Peringatan Keamanan

The oral LD50 of vigabatrin in mice and rats is 2830 mg/kg and 3100 mg/kg, respectively.L13652 Symptoms of overdose tend to involve significant CNS depression - e.g. coma, unconsciousness, and/or drowsiness - with less common symptoms including neurologic disorders (e.g. seizure activity, speech disorder, headache) and psychiatric sequelae (e.g. psychosis, agitation, abnormal behaviour, confusion).L13616

In cases of overdose, symptoms generally resolve with symptomatic and supportive care. Standard measures to remove unabsorbed drug may be employed (e.g. gastric lavage), although an in vitro study found that activated charcoal did not significantly absorb vigabatrin.L13616 Although vigabatrin is not protein-bound, the effectiveness of hemodialysis in drug removal during overdose is unknown - isolated reports of patients in renal failure undergoing hemodialysis who were receiving therapeutic doses of vigabatrin note a reduction in vigabatrin plasma concentrations of 40-60% following dialysis.L13616

Vigabatrin

DB01080

small molecule approved

Deskripsi

Vigabatrin is an analog of gamma-aminobutyric acid (GABA), the main inhibitory neurotransmitter in the central nervous system, used in the treatment of refractory seizures and infantile spasms.L13616 It irreversibly inhibits the enzyme responsible for GABA metabolism, thereby increasing levels of circulating GABA. Although administered as a racemic mixture, only the S(+) enantiomer is pharmacologically active.A202037

It was first introduced as an antiepileptic agent in the United Kingdom in 1989 and was used extensively until 1997, when an association with vision loss became apparent.A202124 Its use is now generally reserved for patients who have failed alternative therapies, and its US approval by the FDA in 2009 mandated the creation of a drug registry to monitor patients for visual deficits.L13661,A202124

Struktur Molekul 2D

Berat 129.157
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal half-life of vigabatrin is approximately 5.7 hours for infants (5m - 2y), 6.8 hours for children (3y - 9y), 9.5 hours for adolescents (10y - 16y), and 10.5 h for adults.[L13616]
Volume Distribusi Vigabatrin is widely distributed throughout the body with a mean steady-state volume of distribution of 1.1 L/kg.[L13616]
Klirens (Clearance) The oral clearance of vigabatrin is 2.4 L/h for infants (5m - 2y), 5.1 L/h for children (3y - 9y), 5.8 L/h for adolescents (10y - 16y), and 7 L/h for adults.[L13616]

Absorpsi

Absorption following oral administration is essentially complete.L13616 The Tmax is approximately 2.5 hours in infants (5m - 2y) and 1 hour in all other age groups.

Metabolisme

Vigabatrin is not metabolized to any significant extent.L13616

Rute Eliminasi

Approximately 95% of the drug is eliminated in the urine within 72 hours of administration, of which ~80% is unchanged parent drug.L13616

Interaksi Makanan

2 Data
  • 1. Take with or without food.
  • 2. Take with plain water. Only mix vigabatrin oral solution powder with plain water.

Interaksi Obat

810 Data
Buprenorphine Vigabatrin 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 Vigabatrin.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Vigabatrin.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Vigabatrin.
Hydrocodone Vigabatrin 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 Vigabatrin.
Magnesium sulfate The therapeutic efficacy of Vigabatrin can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Vigabatrin may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Vigabatrin may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Vigabatrin.
Mirtazapine Vigabatrin 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 Vigabatrin.
Orphenadrine Vigabatrin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Vigabatrin 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 Vigabatrin.
Pramipexole Vigabatrin may increase the sedative activities of Pramipexole.
Ropinirole Vigabatrin may increase the sedative activities of Ropinirole.
Rotigotine Vigabatrin may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Vigabatrin.
Sodium oxybate Vigabatrin may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Vigabatrin 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 Vigabatrin.
Thalidomide Vigabatrin may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Vigabatrin may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Mefloquine The therapeutic efficacy of Vigabatrin can be decreased when used in combination with Mefloquine.
Mianserin The therapeutic efficacy of Vigabatrin can be decreased when used in combination with Mianserin.
Orlistat Orlistat can cause a decrease in the absorption of Vigabatrin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Topotecan Vigabatrin may increase the excretion rate of Topotecan which could result in a lower serum level and potentially a reduction in efficacy.
Phenytoin The serum concentration of Phenytoin can be decreased when it is combined with Vigabatrin.
Fosphenytoin The serum concentration of Fosphenytoin can be decreased when it is combined with Vigabatrin.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Vigabatrin.
Tetracosactide The risk or severity of liver damage can be increased when Tetracosactide is combined with Vigabatrin.
Clonazepam The serum concentration of Clonazepam can be increased when it is combined with Vigabatrin.
Ethanol Vigabatrin may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Vigabatrin 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 Vigabatrin.
Fluvoxamine The risk or severity of adverse effects can be increased when Vigabatrin is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Vigabatrin is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Vigabatrin is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Vigabatrin is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Vigabatrin is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Vigabatrin is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Vigabatrin is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Vigabatrin is combined with Nefazodone.
Escitalopram The risk or severity of adverse effects can be increased when Vigabatrin is combined with Escitalopram.
Zimelidine The risk or severity of adverse effects can be increased when Vigabatrin is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Vigabatrin is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Vigabatrin is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Vigabatrin is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Vigabatrin is combined with Seproxetine.
Indalpine The risk or severity of adverse effects can be increased when Vigabatrin is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Vigabatrin is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Vigabatrin is combined with Alaproclate.
Amitriptyline The risk or severity of CNS depression can be increased when Amitriptyline is combined with Vigabatrin.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Vigabatrin.
Imipramine The risk or severity of CNS depression can be increased when Imipramine is combined with Vigabatrin.
Nortriptyline The risk or severity of CNS depression can be increased when Nortriptyline is combined with Vigabatrin.
Amoxapine The risk or severity of CNS depression can be increased when Amoxapine is combined with Vigabatrin.
Propiomazine The risk or severity of CNS depression can be increased when Propiomazine is combined with Vigabatrin.
Cocaine The risk or severity of methemoglobinemia can be increased when Vigabatrin is combined with Cocaine.
Maprotiline The risk or severity of CNS depression can be increased when Maprotiline is combined with Vigabatrin.
Desipramine The risk or severity of CNS depression can be increased when Vigabatrin is combined with Desipramine.
Pizotifen The risk or severity of CNS depression can be increased when Vigabatrin is combined with Pizotifen.
Dosulepin The risk or severity of CNS depression can be increased when Vigabatrin is combined with Dosulepin.
Doxepin The risk or severity of CNS depression can be increased when Vigabatrin is combined with Doxepin.
Quinidine The therapeutic efficacy of Vigabatrin can be decreased when used in combination with Quinidine.
Zopiclone The risk or severity of adverse effects can be increased when Vigabatrin 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 Vigabatrin.
Botulinum toxin type A The risk or severity of CNS depression can be increased when Botulinum toxin type A is combined with Vigabatrin.
Tryptophan The risk or severity of CNS depression can be increased when Tryptophan is combined with Vigabatrin.
Baclofen Baclofen may increase the central nervous system depressant (CNS depressant) activities of Vigabatrin.
Lorazepam The risk or severity of CNS depression can be increased when Lorazepam is combined with Vigabatrin.
Ethchlorvynol The risk or severity of CNS depression can be increased when Ethchlorvynol is combined with Vigabatrin.
Succinylcholine The risk or severity of CNS depression can be increased when Succinylcholine is combined with Vigabatrin.
Reserpine The risk or severity of CNS depression can be increased when Reserpine is combined with Vigabatrin.
Eletriptan The risk or severity of CNS depression can be increased when Eletriptan is combined with Vigabatrin.
Enflurane The risk or severity of CNS depression can be increased when Enflurane is combined with Vigabatrin.
Temazepam The risk or severity of CNS depression can be increased when Temazepam is combined with Vigabatrin.
Reboxetine The risk or severity of CNS depression can be increased when Reboxetine is combined with Vigabatrin.
Butabarbital The risk or severity of CNS depression can be increased when Butabarbital is combined with Vigabatrin.
Butalbital The risk or severity of CNS depression can be increased when Butalbital is combined with Vigabatrin.
Methysergide The risk or severity of CNS depression can be increased when Methysergide is combined with Vigabatrin.
Cabergoline The risk or severity of CNS depression can be increased when Cabergoline is combined with Vigabatrin.
Topiramate The risk or severity of CNS depression can be increased when Topiramate is combined with Vigabatrin.
Clemastine The risk or severity of CNS depression can be increased when Clemastine is combined with Vigabatrin.
Venlafaxine The risk or severity of CNS depression can be increased when Venlafaxine is combined with Vigabatrin.
Etomidate The risk or severity of CNS depression can be increased when Etomidate is combined with Vigabatrin.
Morphine The risk or severity of CNS depression can be increased when Morphine is combined with Vigabatrin.
Talbutal The risk or severity of CNS depression can be increased when Talbutal is combined with Vigabatrin.
Pentobarbital The risk or severity of CNS depression can be increased when Pentobarbital is combined with Vigabatrin.
Zolmitriptan The risk or severity of CNS depression can be increased when Zolmitriptan is combined with Vigabatrin.
Codeine The risk or severity of CNS depression can be increased when Codeine is combined with Vigabatrin.
Dihydroergotamine The risk or severity of CNS depression can be increased when Dihydroergotamine is combined with Vigabatrin.
Tolcapone The risk or severity of CNS depression can be increased when Tolcapone is combined with Vigabatrin.
Hydromorphone The risk or severity of CNS depression can be increased when Hydromorphone is combined with Vigabatrin.
Olanzapine The risk or severity of CNS depression can be increased when Olanzapine is combined with Vigabatrin.
Cetirizine The risk or severity of CNS depression can be increased when Cetirizine is combined with Vigabatrin.
Protriptyline The risk or severity of CNS depression can be increased when Protriptyline is combined with Vigabatrin.
Trimethadione The risk or severity of CNS depression can be increased when Trimethadione is combined with Vigabatrin.
Clobazam The risk or severity of sedation, somnolence, and CNS depression can be increased when Clobazam is combined with Vigabatrin.

Target Protein

4-aminobutyrate aminotransferase, mitochondrial ABAT

Referensi & Sumber

Artikel (PubMed)
  • PMID: 2757904
    Gram L, Larsson OM, Johnsen A, Schousboe A: Experimental studies of the influence of vigabatrin on the GABA system. Br J Clin Pharmacol. 1989;27 Suppl 1:13S-17S.
  • PMID: 11682253
    Zwanzger P, Baghai TC, Schuele C, Strohle A, Padberg F, Kathmann N, Schwarz M, Moller HJ, Rupprecht R: Vigabatrin decreases cholecystokinin-tetrapeptide (CCK-4) induced panic in healthy volunteers. Neuropsychopharmacology. 2001 Nov;25(5):699-703.
  • PMID: 23118657
    Tulloch JK, Carr RR, Ensom MH: A systematic review of the pharmacokinetics of antiepileptic drugs in neonates with refractory seizures. J Pediatr Pharmacol Ther. 2012 Jan;17(1):31-44. doi: 10.5863/1551-6776-17.1.31.
  • PMID: 9278207
    Jacqz-Aigrain E, Guillonneau M, Rey E, Macher MA, Montes C, Chiron C, Loirat C: Pharmacokinetics of the S(+) and R(-) enantiomers of vigabatrin during chronic dosing in a patient with renal failure. Br J Clin Pharmacol. 1997 Aug;44(2):183-5. doi: 10.1046/j.1365-2125.1997.00636.x.
  • PMID: 8719918
    Davies JA: Mechanisms of action of antiepileptic drugs. Seizure. 1995 Dec;4(4):267-71. doi: 10.1016/s1059-1311(95)80003-4.
  • PMID: 29280765
    Foroozan R: Vigabatrin: Lessons Learned From the United States Experience. J Neuroophthalmol. 2018 Dec;38(4):442-450. doi: 10.1097/WNO.0000000000000609.

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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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