Peringatan Keamanan

The oral LD50 of viloxazine was 2000 mg/kg in rats.L41690

There is limited clinical experience with viloxazine overdose. According to case reports in the literature and postmarketing reports, doses ranging from 1000 mg to 6500 mg, which are 1.7 to 10.8 times the maximum recommended daily dose, resulted in overdose with drowsiness as the most reported symptom. Impaired consciousness, diminished reflexes, and increased heart rate have also been reported. There is no specific antidote for viloxazine overdose.L41685

Viloxazine

DB09185

small molecule approved investigational withdrawn

Deskripsi

Viloxazine is a selective norepinephrine reuptake inhibitor.L41685 For decades, an immediate-release formulation of viloxazine has been used in Europe as an antidepressant. It was first approved in the UK in 1974; however, the immediate-release formulation was discontinued due to business reasons unrelated to drug safety and efficacy. In the US, viloxazine was assigned an orphan drug designation in 1984 under the brand name CATATROL: while this product was intended to treat cataplexy and narcolepsy, the drug was never approved for these therapeutic indications. In April 2021, an extended-release formulation of viloxazine under the brand name QELBREE was approved by the FDA for the treatment of attention deficit hyperactivity disorder (ADHD).A247985

Struktur Molekul 2D

Berat 237.299
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 (± SD) half-life of viloxazine was 7.02 (± 4.74) hours.[L41685]
Volume Distribusi The volume of distribution was 0.73 ± 0.28 L/kg following intravenous administration.[A247985]
Klirens (Clearance) The clearance rate was 124 ± 11 mL/hour/kg following intravenous administration.[A247985]

Absorpsi

Viloxazine is rapidly absorbed following oral administration.A19781,A19786 The relative bioavailability of viloxazine extended-release relative to an immediate-release formulation was about 88%.L41685 Viloxazine Cmax and AUC increase proportionally over a dosage range from 100 mg to 600 mg once daily.L41685 The Cmax ranges between 540 and 1600 ng/mL.A19781 Following administration of a single 200 mg dose, the median Tmax was approximately five hours, with a range of three to nine hours. Steady-state was reached after two days of once-daily administration, and no accumulation was observed. A high-fat meal decreases Cmax and AUC by about 9% and 8%, respectively, and delays Tmax by two hours.L41685

Metabolisme

Viloxazine undergoes CYP2D6-mediated 5-hydroxylation to form 5-hydroxyviloxazine. This metabolite can be glucuronidated by UGT1A9 and UGT2B15 to form 5-hydroxyviloxazine glucuronide,A247110 which is the major metabolite detected in plasma.L41685 Viloxazine can also be glucuronidated to form Viloxazine N-carbamoyl glucuronide.A247110

Rute Eliminasi

Viloxazine is primarily excreted via renal elimination. After administration of radiolabeled viloxazine, 90% of the dose was recovered in urine within the first 24 hours post-dose. Less than 1% of the dose is excreted in the feces.L41685 About 12-15% of the total drug is eliminated as unchanged parent drug.A19781

Interaksi Makanan

1 Data
  • 1. Take with or without food. A high-fat meal decreases drug Cmax and AUC and delays Tmax, but not to a clinically significant extent.

Interaksi Obat

1910 Data
Tizanidine The serum concentration of Tizanidine can be increased when it is combined with Viloxazine.
Buprenorphine Viloxazine 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 Viloxazine.
Dronabinol The serum concentration of Dronabinol can be increased when it is combined with Viloxazine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Viloxazine.
Hydrocodone Viloxazine 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 Viloxazine.
Magnesium sulfate The therapeutic efficacy of Viloxazine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine The metabolism of Methotrimeprazine can be decreased when combined with Viloxazine.
Metyrosine Viloxazine may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Viloxazine.
Mirtazapine The metabolism of Mirtazapine can be decreased when combined with Viloxazine.
Nabilone The metabolism of Nabilone can be decreased when combined with Viloxazine.
Orphenadrine The metabolism of Orphenadrine can be decreased when combined with Viloxazine.
Paraldehyde Viloxazine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel The metabolism of Perampanel can be decreased when combined with Viloxazine.
Pramipexole Viloxazine may increase the sedative activities of Pramipexole.
Rotigotine The metabolism of Rotigotine can be decreased when combined with Viloxazine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Viloxazine.
Sodium oxybate Viloxazine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Viloxazine 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 Viloxazine.
Thalidomide Viloxazine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Viloxazine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Viloxazine.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Viloxazine.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Viloxazine.
Colchicine The metabolism of Colchicine can be decreased when combined with Viloxazine.
Fentanyl The metabolism of Fentanyl can be decreased when combined with Viloxazine.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Viloxazine.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Viloxazine.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Viloxazine.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Viloxazine.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Viloxazine.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Viloxazine.
Zolmitriptan The metabolism of Zolmitriptan can be decreased when combined with Viloxazine.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Viloxazine.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Viloxazine.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Viloxazine.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Viloxazine.
(R)-warfarin The metabolism of (R)-warfarin can be decreased when combined with Viloxazine.
(S)-Warfarin The metabolism of (S)-Warfarin can be decreased when combined with Viloxazine.
Warfarin The metabolism of Warfarin can be decreased when combined with Viloxazine.
Acenocoumarol The metabolism of Acenocoumarol can be decreased when combined with Viloxazine.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Viloxazine.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Viloxazine.
Dicoumarol The risk or severity of adverse effects can be increased when Viloxazine is combined with Dicoumarol.
Phenindione The risk or severity of adverse effects can be increased when Viloxazine is combined with Phenindione.
Phenprocoumon The metabolism of Phenprocoumon can be decreased when combined with Viloxazine.
4-hydroxycoumarin The risk or severity of adverse effects can be increased when Viloxazine is combined with 4-hydroxycoumarin.
Coumarin The risk or severity of adverse effects can be increased when Viloxazine is combined with Coumarin.
Ethyl biscoumacetate The metabolism of Ethyl biscoumacetate can be decreased when combined with Viloxazine.
Fluindione The risk or severity of adverse effects can be increased when Viloxazine is combined with Fluindione.
Clorindione The risk or severity of adverse effects can be increased when Viloxazine is combined with Clorindione.
Diphenadione The metabolism of Diphenadione can be decreased when combined with Viloxazine.
Tioclomarol The risk or severity of adverse effects can be increased when Viloxazine is combined with Tioclomarol.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Viloxazine.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Viloxazine.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Viloxazine.
Ethanol Viloxazine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Viloxazine 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 Viloxazine.
Zimelidine The risk or severity of adverse effects can be increased when Viloxazine is combined with Zimelidine.
Dapoxetine The metabolism of Dapoxetine can be decreased when combined with Viloxazine.
Seproxetine The risk or severity of adverse effects can be increased when Viloxazine is combined with Seproxetine.
Fluvoxamine The metabolism of Fluvoxamine can be decreased when combined with Viloxazine.
Citalopram The metabolism of Citalopram can be decreased when combined with Viloxazine.
Duloxetine The metabolism of Duloxetine can be decreased when combined with Viloxazine.
Trazodone The metabolism of Trazodone can be decreased when combined with Viloxazine.
Paroxetine The metabolism of Paroxetine can be decreased when combined with Viloxazine.
Sertraline The metabolism of Sertraline can be decreased when combined with Viloxazine.
Sibutramine The metabolism of Sibutramine can be decreased when combined with Viloxazine.
Nefazodone The metabolism of Nefazodone can be decreased when combined with Viloxazine.
Escitalopram The metabolism of Escitalopram can be decreased when combined with Viloxazine.
Milnacipran The metabolism of Milnacipran can be decreased when combined with Viloxazine.
Desvenlafaxine The metabolism of Desvenlafaxine can be decreased when combined with Viloxazine.
Levomilnacipran The metabolism of Levomilnacipran can be decreased when combined with Viloxazine.
Indalpine The metabolism of Indalpine can be decreased when combined with Viloxazine.
Ritanserin The risk or severity of adverse effects can be increased when Viloxazine is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Viloxazine is combined with Alaproclate.
Iobenguane Viloxazine can cause a decrease in the absorption of Iobenguane resulting in a reduced serum concentration and potentially a decrease in efficacy.
Terfenadine The metabolism of Terfenadine can be decreased when combined with Viloxazine.
Darifenacin The metabolism of Darifenacin can be decreased when combined with Viloxazine.
Nicardipine The metabolism of Nicardipine can be decreased when combined with Viloxazine.
Cocaine The metabolism of Cocaine can be decreased when combined with Viloxazine.
Oxybutynin The metabolism of Oxybutynin can be decreased when combined with Viloxazine.
Solifenacin The metabolism of Solifenacin can be decreased when combined with Viloxazine.
Umeclidinium The metabolism of Umeclidinium can be decreased when combined with Viloxazine.
Revefenacin The metabolism of Revefenacin can be decreased when combined with Viloxazine.
Otilonium The metabolism of Otilonium can be decreased when combined with Viloxazine.
Benzatropine The metabolism of Benzatropine can be decreased when combined with Viloxazine.
Disopyramide The metabolism of Disopyramide can be decreased when combined with Viloxazine.
Propantheline Propantheline may decrease the excretion rate of Viloxazine which could result in a higher serum level.
Dicyclomine Dicyclomine may decrease the excretion rate of Viloxazine which could result in a higher serum level.
Tolterodine The metabolism of Tolterodine can be decreased when combined with Viloxazine.
Promethazine The metabolism of Promethazine can be decreased when combined with Viloxazine.
Doxacurium The risk or severity of CNS depression can be increased when Doxacurium is combined with Viloxazine.
Flavoxate Flavoxate may decrease the excretion rate of Viloxazine which could result in a higher serum level.
Tiotropium The metabolism of Tiotropium can be decreased when combined with Viloxazine.
Fesoterodine The metabolism of Fesoterodine can be decreased when combined with Viloxazine.

Target Protein

Sodium-dependent noradrenaline transporter SLC6A2
5-hydroxytryptamine receptor 2B HTR2B
5-hydroxytryptamine receptor 2C HTR2C
Alpha-1B adrenergic receptor ADRA1B
Beta-2 adrenergic receptor ADRB2
Histamine H1 receptor HRH1
Histamine H2 receptor HRH2
Muscarinic acetylcholine receptor M1 CHRM1
Muscarinic acetylcholine receptor M2 CHRM2
Muscarinic acetylcholine receptor M3 CHRM3
Muscarinic acetylcholine receptor M4 CHRM4
Amine oxidase [flavin-containing] A MAOA
Amine oxidase [flavin-containing] B MAOB

Referensi & Sumber

Artikel (PubMed)
  • PMID: 324751
    Pinder RM, Brogden RN, Speight TM, Avery GS: Viloxazine: a review of its pharmacological properties and therapeutic efficacy in depressive illness. Drugs. 1977 Jun;13(6):401-21.
  • PMID: 2761683
    Kergueris MF, Bourin M, Ribeyrol M, Beneroso N, Normand YL, Larousse C: Comparative pharmacokinetic study of conventional and sustained-release viloxazine in normal volunteers. Neuropsychobiology. 1989;20(3):136-40.
  • PMID: 32394778
    Yu C: Metabolism and in vitro drug-drug interaction assessment of viloxazine. Xenobiotica. 2020 Nov;50(11):1285-1300. doi: 10.1080/00498254.2020.1767319. Epub 2020 Jun 10.
  • PMID: 34975586
    Edinoff AN, Akuly HA, Wagner JH, Boudreaux MA, Kaplan LA, Yusuf S, Neuchat EE, Cornett EM, Boyer AG, Kaye AM, Kaye AD: Viloxazine in the Treatment of Attention Deficit Hyperactivity Disorder. Front Psychiatry. 2021 Dec 17;12:789982. doi: 10.3389/fpsyt.2021.789982. eCollection 2021.
  • PMID: 32943948
    Yu C, Garcia-Olivares J, Candler S, Schwabe S, Maletic V: New Insights into the Mechanism of Action of Viloxazine: Serotonin and Norepinephrine Modulating Properties. J Exp Pharmacol. 2020 Aug 25;12:285-300. doi: 10.2147/JEP.S256586. eCollection 2020.
  • PMID: 34003459
    Findling RL, Candler SA, Nasser AF, Schwabe S, Yu C, Garcia-Olivares J, O'Neal W, Newcorn JH: Viloxazine in the Management of CNS Disorders: A Historical Overview and Current Status. CNS Drugs. 2021 Jun;35(6):643-653. doi: 10.1007/s40263-021-00825-w. Epub 2021 May 18.

Contoh Produk & Brand

Produk: 3 • International brands: 1
Produk
  • Qelbree
    Capsule, extended release • 100 mg/1 • Oral • US • Approved
  • Qelbree
    Capsule, extended release • 150 mg/1 • Oral • US • Approved
  • Qelbree
    Capsule, extended release • 200 mg/1 • Oral • US • Approved
International Brands
  • Emovit

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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