Peringatan Keamanan

A study performed in monkeys self-administering vanoxerine suggests that the self-administration of this drug in humans may develop behaviorally toxic effects.A248585

Vanoxerine

DB03701

small molecule investigational

Deskripsi

Vanoxerine is a highly selective dopamine transporter antagonist. It was synthesized in the late 1970s and developed as a potential treatment for depression.A19824 Vanoxerine was later evaluated as a potential treatment for cocaine addiction due to its ability to block dopamine reuptake with a slower dissociation rate than cocaine.A37914 Although several studies have suggested that the profile of vanoxerine is safer than that of cocaine,A19824,A248550 other studies have found that vanoxerine has at least moderate potential to be abused by humans.A248585 More recently, vanoxerine was tested as a potential anti-arrhythmic and anti-atrial fibrillatory agent due to its ability to block the hKV11.1 (hERG) cardiac potassium channel.A248555 Vanoxerine is an investigational drug and has not been approved for therapeutic use.

Struktur Molekul 2D

Berat 450.574
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 vanoxerine was 53.5 h at 75 mg/day and 66 h at 125 mg/day.[A248580]
Volume Distribusi Vanoxerine is capable of crossing the blood-brain barrier and distributing to several organs such as fat tissue, lungs, liver and the gastrointestinal tract.[A248580] Vanoxerine has a large volume of distribution.[A248580]
Klirens (Clearance) At 25, 75 and 125 mg/day, vanoxerine had a corresponding oral clearance of 660, 478 and 250 L/h.

Absorpsi

At doses of 25, 75 or 125 mg, vanoxerine had a corresponding Cmax of 17.9, 81.1 and 236.5 nmol/L and a corresponding AUC of 81, 365 and 1116 h?nmol/L when given orally to healthy male volunteers (n=14).A248580 In this same set of subjects, tmax was reached at 0.91, 0.93 and 1.13 h at oral doses of 25, 75 or 125 mg, respectively. The oral bioavailability of this drug depends on food intake. Compared with those fasting, the bioavailability of vanoxerine in volunteers taking a low-fat and a high-fat meal was 76% and 255% higher, respectively.A248580

Metabolisme

In vitro studies suggest that vanoxerine is mostly metabolized by CYP3A4. CYP2C8 and CYP2E1 may also contribute to the metabolism of this drug.A248555 CYP3A4 selective-inhibitors may interact with vanoxerine.A248555

Rute Eliminasi

The majority of vanoxerine is excreted in urine, bile and feces.L41825

Interaksi Obat

107 Data
Pitolisant The serum concentration of Vanoxerine can be decreased when it is combined with Pitolisant.
Metreleptin The metabolism of Vanoxerine can be increased when combined with Metreleptin.
Solriamfetol The risk or severity of adverse effects can be increased when Solriamfetol is combined with Vanoxerine.
Cenobamate The serum concentration of Vanoxerine can be decreased when it is combined with Cenobamate.
Ritonavir The serum concentration of Vanoxerine can be increased when it is combined with Ritonavir.
Haloperidol The serum concentration of Haloperidol can be increased when it is combined with Vanoxerine.
Tucatinib The metabolism of Tucatinib can be decreased when combined with Vanoxerine.
Abametapir The serum concentration of Vanoxerine can be increased when it is combined with Abametapir.
Satralizumab The serum concentration of Vanoxerine can be decreased when it is combined with Satralizumab.
Sotorasib The serum concentration of Vanoxerine can be decreased when it is combined with Sotorasib.
Cyclosporine The metabolism of Vanoxerine can be decreased when combined with Cyclosporine.
Fluvoxamine The metabolism of Vanoxerine can be decreased when combined with Fluvoxamine.
Fluconazole The metabolism of Vanoxerine can be decreased when combined with Fluconazole.
Erythromycin The serum concentration of Vanoxerine can be increased when it is combined with Erythromycin.
Ziprasidone The metabolism of Vanoxerine can be decreased when combined with Ziprasidone.
Isradipine The metabolism of Vanoxerine can be decreased when combined with Isradipine.
Diltiazem The metabolism of Vanoxerine can be decreased when combined with Diltiazem.
Clozapine The metabolism of Vanoxerine can be decreased when combined with Clozapine.
Ciprofloxacin The metabolism of Vanoxerine can be decreased when combined with Ciprofloxacin.
Nicardipine The metabolism of Vanoxerine can be decreased when combined with Nicardipine.
Verapamil The metabolism of Vanoxerine can be decreased when combined with Verapamil.
Aprepitant The metabolism of Vanoxerine can be decreased when combined with Aprepitant.
Isoniazid The metabolism of Vanoxerine can be decreased when combined with Isoniazid.
Primaquine The metabolism of Vanoxerine can be decreased when combined with Primaquine.
Miconazole The metabolism of Vanoxerine can be decreased when combined with Miconazole.
Fusidic acid The metabolism of Vanoxerine can be decreased when combined with Fusidic acid.
Zimelidine The metabolism of Vanoxerine can be decreased when combined with Zimelidine.
Dronedarone The metabolism of Vanoxerine can be decreased when combined with Dronedarone.
Milnacipran The metabolism of Vanoxerine can be decreased when combined with Milnacipran.
Simeprevir The metabolism of Vanoxerine can be decreased when combined with Simeprevir.
Isavuconazonium The metabolism of Vanoxerine can be decreased when combined with Isavuconazonium.
Desvenlafaxine The metabolism of Vanoxerine can be decreased when combined with Desvenlafaxine.
Nilvadipine The metabolism of Vanoxerine can be decreased when combined with Nilvadipine.
Seproxetine The metabolism of Vanoxerine can be decreased when combined with Seproxetine.
Linagliptin The metabolism of Vanoxerine can be decreased when combined with Linagliptin.
Indalpine The metabolism of Vanoxerine can be decreased when combined with Indalpine.
Netupitant The metabolism of Vanoxerine can be decreased when combined with Netupitant.
Barnidipine The metabolism of Vanoxerine can be decreased when combined with Barnidipine.
Benidipine The metabolism of Vanoxerine can be decreased when combined with Benidipine.
Venetoclax The metabolism of Vanoxerine can be decreased when combined with Venetoclax.
Isavuconazole The metabolism of Vanoxerine can be decreased when combined with Isavuconazole.
Fosnetupitant The metabolism of Vanoxerine can be decreased when combined with Fosnetupitant.
Berotralstat The metabolism of Vanoxerine can be decreased when combined with Berotralstat.
Midostaurin The metabolism of Vanoxerine can be decreased when combined with Midostaurin.
Voriconazole The metabolism of Vanoxerine can be decreased when combined with Voriconazole.
Danazol The metabolism of Vanoxerine can be decreased when combined with Danazol.
Nelfinavir The metabolism of Vanoxerine can be decreased when combined with Nelfinavir.
Indinavir The metabolism of Vanoxerine can be decreased when combined with Indinavir.
Terfenadine The metabolism of Vanoxerine can be decreased when combined with Terfenadine.
Efavirenz The metabolism of Vanoxerine can be decreased when combined with Efavirenz.
Ergotamine The metabolism of Vanoxerine can be decreased when combined with Ergotamine.
Amprenavir The metabolism of Vanoxerine can be decreased when combined with Amprenavir.
Delavirdine The metabolism of Vanoxerine can be decreased when combined with Delavirdine.
Methimazole The metabolism of Vanoxerine can be decreased when combined with Methimazole.
Conivaptan The metabolism of Vanoxerine can be decreased when combined with Conivaptan.
Tipranavir The metabolism of Vanoxerine can be decreased when combined with Tipranavir.
Telithromycin The metabolism of Vanoxerine can be decreased when combined with Telithromycin.
Ketoconazole The metabolism of Vanoxerine can be decreased when combined with Ketoconazole.
Atazanavir The metabolism of Vanoxerine can be decreased when combined with Atazanavir.
Amiodarone The metabolism of Vanoxerine can be decreased when combined with Amiodarone.
Nefazodone The metabolism of Vanoxerine can be decreased when combined with Nefazodone.
Itraconazole The metabolism of Vanoxerine can be decreased when combined with Itraconazole.
Clarithromycin The metabolism of Vanoxerine can be decreased when combined with Clarithromycin.
Saquinavir The metabolism of Vanoxerine can be decreased when combined with Saquinavir.
Posaconazole The metabolism of Vanoxerine can be decreased when combined with Posaconazole.
Darunavir The metabolism of Vanoxerine can be decreased when combined with Darunavir.
Lopinavir The metabolism of Vanoxerine can be decreased when combined with Lopinavir.
Ditiocarb The metabolism of Vanoxerine can be decreased when combined with Ditiocarb.
Nilotinib The metabolism of Vanoxerine can be decreased when combined with Nilotinib.
Telaprevir The metabolism of Vanoxerine can be decreased when combined with Telaprevir.
Lonafarnib The metabolism of Vanoxerine can be decreased when combined with Lonafarnib.
Boceprevir The metabolism of Vanoxerine can be decreased when combined with Boceprevir.
Elvitegravir The metabolism of Vanoxerine can be decreased when combined with Elvitegravir.
Stiripentol The metabolism of Vanoxerine can be decreased when combined with Stiripentol.
Ribociclib The metabolism of Vanoxerine can be decreased when combined with Ribociclib.
Danoprevir The metabolism of Vanoxerine can be decreased when combined with Danoprevir.
Troleandomycin The metabolism of Vanoxerine can be decreased when combined with Troleandomycin.
Phenytoin The metabolism of Vanoxerine can be increased when combined with Phenytoin.
Pentobarbital The metabolism of Vanoxerine can be increased when combined with Pentobarbital.
Carbamazepine The metabolism of Vanoxerine can be increased when combined with Carbamazepine.
Mitotane The metabolism of Vanoxerine can be increased when combined with Mitotane.
Primidone The metabolism of Vanoxerine can be increased when combined with Primidone.
Rifampin The metabolism of Vanoxerine can be increased when combined with Rifampicin.
Phenobarbital The metabolism of Vanoxerine can be increased when combined with Phenobarbital.
Dexamethasone The metabolism of Vanoxerine can be increased when combined with Dexamethasone.
Fosphenytoin The metabolism of Vanoxerine can be increased when combined with Fosphenytoin.
St. John's Wort The metabolism of Vanoxerine can be increased when combined with St. John's Wort.
Enzalutamide The serum concentration of Vanoxerine can be decreased when it is combined with Enzalutamide.
Lumacaftor The metabolism of Vanoxerine can be increased when combined with Lumacaftor.
Apalutamide The serum concentration of Vanoxerine can be decreased when it is combined with Apalutamide.
Rifapentine The metabolism of Vanoxerine can be increased when combined with Rifapentine.
Curcumin The metabolism of Vanoxerine can be decreased when combined with Curcumin.
Somatrogon The metabolism of Vanoxerine can be increased when combined with Somatrogon.
Levoketoconazole The metabolism of Vanoxerine can be decreased when combined with Levoketoconazole.
Mavacamten The serum concentration of Vanoxerine can be decreased when it is combined with Mavacamten.
Viloxazine The metabolism of Vanoxerine can be decreased when combined with Viloxazine.
Ivosidenib The metabolism of Vanoxerine can be increased when combined with Ivosidenib.
Dabrafenib The serum concentration of Vanoxerine can be decreased when it is combined with Dabrafenib.
Telotristat ethyl The serum concentration of Vanoxerine can be decreased when it is combined with Telotristat ethyl.
Avanafil The serum concentration of Avanafil can be increased when it is combined with Vanoxerine.

Target Protein

Sodium-dependent dopamine transporter SLC6A3
HERG human cardiac K+ channel KCNH2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 11249581
    Preti A: Vanoxerine National Institute on Drug Abuse. Curr Opin Investig Drugs. 2000 Oct;1(2):241-51.
  • PMID: 2150527
    Sogaard U, Michalow J, Butler B, Lund Laursen A, Ingersen SH, Skrumsager BK, Rafaelsen OJ: A tolerance study of single and multiple dosing of the selective dopamine uptake inhibitor GBR 12909 in healthy subjects. Int Clin Psychopharmacol. 1990 Oct;5(4):237-51. doi: 10.1097/00004850-199010000-00001.
  • PMID: 17897630
    Rothman RB, Baumann MH, Prisinzano TE, Newman AH: Dopamine transport inhibitors based on GBR12909 and benztropine as potential medications to treat cocaine addiction. Biochem Pharmacol. 2008 Jan 1;75(1):2-16. doi: 10.1016/j.bcp.2007.08.007. Epub 2007 Aug 9.
  • PMID: 19817928
    Lacerda AE, Kuryshev YA, Yan GX, Waldo AL, Brown AM: Vanoxerine: cellular mechanism of a new antiarrhythmic. J Cardiovasc Electrophysiol. 2010 Mar;21(3):301-10. doi: 10.1111/j.1540-8167.2009.01623.x. Epub 2009 Oct 8.
  • PMID: 26616666
    Obejero-Paz CA, Bruening-Wright A, Kramer J, Hawryluk P, Tatalovic M, Dittrich HC, Brown AM: Quantitative Profiling of the Effects of Vanoxerine on Human Cardiac Ion Channels and its Application to Cardiac Risk. Sci Rep. 2015 Nov 30;5:17623. doi: 10.1038/srep17623.
  • PMID: 33074476
    Hagiwara-Nagasawa M, Kambayashi R, Goto A, Nunoi Y, Izumi-Nakaseko H, Takei Y, Matsumoto A, Sugiyama A: Cardiohemodynamic and Arrhythmogenic Effects of the Anti-Atrial Fibrillatory Compound Vanoxerine in Halothane-Anesthetized Dogs. Cardiovasc Toxicol. 2021 Mar;21(3):206-215. doi: 10.1007/s12012-020-09612-3. Epub 2020 Oct 19.
  • PMID: 25684233
    Dittrich HC, Feld GK, Bahnson TD, Camm AJ, Golitsyn S, Katz A, Koontz JI, Kowey PR, Waldo AL, Brown AM: COR-ART: A multicenter, randomized, double-blind, placebo-controlled dose-ranging study to evaluate single oral doses of vanoxerine for conversion of recent-onset atrial fibrillation or flutter to normal sinus rhythm. Heart Rhythm. 2015 Jun;12(6):1105-12. doi: 10.1016/j.hrthm.2015.02.014. Epub 2015 Feb 12.
  • PMID: 8289134
    Ingwersen SH, Snel S, Mant TG, Edwards D: Nonlinear multiple-dose pharmacokinetics of the dopamine reuptake inhibitor vanoxerine. J Pharm Sci. 1993 Nov;82(11):1164-6. doi: 10.1002/jps.2600821120.
Menampilkan 8 dari 9 artikel.

Contoh Produk & Brand

Produk: 0 • International brands: 0
Belum ada data produk/brand untuk obat ini pada database. Jalankan import DrugBank untuk mengisi field produk/brand.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul