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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
  • Cytisine is an alkaloid that is found naturally in several plant genera such as Laburnum and Cytisus of the family Fabaceae. Recent studies have shown it to be a more effective and significantly more affordable smoking cessation treatment than nicotine replacement therapy. Also known as baptitoxine or sophorine, cytisine has been used as a smoking cessation treatment since 1964, and is relatively unknown in regions outside of central and Eastern Europe. Cytisine is a partial nicotinic acetylcholine agonist with a half-life of 4.8 hours. Recent Phase III clinical trials using Tabex (a brand of Cytisine marketed by Sopharma AD) have shown similar efficacy to varenicline, but at a fraction of the cost. (en)
http://linked.open...generalReferences
  • # Walker N, Howe C, Glover M, McRobbie H, Barnes J, Nosa V, Parag V, Bassett B, Bullen C: Cytisine versus nicotine for smoking cessation. N Engl J Med. 2014 Dec 18;371(25):2353-62. doi: 10.1056/NEJMoa1407764. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/25517706 # http://www.tabex.net/tabex-patient-use-details.php # Houlihan LM, Slater Y, Guerra DL, Peng JH, Kuo YP, Lukas RJ, Cassels BK, Bermudez I: Activity of cytisine and its brominated isosteres on recombinant human alpha7, alpha4beta2 and alpha4beta4 nicotinic acetylcholine receptors. J Neurochem. 2001 Sep;78(5):1029-43. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/11553677 # Tutka P, Zatonski W: Cytisine for the treatment of nicotine addiction: from a molecule to therapeutic efficacy. Pharmacol Rep. 2006 Nov-Dec;58(6):777-98. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17220536 # Cooper JC, Gutbrod O, Witzemann V, Methfessel C: Pharmacology of the nicotinic acetylcholine receptor from fetal rat muscle expressed in Xenopus oocytes. Eur J Pharmacol. 1996 Aug 15;309(3):287-98. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/8874153 (en)
http://linked.open...gy/drugbank/group
  • approved (en)
  • investigational (en)
http://linked.open...drugbank/halfLife
  • 4.8 hours. (en)
http://linked.open...ugbank/indication
  • Indicated for use in smoking cessation. (en)
sameAs
Title
  • Cytisine (en)
adms:identifier
http://linked.open...mechanismOfAction
  • Cytisine is a low efficacy partial agonist of ⍺4-β2 nicotinic acetylcholine receptors. These which are believed to be central to the effect of nicotine (NIC) on the reward pathway and facilitate addiction. Cytisine reduces the effects of NIC on dopamine release in the mesolimbic system when given alone, while simultaneously attenuating NIC withdrawal symptoms that accompany cessation attempts. (en)
http://linked.open.../drugbank/synonym
  • Baptitoxine (en)
  • Sophorine (en)
  • Ulexin (en)
  • (1R,5S)-1,2,3,4,5,6-Hexahydro-1,5-methano-8H-pyrido[1,2a][1,5]diazocin-8-one (en)
http://linked.open...drugbank/toxicity
  • The therapeutic index of cytisine is wide. -Large doses can interfere with breathing and cause death. From MSDS: orl-mus LD50:101 mg/kg ipr-mus LD50:8550 ug/kg ivn-mus LD50:1730 ug/kg scu-rat LD50:8750 ug/kg (en)
http://linked.open...umeOfDistribution
  • Oral: 6.2 l/kg Oral (5 mg/kg; tested in rabbits). (en)
http://linked.open...ynthesisReference
  • ORGANIC SYNTHESES, 2006, 83, 141. "Synthesis of (+)-(1R,@S,9S)-11-Methyl-7,11-Diazatricyclo[7.3.1.02.7]tridecane, a (+)sparteine surrogate," DOI: 10.15227/orgsyn.083.0141 (en)
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
http://linked.open...ogy/drugbank/logP
http://linked.open...ogy/drugbank/logS
http://linked.open...nd-Acceptor-Count
http://linked.open...-Bond-Donor-Count
http://linked.open...drugbank/InChIKey
http://linked.open...urface-Area--PSA-
http://linked.open...nk/Polarizability
http://linked.open...bank/Refractivity
http://linked.open...atable-Bond-Count
http://linked.open...casRegistryNumber
  • 485-35-8 (en)
http://linked.open...rugbank/clearance
  • Renal: 43 mL/min. (en)
http://linked.open...k/Bioavailability
http://linked.open...ank/Boiling-Point
http://linked.open...bank/Ghose-Filter
http://linked.open...nk/MDDR-Like-Rule
http://linked.open...ank/Melting-Point
http://linked.open...k/Number-of-Rings
http://linked.open...siological-Charge
http://linked.open...bank/Rule-of-Five
http://linked.open...tional-IUPAC-Name
http://linked.open...-strongest-basic-
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