Riluzole

DB00740

small molecule approved investigational

Deskripsi

A glutamate antagonist (receptors, glutamate) used as an anticonvulsant (anticonvulsants) and to prolong the survival of patients with amyotrophic lateral sclerosis. Riluzole is marketed as Rilutek by Sanofi.

Struktur Molekul 2D

Berat 234.198
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean elimination half-life of riluzole is 12 hours (CV=35%) after repeated doses.
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Riluzole is well-absorbed (approximately 90%), with average absolute oral bioavailability of about 60% (CV=30%). A high fat meal decreases absorption, reducing AUC by about 20% and peak blood levels by about 45%.

Metabolisme

Riluzole is extensively metabolized to six major and a number of minor metabolites, which have not all been identified to date. Metabolism is mostly hepatic, consisting of cytochrome P450–dependent hydroxylation and glucuronidation. CYP1A2 is the primary isozyme involved in N-hydroxylation; CYP2D6, CYP2C19, CYP3A4, and CYP2E1 are considered unlikely to contribute significantly to riluzole metabolism in humans.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Makanan

1 Data
  • 1. Take on an empty stomach. Take at least 1 hour before or 2 hours after meals.

Interaksi Obat

1090 Data
Deferasirox The serum concentration of Riluzole can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Riluzole can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Riluzole can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Riluzole can be decreased when it is combined with Teriflunomide.
Buprenorphine Riluzole 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 Riluzole.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Riluzole.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Riluzole.
Hydrocodone Riluzole 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 Riluzole.
Magnesium sulfate The therapeutic efficacy of Riluzole can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Riluzole may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Riluzole may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Riluzole.
Mirtazapine Riluzole 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 Riluzole.
Orphenadrine Riluzole may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Riluzole 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 Riluzole.
Pramipexole Riluzole may increase the sedative activities of Pramipexole.
Ropinirole Riluzole may increase the sedative activities of Ropinirole.
Rotigotine Riluzole may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Riluzole.
Sodium oxybate Riluzole may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Riluzole 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 Riluzole.
Thalidomide Riluzole may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Riluzole may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Mefloquine The therapeutic efficacy of Riluzole can be decreased when used in combination with Mefloquine.
Mianserin The therapeutic efficacy of Riluzole can be decreased when used in combination with Mianserin.
Orlistat Orlistat can cause a decrease in the absorption of Riluzole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Topotecan Riluzole 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 Riluzole.
Tetracosactide The risk or severity of liver damage can be increased when Tetracosactide is combined with Riluzole.
Abiraterone The serum concentration of Riluzole can be increased when it is combined with Abiraterone.
Cyproterone acetate The metabolism of Riluzole can be increased when combined with Cyproterone acetate.
Ethanol Riluzole may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Riluzole 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 Riluzole.
Citalopram The risk or severity of adverse effects can be increased when Riluzole is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Riluzole is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Riluzole is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Riluzole is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Riluzole is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Riluzole is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Riluzole is combined with Nefazodone.
Escitalopram The risk or severity of adverse effects can be increased when Riluzole is combined with Escitalopram.
Zimelidine The risk or severity of adverse effects can be increased when Riluzole is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Riluzole is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Riluzole is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Riluzole is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Riluzole is combined with Seproxetine.
Indalpine The risk or severity of adverse effects can be increased when Riluzole is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Riluzole is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Riluzole is combined with Alaproclate.
Amitriptyline The risk or severity of CNS depression can be increased when Amitriptyline is combined with Riluzole.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Riluzole.
Nortriptyline The risk or severity of CNS depression can be increased when Nortriptyline is combined with Riluzole.
Amoxapine The risk or severity of CNS depression can be increased when Amoxapine is combined with Riluzole.
Propiomazine The risk or severity of CNS depression can be increased when Riluzole is combined with Propiomazine.
Cocaine The risk or severity of methemoglobinemia can be increased when Riluzole is combined with Cocaine.
Maprotiline The risk or severity of CNS depression can be increased when Riluzole is combined with Maprotiline.
Doxepin The risk or severity of CNS depression can be increased when Riluzole is combined with Doxepin.
Desipramine The risk or severity of CNS depression can be increased when Riluzole is combined with Desipramine.
Pizotifen The risk or severity of CNS depression can be increased when Riluzole is combined with Pizotifen.
Dosulepin The risk or severity of CNS depression can be increased when Riluzole is combined with Dosulepin.
Zopiclone The risk or severity of adverse effects can be increased when Riluzole is combined with Zopiclone.
Primidone The metabolism of Riluzole can be increased when combined with Primidone.
Rifampin The metabolism of Riluzole can be increased when combined with Rifampicin.
Albendazole The metabolism of Riluzole can be increased when combined with Albendazole.
Caffeine The metabolism of Riluzole can be decreased when combined with Caffeine.
Moxifloxacin The metabolism of Riluzole can be decreased when combined with Moxifloxacin.
Lidocaine The risk or severity of methemoglobinemia can be increased when Riluzole is combined with Lidocaine.
Mexiletine The metabolism of Riluzole can be decreased when combined with Mexiletine.
Alosetron The metabolism of Riluzole can be decreased when combined with Alosetron.
Ketoconazole The metabolism of Riluzole can be decreased when combined with Ketoconazole.
Gatifloxacin The metabolism of Riluzole can be decreased when combined with Gatifloxacin.
Lobeglitazone The metabolism of Riluzole can be decreased when combined with Lobeglitazone.
Pazufloxacin The metabolism of Riluzole can be decreased when combined with Pazufloxacin.
Osilodrostat The metabolism of Riluzole can be decreased when combined with Osilodrostat.
Botulinum toxin type B The risk or severity of CNS depression can be increased when Botulinum toxin type B is combined with Riluzole.
Botulinum toxin type A The risk or severity of CNS depression can be increased when Botulinum toxin type A is combined with Riluzole.
Tryptophan The risk or severity of CNS depression can be increased when Tryptophan is combined with Riluzole.
Baclofen Baclofen may increase the central nervous system depressant (CNS depressant) activities of Riluzole.
Lorazepam The risk or severity of CNS depression can be increased when Lorazepam is combined with Riluzole.
Ethchlorvynol The risk or severity of CNS depression can be increased when Ethchlorvynol is combined with Riluzole.
Succinylcholine The risk or severity of CNS depression can be increased when Succinylcholine is combined with Riluzole.
Reserpine The risk or severity of CNS depression can be increased when Reserpine is combined with Riluzole.
Eletriptan The risk or severity of CNS depression can be increased when Eletriptan is combined with Riluzole.
Enflurane The risk or severity of CNS depression can be increased when Enflurane is combined with Riluzole.
Temazepam The risk or severity of CNS depression can be increased when Temazepam is combined with Riluzole.
Reboxetine The risk or severity of CNS depression can be increased when Reboxetine is combined with Riluzole.
Butabarbital The risk or severity of CNS depression can be increased when Butabarbital is combined with Riluzole.
Butalbital The risk or severity of CNS depression can be increased when Butalbital is combined with Riluzole.
Methysergide The risk or severity of CNS depression can be increased when Methysergide is combined with Riluzole.
Cabergoline The risk or severity of CNS depression can be increased when Cabergoline is combined with Riluzole.
Phenytoin The risk or severity of CNS depression can be increased when Phenytoin is combined with Riluzole.
Topiramate The risk or severity of CNS depression can be increased when Topiramate is combined with Riluzole.
Clemastine The risk or severity of CNS depression can be increased when Clemastine is combined with Riluzole.
Venlafaxine The risk or severity of CNS depression can be increased when Venlafaxine is combined with Riluzole.

Target Protein

Sodium channel protein type 5 subunit alpha SCN5A
Sodium channel protein type 11 subunit alpha SCN11A
Cystine/glutamate transporter SLC7A11

Referensi & Sumber

Synthesis reference: Pratap Padi, Madhusudhan Ganta, Satyanarayana Bollikonda, Sridhar Chaganti, Ramulu Akula, Loka Maheshwari Dommati, "PROCESS FOR PREPARING RILUZOLE." U.S. Patent US20080108827, issued May 08, 2008.
Artikel (PubMed)
  • PMID: 9262334
    Song JH, Huang CS, Nagata K, Yeh JZ, Narahashi T: Differential action of riluzole on tetrodotoxin-sensitive and tetrodotoxin-resistant sodium channels. J Pharmacol Exp Ther. 1997 Aug;282(2):707-14.
  • PMID: 15993857
    Coric V, Taskiran S, Pittenger C, Wasylink S, Mathalon DH, Valentine G, Saksa J, Wu YT, Gueorguieva R, Sanacora G, Malison RT, Krystal JH: Riluzole augmentation in treatment-resistant obsessive-compulsive disorder: an open-label trial. Biol Psychiatry. 2005 Sep 1;58(5):424-8.
  • PMID: 15752377
    van Kan HJ, Groeneveld GJ, Kalmijn S, Spieksma M, van den Berg LH, Guchelaar HJ: Association between CYP1A2 activity and riluzole clearance in patients with amyotrophic lateral sclerosis. Br J Clin Pharmacol. 2005 Mar;59(3):310-3.
  • PMID: 14702270
    Zarate CA Jr, Payne JL, Quiroz J, Sporn J, Denicoff KK, Luckenbaugh D, Charney DS, Manji HK: An open-label trial of riluzole in patients with treatment-resistant major depression. Am J Psychiatry. 2004 Jan;161(1):171-4.
  • PMID: 18172433
    Mathew SJ, Manji HK, Charney DS: Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. doi: 10.1038/sj.npp.1301652. Epub 2008 Jan 2.
  • PMID: 18445055
    Lamanauskas N, Nistri A: Riluzole blocks persistent Na+ and Ca2+ currents and modulates release of glutamate via presynaptic NMDA receptors on neonatal rat hypoglossal motoneurons in vitro. Eur J Neurosci. 2008 May;27(10):2501-14. doi: 10.1111/j.1460-9568.2008.06211.x. Epub 2008 Apr 26.

Contoh Produk & Brand

Produk: 34 • International brands: 8
Produk
  • Apo-riluzole
    Tablet • 50 mg • Oral • Canada • Generic • Approved
  • Exservan
    Film • 50 mg/1 • Oral • US • Approved
  • Exservan
    Film • 50 mg/1 • Oral • US • Approved
  • Exservan
    Film • 50 mg/1 • Oral • US • Approved
  • Mylan-riluzole
    Tablet • 50 mg • Oral • Canada • Generic • Approved
  • Rilutek
    Tablet • 50 mg/1 • Oral • US • Approved
  • Rilutek
    Tablet • 50 mg/1 • Oral • US • Approved
  • Rilutek
    Tablet, film coated • 50 mg/1 • Oral • US • Approved
Menampilkan 8 dari 34 produk.
International Brands
  • Fanizan — Actavis
  • Laidec — Sun Pro
  • Lizolorol — Actavis
  • Lizorolol — ratiopharm
  • Rilustad — STADA
  • Sclefic — Actavis
  • Xie Yi Li — Lunan Pharm
  • Zolerilis — Actavis

Sekuens Gen/Protein (FASTA)

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