Peringatan Keamanan

There is limited clinical experience with daridorexant overdose. In clinical pharmacology studies, healthy subjects were administered single doses of up to 200 mg, four times the maximum recommended dose. Somnolence, muscle weakness, cataplexy-like symptoms, sleep paralysis, disturbance in attention, fatigue, headache, and constipation were observed in these patients.

There is no specific antidote to overdosage of daridorexant. In the event of an overdose, general symptomatic and supportive medical care, along with immediate gastric lavage where appropriate, should be provided in addition to careful monitoring. Dialysis is unlikely to be effective as daridorexant is highly protein-bound.L39655

Daridorexant

DB15031

small molecule approved

Deskripsi

Daridorexant, formerly known as nemorexant, is a selective dual orexin receptor antagonist used to treat insomnia. Insomnia is characterized by difficulties with sleep onset and/or sleep maintenance and impairment of daytime functioning. It chronically affects the person's daily functioning and long-term health effects, as insomnia is often associated with comorbidities such as hypertension, diabetes, and depression. Conventional treatments for insomnia include drugs targeting gamma-aminobutyric acid type-A (GABA-A), serotonin, histamine, or melatonin receptors; however, undesirable side effects are frequently reported, such as next-morning residual sleepiness, motor incoordination, falls, memory and cognitive impairment. Novel drugs that target orexin receptors gained increasing attention after discovering the role of orexin signalling pathway in wakefulness and almorexant, an orexin receptor antagonist that improved sleep. Daridorexant was designed via an intensive drug discovery program to improve the potency and maximize the duration of action while minimizing next-morning residual activity.A244225

Daridorexant works on orexin receptors OX1R and OX2R to block the binding of orexins, which are wake-promoting neuropeptides and endogenous ligands to these receptors. Daridorexant reduces overactive wakefulness: in the investigational trials, daridorexant reportedly improved sleep and daytime functioning in patients with insomnia.A244225 It was approved by the FDA on January 10, 2022, under the name QUVIVIQ.L39660 as the second orexin receptor antagonist approved to treat insomnia following suvorexant.A244280 Daridorexant was approved by the European Commission on May 3, 2022, as the first dual orexin receptor antagonist approved in the market,L41725 and by Health Canada on April 26, 2023.L46307

Struktur Molekul 2D

Berat 450.93
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 is approximately 8 hours.[L39655]
Volume Distribusi Daridorexant has a volume of distribution of 31 L. The blood to plasma ratio is 0.64.[L39655] It effectively passes the blood-brain barrier.[A244225]
Klirens (Clearance) There is limited information on clearance.

Absorpsi

Daridorexant reaches peak plasma concentrations within one to two hours. Daridorexant has an absolute bioavailability of 62%. While a high-fat and high-calorie meal delayed the Tmax by 1.3 hours and decreased the Cmax by 16% in healthy subjects, the total exposure (AUC) was not affected.L39655

Metabolisme

Daridorexant undergoes extensive metabolism primarily mediated by CYP3A4 (89%),L39655 mostly via oxidative transformations.A244285 Other CYP enzymes individually contribute to less than 3% of metabolic clearance of daridorexant.L39655

Rute Eliminasi

The primary route of excretion is via feces, accounting for approximately 57% of drug excretion. About 28% of the drug is excreted via urine primarily in the form of metabolites. Trace amounts of the parent drug were found in feces and urine.L39655

Interaksi Makanan

1 Data
  • 1. Avoid alcohol. Concomitant use of alcohol with daridorexant may lead to additive impairment of psychomotor performance and risk of CNS depression .

Interaksi Obat

771 Data
Buprenorphine Daridorexant 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 Daridorexant.
Dronabinol The risk or severity of CNS depression can be increased when Dronabinol is combined with Daridorexant.
Droperidol The risk or severity of CNS depression can be increased when Droperidol is combined with Daridorexant.
Hydrocodone Daridorexant 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 Daridorexant.
Magnesium sulfate The therapeutic efficacy of Daridorexant can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine The risk or severity of CNS depression can be increased when Methotrimeprazine is combined with Daridorexant.
Metyrosine Daridorexant may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Daridorexant.
Mirtazapine The risk or severity of CNS depression can be increased when Mirtazapine is combined with Daridorexant.
Nabilone The risk or severity of CNS depression can be increased when Nabilone is combined with Daridorexant.
Orphenadrine The risk or severity of CNS depression can be increased when Orphenadrine is combined with Daridorexant.
Paraldehyde The risk or severity of CNS depression can be increased when Paraldehyde is combined with Daridorexant.
Perampanel The risk or severity of CNS depression can be increased when Perampanel is combined with Daridorexant.
Pramipexole Daridorexant may increase the sedative activities of Pramipexole.
Ropinirole Daridorexant may increase the sedative activities of Ropinirole.
Rotigotine The risk or severity of CNS depression can be increased when Rotigotine is combined with Daridorexant.
Rufinamide The risk or severity of CNS depression can be increased when Rufinamide is combined with Daridorexant.
Sodium oxybate Daridorexant may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Daridorexant 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 Daridorexant.
Thalidomide Daridorexant may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Daridorexant 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 Daridorexant.
Ethanol Daridorexant may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Daridorexant may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine The risk or severity of CNS depression can be increased when Brimonidine is combined with Daridorexant.
Fluvoxamine The metabolism of Daridorexant can be decreased when combined with Fluvoxamine.
Citalopram The risk or severity of CNS depression can be increased when Citalopram is combined with Daridorexant.
Fluoxetine Daridorexant may increase the central nervous system depressant (CNS depressant) activities of Fluoxetine.
Duloxetine The risk or severity of CNS depression can be increased when Duloxetine is combined with Daridorexant.
Trazodone The risk or severity of CNS depression can be increased when Trazodone is combined with Daridorexant.
Paroxetine The risk or severity of CNS depression can be increased when Paroxetine is combined with Daridorexant.
Sertraline The risk or severity of CNS depression can be increased when Sertraline is combined with Daridorexant.
Sibutramine The risk or severity of CNS depression can be increased when Sibutramine is combined with Daridorexant.
Nefazodone The metabolism of Daridorexant can be decreased when combined with Nefazodone.
Escitalopram The risk or severity of CNS depression can be increased when Escitalopram is combined with Daridorexant.
Zimelidine The metabolism of Daridorexant can be decreased when combined with Zimelidine.
Dapoxetine The risk or severity of CNS depression can be increased when Dapoxetine is combined with Daridorexant.
Milnacipran The metabolism of Daridorexant can be decreased when combined with Milnacipran.
Desvenlafaxine The metabolism of Daridorexant can be decreased when combined with Desvenlafaxine.
Seproxetine The metabolism of Daridorexant can be decreased when combined with Seproxetine.
Indalpine The metabolism of Daridorexant can be decreased when combined with Indalpine.
Ritanserin The risk or severity of CNS depression can be increased when Ritanserin is combined with Daridorexant.
Alaproclate The risk or severity of CNS depression can be increased when Alaproclate is combined with Daridorexant.
Tramadol The risk or severity of CNS depression can be increased when Daridorexant is combined with Tramadol.
Ziprasidone The risk or severity of adverse effects can be increased when Daridorexant is combined with Ziprasidone.
Amitriptyline The risk or severity of CNS depression can be increased when Amitriptyline is combined with Daridorexant.
Olanzapine The risk or severity of CNS depression can be increased when Olanzapine is combined with Daridorexant.
Terfenadine The metabolism of Daridorexant can be decreased when combined with Terfenadine.
Clozapine The metabolism of Daridorexant can be decreased when combined with Clozapine.
Promazine The risk or severity of CNS depression can be increased when Promazine is combined with Daridorexant.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Daridorexant.
Imipramine The risk or severity of CNS depression can be increased when Imipramine is combined with Daridorexant.
Chlorpromazine The risk or severity of CNS depression can be increased when Chlorpromazine is combined with Daridorexant.
Gallamine triethiodide The risk or severity of CNS depression can be increased when Gallamine triethiodide is combined with Daridorexant.
Triflupromazine The risk or severity of CNS depression can be increased when Triflupromazine is combined with Daridorexant.
Nortriptyline The risk or severity of CNS depression can be increased when Nortriptyline is combined with Daridorexant.
Amoxapine The risk or severity of CNS depression can be increased when Amoxapine is combined with Daridorexant.
Lamotrigine The risk or severity of CNS depression can be increased when Lamotrigine is combined with Daridorexant.
Nicardipine The metabolism of Daridorexant can be decreased when combined with Nicardipine.
Rocuronium The risk or severity of CNS depression can be increased when Rocuronium is combined with Daridorexant.
Scopolamine The risk or severity of CNS depression can be increased when Scopolamine is combined with Daridorexant.
Clidinium The risk or severity of CNS depression can be increased when Clidinium is combined with Daridorexant.
Propiomazine The risk or severity of CNS depression can be increased when Propiomazine is combined with Daridorexant.
Brompheniramine The risk or severity of CNS depression can be increased when Brompheniramine is combined with Daridorexant.
Flupentixol Flupentixol may increase the sedative activities of Daridorexant.
Maprotiline The risk or severity of CNS depression can be increased when Maprotiline is combined with Daridorexant.
Promethazine The risk or severity of CNS depression can be increased when Promethazine is combined with Daridorexant.
Diphenhydramine The risk or severity of CNS depression can be increased when Diphenhydramine is combined with Daridorexant.
Doxacurium The risk or severity of CNS depression can be increased when Doxacurium is combined with Daridorexant.
Doxepin The risk or severity of CNS depression can be increased when Doxepin is combined with Daridorexant.
Desipramine The risk or severity of CNS depression can be increased when Desipramine is combined with Daridorexant.
Quetiapine The risk or severity of CNS depression can be increased when Quetiapine is combined with Daridorexant.
Mivacurium The risk or severity of CNS depression can be increased when Mivacurium is combined with Daridorexant.
Aripiprazole The risk or severity of CNS depression can be increased when Aripiprazole is combined with Daridorexant.
Chlorprothixene The risk or severity of CNS depression can be increased when Chlorprothixene is combined with Daridorexant.
Metocurine The risk or severity of CNS depression can be increased when Metocurine is combined with Daridorexant.
Pancuronium The risk or severity of CNS depression can be increased when Pancuronium is combined with Daridorexant.
Pipecuronium The risk or severity of CNS depression can be increased when Pipecuronium is combined with Daridorexant.
Rapacuronium The risk or severity of CNS depression can be increased when Rapacuronium is combined with Daridorexant.
Pizotifen The risk or severity of CNS depression can be increased when Pizotifen is combined with Daridorexant.
Benactyzine The risk or severity of CNS depression can be increased when Benactyzine is combined with Daridorexant.
Dosulepin The risk or severity of CNS depression can be increased when Dosulepin is combined with Daridorexant.
Emepronium The risk or severity of CNS depression can be increased when Emepronium is combined with Daridorexant.
Eszopiclone The risk or severity of CNS depression can be increased when Daridorexant is combined with Eszopiclone.
Zopiclone The risk or severity of CNS depression can be increased when Zopiclone is combined with Daridorexant.
Phenytoin The metabolism of Daridorexant can be increased when combined with Phenytoin.
Pentobarbital The metabolism of Daridorexant can be increased when combined with Pentobarbital.
Carbamazepine The metabolism of Daridorexant can be increased when combined with Carbamazepine.
Mitotane The metabolism of Daridorexant can be increased when combined with Mitotane.
Primidone The metabolism of Daridorexant can be increased when combined with Primidone.
Rifampin The metabolism of Daridorexant can be increased when combined with Rifampicin.
Phenobarbital The metabolism of Daridorexant can be increased when combined with Phenobarbital.
Rifapentine The metabolism of Daridorexant can be increased when combined with Rifapentine.
Dexamethasone The metabolism of Daridorexant can be increased when combined with Dexamethasone.
Fosphenytoin The metabolism of Daridorexant can be increased when combined with Fosphenytoin.
St. John's Wort The metabolism of Daridorexant can be increased when combined with St. John's Wort.
Midostaurin The metabolism of Daridorexant can be decreased when combined with Midostaurin.

Target Protein

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

Referensi & Sumber

Artikel (PubMed)
  • PMID: 34415378
    Roch C, Bergamini G, Steiner MA, Clozel M: Nonclinical pharmacology of daridorexant: a new dual orexin receptor antagonist for the treatment of insomnia. Psychopharmacology (Berl). 2021 Oct;238(10):2693-2708. doi: 10.1007/s00213-021-05954-0. Epub 2021 Aug 20.
  • PMID: 30338596
    Herring WJ, Roth T, Krystal AD, Michelson D: Orexin receptor antagonists for the treatment of insomnia and potential treatment of other neuropsychiatric indications. J Sleep Res. 2019 Apr;28(2):e12782. doi: 10.1111/jsr.12782. Epub 2018 Oct 18.
  • PMID: 30727881
    Muehlan C, Fischer H, Zimmer D, Aissaoui H, Grimont J, Boss C, Croft M, van Gerven J, Krahenbuhl S, Dingemanse J: Metabolism of the Dual Orexin Receptor Antagonist ACT-541468, Based on Microtracer/ Accelerator Mass Spectrometry. Curr Drug Metab. 2019;20(4):254-265. doi: 10.2174/1389200220666190206141814.
  • PMID: 30092886
    Janto K, Prichard JR, Pusalavidyasagar S: An Update on Dual Orexin Receptor Antagonists and Their Potential Role in Insomnia Therapeutics. J Clin Sleep Med. 2018 Aug 15;14(8):1399-1408. doi: 10.5664/jcsm.7282.

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