Peringatan Keamanan

Although there have not been any cases of overdosage reported, the symptoms are likely to be somnolence, coma, extrapyramidal symptoms, convulsions, hypotension, shock, or hyper- or hypothermia.

Neuroleptic malignant syndrome may occur. Zuclopenthixol may potentiate anticholinergic effects of concurrent medications. Zuclopenthixol has a demonstrated antiemetic effect in animals, and may mask signs of toxicity due to other drug overdoses, or may mask symptoms of disease.

Zuclopenthixol

DB01624

small molecule approved investigational

Deskripsi

Zuclopenthixol, also known as Zuclopentixol or Zuclopenthixolum, is an antipsychotic agent. Zuclopenthixol is a thioxanthene-based neuroleptic with therapeutic actions similar to the phenothiazine antipsychotics. It is an antagonist at D1 and D2 dopamine receptors. Major brands of zuclopenthixol are Cisordinol, Acuphase, and Clopixol. This drug is a liquid. This compound belongs to the thioxanthenes. These are organic polycyclic compounds containing a thioxanthene moiety, which is an aromatic tricycle derived from xanthene by replacing the oxygen atom with a sulfur atom. Known drug targets of zuclopenthixol include 5-hydroxytryptamine receptor 2A, D(1B) dopamine receptor, D(2) dopamine receptor, D(1A) dopamine receptor, and alpha-1A adrenergic receptor. It is known that zuclopenthixol is metabolized by Cytochrome P450 2D6. Zuclopenthixol was approved for use in Canada in 2011, but is not approved for use in the United States.

Struktur Molekul 2D

Berat 400.965
Wujud liquid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 20 hours (range 12-28 hours) for the tablet form, 19 days for the depot form.
Volume Distribusi 20 L/kg.
Klirens (Clearance) approximately 0.9 L/min.

Absorpsi

Upon reaching the body water phase, the decanoate ester is slowly released from the oil depot, which is resultantly hydrolyzed to the active substance, zuclopenthixol. The decanoate ester provides a means of slow release since zuclopenthixol itself is a short-acting drug.

Metabolisme

The metabolism of zuclopenthixol is mainly by sulphoxidation, side chain N-dealkylation and glucuronic acid conjugation. The metabolites are devoid of pharmacological activity.

Rute Eliminasi

Primarily in the feces with approximately 10% in the urine.

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Acute alcohol intoxication is a contraindication for zuclopenthixol therapy.
  • 2. Take with or without food.

Interaksi Obat

1755 Data
Phenytoin The metabolism of Zuclopenthixol can be increased when combined with Phenytoin.
Fosphenytoin The metabolism of Zuclopenthixol can be increased when combined with Fosphenytoin.
Valsartan Zuclopenthixol may decrease the antihypertensive activities of Valsartan.
Ramipril Zuclopenthixol may decrease the antihypertensive activities of Ramipril.
Remikiren Zuclopenthixol may decrease the antihypertensive activities of Remikiren.
Torasemide Zuclopenthixol may decrease the antihypertensive activities of Torasemide.
Guanadrel Zuclopenthixol may decrease the antihypertensive activities of Guanadrel.
Olmesartan Zuclopenthixol may decrease the antihypertensive activities of Olmesartan.
Chlorthalidone Zuclopenthixol may decrease the antihypertensive activities of Chlorthalidone.
Nitroprusside Zuclopenthixol may decrease the antihypertensive activities of Nitroprusside.
Minoxidil Zuclopenthixol may decrease the antihypertensive activities of Minoxidil.
Bendroflumethiazide Zuclopenthixol may decrease the antihypertensive activities of Bendroflumethiazide.
Fosinopril Zuclopenthixol may decrease the antihypertensive activities of Fosinopril.
Trandolapril Zuclopenthixol may decrease the antihypertensive activities of Trandolapril.
Metolazone Zuclopenthixol may decrease the antihypertensive activities of Metolazone.
Benazepril Zuclopenthixol may decrease the antihypertensive activities of Benazepril.
Cyclothiazide Zuclopenthixol may decrease the antihypertensive activities of Cyclothiazide.
Candoxatril Zuclopenthixol may decrease the antihypertensive activities of Candoxatril.
Mecamylamine Zuclopenthixol may decrease the antihypertensive activities of Mecamylamine.
Lisinopril Zuclopenthixol may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Zuclopenthixol may decrease the antihypertensive activities of Nitroglycerin.
Hydroflumethiazide Zuclopenthixol may decrease the antihypertensive activities of Hydroflumethiazide.
Cryptenamine Zuclopenthixol may decrease the antihypertensive activities of Cryptenamine.
Perindopril Zuclopenthixol may decrease the antihypertensive activities of Perindopril.
Candesartan cilexetil Zuclopenthixol may decrease the antihypertensive activities of Candesartan cilexetil.
Eprosartan Zuclopenthixol may decrease the antihypertensive activities of Eprosartan.
Chlorothiazide Zuclopenthixol may decrease the antihypertensive activities of Chlorothiazide.
Quinapril Zuclopenthixol may decrease the antihypertensive activities of Quinapril.
Telmisartan Zuclopenthixol may decrease the antihypertensive activities of Telmisartan.
Trichlormethiazide Zuclopenthixol may decrease the antihypertensive activities of Trichlormethiazide.
Deserpidine Zuclopenthixol may decrease the antihypertensive activities of Deserpidine.
Pentolinium Zuclopenthixol may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Zuclopenthixol may decrease the antihypertensive activities of Trimethaphan.
Diazoxide Zuclopenthixol may decrease the antihypertensive activities of Diazoxide.
Epoprostenol Zuclopenthixol may decrease the antihypertensive activities of Epoprostenol.
Polythiazide Zuclopenthixol may decrease the antihypertensive activities of Polythiazide.
Cilazapril Zuclopenthixol may decrease the antihypertensive activities of Cilazapril.
Saprisartan Zuclopenthixol may decrease the antihypertensive activities of Saprisartan.
Spirapril Zuclopenthixol may decrease the antihypertensive activities of Spirapril.
Tienilic acid Zuclopenthixol may decrease the antihypertensive activities of Tienilic acid.
Diethylnorspermine Zuclopenthixol may decrease the antihypertensive activities of Diethylnorspermine.
Temocapril Zuclopenthixol may decrease the antihypertensive activities of Temocapril.
Nicorandil Zuclopenthixol may decrease the antihypertensive activities of Nicorandil.
Rauwolfia serpentina root Zuclopenthixol may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Zuclopenthixol may decrease the antihypertensive activities of Enalaprilat.
Angiotensin 1-7 Zuclopenthixol may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Zuclopenthixol may decrease the antihypertensive activities of Imidapril.
BQ-123 Zuclopenthixol may decrease the antihypertensive activities of BQ-123.
Dihydralazine Zuclopenthixol may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Zuclopenthixol may decrease the antihypertensive activities of Zofenopril.
Guanoxan Zuclopenthixol may decrease the antihypertensive activities of Guanoxan.
Delapril Zuclopenthixol may decrease the antihypertensive activities of Delapril.
Vincamine Zuclopenthixol may decrease the antihypertensive activities of Vincamine.
Linsidomine Zuclopenthixol may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Zuclopenthixol may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Zuclopenthixol may decrease the antihypertensive activities of Tolonidine.
Endralazine Zuclopenthixol may decrease the antihypertensive activities of Endralazine.
Cadralazine Zuclopenthixol may decrease the antihypertensive activities of Cadralazine.
Cyclopenthiazide Zuclopenthixol may decrease the antihypertensive activities of Cyclopenthiazide.
Bietaserpine Zuclopenthixol may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Zuclopenthixol may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Zuclopenthixol may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Zuclopenthixol may decrease the antihypertensive activities of Guanoclor.
Muzolimine Zuclopenthixol may decrease the antihypertensive activities of Muzolimine.
Xipamide Zuclopenthixol may decrease the antihypertensive activities of Xipamide.
Candesartan Zuclopenthixol may decrease the antihypertensive activities of Candesartan.
Tocopherylquinone Zuclopenthixol may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Zuclopenthixol may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Zuclopenthixol may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Zuclopenthixol may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Zuclopenthixol may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Zuclopenthixol may decrease the antihypertensive activities of Quinaprilat.
Furosemide Zuclopenthixol may decrease the antihypertensive activities of Furosemide.
Enalapril Zuclopenthixol may decrease the antihypertensive activities of Enalapril.
Captopril Zuclopenthixol may decrease the antihypertensive activities of Captopril.
Guanethidine Zuclopenthixol may decrease the antihypertensive activities of Guanethidine.
Ambrisentan Zuclopenthixol may decrease the antihypertensive activities of Ambrisentan.
Pinacidil Zuclopenthixol may decrease the antihypertensive activities of Pinacidil.
Riociguat Zuclopenthixol may decrease the antihypertensive activities of Riociguat.
Macitentan Zuclopenthixol may decrease the antihypertensive activities of Macitentan.
Aliskiren Zuclopenthixol may decrease the antihypertensive activities of Aliskiren.
Selexipag Zuclopenthixol may decrease the antihypertensive activities of Selexipag.
Eplerenone Zuclopenthixol may decrease the antihypertensive activities of Eplerenone.
Levamlodipine Zuclopenthixol may decrease the antihypertensive activities of Levamlodipine.
Buthiazide Zuclopenthixol may decrease the antihypertensive activities of Buthiazide.
Azilsartan medoxomil Zuclopenthixol may decrease the antihypertensive activities of Azilsartan medoxomil.
Buprenorphine Zuclopenthixol 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 Zuclopenthixol.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Zuclopenthixol.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Zuclopenthixol.
Hydrocodone Zuclopenthixol may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Zuclopenthixol can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Zuclopenthixol may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Zuclopenthixol may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Zuclopenthixol.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Zuclopenthixol.
Orphenadrine Zuclopenthixol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Zuclopenthixol may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Zuclopenthixol.
Rotigotine Zuclopenthixol may increase the sedative activities of Rotigotine.

Target Protein

D(1A) dopamine receptor DRD1
D(1B) dopamine receptor DRD5
D(2) dopamine receptor DRD2
Alpha-1A adrenergic receptor ADRA1A
Alpha-2A adrenergic receptor ADRA2A
5-hydroxytryptamine receptor 2A HTR2A
Histamine H1 receptor HRH1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 12957216
    Khalifa AE: Zuclopenthixol facilitates memory retrieval in rats: possible involvement of noradrenergic and serotonergic mechanisms. Pharmacol Biochem Behav. 2003 Jul;75(4):755-62.
  • PMID: 23771405
    Fond G, Macgregor A, Tamouza R, Hamdani N, Meary A, Leboyer M, Dubremetz JF: Comparative analysis of anti-toxoplasmic activity of antipsychotic drugs and valproate. Eur Arch Psychiatry Clin Neurosci. 2014 Mar;264(2):179-83. doi: 10.1007/s00406-013-0413-4. Epub 2013 Jun 15.
  • PMID: 22513898
    Jayakody K, Gibson RC, Kumar A, Gunadasa S: Zuclopenthixol acetate for acute schizophrenia and similar serious mental illnesses. Cochrane Database Syst Rev. 2012 Apr 18;4:CD000525. doi: 10.1002/14651858.CD000525.pub3.
  • PMID: 22718540
    Nielsen MK, Johansen SS: Simultaneous determination of 25 common pharmaceuticals in whole blood using ultra-performance liquid chromatography-tandem mass spectrometry. J Anal Toxicol. 2012 Sep;36(7):497-506. doi: 10.1093/jat/bks054. Epub 2012 Jun 19.
  • PMID: 15497819
    Khalifa AE: Pro-oxidant activity of zuclopenthixol in vivo: differential effect of the drug on brain oxidative status of scopolamine-treated rats. Hum Exp Toxicol. 2004 Aug;23(9):439-45.
  • PMID: 20175668
    Hood S, Orr K, Bennett L, Davies S: Severe laryngeal dystonia in a patient receiving zuclopenthixol "Acuphase" and fluoxetine. Australas Psychiatry. 2010 Apr;18(2):174-6. doi: 10.3109/10398560903473686.
Link

Contoh Produk & Brand

Produk: 12 • International brands: 4
Produk
  • Clopixol - Tab 10mg
    Tablet • 10 mg / tab • Oral • Canada • Approved
  • Clopixol - Tab 25mg
    Tablet • 25 mg / tab • Oral • Canada • Approved
  • Clopixol - Tab 40mg
    Tablet • 40 mg / tab • Oral • Canada • Approved
  • Clopixol Acuphase - Liq Im 50mg/ml
    Liquid • 50 mg / mL • Intramuscular • Canada • Approved
  • Clopixol Depot - Liq Im 200mg/ml
    Liquid • 200 mg / mL • Intramuscular • Canada • Approved
  • Clopixol Depot - Liq Im 500mg/ml
    Liquid • 500 mg / mL • Intramuscular • Canada • Approved
  • Clopixol Depot 200mg/ml
    Solution • 200 mg / mL • Intramuscular • Canada • Approved
  • Clopixol Depot 500mg/ml
    Liquid • 500 mg / mL • Intramuscular • Canada • Approved
Menampilkan 8 dari 12 produk.
International Brands
  • Acuphase — H. Lundbeck A/S
  • Ciatyl-Z — Bayer Vital
  • Cisordinol — H. Lundbeck A/S
  • Clopixol — H. Lundbeck A/S

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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