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Namespace Prefixes

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Statements

Subject Item
n2:DB08872
rdf:type
n3:Drug
n3: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).
n3:dosage
n16:271B59BF-363D-11E5-9242-09173F13E4C5 n16:271B59C0-363D-11E5-9242-09173F13E4C5
n3: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
n3:group
approved
n3:halfLife
The elimination half-life of gabapentin is 5.1 to 6.0 hours.
n3:indication
For the treatment of adult Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN).
owl:sameAs
n14:DB08872
dcterms:title
gabapentin enacarbil
adms:identifier
n5:DB08872 n7:D09539 n8:68840 n9:Gabapentin_enacarbil
n3: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.
n3:routeOfElimination
Gabapentin enacarbil is eliminated primarily in the urine (94%) and to a lesser extent in the feces (5%).
n3:synonym
XP13512 Gabapentina enacarbilo Horizant Gabapentine enacarbil XP 13512 XP-13512 Gabapentinum enacarbilum
n3:toxicity
Most common adverse reactions are headache, dizziness, and somnolence.
n3:volumeOfDistribution
The volume of distribution is 76L.
n3:foodInteraction
No food effects.
n3:proteinBinding
Gabapentin plasma protein binding is less than 3%.
n3:synthesisReference
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.
foaf:page
n11:horizant-drug.htm n12:gabapentin-enacarbil-side-effects.html
n3:Water-Solubility
n6:271B59C1-363D-11E5-9242-09173F13E4C5
n3:pKa
n6:271B59C3-363D-11E5-9242-09173F13E4C5
n3:absorption
Gabapentin enacarbil is absorbed in the intestines by active transport through the proton-linked monocarboxylate transporter, MCT-1.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
478296-72-9
n3:clearance
Renal clearance of gabapentin is 5 to 7 L/hr.
n3:Melting-Point
n6:271B59C2-363D-11E5-9242-09173F13E4C5