About: Zuclopenthixol     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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http://linked.open...gbank/description
  • 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. (en)
http://linked.open...generalReferences
  • # Khalifa AE: Zuclopenthixol facilitates memory retrieval in rats: possible involvement of noradrenergic and serotonergic mechanisms. Pharmacol Biochem Behav. 2003 Jul;75(4):755-62. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/12957216 # 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. 2013 Jun 15. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23771405 # 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. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/22513898 # 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. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/22718540 # 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. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/15497819 # 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. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/20175668 # http://medicaid.alabama.gov/documents/2.0_Newsroom/2.4_Procurement/2.4.3_Pharm_Support_ITB/2.4.3_Antipsychotic_Agents_Class_Review_8-10-11.pdf # http://www.mentalhealth.com/drug/p30-z03.html (en)
http://linked.open...gy/drugbank/group
  • approved (en)
  • investigational (en)
http://linked.open...drugbank/halfLife
  • 20 hours (range 12-28 hours) for the tablet form, 19 days for the depot form. (en)
http://linked.open...ugbank/indication
  • Used in the management of acute psychoses such as mania or schizophrenia. However, the use of zuclopenthixol acetate in psychiatric emergencies as an alternative to standard treatments (haloperidol, clotiapine, etc.) should be cautioned, since well executed and documented trials of zuclopenthixol acetate for this use have yet to be conducted. Zuclopenthixol acetate is not intended for long-term use. (en)
sameAs
Title
  • Zuclopenthixol (en)
adms:identifier
http://linked.open...mechanismOfAction
  • Zuclopenthixol is a typical antipsychotic neuroleptic drug of the thioxanthene class. It mainly acts by antagonism of D1 and D2 dopamine receptors. Zuclopenthixol also has high affinity for alpha1-adrenergic and 5-HT2 receptors. It has weaker histamine H1 receptor blocking activity, and even lower affinity for muscarinic cholinergic and alpha2-adrenergic receptors. (en)
http://linked.open...outeOfElimination
  • Primarily in the feces with approximately 10% in the urine. (en)
http://linked.open.../drugbank/synonym
  • Zuclopenthixolum (en)
  • Zuclopentixol (en)
  • cis-Clopenthixol (en)
http://linked.open...drugbank/toxicity
  • 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. (en)
http://linked.open...umeOfDistribution
  • 20 L/kg. (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open...nk/proteinBinding
  • 98-99% (en)
http://linked.open...ogy/drugbank/salt
  • (en)
http://linked.open...y/mesh/hasConcept
foaf:page
http://linked.open...ugbank/IUPAC-Name
http://linked.open...gy/drugbank/InChI
http://linked.open...Molecular-Formula
http://linked.open.../Molecular-Weight
http://linked.open...noisotopic-Weight
http://linked.open...y/drugbank/SMILES
http://linked.open.../Water-Solubility
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http://linked.open...nk/Polarizability
http://linked.open...bank/Refractivity
http://linked.open...atable-Bond-Count
http://linked.open...ugbank/absorption
  • 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. (en)
http://linked.open.../affectedOrganism
  • Humans and other mammals (en)
http://linked.open...casRegistryNumber
  • 53772-83-1 (en)
http://linked.open...drugbank/category
  • (en)
http://linked.open...rugbank/clearance
  • approximately 0.9 L/min. (en)
http://linked.open...gbank/containedIn
http://linked.open...k/Bioavailability
http://linked.open...bank/Ghose-Filter
http://linked.open...nk/MDDR-Like-Rule
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http://linked.open...bank/Rule-of-Five
http://linked.open...tional-IUPAC-Name
http://linked.open...strongest-acidic-
http://linked.open...-strongest-basic-
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