Peringatan Keamanan

Most common adverse reactions are headache, dizziness, and somnolence.

Gabapentin enacarbil

DB08872

small molecule approved investigational

Deskripsi

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).

Struktur Molekul 2D

Berat 329.393
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of gabapentin is 5.1 to 6.0 hours.
Volume Distribusi The volume of distribution is 76L.
Klirens (Clearance) Renal clearance of gabapentin is 5 to 7 L/hr.

Absorpsi

Gabapentin enacarbil is absorbed in the intestines by active transport through the proton-linked monocarboxylate transporter, MCT-1.

Metabolisme

Gabapentin enacarbil does not interact with any of the major cytochrome P450 enzymes.

Rute Eliminasi

Gabapentin enacarbil is eliminated primarily in the urine (94%) and to a lesser extent in the feces (5%).

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

1299 Data
Buprenorphine Gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Gabapentin enacarbil.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Gabapentin enacarbil.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Gabapentin enacarbil.
Hydrocodone Gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Gabapentin enacarbil.
Magnesium sulfate The therapeutic efficacy of Gabapentin enacarbil can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Gabapentin enacarbil may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Gabapentin enacarbil.
Mirtazapine Gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Gabapentin enacarbil.
Orphenadrine Gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Gabapentin enacarbil.
Pramipexole Gabapentin enacarbil may increase the sedative activities of Pramipexole.
Ropinirole Gabapentin enacarbil may increase the sedative activities of Ropinirole.
Rotigotine Gabapentin enacarbil may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Gabapentin enacarbil.
Sodium oxybate Gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Gabapentin enacarbil.
Thalidomide Gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Gabapentin enacarbil.
Magnesium oxide The serum concentration of Gabapentin enacarbil can be decreased when it is combined with Magnesium oxide.
Aluminum hydroxide The serum concentration of Gabapentin enacarbil can be decreased when it is combined with Aluminum hydroxide.
Magaldrate The serum concentration of Gabapentin enacarbil can be decreased when it is combined with Magaldrate.
Magnesium hydroxide The serum concentration of Gabapentin enacarbil can be decreased when it is combined with Magnesium hydroxide.
Magnesium trisilicate The serum concentration of Gabapentin enacarbil can be decreased when it is combined with Magnesium trisilicate.
Magnesium carbonate The serum concentration of Gabapentin enacarbil can be decreased when it is combined with Magnesium carbonate.
Magnesium silicate The serum concentration of Gabapentin enacarbil can be decreased when it is combined with Magnesium silicate.
Aluminium acetoacetate The serum concentration of Gabapentin enacarbil can be decreased when it is combined with Aluminium acetoacetate.
Hydrotalcite The serum concentration of Gabapentin enacarbil can be decreased when it is combined with Hydrotalcite.
Magnesium peroxide The serum concentration of Gabapentin enacarbil can be decreased when it is combined with Magnesium peroxide.
Almasilate The serum concentration of Gabapentin enacarbil can be decreased when it is combined with Almasilate.
Aluminium glycinate The serum concentration of Gabapentin enacarbil can be decreased when it is combined with Aluminium glycinate.
Aloglutamol The serum concentration of Gabapentin enacarbil can be decreased when it is combined with Aloglutamol.
Aluminium phosphate The serum concentration of Gabapentin enacarbil can be decreased when it is combined with Aluminium phosphate.
Ethanol Gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Gabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Gabapentin enacarbil.
Fluvoxamine The risk or severity of adverse effects can be increased when Gabapentin enacarbil is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Gabapentin enacarbil is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Gabapentin enacarbil is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Gabapentin enacarbil is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Gabapentin enacarbil is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Gabapentin enacarbil is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Gabapentin enacarbil is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Gabapentin enacarbil is combined with Nefazodone.
Escitalopram The risk or severity of adverse effects can be increased when Gabapentin enacarbil is combined with Escitalopram.
Zimelidine The risk or severity of adverse effects can be increased when Gabapentin enacarbil is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Gabapentin enacarbil is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Gabapentin enacarbil is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Gabapentin enacarbil is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Gabapentin enacarbil is combined with Seproxetine.
Levomilnacipran Gabapentin enacarbil may decrease the excretion rate of Levomilnacipran which could result in a higher serum level.
Indalpine The risk or severity of adverse effects can be increased when Gabapentin enacarbil is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Gabapentin enacarbil is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Gabapentin enacarbil is combined with Alaproclate.
Benzatropine Benzatropine may decrease the excretion rate of Gabapentin enacarbil which could result in a higher serum level.
Disopyramide Disopyramide may decrease the excretion rate of Gabapentin enacarbil which could result in a higher serum level.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Gabapentin enacarbil.
Nortriptyline The risk or severity of CNS depression can be increased when Nortriptyline is combined with Gabapentin enacarbil.
Amoxapine The risk or severity of CNS depression can be increased when Amoxapine is combined with Gabapentin enacarbil.
Propiomazine The risk or severity of CNS depression can be increased when Propiomazine is combined with Gabapentin enacarbil.
Propantheline Propantheline may decrease the excretion rate of Gabapentin enacarbil which could result in a higher serum level.
Dicyclomine Dicyclomine may decrease the excretion rate of Gabapentin enacarbil which could result in a higher serum level.
Maprotiline The risk or severity of CNS depression can be increased when Maprotiline is combined with Gabapentin enacarbil.
Tolterodine Tolterodine may decrease the excretion rate of Gabapentin enacarbil which could result in a higher serum level.
Flavoxate Flavoxate may decrease the excretion rate of Gabapentin enacarbil which could result in a higher serum level.
Tiotropium Tiotropium may decrease the excretion rate of Gabapentin enacarbil which could result in a higher serum level.
Pizotifen The risk or severity of CNS depression can be increased when Pizotifen is combined with Gabapentin enacarbil.
Fesoterodine Fesoterodine may decrease the excretion rate of Gabapentin enacarbil which could result in a higher serum level.
Aclidinium Gabapentin enacarbil may decrease the excretion rate of Aclidinium which could result in a higher serum level.
Trimebutine Gabapentin enacarbil may decrease the excretion rate of Trimebutine which could result in a higher serum level.
Dosulepin The risk or severity of CNS depression can be increased when Gabapentin enacarbil is combined with Dosulepin.
Imidafenacin Gabapentin enacarbil may decrease the excretion rate of Imidafenacin which could result in a higher serum level.
Propiverine Gabapentin enacarbil may decrease the excretion rate of Propiverine which could result in a higher serum level.
Amitriptyline The risk or severity of CNS depression can be increased when Amitriptyline is combined with Gabapentin enacarbil.
Imipramine The risk or severity of CNS depression can be increased when Imipramine is combined with Gabapentin enacarbil.
Doxepin The risk or severity of CNS depression can be increased when Doxepin is combined with Gabapentin enacarbil.
Desipramine The risk or severity of CNS depression can be increased when Desipramine is combined with Gabapentin enacarbil.
Zopiclone The risk or severity of adverse effects can be increased when Gabapentin enacarbil is combined with Zopiclone.
Botulinum toxin type B The risk or severity of CNS depression can be increased when Botulinum toxin type B is combined with Gabapentin enacarbil.
Botulinum toxin type A The risk or severity of CNS depression can be increased when Botulinum toxin type A is combined with Gabapentin enacarbil.
Tryptophan The risk or severity of CNS depression can be increased when Tryptophan is combined with Gabapentin enacarbil.
Baclofen Baclofen may increase the central nervous system depressant (CNS depressant) activities of Gabapentin enacarbil.
Lorazepam The risk or severity of CNS depression can be increased when Lorazepam is combined with Gabapentin enacarbil.
Ethchlorvynol The risk or severity of CNS depression can be increased when Ethchlorvynol is combined with Gabapentin enacarbil.
Succinylcholine The risk or severity of CNS depression can be increased when Succinylcholine is combined with Gabapentin enacarbil.
Eletriptan The risk or severity of CNS depression can be increased when Eletriptan is combined with Gabapentin enacarbil.
Enflurane The risk or severity of CNS depression can be increased when Enflurane is combined with Gabapentin enacarbil.
Temazepam The risk or severity of CNS depression can be increased when Temazepam is combined with Gabapentin enacarbil.
Reboxetine The risk or severity of CNS depression can be increased when Reboxetine is combined with Gabapentin enacarbil.
Butabarbital The risk or severity of CNS depression can be increased when Butabarbital is combined with Gabapentin enacarbil.
Butalbital The risk or severity of CNS depression can be increased when Butalbital is combined with Gabapentin enacarbil.
Methysergide The risk or severity of CNS depression can be increased when Methysergide is combined with Gabapentin enacarbil.
Cabergoline The risk or severity of CNS depression can be increased when Cabergoline is combined with Gabapentin enacarbil.
Phenytoin The risk or severity of CNS depression can be increased when Phenytoin is combined with Gabapentin enacarbil.

Target Protein

Sodium-dependent multivitamin transporter SLC5A6
Voltage-dependent calcium channel subunit alpha-2/delta-1 CACNA2D1
Voltage-dependent calcium channel subunit alpha-2/delta-2 CACNA2D2

Referensi & Sumber

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.
Artikel (PubMed)
  • PMID: 15146028
    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.
  • PMID: 16732716
    Bialer M: New antiepileptic drugs that are second generation to existing antiepileptic drugs. Expert Opin Investig Drugs. 2006 Jun;15(6):637-47.
  • PMID: 15146029
    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.

Contoh Produk & Brand

Produk: 6 • International brands: 0
Produk
  • Horizant
    Tablet, extended release • 300 mg/1 • Oral • US • Approved
  • Horizant
    Tablet, extended release • 600 mg/1 • Oral • US • Approved
  • Horizant
    Tablet, extended release • 300 mg/1 • Oral • US • Approved
  • Horizant
    Tablet, extended release • 300 mg/1 • Oral • US • Approved
  • Horizant
    Tablet, extended release • 600 mg/1 • Oral • US • Approved
  • Horizant
    Tablet, extended release • 300 mg/1 • Oral • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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