Amoksapin

Из Википедије, слободне енциклопедије
Jump to navigation Jump to search
Amoksapin
Amoxapine.svg
IUPAC ime
2-hloro-11-(piperazin-1-il)dibenzo[b,f][1,4]oksazepin
Klinički podaci
Prodajno ime Asendin
Drugs.com Monografija
MedlinePlus a682202
Kategorija trudnoće
  • US: C (Mogući rizik)
Način primene Oralnot
Pravni status
Pravni status
Farmakokinetički podaci
Bioraspoloživost ?
Vezivanje proteina 90%[1]
Metabolizam Hepatički (citohrom P450)
Poluvreme eliminacije 8-10 sata (30 sata za glavne metabolite)[1]
Izlučivanje Renal
Identifikatori
CAS broj 14028-44-5 ДаY
ATC kod N06AA17 (WHO)
PubChem CID 2170
IUPHAR/BPS 201
DrugBank DB00543 ДаY
ChemSpider 2085 ДаY
UNII R63VQ857OT ДаY
KEGG D00228 ДаY
ChEBI CHEBI:2675 ДаY
ChEMBL CHEMBL1113 ДаY
Hemijski podaci
Formula C17H16ClN3O
Molarna masa 313,781 g/mol

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[уреди]

Amoksapin ispoljava mnoštvo farmakoloških efekata. On je umeren i jak inhibitor preuzimanja serotonina i norepinefrina, respektivno,[2] i vezuje se za 5-HT2A,[3] 5-HT2B,[4] 5-HT2C,[3] 5-HT3,[5] 5-HT6,[6] 5-HT7,[6] D2,[7] α1-adrenergički,[7] D3[8], D4,[8] i H1 receptor[7] 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,[5] 5-HT1B,[5] D1,[9] α2-adrenergički,[7] H4,[10] mACh,[7] i GABAA receptor,[9] i nema afiniteta za β-adrenergičke receptore ili za alosterna benzodiazepinska mesta na GABAA receptoru.[9]

Reference[уреди]

  1. 1,0 1,1 Kinney JL, Evans RL (1982). „Evaluation of amoxapine”. Clinical Pharmacy. 1 (5): 417—24. PMID 6764165. 
  2. ^ Tatsumi M, Groshan K, Blakely RD, Richelson E (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. 
  3. 3,0 3,1 Pälvimäki EP; Roth BL; Majasuo H; et al. (1996). „Interactions of selective serotonin reuptake inhibitors with the serotonin 5-HT2c receptor”. Psychopharmacology. 126 (3): 234—40. PMID 8876023. doi:10.1007/BF02246453. 
  4. ^ Glusa E, Pertz HH (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 1572101Слободан приступ. PMID 10821800. doi:10.1038/sj.bjp.0703341. 
  5. 5,0 5,1 5,2 Gozlan H, Saddiki-Traki F, Merahi N, Laguzzi R, Hamon M (1991). „[Preclinical pharmacology of amoxapine and amitriptyline. Implications of serotoninergic and opiodergic systems in their central effect in rats]”. L'Encéphale (на језику: French). 17 Spec No 3: 415—22. PMID 1666997. 
  6. 6,0 6,1 Roth BL; Craigo SC; Choudhary MS; et al. (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. 
  7. 7,0 7,1 7,2 7,3 7,4 Richelson E, Nelson A (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. 
  8. 8,0 8,1 Burstein ES; Ma J; Wong S; et al. (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. 
  9. 9,0 9,1 9,2 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 (на језику: Chinese). 25 (12): 881—5. PMID 1966571. 
  10. ^ Lim HD, van Rijn RM, Ling P, Bakker RA, Thurmond RL, Leurs R (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. 

Vidi još[уреди]

Spoljašnje veze[уреди]

Star of life.svgMolimo Vas, obratite pažnju na važno upozorenje
u vezi sa temama iz oblasti medicine (zdravlja).