Silodosin

Silodosin
(IUPAC) ime
	1-(3-hidroksipropil)-5-[(2R)-({2-[2-[2-(2,2,2-trifluoroetoksi)fenoksi]etil}amino)propil]indolin-7-karboksamid
Klinički podaci
Identifikatori
CAS broj	160970-54-7
ATC kod	G04CA04
PubChem	5312125
ChemSpider	4471557
UNII	CUZ39LUY82
ChEMBL	CHEMBL24778
Hemijski podaci
Formula	C25H32F3N3O4
Mol. masa	495,534 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C25H32F3N3O4/c1-17(30-8-12-34-21-5-2-3-6-22(21)35-16-25(26,27)28)13-18-14-19-7-10-31(9-4-11-32)23(19)20(15-18)24(29)33/h2-3,5-6,14-15,17,30,32H,4,7-13,16H2,1H3,(H2,29,33)/t17-/m1/s1 ; Key: PNCPYILNMDWPEY-QGZVFWFLSA-N
Sinonimi	KAD-3213, KMD-3213
Farmakokinetički podaci
Bioraspoloživost	32%
Vezivanje za proteine plazme	97%
Metabolizam	Hepatička glukuronidacija (UGT2B7-posredovana); takođe manje CYP3A4 učešće
Poluvreme eliminacije	13±8 sata
Izlučivanje	Renalno ili fekalno
Farmakoinformacioni podaci
Trudnoća	B(US)
Pravni status	℞ Prescription only
Način primene	Oralno

Silodosin (Rapaflo, Silodiks, Rapilif, Silodal, Urief) je lek za simptomatički tretman benignog uvećanja prostate. On deluje kao antagonist α₁-adrenoceptor sa visokom selektivnošću (selektivnost za prostatu).^[5]

Farmakologija

Pošto je silodosin veoma selektivan inhibitor α_1A adrenergičkog receptora, on praktično ne uzrokuje ortostatičku hipotenziju (što je u kontrastu sa drugim α₁ blokatorima). S druge strane, visoka selektivnost uzrokuje probleme sa ejakulacijom.^[6]

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
↑ 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
↑ Yoshida M, Homma Y, Kawabe K (December 2007). „Silodosin, a novel selective alpha 1A-adrenoceptor selective antagonist for the treatment of benign prostatic hyperplasia”. Expert Opin Investig Drugs 16 (12): 1955–65. DOI:10.1517/13543784.16.12.1955. PMID 18042003.
↑ Schubert-Zsilavecz, M, Wurglics, M, Neue Arzneimittel 2008/2009

Vanjske veze

	Portal Medicina
	Portal Hemija

Watson Pharm., Inc.- Press Release Arhivirano 2006-11-10 na Wayback Machine-u
Medspace.com article Arhivirano 2008-10-14 na Wayback Machine-u
Rapaflo Official Site

[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] 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

[pmid18042003-5] Yoshida M, Homma Y, Kawabe K (December 2007). „Silodosin, a novel selective alpha 1A-adrenoceptor selective antagonist for the treatment of benign prostatic hyperplasia”. Expert Opin Investig Drugs 16 (12): 1955–65. DOI:10.1517/13543784.16.12.1955. PMID 18042003.

[6] Schubert-Zsilavecz, M, Wurglics, M, Neue Arzneimittel 2008/2009

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