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Doksazosin

Doksazosin
IUPAC ime
(RS)-24-[(2,3-dihidro-1,4-benzodioksin-2-il)karbonil]piperazin-1-il6,7-dimetoksihinazolin-4-amin
Klinički podaci
Prodajno imeKardura
Drugs.comMonografija
MedlinePlusa693045
Način primeneoralno
Pravni status
Pravni status
  • ℞ (Prescription only)
Farmakokinetički podaci
Bioraspoloživost65%
Vezivanje proteina98%
MetabolizamHepatički
Poluvreme eliminacije22 sata
Identifikatori
CAS broj74191-85-8 ДаY
ATC kodC02CA04 (WHO)
PubChemCID 3157
DrugBankDB00590 ДаY
ChemSpider3045 ДаY
UNIINW1291F1W8 ДаY
KEGGD07874 ДаY
ChEBICHEBI:4708 ДаY
ChEMBLCHEMBL707 ДаY
Hemijski podaci
FormulaC23H25N5O5
Molarna masa451,475 g/mol
  • O=C(N3CCN(c2nc1cc(OC)c(OC)cc1c(n2)N)CC3)C4Oc5c(OC4)cccc5
  • 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) ДаY
  • Key:RUZYUOTYCVRMRZ-UHFFFAOYSA-N ДаY

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.[1] Pfizer je lansirao sofisticiranu kampanju kontrole štete početkom 2000, tako da prodaja u velikoj meri nije bila umanjena, uprkos rezultata studije.[2]

Nedavne studije su ustanovile da je doksazosin delotvoran u treatiranju erektilalne disfunkcije (ED).[3] Takođe je pokazano da je doksazosin u izvesnoj meri efektivan u tretiranju hroničnog epididimitisa.[4]

Reference

  1. ^ Piller LB; Davis BR; Cutler JA; et al. (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. PMC 149403 Слободан приступ. PMID 12459039. doi:10.1186/1468-6708-3-10. 
  2. ^ „Marketing: Spin doctors soft pedal data on antihypertensives”. BMJ. 18. 1. 2003. Приступљено 26. 5. 2008. 
  3. ^ „Antihypertensive Drugs and Patients With Erectile Dysfunction”. 
  4. ^ Zhou, YC; Xia GS; et al. (2010—2012). „Kidney-tonifying and dampness-expelling Chinese herbal medicine combined with doxazosin for the treatment of chronic epididymitis”. Zhonghua Nan Ke Xue (на језику: Chinese). 16 (12): 1143—6. 

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