Darifenacin

Darifenacin
(IUPAC) ime
	(S)-2-[1-[2-(2,3-dihidrobenzofuran-5-il)etil] pirolidin-3-il] -2,2-difenil-acetamid
Klinički podaci
Robne marke	Enablex
AHFS/Drugs.com	Monografija
MedlinePlus	a605039
Identifikatori
CAS broj	133099-04-4
ATC kod	G04BD10
PubChem	444031
DrugBank	APRD00903
ChemSpider	392054
UNII	APG9819VLM
KEGG	D01699
ChEBI	CHEBI:391960
ChEMBL	CHEMBL1346
Hemijski podaci
Formula	C28H30N2O2
Mol. masa	426,55 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C28H30N2O2/c29-27(31)28(23-7-3-1-4-8-23,24-9-5-2-6-10-24)25-14-17-30(20-25)16-13-21-11-12-26-22(19-21)15-18-32-26/h1-12,19,25H,13-18,20H2,(H2,29,31)/t25-/m1/s1 ; Key: HXGBXQDTNZMWGS-RUZDIDTESA-N
Farmakokinetički podaci
Bioraspoloživost	15 do 19% (zavisno od doze)
Vezivanje za proteine plazme	98%
Metabolizam	Hepatički (CYP2D6 i CYP3A4)
Poluvreme eliminacije	13 do 19 sati
Izlučivanje	Renalno (60%) i bilijarno (40%)
Farmakoinformacioni podaci
Trudnoća	B3(AU) C(US)
Pravni status	POM (UK) ℞-only (SAD)
Način primene	Oralno

Darifenacin (Enablex, Emseleks) je lek koji se koristi za lečenje urinarne inkontinencije.^[6] Njega je ranije prodavao Novartis; međutim 2010. SAD prava su prodata kompaniji Warner Chilcott.^[7]

Mehanizam dejstva

Darifenacin deluje putem blokiranja M₃ muskarinskog acetilholinskog receptora, koji je primarno odgovoran za kontrakcije mišića mokraćne bešike. On time smanjuje hitnost urinacije.

Ovaj lek se ne preporučuje za upotrebu kod pacijenata sa urinarnom retencijom. Antiholinergijski agensi, kao što je Enableks, isto tako mogu da uzrokuju konstipaciju i zamagljeni vid. Toplotna iznurenost (usled umanjenog znojenja) se može javiti kad se antiholinergici koriste u toploj sredini.^[8]

Reference

↑ 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. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ 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.
↑ 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. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit
↑ 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.
↑ 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. DOI:10.1093/nar/gkr777. PMID 21948594. edit
↑ F Haab, L Stewart (2004). „Darifenacin, an M3 selective receptor antagonist, is an effective and well-tolerated once-daily treatment for overactive bladder”. European urology (Elsevier).
↑ „Enablex (darifenacin)”. Arhivirano iz originala na datum 2008-02-03. Pristupljeno 2014-04-05.
↑ „Enablex on drugs.com”. Arhivirano iz originala na datum 2014-02-10. Pristupljeno 2014-04-05.

Vanjske veze

	Portal Medicina
	Portal Hemija

Enableks Arhivirano 2008-02-03 na Wayback Machine-u

[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. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. 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. DOI:10.1186/1758-2946-2-3. PMID 20331846. 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. DOI:10.1093/nar/gkr777. PMID 21948594. edit

[6] F Haab, L Stewart (2004). „Darifenacin, an M3 selective receptor antagonist, is an effective and well-tolerated once-daily treatment for overactive bladder”. European urology (Elsevier).

[7] „Enablex (darifenacin)”. Arhivirano iz originala na datum 2008-02-03. Pristupljeno 2014-04-05.

[8] „Enablex on drugs.com”. Arhivirano iz originala na datum 2014-02-10. Pristupljeno 2014-04-05.

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