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Klomipramin (Anafranil) je triciklični antidepresiv (TCA). On je razvijen tokom 1960-tih i od tog vremena je u kliničkoj upotrebi širom sveta.[2][3][4][5]

Klomipramin
Clomipramine.svg
IUPAC ime
3-(3-hloro-10,11-dihidro-5H-dibenzo[b,f]azepin-5-il)-N,N-dimetilpropan-1-amin
Klinički podaci
Prodajno imeAnafranil
Drugs.comMonografija
MedlinePlusa697002
Kategorija trudnoće
Način primeneOralno, IM, IV
Pravni status
Pravni status
  • ℞ (Prescription only)
Farmakokinetički podaci
BioraspoloživostOralno ~50%
MetabolizamHepatički
Poluvreme eliminacijeKlomipramin ~35 sata
Desmetilklomipramin (glavni aktivni metabolit) ~50 sata
IzlučivanjeRenalno
Identifikatori
CAS broj303-49-1 ДаY
ATC kodN06AA04 (WHO)
PubChemCID 2801
IUPHAR/BPS2398
DrugBankDB01242 ДаY
ChemSpider2699 ДаY
UNIINUV44L116D ДаY
KEGGD07727 ДаY
ChEBICHEBI:47780 ДаY
ChEMBLCHEMBL415 ДаY
Hemijski podaci
FormulaC19H23ClN2
Molarna masa314,9 g/mol

FarmakologijaУреди

Klomipramin je blokator sledećih transportera:[6]

On je antagonist/inverzni agonist sledećih receptora:[6][7][8][9]

Aktivni metabolit klomipramina, desmetilklomipramin ispoljava sledeći afinitet:

Vidi jošУреди

ReferenceУреди

  1. ^ DailyMed: About DailyMed
  2. ^ Lemke, T.L., Williams, D.A., Roche, V.T., & Zito, S.W., 2012. Foye's Principles of Medicinal Chemistry. 7th ed. Baltimore, MD: Lippincott Williams & Wilkins, p. 605.
  3. ^ Healy, D. (2004). Let them eat Prozac: The unhealthy relationship between the pharmaceutical industry and depression. New York: New York University Press, p. 23.
  4. ^ Beaumont, G., & Healy, D. (1993). The place of clomipramine in the development of psychopharmacology. Journal of Psychopharmacology, 7, 383–393.
  5. ^ Pichot, P. (1996). The discovery of chlorpromazine and the place of psychopharmacology in the history of psychiatry. The Psychopharmacologists (Vol. 1, pp. 1–21). London, England: Chapman & Hall.
  6. 6,0 6,1 Millan MJ; Gobert A; Lejeune F; et al. (2001). „S33005, a novel ligand at both serotonin and norepinephrine transporters: I. Receptor binding, electrophysiological, and neurochemical profile in comparison with venlafaxine, reboxetine, citalopram, and clomipramine”. The Journal of Pharmacology and Experimental Therapeutics. 298 (2): 565—80. PMID 11454918. 
  7. ^ Monsma FJ, Shen Y, Ward RP, Hamblin MW, Sibley DR (1993). „Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs”. Molecular Pharmacology. 43 (3): 320—7. PMID 7680751. 
  8. ^ Ruat M; Traiffort E; Leurs R; et al. (1993). „Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation”. Proceedings of the National Academy of Sciences of the United States of America. 90 (18): 8547—51. PMC 47394 . PMID 8397408. doi:10.1073/pnas.90.18.8547. 
  9. ^ Toll L; Berzetei-Gurske IP; Polgar WE; et al. (1998). „Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications”. NIDA Research Monograph. 178: 440—66. PMID 9686407. 
  10. ^ P K Gillman (2007). „Tricyclic antidepressant pharmacology and therapeutic drug interactions updated”. Br J Pharmacol. 151 (6): 737—748. PMC 2014120 . PMID 17471183. doi:10.1038/sj.bjp.0707253. 
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