Peringatan Keamanan

No carcinogenesis or fertility impairment found. Overdose is associated with somnolence and dizziness FDA Label.

Brivaracetam

DB05541

small molecule approved investigational

Deskripsi

Brivaracetam is a racetam derivative of levetiracetam used in the treatment of partial-onset seizures. Brivaracetam binds SV2A with 20 times higher affinity than levetiracetam A19184. It is available under the brand name Briviact made by UCB. Briviact received FDA approval on February 19, 2016 L760.

Struktur Molekul 2D

Berat 212.2887
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 7-8h [A19180].
Volume Distribusi 0.5L/kg [FDA Label].
Klirens (Clearance) CL/F of 0.7-1.07 mL/min kg [A19187]. Clearance is primarily metabolic with less than 10% of the parent drug excreted unchanged.

Absorpsi

Nearly 100% oral bioavailability A19180.

Metabolisme

Primarily metabolized by hydrolysis of the acetamide moeity to form a carboxylic acid metabolite A19188. Another metabolite is created via oxidation of the propyl side chain by CYP2C8 as well as CYP3A4, CYP2C19, and CYP2B6. Some conjugation with glucuronic acid and taurine account for a small amount of metabolism.

Rute Eliminasi

\>95% excreted in urine with <10% of the parent compound unchanged. <1% excreted in feces FDA Label.

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Taking Brivaracetam with alcohol may increase alcohol's effects on attention, memory, and psychomotor functioning.
  • 2. Take with or without food.

Interaksi Obat

1652 Data
Buprenorphine Brivaracetam 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 Brivaracetam.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Brivaracetam.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Brivaracetam.
Hydrocodone Brivaracetam 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 Brivaracetam.
Magnesium sulfate The therapeutic efficacy of Brivaracetam can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Brivaracetam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Brivaracetam may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Brivaracetam.
Mirtazapine Brivaracetam 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 Brivaracetam.
Orphenadrine Brivaracetam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Brivaracetam 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 Brivaracetam.
Pramipexole Brivaracetam may increase the sedative activities of Pramipexole.
Ropinirole Brivaracetam may increase the sedative activities of Ropinirole.
Rotigotine Brivaracetam may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Brivaracetam.
Sodium oxybate Brivaracetam may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Brivaracetam 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 Brivaracetam.
Thalidomide Brivaracetam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Brivaracetam may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Mefloquine The therapeutic efficacy of Brivaracetam can be decreased when used in combination with Mefloquine.
Mianserin The therapeutic efficacy of Brivaracetam can be decreased when used in combination with Mianserin.
Orlistat Orlistat can cause a decrease in the absorption of Brivaracetam resulting in a reduced serum concentration and potentially a decrease in efficacy.
Topotecan Brivaracetam may increase the excretion rate of Topotecan which could result in a lower serum level and potentially a reduction in efficacy.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Brivaracetam.
Tetracosactide The risk or severity of liver damage can be increased when Tetracosactide is combined with Brivaracetam.
Ethanol Brivaracetam may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Brivaracetam 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 Brivaracetam.
Fluvoxamine The risk or severity of adverse effects can be increased when Brivaracetam is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Brivaracetam is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Brivaracetam is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Brivaracetam is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Brivaracetam is combined with Paroxetine.
Sibutramine The risk or severity of adverse effects can be increased when Brivaracetam is combined with Sibutramine.
Escitalopram The risk or severity of adverse effects can be increased when Brivaracetam is combined with Escitalopram.
Zimelidine The risk or severity of adverse effects can be increased when Brivaracetam is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Brivaracetam is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Brivaracetam is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Brivaracetam is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Brivaracetam is combined with Seproxetine.
Levomilnacipran Brivaracetam 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 Brivaracetam is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Brivaracetam is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Brivaracetam is combined with Alaproclate.
Benzatropine Benzatropine may decrease the excretion rate of Brivaracetam which could result in a higher serum level.
Disopyramide Disopyramide may decrease the excretion rate of Brivaracetam which could result in a higher serum level.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Brivaracetam.
Amoxapine The risk or severity of CNS depression can be increased when Amoxapine is combined with Brivaracetam.
Propiomazine The risk or severity of CNS depression can be increased when Propiomazine is combined with Brivaracetam.
Propantheline Propantheline may decrease the excretion rate of Brivaracetam which could result in a higher serum level.
Dicyclomine Dicyclomine may decrease the excretion rate of Brivaracetam which could result in a higher serum level.
Cocaine The risk or severity of methemoglobinemia can be increased when Brivaracetam is combined with Cocaine.
Maprotiline The risk or severity of CNS depression can be increased when Maprotiline is combined with Brivaracetam.
Tolterodine Tolterodine may decrease the excretion rate of Brivaracetam which could result in a higher serum level.
Flavoxate Flavoxate may decrease the excretion rate of Brivaracetam which could result in a higher serum level.
Tiotropium Tiotropium may decrease the excretion rate of Brivaracetam which could result in a higher serum level.
Pizotifen The risk or severity of CNS depression can be increased when Brivaracetam is combined with Pizotifen.
Fesoterodine Brivaracetam may decrease the excretion rate of Fesoterodine which could result in a higher serum level.
Aclidinium Brivaracetam may decrease the excretion rate of Aclidinium which could result in a higher serum level.
Trimebutine Brivaracetam may decrease the excretion rate of Trimebutine which could result in a higher serum level.
Imidafenacin Brivaracetam may decrease the excretion rate of Imidafenacin which could result in a higher serum level.
Propiverine Brivaracetam may decrease the excretion rate of Propiverine which could result in a higher serum level.
Quetiapine The risk or severity of CNS depression can be increased when Quetiapine is combined with Brivaracetam.
Nortriptyline The risk or severity of CNS depression can be increased when Nortriptyline is combined with Brivaracetam.
Amitriptyline The risk or severity of CNS depression can be increased when Amitriptyline is combined with Brivaracetam.
Doxepin The risk or severity of CNS depression can be increased when Doxepin is combined with Brivaracetam.
Imipramine The risk or severity of CNS depression can be increased when Imipramine is combined with Brivaracetam.
Desipramine The risk or severity of CNS depression can be increased when Desipramine is combined with Brivaracetam.
Zopiclone The risk or severity of adverse effects can be increased when Brivaracetam 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 Brivaracetam.
Botulinum toxin type A The risk or severity of CNS depression can be increased when Botulinum toxin type A is combined with Brivaracetam.
Tryptophan The risk or severity of CNS depression can be increased when Tryptophan is combined with Brivaracetam.
Baclofen Baclofen may increase the central nervous system depressant (CNS depressant) activities of Brivaracetam.
Lorazepam The risk or severity of CNS depression can be increased when Lorazepam is combined with Brivaracetam.
Ethchlorvynol The risk or severity of CNS depression can be increased when Ethchlorvynol is combined with Brivaracetam.
Succinylcholine The risk or severity of CNS depression can be increased when Succinylcholine is combined with Brivaracetam.
Enflurane The risk or severity of CNS depression can be increased when Enflurane is combined with Brivaracetam.
Temazepam The risk or severity of CNS depression can be increased when Temazepam is combined with Brivaracetam.
Reboxetine The risk or severity of CNS depression can be increased when Reboxetine is combined with Brivaracetam.
Butabarbital The risk or severity of CNS depression can be increased when Butabarbital is combined with Brivaracetam.
Butalbital The risk or severity of CNS depression can be increased when Butalbital is combined with Brivaracetam.
Cabergoline The risk or severity of CNS depression can be increased when Cabergoline is combined with Brivaracetam.
Topiramate The risk or severity of CNS depression can be increased when Topiramate is combined with Brivaracetam.
Clemastine The risk or severity of CNS depression can be increased when Clemastine is combined with Brivaracetam.
Venlafaxine The risk or severity of CNS depression can be increased when Venlafaxine is combined with Brivaracetam.
Etomidate The risk or severity of CNS depression can be increased when Etomidate is combined with Brivaracetam.
Morphine The risk or severity of CNS depression can be increased when Morphine is combined with Brivaracetam.
Talbutal The risk or severity of CNS depression can be increased when Talbutal is combined with Brivaracetam.
Zolmitriptan The risk or severity of CNS depression can be increased when Zolmitriptan is combined with Brivaracetam.
Tolcapone The risk or severity of CNS depression can be increased when Tolcapone is combined with Brivaracetam.
Hydromorphone The risk or severity of CNS depression can be increased when Hydromorphone is combined with Brivaracetam.
Olanzapine The risk or severity of CNS depression can be increased when Olanzapine is combined with Brivaracetam.
Cetirizine The risk or severity of CNS depression can be increased when Cetirizine is combined with Brivaracetam.
Protriptyline The risk or severity of CNS depression can be increased when Protriptyline is combined with Brivaracetam.
Trimethadione The risk or severity of CNS depression can be increased when Trimethadione is combined with Brivaracetam.

Target Protein

Synaptic vesicle glycoprotein 2A SV2A
Sodium channel protein SCN1A

Referensi & Sumber

Artikel (PubMed)
  • PMID: 18341673
    Rolan P, Sargentini-Maier ML, Pigeolet E, Stockis A: The pharmacokinetics, CNS pharmacodynamics and adverse event profile of brivaracetam after multiple increasing oral doses in healthy men. Br J Clin Pharmacol. 2008 Jul;66(1):71-5. doi: 10.1111/j.1365-2125.2008.03158.x. Epub 2008 Mar 13.
  • PMID: 21575627
    Gillard M, Fuks B, Leclercq K, Matagne A: Binding characteristics of brivaracetam, a selective, high affinity SV2A ligand in rat, mouse and human brain: relationship to anti-convulsant properties. Eur J Pharmacol. 2011 Aug 16;664(1-3):36-44. doi: 10.1016/j.ejphar.2011.04.064. Epub 2011 May 8.
  • PMID: 27265781
    Tokudome K, Okumura T, Shimizu S, Mashimo T, Takizawa A, Serikawa T, Terada R, Ishihara S, Kunisawa N, Sasa M, Ohno Y: Synaptic vesicle glycoprotein 2A (SV2A) regulates kindling epileptogenesis via GABAergic neurotransmission. Sci Rep. 2016 Jun 6;6:27420. doi: 10.1038/srep27420.
  • PMID: 19914041
    Zona C, Pieri M, Carunchio I, Curcio L, Klitgaard H, Margineanu DG: Brivaracetam (ucb 34714) inhibits Na(+) current in rat cortical neurons in culture. Epilepsy Res. 2010 Jan;88(1):46-54. doi: 10.1016/j.eplepsyres.2009.09.024. Epub 2009 Nov 13.
  • PMID: 17223857
    Sargentini-Maier ML, Rolan P, Connell J, Tytgat D, Jacobs T, Pigeolet E, Riethuisen JM, Stockis A: The pharmacokinetics, CNS pharmacodynamics and adverse event profile of brivaracetam after single increasing oral doses in healthy males. Br J Clin Pharmacol. 2007 Jun;63(6):680-8. Epub 2007 Jan 12.
  • PMID: 17908923
    Sargentini-Maier ML, Espie P, Coquette A, Stockis A: Pharmacokinetics and metabolism of 14C-brivaracetam, a novel SV2A ligand, in healthy subjects. Drug Metab Dispos. 2008 Jan;36(1):36-45. Epub 2007 Oct 1.

Contoh Produk & Brand

Produk: 48 • International brands: 1
Produk
  • Apo-brivaracetam
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Apo-brivaracetam
    Tablet • 25 mg • Oral • Canada • Generic • Approved
  • Apo-brivaracetam
    Tablet • 50 mg • Oral • Canada • Generic • Approved
  • Apo-brivaracetam
    Tablet • 75 mg • Oral • Canada • Generic • Approved
  • Apo-brivaracetam
    Tablet • 100 mg • Oral • Canada • Generic • Approved
  • Auro-brivaracetam
    Tablet • 50 mg • Oral • Canada • Generic • Approved
  • Auro-brivaracetam
    Tablet • 100 mg • Oral • Canada • Generic • Approved
  • Briviact
    Tablet, film coated • 10 mg • Oral • EU • Approved
Menampilkan 8 dari 48 produk.
International Brands
  • Rikelta — UCB

Sekuens Gen/Protein (FASTA)

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