About: gabapentin enacarbil     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

AttributesValues
rdf:type
http://linked.open...gbank/description
  • Gabapentin enacarbil is marketed under the name Horizant®. It is a prodrug of gabapentin, and indicated in adults for the treatment of Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN). (en)
http://linked.open...y/drugbank/dosage
http://linked.open...generalReferences
  • # Cundy KC, Annamalai T, Bu L, De Vera J, Estrela J, Luo W, Shirsat P, Torneros A, Yao F, Zou J, Barrett RW, Gallop MA: 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 Oct;311(1):324-33. Epub 2004 May 14. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15146029 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
http://linked.open...drugbank/halfLife
  • The elimination half-life of gabapentin is 5.1 to 6.0 hours. (en)
http://linked.open...ugbank/indication
  • For the treatment of adult Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN). (en)
sameAs
Title
  • gabapentin enacarbil (en)
adms:identifier
http://linked.open...mechanismOfAction
  • Although the exact mechanism of action of gabapentin in RLS and PHN is unknown, it is presumed to involve the descending noradrenergic system, resulting in the activation of spinal alpha2-adrenergic receptors. (en)
http://linked.open...outeOfElimination
  • Gabapentin enacarbil is eliminated primarily in the urine (94%) and to a lesser extent in the feces (5%). (en)
http://linked.open.../drugbank/synonym
  • XP13512 (en)
  • Gabapentina enacarbilo (en)
  • Gabapentine enacarbil (en)
  • Gabapentinum enacarbilum (en)
  • Horizant (en)
  • XP 13512 (en)
  • XP-13512 (en)
http://linked.open...drugbank/toxicity
  • Most common adverse reactions are headache, dizziness, and somnolence. (en)
http://linked.open...umeOfDistribution
  • The volume of distribution is 76L. (en)
http://linked.open...k/foodInteraction
  • No food effects. (en)
http://linked.open...nk/proteinBinding
  • Gabapentin plasma protein binding is less than 3%. (en)
http://linked.open...ynthesisReference
  • 1. Cundy KC, Branch R, Chernov-Rogan T, Dias T, Estrada T, Hold K, Koller K, Liu X, Mann A, Panuwat M, Raillard SP, Upadhyay S, Wu QQ, Xiang JN, Yan H, Zerangue N, Zhou CX, Barrett RW, Gallop MA: XP13512 [(+/-)-1-([(alpha-isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane acetic acid], a novel gabapentin prodrug: I. Design, synthesis, enzymatic conversion to gabapentin, and transport by intestinal solute transporters. J Pharmacol Exp Ther. 2004 Oct;311(1):315-23. Epub 2004 May 14. (en)
foaf:page
http://linked.open.../Water-Solubility
http://linked.open...logy/drugbank/pKa
http://linked.open...ugbank/absorption
  • Gabapentin enacarbil is absorbed in the intestines by active transport through the proton-linked monocarboxylate transporter, MCT-1. (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 478296-72-9 (en)
http://linked.open...rugbank/clearance
  • Renal clearance of gabapentin is 5 to 7 L/hr. (en)
http://linked.open...ank/Melting-Point
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