Detail

gabapentin enacarbil

Description

Name: gabapentin enacarbil
Type: small molecule
Groups: approved
Indication: For the treatment of adult Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN).
Accession Number: DB08872 ( DB08872)
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).
Structure:
Prescription Products:
NameDosageStrengthRouteMarketing StartMarketing EndCountry
Horizanttablet, extended release600 mg/1oral01-05-2013US
Horizanttablet, extended release300 mg/1oral01-05-2013US

Generic Prescription Products: Not Available
Over the Counter Products: Not Available
International Brands
  • No Brands

Brand Names
  • No Brands

Brand Mixtures
Brand NameIngredients
Horizantgabapentin enacarbil
Horizantgabapentin enacarbil

Categories
  • No Category

Pharmacology

Indication: For the treatment of adult Restless Legs Syndrome (RLS) and postherpetic neuralgia (PHN).
Pharmacodynamics: Not Available
Mechanism of action: 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.
Absorption: Gabapentin enacarbil is absorbed in the intestines by active transport through the proton-linked monocarboxylate transporter, MCT-1.
Volume of distribution:
    The volume of distribution is 76L.

Protein binding: Gabapentin plasma protein binding is less than 3%.
Metabolism: Not Available
Route of elimination: Gabapentin enacarbil is eliminated primarily in the urine (94%) and to a lesser extent in the feces (5%).
Half life: The elimination half-life of gabapentin is 5.1 to 6.0 hours.
Clearance: Not Available
Toxicity: Most common adverse reactions are headache, dizziness, and somnolence.
Affected organisms
  • Not Available

SNP Mediated Adverse Drug Reactions
  • Not Available

Pharmacoeconomics

Manufacturers:
  • Not Available

Packagers:
  • Not Available

Dosage forms
FormRouteStrength
Tablet, extended releaseoral300 mg/1
Tablet, extended releaseoral600 mg/1

Prices
Unit descriptionCostUnit

Patents
CountryPatent NumberApprovedExpires (estimated)

Interactions

Drug Interactions
DrugInteraction
Azelastinegabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with gabapentin enacarbil.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil.
Buprenorphinegabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil.
EthanolEthanol may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil.
Hydrocodonegabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with gabapentin enacarbil.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil.
Methotrimeprazinegabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosinegabapentin enacarbil may increase the sedative activities of Metyrosine.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil.
Mirtazapinegabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil.
Orphenadrinegabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehydegabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Paroxetine.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil.
Pramipexolegabapentin enacarbil may increase the sedative activities of Pramipexole.
Ropinirolegabapentin enacarbil may increase the sedative activities of Ropinirole.
Rotigotinegabapentin enacarbil may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with gabapentin enacarbil.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil.
Suvorexantgabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of gabapentin enacarbil.
Thalidomidegabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidemgabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.

Food Interactions:
  • No food effects.

Taxonomy

Kingdom: Not Available
Super Class: Not Available
Class: Not Available
Sub Class: Not Available
Direct Parent: Not Available
Alternative Parents:
  • Not Available

substituent:
  • Not Available

References

Synthesis Reference: 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.
General Reference: # 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
External Links:
ResourceLink
RxListhttp://www.rxlist.com/horizant-drug.htm
Drugs.comhttp://www.drugs.com/sfx/gabapentin-enacarbil-side-effects.html

ATC Codes:
  • Not Available

AHFS Codes:
  • Not Available

MSDS: Download
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