Amoksapin

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Amoksapin
(IUPAC) ime
2-hloro-11-(piperazin-1-il)dibenzo[b,f][1,4]oksazepin
Klinički podaci
Robne marke Asendin
AHFS/Drugs.com Monografija
MedlinePlus a682202
Identifikatori
CAS broj 14028-44-5
ATC kod N06AA17
PubChem[1][2] 2170
DrugBank DB00543
ChemSpider[3] 2085
UNII R63VQ857OT YesY
KEGG[4] D00228 YesY
ChEBI CHEBI:2675 YesY
ChEMBL[5] CHEMBL1113 YesY
Hemijski podaci
Formula C17H16ClN3O 
Mol. masa 313,781 g/mol
SMILES eMolekuli & PubHem
Farmakokinetički podaci
Bioraspoloživost  ?
Vezivanje za proteine plazme 90%[6]
Metabolizam Hepatički (citohrom P450)
Poluvreme eliminacije 8-10 sata (30 sata za glavne metabolite)[6]
Izlučivanje Renal
Farmakoinformacioni podaci
Trudnoća C(US)
Pravni status -only (SAD)
Način primene Oralnot

Amoksapin (Amokisan, Asendin, Asendis, Defanil, Demoloks, Moksadil) je tetraciklični antidepresiv iz dibenzoksazepinske familije, mada se on često klasifikuje kao sekundarni aminski triciklični antidepresiv. On je N-demetilisani metabolit Loksapina.

Farmakologija[uredi - уреди | uredi izvor]

Amoksapin ispoljava mnoštvo farmakoloških efekata. On je umeren i jak inhibitor preuzimanja serotonina i norepinefrina, respektivno,[7] i vezuje se za 5-HT2A,[8] 5-HT2B,[9] 5-HT2C,[8] 5-HT3,[10] 5-HT6,[11] 5-HT7,[11] D2,[12] α1-adrenergički,[12] D3[13], D4,[13] i H1 receptor[12] sa promenljivim ali značajnim afinitetom, na njijima deluje kao antagonist (ili inverzni agonist u zavisnosti od receptora) na svim aktivnim mestima. On ima slab i zanemarljiv afinitet za dopaminski transporter i 5-HT1A,[10] 5-HT1B,[10] D1,[14] α2-adrenergički,[12] H4,[15] mACh,[12] i GABAA receptor,[14] i nema afiniteta za β-adrenergičke receptore ili za alosterna benzodiazepinska mesta na GABAA receptoru.[14]

Reference[uredi - уреди | uredi izvor]

  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). "PubChem as a public resource for drug discovery.". Drug Discov Today 15 (23-24): 1052–7. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). "Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities". Annual Reports in Computational Chemistry 4: 217–241. doi:10.1016/S1574-1400(08)00012-1. 
  3. Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). "Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining". J Cheminform 2 (1): 3. PMID 20331846. doi:10.1186/1758-2946-2-3.  edit
  4. Joanne Wixon, Douglas Kell (2000). "Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG". Yeast 17 (1): 48–55. doi:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H. 
  5. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). "ChEMBL: a large-scale bioactivity database for drug discovery". Nucleic Acids Res 40 (Database issue): D1100–7. PMID 21948594. doi:10.1093/nar/gkr777.  edit
  6. 6,0 6,1 Kinney JL, Evans RL (1982). "Evaluation of amoxapine". Clinical Pharmacy 1 (5): 417–24. PMID 6764165. 
  7. Tatsumi M, Groshan K, Blakely RD, Richelson E (December 1997). "Pharmacological profile of antidepressants and related compounds at human monoamine transporters". European Journal of Pharmacology 340 (2–3): 249–58. PMID 9537821. doi:10.1016/S0014-2999(97)01393-9. 
  8. 8,0 8,1 Pälvimäki EP, Roth BL, Majasuo H et al. (August 1996). "Interactions of selective serotonin reuptake inhibitors with the serotonin 5-HT2c receptor". Psychopharmacology 126 (3): 234–40. PMID 8876023. doi:10.1007/BF02246453. 
  9. Glusa E, Pertz HH (June 2000). "Further evidence that 5-HT-induced relaxation of pig pulmonary artery is mediated by endothelial 5-HT2B receptors". British Journal of Pharmacology 130 (3): 692–8. PMC 1572101. PMID 10821800. doi:10.1038/sj.bjp.0703341. 
  10. 10,0 10,1 10,2 Gozlan H, Saddiki-Traki F, Merahi N, Laguzzi R, Hamon M (December 1991). "[Preclinical pharmacology of amoxapine and amitriptyline. Implications of serotoninergic and opiodergic systems in their central effect in rats]". L'Encéphale (in French). 17 Spec No 3: 415–22. PMID 1666997. 
  11. 11,0 11,1 Roth BL, Craigo SC, Choudhary MS et al. (March 1994). "Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors". The Journal of Pharmacology and Experimental Therapeutics 268 (3): 1403–10. PMID 7908055. 
  12. 12,0 12,1 12,2 12,3 12,4 Richelson E, Nelson A (July 1984). "Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro". The Journal of Pharmacology and Experimental Therapeutics 230 (1): 94–102. PMID 6086881. 
  13. 13,0 13,1 Burstein ES, Ma J, Wong S et al. (December 2005). "Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonist". The Journal of Pharmacology and Experimental Therapeutics 315 (3): 1278–87. PMID 16135699. doi:10.1124/jpet.105.092155. 
  14. 14,0 14,1 14,2 Wei HB, Niu XY (1990). "[Comparison of the affinities of amoxapine and loxapine for various receptors in rat brain and the receptor down-regulation after chronic administration]". Yao Xue Xue Bao = Acta Pharmaceutica Sinica (in Chinese) 25 (12): 881–5. PMID 1966571. 
  15. Lim HD, van Rijn RM, Ling P, Bakker RA, Thurmond RL, Leurs R (September 2005). "Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist". The Journal of Pharmacology and Experimental Therapeutics 314 (3): 1310–21. PMID 15947036. doi:10.1124/jpet.105.087965. 

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