Peringatan Keamanan

Dose-limiting adverse effects are sedation, parkinsonism, akathsia, and depression.
LD50 oral, mouse: 550 mg/kg

Tetrabenazine

DB04844

small molecule approved investigational

Deskripsi

A drug formerly used as an antipsychotic but now used primarily in the symptomatic treatment of various hyperkinetic disorders. It is a monoamine depletor and used as symptomatic treatment of chorea associated with Huntington's disease. FDA approved on August 15, 2008.

Struktur Molekul 2D

Berat 317.4226
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) There is interindividual variability in elimination half-life.[A39004] The elimination half-life of tetrabenazine was 10 hours following intravenous bolus administration.[A251120] The oral half-lives of its metabolites, ?-HTBZ, ?-HTBZ and 9-desmethyl-?-DHTBZ, are seven hours, five hours and 12 hours, respectively.[L42565] Following a single oral dose of 25 mg tetrabenazine, the elimination half-life was approximately 17.5 hours in subjects with hepatic impairment.[L42565]
Volume Distribusi Steady State, IV, in HD or tardive dyskinesia patients: 385L. Tetrabenazine is rapidly distributed to the brain following IV injection. The site with the highest binding is the striatum, while the lowest binding was observed in the cortex.
Klirens (Clearance) IV, 1.67 L/min in HD or tardive dyskinesia patients

Absorpsi

Following oral administration of tetrabenazine, the extent of absorption is at least 75%. After single oral doses ranging from 12.5 to 50 mg, plasma concentrations of tetrabenazine are generally below the limit of detection because of the rapid and extensive hepatic metabolism of tetrabenazine. Food does not affect the absorption of tetrabenazine. Cmax, oral = 4.8 ng/mL in HD or tardive dyskinesia patients; Tmax, oral = 69 min in HD or tardive dyskinesia patients

Metabolisme

Tetrabenazine is hepatically metabolized. Carbonyl reductase in the liver is responsible for the formation of two major active metabolites: ?-dihydrotetrabenazine (?-HTBZ) and ?-dihydrotetrabenazine (?-HTBZ). ?-HTBZ is further metabolized into 9-desmethyl-?-DHTBZ, a minor metabolite by CYP2D6 and with some contribution of CYP1A2. ?-HTBZ is metabolized to another major circulating metabolite, 9-desmethyl-?-DHTBZ, by CYP2D6. The Tmax of this metabolite is 2 hours post-administration of tetrabenazine.

Rute Eliminasi

After oral administration, tetrabenazine is extensively hepatically metabolized, and the metabolites are primarily renally eliminated (75%). Tetrabenazine is also cleared fecally (7% to 16%). Unchanged tetrabenazine has not been found in human urine. Urinary excretion of ?-HTBZ or ?-HTBZ (the major metabolites) accounted for less than 10% of the administered dose.

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Ingesting alcohol may increase the drowsiness caused by tetrabenazine.
  • 2. Take with or without food.

Interaksi Obat

783 Data
Moricizine The risk or severity of adverse effects can be increased when Moricizine is combined with Tetrabenazine.
Alimemazine The risk or severity of adverse effects can be increased when Alimemazine is combined with Tetrabenazine.
Lithium cation The risk or severity of adverse effects can be increased when Lithium cation is combined with Tetrabenazine.
Osanetant The risk or severity of adverse effects can be increased when Osanetant is combined with Tetrabenazine.
Bifeprunox The risk or severity of adverse effects can be increased when Bifeprunox is combined with Tetrabenazine.
BL-1020 The risk or severity of adverse effects can be increased when BL-1020 is combined with Tetrabenazine.
Cariprazine The risk or severity of adverse effects can be increased when Cariprazine is combined with Tetrabenazine.
Amperozide The risk or severity of adverse effects can be increased when Amperozide is combined with Tetrabenazine.
Cyamemazine The risk or severity of adverse effects can be increased when Cyamemazine is combined with Tetrabenazine.
Brexpiprazole The risk or severity of adverse effects can be increased when Brexpiprazole is combined with Tetrabenazine.
Brilaroxazine The risk or severity of adverse effects can be increased when Brilaroxazine is combined with Tetrabenazine.
Propiopromazine The risk or severity of adverse effects can be increased when Propiopromazine is combined with Tetrabenazine.
Bromperidol The risk or severity of adverse effects can be increased when Bromperidol is combined with Tetrabenazine.
Prothipendyl The risk or severity of adverse effects can be increased when Prothipendyl is combined with Tetrabenazine.
Butaperazine The risk or severity of adverse effects can be increased when Butaperazine is combined with Tetrabenazine.
Clothiapine The risk or severity of adverse effects can be increased when Clothiapine is combined with Tetrabenazine.
Chlorproethazine The risk or severity of adverse effects can be increased when Chlorproethazine is combined with Tetrabenazine.
Oxypertine The risk or severity of adverse effects can be increased when Oxypertine is combined with Tetrabenazine.
Thiazinam The risk or severity of adverse effects can be increased when Thiazinam is combined with Tetrabenazine.
Veralipride The risk or severity of adverse effects can be increased when Veralipride is combined with Tetrabenazine.
Moperone The risk or severity of adverse effects can be increased when Moperone is combined with Tetrabenazine.
Thiopropazate The risk or severity of adverse effects can be increased when Thiopropazate is combined with Tetrabenazine.
Mosapramine The risk or severity of adverse effects can be increased when Mosapramine is combined with Tetrabenazine.
Dixyrazine The risk or severity of adverse effects can be increased when Dixyrazine is combined with Tetrabenazine.
Aripiprazole lauroxil The risk or severity of adverse effects can be increased when Aripiprazole lauroxil is combined with Tetrabenazine.
Perphenazine enanthate The risk or severity of adverse effects can be increased when Perphenazine enanthate is combined with Tetrabenazine.
Levosulpiride The risk or severity of adverse effects can be increased when Levosulpiride is combined with Tetrabenazine.
Thioridazine The metabolism of Tetrabenazine can be decreased when combined with Thioridazine.
Methotrimeprazine The metabolism of Tetrabenazine can be decreased when combined with Methotrimeprazine.
Cisapride The metabolism of Tetrabenazine can be decreased when combined with Cisapride.
Paroxetine The metabolism of Tetrabenazine can be decreased when combined with Paroxetine.
Quinidine The metabolism of Tetrabenazine can be decreased when combined with Quinidine.
Cinacalcet The metabolism of Tetrabenazine can be decreased when combined with Cinacalcet.
Bupropion The metabolism of Tetrabenazine can be decreased when combined with Bupropion.
Orphenadrine The metabolism of Tetrabenazine can be decreased when combined with Orphenadrine.
Propafenone The metabolism of Tetrabenazine can be decreased when combined with Propafenone.
Halofantrine The metabolism of Tetrabenazine can be decreased when combined with Halofantrine.
Glycerol phenylbutyrate The metabolism of Tetrabenazine can be decreased when combined with Glycerol phenylbutyrate.
Dacomitinib The metabolism of Tetrabenazine can be decreased when combined with Dacomitinib.
Tranylcypromine The risk or severity of adverse effects can be increased when Tranylcypromine is combined with Tetrabenazine.
Phenelzine The risk or severity of adverse effects can be increased when Phenelzine is combined with Tetrabenazine.
Selegiline The risk or severity of adverse effects can be increased when Selegiline is combined with Tetrabenazine.
Moclobemide The risk or severity of adverse effects can be increased when Moclobemide is combined with Tetrabenazine.
Isocarboxazid The risk or severity of adverse effects can be increased when Isocarboxazid is combined with Tetrabenazine.
Rasagiline The risk or severity of adverse effects can be increased when Rasagiline is combined with Tetrabenazine.
Pargyline The risk or severity of adverse effects can be increased when Pargyline is combined with Tetrabenazine.
Minaprine The risk or severity of adverse effects can be increased when Minaprine is combined with Tetrabenazine.
Iproniazid The risk or severity of adverse effects can be increased when Iproniazid is combined with Tetrabenazine.
Nialamide The risk or severity of adverse effects can be increased when Nialamide is combined with Tetrabenazine.
Pirlindole The risk or severity of adverse effects can be increased when Pirlindole is combined with Tetrabenazine.
Toloxatone The risk or severity of adverse effects can be increased when Toloxatone is combined with Tetrabenazine.
Hydracarbazine The risk or severity of adverse effects can be increased when Hydracarbazine is combined with Tetrabenazine.
Methylene blue The risk or severity of adverse effects can be increased when Methylene blue is combined with Tetrabenazine.
Benmoxin The risk or severity of adverse effects can be increased when Benmoxin is combined with Tetrabenazine.
Mebanazine The risk or severity of adverse effects can be increased when Mebanazine is combined with Tetrabenazine.
Octamoxin The risk or severity of adverse effects can be increased when Octamoxin is combined with Tetrabenazine.
Pheniprazine The risk or severity of adverse effects can be increased when Pheniprazine is combined with Tetrabenazine.
Phenoxypropazine The risk or severity of adverse effects can be increased when Phenoxypropazine is combined with Tetrabenazine.
Pivhydrazine The risk or severity of adverse effects can be increased when Pivhydrazine is combined with Tetrabenazine.
Safrazine The risk or severity of adverse effects can be increased when Safrazine is combined with Tetrabenazine.
Caroxazone The risk or severity of adverse effects can be increased when Caroxazone is combined with Tetrabenazine.
Furazolidone The risk or severity of adverse effects can be increased when Furazolidone is combined with Tetrabenazine.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline The risk or severity of adverse effects can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Tetrabenazine.
Harmaline The risk or severity of adverse effects can be increased when Harmaline is combined with Tetrabenazine.
Brofaromine The risk or severity of adverse effects can be increased when Brofaromine is combined with Tetrabenazine.
Procaine The risk or severity of adverse effects can be increased when Procaine is combined with Tetrabenazine.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Tetrabenazine.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Tetrabenazine.
Safinamide The risk or severity of adverse effects can be increased when Safinamide is combined with Tetrabenazine.
Clorgiline The risk or severity of adverse effects can be increased when Clorgiline is combined with Tetrabenazine.
Metyrosine The risk or severity of adverse effects can be increased when Metyrosine is combined with Tetrabenazine.
Mirabegron The serum concentration of Tetrabenazine can be increased when it is combined with Mirabegron.
Metoclopramide The risk or severity of adverse effects can be increased when Metoclopramide is combined with Tetrabenazine.
Leuprolide The risk or severity of QTc prolongation can be increased when Leuprolide is combined with Tetrabenazine.
Goserelin The risk or severity of QTc prolongation can be increased when Goserelin is combined with Tetrabenazine.
Erythromycin The risk or severity of QTc prolongation can be increased when Erythromycin is combined with Tetrabenazine.
Azithromycin The risk or severity of QTc prolongation can be increased when Azithromycin is combined with Tetrabenazine.
Moxifloxacin The risk or severity of QTc prolongation can be increased when Moxifloxacin is combined with Tetrabenazine.
Sulfisoxazole The risk or severity of QTc prolongation can be increased when Sulfisoxazole is combined with Tetrabenazine.
Methadone The risk or severity of QTc prolongation can be increased when Methadone is combined with Tetrabenazine.
Diltiazem The risk or severity of QTc prolongation can be increased when Diltiazem is combined with Tetrabenazine.
Nimodipine The risk or severity of QTc prolongation can be increased when Nimodipine is combined with Tetrabenazine.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Tetrabenazine.
Ciprofloxacin The risk or severity of QTc prolongation can be increased when Ciprofloxacin is combined with Tetrabenazine.
Fluorouracil The risk or severity of QTc prolongation can be increased when Fluorouracil is combined with Tetrabenazine.
Perflutren The risk or severity of QTc prolongation can be increased when Perflutren is combined with Tetrabenazine.
Cinnarizine The risk or severity of QTc prolongation can be increased when Cinnarizine is combined with Tetrabenazine.
Atropine The risk or severity of QTc prolongation can be increased when Atropine is combined with Tetrabenazine.
Efavirenz The risk or severity of QTc prolongation can be increased when Efavirenz is combined with Tetrabenazine.
Adenosine The risk or severity of QTc prolongation can be increased when Adenosine is combined with Tetrabenazine.
Pentamidine The risk or severity of QTc prolongation can be increased when Pentamidine is combined with Tetrabenazine.
Gadobenic acid The risk or severity of QTc prolongation can be increased when Gadobenic acid is combined with Tetrabenazine.
Carbinoxamine The risk or severity of QTc prolongation can be increased when Carbinoxamine is combined with Tetrabenazine.
Dolasetron The risk or severity of QTc prolongation can be increased when Dolasetron is combined with Tetrabenazine.
Roxithromycin The risk or severity of QTc prolongation can be increased when Roxithromycin is combined with Tetrabenazine.
Nalidixic acid The risk or severity of QTc prolongation can be increased when Nalidixic acid is combined with Tetrabenazine.
Cinoxacin The risk or severity of QTc prolongation can be increased when Cinoxacin is combined with Tetrabenazine.
Loperamide The risk or severity of QTc prolongation can be increased when Loperamide is combined with Tetrabenazine.
Granisetron The risk or severity of QTc prolongation can be increased when Granisetron is combined with Tetrabenazine.
Ondansetron The risk or severity of QTc prolongation can be increased when Ondansetron is combined with Tetrabenazine.

Target Protein

Synaptic vesicular amine transporter SLC18A2
D(2) dopamine receptor DRD2

Referensi & Sumber

Synthesis reference: Michael James Rishel, Kande Kankananamalage Dayarathna Amarasinghe, Sean Richard Dinn, Bruce Fletcher Johnson, "METHOD FOR MAKING TETRABENAZINE COMPOUNDS." U.S. Patent US20080306267, issued December 11, 2008.
Artikel (PubMed)
  • PMID: 9040721
    Jankovic J, Beach J: Long-term effects of tetrabenazine in hyperkinetic movement disorders. Neurology. 1997 Feb;48(2):358-62.
  • PMID: 20869622
    Guay DR: Tetrabenazine, a monoamine-depleting drug used in the treatment of hyperkinetic movement disorders. Am J Geriatr Pharmacother. 2010 Aug;8(4):331-73. doi: 10.1016/j.amjopharm.2010.08.006.
  • PMID: 19750050
    Yero T, Rey JA: Tetrabenazine (Xenazine), An FDA-Approved Treatment Option For Huntington's Disease-Related Chorea. P T. 2008 Dec;33(12):690-4.
  • PMID: 3709613
    Roberts MS, McLean S, Millingen KS, Galloway HM: The pharmacokinetics of tetrabenazine and its hydroxy metabolite in patients treated for involuntary movement disorders. Eur J Clin Pharmacol. 1986;29(6):703-8. doi: 10.1007/BF00615962.

Contoh Produk & Brand

Produk: 36 • International brands: 1
Produk
  • Apo-tetrabenazine
    Tablet • 25 mg • Oral • Canada • Generic • Approved
  • Nitoman
    Tablet • 25 mg • Oral • Canada • Approved
  • PMS-tetrabenazine
    Tablet • 25 mg • Oral • Canada • Generic • Approved
  • Tetrabenazine
    Tablet • 12.5 mg/1 • Oral • US • Generic • Approved
  • Tetrabenazine
    Tablet • 25 mg/1 • Oral • US • Generic • Approved
  • Tetrabenazine
    Tablet • 12.5 mg/1 • Oral • US • Generic • Approved
  • Tetrabenazine
    Tablet • 25 mg/1 • Oral • US • Generic • Approved
  • Tetrabenazine
    Tablet, coated • 12.5 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 36 produk.
International Brands
  • Rubigen

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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