| 词条 | Doxazosin |
| 释义 |
| Watchedfields = changed | verifiedrevid = 461091393 | IUPAC_name = (RS)-2-[4-(2,3-Dihydro-1,4-benzodioxine-2-carbonyl)piperazin-1-yl]-6,7-dimethoxyquinazolin-4-amine | image = Doxazosin.svg | width = 275 | chirality = Racemic mixture | image2 = Doxazosin ball-and-stick.png | tradename = Cardura, Carduran, others | Drugs.com = {{drugs.com|monograph|doxazosin-mesylate}} | MedlinePlus = a693045 | pregnancy_category = | legal_status = Rx-only | routes_of_administration = By mouth (tablets) | bioavailability = 65% | protein_bound = 98% | metabolism = Liver | elimination_half-life = 22 hours | IUPHAR_ligand = 7170 | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 74191-85-8 | ATC_prefix = C02 | ATC_suffix = CA04 | ATC_supplemental = | PubChem = 3157 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = DB00590 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 3045 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = NW1291F1W8 | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D07874 | ChEBI_Ref = {{ebicite|correct|EBI}} | ChEBI = 4708 | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 707 | C=23 | H=25 | N=5 | O=5 | molecular_weight = 451.475 g/mol | smiles = O=C(N3CCN(c2nc1cc(OC)c(OC)cc1c(n2)N)CC3)C4Oc5c(OC4)cccc5 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 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) | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = RUZYUOTYCVRMRZ-UHFFFAOYSA-N }}Doxazosin, sold under the brand names Cardura among others, is a medication used to treat symptoms of an enlarged prostate and high blood pressure.[1] For high blood pressure, it is a less preferred option.[1] It is taken by mouth.[1] Common side effects include dizziness, sleepiness, swelling, nausea, shortness of breath, and abdominal pain.[1] Severe side effects may include low blood pressure with standing, an irregular heart beat, and priapism.[1][6] Prostate cancer should be ruled out before starting treatment.[1] It is a α1-selective adrenergic blocker in the quinazoline class of compounds.[1] Doxazosin was patented in 1977 and came into medical use in 1988.[2] It is avaliable as a generic medication.[6] A month supply in the United Kingdom costs the NHS about 0.50 £ as of 2019.[3] In the United States the wholesale cost of this amount is about 5.50 USD.[4] In 2016 it was the 157th most prescribed medication in the United States with more than 4 million prescriptions.[5] Medical usesHigh blood pressureDoxazosin is usually added to other antihypertensive therapy such as calcium channel antagonists, diuretics, beta-adrenoreceptor antagonists, angiotensin-converting enzyme inhibitors and angiotensin-2 receptor blockers.[6] Doxazosin is generally considered to be safe, well-tolerated and effective as an add-on antihypertensive drug.[7] Like other alpha-1 receptor antagonists, it has a role in the peri-operative management of pheochromocytoma.[8] Benign prostatic hypertrophyDoxazosin is considered to be effective in reducing urinary symptom scores and improving peak urinary flow in men with benign prostatic hypertrophy.[9] HistoryIn March 2000, the Antihypertensive and Lipid Lowering Treatment to Prevent Heart Attack Trial (ALLHAT) study stopped its arm of the trial looking at alpha blockers, because doxazosin was less effective than a simple diuretic, and because patients on doxazosin had a 25% higher rate of cardiovascular disease and twice the rate of congestive heart failure as patients on diuretics.[10] Pfizer, aware of the results before publication, launched a marketing campaign in early 2000, and sales were largely unaffected, despite the dangers highlighted by the study.[11][12] References1. ^1 2 3 4 5 6 {{cite web |title=Doxazosin Mesylate Monograph for Professionals |url=https://www.drugs.com/monograph/doxazosin-mesylate.html |website=Drugs.com |publisher=American Society of Health-System Pharmacists |accessdate=17 March 2019 |language=en}} 2. ^{{cite book |last1=Fischer |first1=Jnos |last2=Ganellin |first2=C. Robin |title=Analogue-based Drug Discovery |date=2006 |publisher=John Wiley & Sons |isbn=9783527607495 |page=455 |url=https://books.google.ca/books?id=FjKfqkaKkAAC&pg=PA455|language=en}} 3. ^1 2 {{cite book|title=British national formulary : BNF 76|date=2018|publisher=Pharmaceutical Press|isbn=9780857113382|pages=765|edition=76}} 4. ^{{cite web |title=NADAC as of 2019-02-27 |url=https://data.medicaid.gov/Drug-Pricing-and-Payment/NADAC-as-of-2019-02-27/s7c9-pfa6 |website=Centers for Medicare and Medicaid Services |accessdate=3 March 2019 |language=en}} 5. ^{{cite web |title=The Top 300 of 2019 |url=https://clincalc.com/DrugStats/Top300Drugs.aspx |website=clincalc.com |accessdate=22 December 2018}} 6. ^{{cite journal | vauthors = Wykretowicz A, Guzik P, Wysocki H | title = Doxazosin in the current treatment of hypertension | journal = Expert Opinion on Pharmacotherapy | volume = 9 | issue = 4 | pages = 625–33 | date = March 2008 | pmid = 18312163 | doi = 10.1517/14656566.9.4.625 }} 7. ^{{cite journal | vauthors = Chapman N, Chen CY, Fujita T, Hobbs FD, Kim SJ, Staessen JA, Tanomsup S, Wang JG, Williams B | title = Time to re-appraise the role of alpha-1 adrenoceptor antagonists in the management of hypertension? | journal = Journal of Hypertension | volume = 28 | issue = 9 | pages = 1796–803 | date = September 2010 | pmid = 20543713 | doi = 10.1097/HJH.0b013e32833b912c }} 8. ^{{cite journal | vauthors = Mazza A, Armigliato M, Marzola MC, Schiavon L, Montemurro D, Vescovo G, Zuin M, Chondrogiannis S, Ravenni R, Opocher G, Colletti PM, Rubello D | title = Anti-hypertensive treatment in pheochromocytoma and paraganglioma: current management and therapeutic features | journal = Endocrine | volume = 45 | issue = 3 | pages = 469–78 | date = April 2014 | pmid = 23817839 | doi = 10.1007/s12020-013-0007-y }} 9. ^{{cite journal | vauthors = Yuan J, Liu Y, Yang Z, Qin X, Yang K, Mao C | title = The efficacy and safety of alpha-1 blockers for benign prostatic hyperplasia: an overview of 15 systematic reviews | journal = Current Medical Research and Opinion | volume = 29 | issue = 3 | pages = 279–87 | date = March 2013 | pmid = 23323875 | doi = 10.1185/03007995.2013.766594 }} 10. ^{{cite journal | vauthors = Piller LB, Davis BR, Cutler JA, Cushman WC, Wright JT, Williamson JD, Leenen FH, Einhorn PT, Randall OS, Golden JS, Haywood LJ | title = Validation of Heart Failure Events in the Antihypertensive and Lipid Lowering Treatment to Prevent Heart Attack Trial (ALLHAT) Participants Assigned to Doxazosin and Chlorthalidone | journal = Current Controlled Trials in Cardiovascular Medicine | volume = 3 | issue = 1 | pages = 10 | date = November 2002 | pmid = 12459039 | pmc = 149403 | doi = 10.1186/1468-6708-3-10 }} 11. ^Goldacre, Ben (2012) Bad Pharma How drug companies mislead doctors and harm patients, Fourth Estate, {{ISBN|0007350740}}. 12. ^{{cite journal | vauthors = Lenzer J | title = Spin doctors soft pedal data on antihypertensives | journal = BMJ | volume = 326(7381) | pages = 170 | date = 2003-01-18 | pmc = 1128917 | doi = 10.1136/bmj.326.7381.170 }} External links
7 : Alpha blockers|Benzodioxans|Carboxamides|Phenol ethers|Piperazines|Quinazolines|RTT |
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