Peringatan Keamanan

Dose-related somnolence and CNS depression are the most common adverse effects associated with the use of suvorexant. It has also been shown to impair driving skills and may increase the risk of falling asleep while driving. Next-day impairments are found to be highest if suvorexant is taken with less than a full night of sleep remaining, with higher doses, or if co-administered with other CNS depressants or CYP3A inhibitors. Complex behaviours such as sleep driving, preparing and eating food, and making phone calls have been reported in association with the use of hypnotics such as suvorexant. A dose-dependant increase in suicidal ideation has been observed, especially in patients with a previous diagnosis of depression. Sleep paralysis, hypnagogic/hypnopompic hallucinations including vivid and disturbing perceptions, and mild cataplexy have also been reported. There are no adequate studies in pregnant women to ensure its safety during pregnancy or breast feeding.

Suvorexant

DB09034

small molecule approved investigational

Deskripsi

Suvorexant is a selective dual antagonist of orexin receptors OX1R and OX2R that promotes sleep by reducing wakefulness and arousal. It has been approved for the treatment of insomnia.

Struktur Molekul 2D

Berat 450.93
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Mean half life is approximately 12 hours.
Volume Distribusi Mean volume of distribution is approximately 49 litres.
Klirens (Clearance) -

Absorpsi

Peak concentrations occur at a median Tmax of 2 hours under fasted conditions. Ingestion of suvorexant with a high-fat meal has no effect on AUC or Cmax, but may delay Tmax by approximately 1.5 hours. Mean absolute bioavailability of 10 mg is 82%.

Metabolisme

Suvorexant is primarily metabolized by cytochrome-P450 3A4 enzyme (CYP3A4) with a minor contribution from CYP2C19. Major circulating metabolites are suvorexant and a hydroxy-suvorexant metabolite, which is not expected to be pharmacologically active. There is potential for drug-drug interactions with drugs that inhibit or induce CYP3A4 activity.

Rute Eliminasi

Approximately 66% is eliminated in feces and 23% is eliminated in urine.

Interaksi Makanan

1 Data
  • 1. Avoid grapefruit products.

Interaksi Obat

1158 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Suvorexant.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Suvorexant.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Suvorexant.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Suvorexant.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Suvorexant.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Suvorexant.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Suvorexant.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Suvorexant.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Suvorexant.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Suvorexant.
Silodosin The excretion of Silodosin can be decreased when combined with Suvorexant.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Suvorexant.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Metyrosine Suvorexant may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Pramipexole Suvorexant may increase the sedative activities of Pramipexole.
Ropinirole Suvorexant may increase the sedative activities of Ropinirole.
Botulinum toxin type B Botulinum toxin type B may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Botulinum toxin type A Botulinum toxin type A may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tryptophan Tryptophan may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Fluvoxamine Fluvoxamine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Baclofen Baclofen may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Lorazepam Lorazepam may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Ethchlorvynol Ethchlorvynol may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tramadol Tramadol may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Succinylcholine Succinylcholine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Reserpine Reserpine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Citalopram Citalopram may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Eletriptan Eletriptan may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Enflurane Enflurane may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Pregabalin Pregabalin may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Temazepam Temazepam may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Reboxetine Reboxetine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Butabarbital Butabarbital may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Butalbital Butalbital may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Ziprasidone Ziprasidone may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Methysergide Methysergide may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Cabergoline Cabergoline may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Phenytoin Phenytoin may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Topiramate Topiramate may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Clemastine Clemastine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Venlafaxine Venlafaxine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Etomidate Etomidate may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Morphine Morphine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Talbutal Talbutal may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Pentobarbital Pentobarbital may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Valproic acid Valproic acid may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Zolmitriptan Zolmitriptan may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Codeine Codeine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Dihydroergotamine Dihydroergotamine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Amitriptyline Amitriptyline may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tolcapone Tolcapone may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Hydromorphone Hydromorphone may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Olanzapine Olanzapine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Cetirizine Cetirizine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Protriptyline Protriptyline may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Trimethadione Trimethadione may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Clobazam Clobazam may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Chlorzoxazone Chlorzoxazone may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Clozapine Clozapine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Mirtazapine Mirtazapine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Meprobamate Meprobamate may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Thiethylperazine Thiethylperazine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Palonosetron Palonosetron may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Sulpiride Sulpiride may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Carisoprodol Carisoprodol may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Eszopiclone Eszopiclone may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Alprazolam Alprazolam may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Dexbrompheniramine Dexbrompheniramine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Loxapine Loxapine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Remoxipride Remoxipride may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Metocurine iodide Metocurine iodide may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Secobarbital Secobarbital may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Promazine Promazine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Methocarbamol Methocarbamol may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Zolpidem Zolpidem may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Triprolidine Triprolidine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Prochlorperazine Prochlorperazine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Cyproheptadine Cyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Meperidine Meperidine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Imipramine Imipramine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Metharbital Metharbital may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Quinine Quinine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Fluoxetine Fluoxetine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Methohexital Methohexital may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Chlordiazepoxide Chlordiazepoxide may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Duloxetine Duloxetine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Chlorpromazine Chlorpromazine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Gallamine triethiodide Gallamine triethiodide may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Entacapone Entacapone may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Oxycodone Oxycodone may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Haloperidol Haloperidol may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Triflupromazine Triflupromazine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Dextromethorphan Dextromethorphan may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Mephenytoin Mephenytoin may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Nortriptyline Nortriptyline may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Amoxapine Amoxapine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.

Target Protein

Orexin/Hypocretin receptor type 1 HCRTR1
Orexin receptor type 2 HCRTR2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 23702225
    Palasz A, Lapray D, Peyron C, Rojczyk-Golebiewska E, Skowronek R, Markowski G, Czajkowska B, Krzystanek M, Wiaderkiewicz R: Dual orexin receptor antagonists - promising agents in the treatment of sleep disorders. Int J Neuropsychopharmacol. 2014 Jan;17(1):157-68. doi: 10.1017/S1461145713000552. Epub 2013 May 23.
  • PMID: 25667197
    Patel KV, Aspesi AV, Evoy KE: Suvorexant: a dual orexin receptor antagonist for the treatment of sleep onset and sleep maintenance insomnia. Ann Pharmacother. 2015 Apr;49(4):477-83. doi: 10.1177/1060028015570467. Epub 2015 Feb 9.
  • PMID: 25397996
    Reddy A, Puvvada SC, Kommisetti S, El-Mallakh RS, Lippmann S: Suvorexant: something new for sleep? Acta Neuropsychiatr. 2015 Feb;27(1):53-5. doi: 10.1017/neu.2014.31. Epub 2014 Nov 14.
  • PMID: 24680372
    Michelson D, Snyder E, Paradis E, Chengan-Liu M, Snavely DB, Hutzelmann J, Walsh JK, Krystal AD, Benca RM, Cohn M, Lines C, Roth T, Herring WJ: Safety and efficacy of suvorexant during 1-year treatment of insomnia with subsequent abrupt treatment discontinuation: a phase 3 randomised, double-blind, placebo-controlled trial. Lancet Neurol. 2014 May;13(5):461-71. doi: 10.1016/S1474-4422(14)70053-5. Epub 2014 Mar 27.
  • PMID: 25291725
    Howland RH: Suvorexant: a novel therapy for the treatment of insomnia. J Psychosoc Nurs Ment Health Serv. 2014 Oct;52(10):23-6. doi: 10.3928/02793695-20140924-01.

Contoh Produk & Brand

Produk: 8 • International brands: 0
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Sekuens Gen/Protein (FASTA)

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