UK
                [2 ]Department of Anaesthetics, The Royal Marsden NHS Foundation Trust, London, UK
                Author notes
                Correspondence: Paul Farquhar-Smith, Department of Anaesthetics, The Royal Marsden NHS Foundation Trust, Fulham Road, London, SW3 6JJ, UK, Tel +44 207 352 8171 ext 2727, Fax +44 207 808 2726, Email paul.farquhar-smith@ 123456rmh.nhs.uk
                Article
                tcrm-9-469
                10.2147/TCRM.S50212
                3861364
                24353426
                8cf0104b-8adb-44c2-aa75-754e6d349856
                © 2013 Thomas and Farquhar-Smith. This work is published by Dove Medical Press Ltd, and licensed under Creative Commons Attribution – Non Commercial (unported, v3.0) License

                The full terms of the License are available at http://creativecommons.org/licenses/by-nc/3.0/. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Ltd, provided the work is properly attributed.

                History
                Categories
                Review

                Medicine
                postherpetic neuralgia,herpes zoster,garbapentin enacarbil
                Medicine
                postherpetic neuralgia, herpes zoster, garbapentin enacarbil

                Comments

                Comment on this article