Doksazosin

Doksazosin
(IUPAC) ime
	(RS)-24-[(2,3-dihidro-1,4-benzodioksin-2-il)karbonil]piperazin-1-il6,7-dimetoksihinazolin-4-amin
Klinički podaci
Robne marke	Kardura
AHFS/Drugs.com	Monografija
MedlinePlus	a693045
Identifikatori
CAS broj	74191-85-8
ATC kod	C02CA04
PubChem	3157
DrugBank	DB00590
ChemSpider	3045
UNII	NW1291F1W8
KEGG	D07874
ChEBI	CHEBI:4708
ChEMBL	CHEMBL707
Hemijski podaci
Formula	C23H25N5O5
Mol. masa	451,475 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C23H25N5O5/c1-30-18-11-14-15(12-19(18)31-2)25-23(26-21(14)24)28-9-7-27(8-10-28)22(29)20-13-32-16-5-3-4-6-17(16)33-20/h3-6,11-12,20H,7-10,13H2,1-2H3,(H2,24,25,26) ; Key: RUZYUOTYCVRMRZ-UHFFFAOYSA-N
Farmakokinetički podaci
Bioraspoloživost	65%
Vezivanje za proteine plazme	98%
Metabolizam	Hepatički
Poluvreme eliminacije	22 sata
Farmakoinformacioni podaci
Trudnoća	?
Pravni status	℞ Prescription only
Način primene	oralno

Doksazosin mesilat, hinazolinsko jedinjenje koje Pfizer prodaje pod imenima Kardura i Karduran, je α1a-selektivni alfa blokator koji se koristi za tretiranje visokog krvnog pritiska i urinarne retencije vezane za benigno uvećanje prostate (BPH).

On je alfa blokator koji inhibira vezivanje norepinefrina (oslobođenog iz simpatetičkih nevnih terminala) za alfa-1 receptore na membrani vaskularnih ćelija glatkih mišića. Primarni efekat ove inhibicije je relaksirani vaskularni ton mišića (vazodilatacija), čime se smanjuje periferni vaskularni otpor, i to dovodi od umanjenja krvnog pritiska.

Efikasnost

Marta 2000, ALLHAT studija je zaustavila svoja ispitivanja, jer je doksazosin bio manje efektivan od jednostavnih diuretika, i zato što su pacijenti imali 25% viši nivo kardiovaskularnih bolesti i dvaput viši nivo kongestivnog zatajenja srca od pacijenata na diureticima.^[6] Pfizer je lansirao sofisticiranu kampanju kontrole štete početkom 2000, tako da prodaja u velikoj meri nije bila umanjena, uprkos rezultata studije.^[7]

Nedavne studije su ustanovile da je doksazosin delotvoran u treatiranju erektilalne disfunkcije (ED).^[8] Takođe je pokazano da je doksazosin u izvesnoj meri efektivan u tretiranju hroničnog epididimitisa.^[9]

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
↑ Piller LB, Davis BR, Cutler JA, et al. (November 2002). „Validation of Heart Failure Events in the Antihypertensive and Lipid Lowering Treatment to Prevent Heart Attack Trial (ALLHAT) Participants Assigned to Doxazosin and Chlorthalidone”. Curr Control Trials Cardiovasc Med 3 (1): 10. DOI:10.1186/1468-6708-3-10. PMC 149403. PMID 12459039.
↑ „Marketing: Spin doctors soft pedal data on antihypertensives”. BMJ. 2003-01-18. Pristupljeno 2008-05-26.
↑ „Antihypertensive Drugs and Patients With Erectile Dysfunction”.
↑ Zhou, YC; Xia GS, Xue YY, Zhang XD, Zheng LW, Jin BF (2010). „Kidney-tonifying and dampness-expelling Chinese herbal medicine combined with doxazosin for the treatment of chronic epididymitis” (Chinese). Zhonghua Nan Ke Xue 16 (12): 1143-6.

Spoljašnje veze

	Portal Medicina
	Portal Hemija

Information about Cardura from rxlist.com Arhivirano 2008-06-25 na Wayback Machine-u
Cardura XL product website Arhivirano 2010-08-23 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

[Piller2002-6] Piller LB, Davis BR, Cutler JA, et al. (November 2002). „Validation of Heart Failure Events in the Antihypertensive and Lipid Lowering Treatment to Prevent Heart Attack Trial (ALLHAT) Participants Assigned to Doxazosin and Chlorthalidone”. Curr Control Trials Cardiovasc Med 3 (1): 10. DOI:10.1186/1468-6708-3-10. PMC 149403. PMID 12459039.

[7] „Marketing: Spin doctors soft pedal data on antihypertensives”. BMJ. 2003-01-18. Pristupljeno 2008-05-26.

[8] „Antihypertensive Drugs and Patients With Erectile Dysfunction”.

[9] Zhou, YC; Xia GS, Xue YY, Zhang XD, Zheng LW, Jin BF (2010). „Kidney-tonifying and dampness-expelling Chinese herbal medicine combined with doxazosin for the treatment of chronic epididymitis” (Chinese). Zhonghua Nan Ke Xue 16 (12): 1143-6.

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