Doxazosin

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]

Doxazosin
Clinical data
Trade namesCardura, Carduran, others
AHFS/Drugs.comMonograph
MedlinePlusa693045
Routes of
administration		By mouth (tablets)
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability65%
Protein binding98%
MetabolismLiver
Elimination half-life22 hours
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.128.642
Chemical and physical data
FormulaC23H25N5O5
Molar mass451.483 g·mol−1
3D model (JSmol)
ChiralityRacemic mixture
  (verify)

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][2] 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.[3] It is available as a generic medication.[2] In 2017, it was the 150th most commonly prescribed medication in the United States, with more than four million prescriptions.[4][5]

Medical uses

High blood pressure

Doxazosin 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 hypertrophy

Doxazosin is considered to be effective in reducing urinary symptom scores and improving peak urinary flow in men with benign prostatic hypertrophy.[9]

History

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]

References
  1. "Doxazosin Mesylate Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 17 March 2019.
  2. British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 765. ISBN 9780857113382.
  3. Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 455. ISBN 9783527607495.
  4. "The Top 300 of 2020". ClinCalc. Retrieved 11 April 2020.
  5. "Doxazosin Mesylate - Drug Usage Statistics". ClinCalc. Retrieved 11 April 2020.
  6. Wykretowicz A, Guzik P, Wysocki H (March 2008). "Doxazosin in the current treatment of hypertension". Expert Opinion on Pharmacotherapy. 9 (4): 625–33. doi:10.1517/14656566.9.4.625. PMID 18312163. S2CID 42056694.
  7. Chapman N, Chen CY, Fujita T, Hobbs FD, Kim SJ, Staessen JA, Tanomsup S, Wang JG, Williams B (September 2010). "Time to re-appraise the role of alpha-1 adrenoceptor antagonists in the management of hypertension?". Journal of Hypertension. 28 (9): 1796–803. doi:10.1097/HJH.0b013e32833b912c. PMID 20543713. S2CID 31819062.
  8. Mazza A, Armigliato M, Marzola MC, Schiavon L, Montemurro D, Vescovo G, Zuin M, Chondrogiannis S, Ravenni R, Opocher G, Colletti PM, Rubello D (April 2014). "Anti-hypertensive treatment in pheochromocytoma and paraganglioma: current management and therapeutic features". Endocrine. 45 (3): 469–78. doi:10.1007/s12020-013-0007-y. PMID 23817839. S2CID 25504151.
  9. Yuan J, Liu Y, Yang Z, Qin X, Yang K, Mao C (March 2013). "The efficacy and safety of alpha-1 blockers for benign prostatic hyperplasia: an overview of 15 systematic reviews". Current Medical Research and Opinion. 29 (3): 279–87. doi:10.1185/03007995.2013.766594. PMID 23323875. S2CID 26341029.
  10. Piller LB, Davis BR, Cutler JA, Cushman WC, Wright JT, Williamson JD, Leenen FH, Einhorn PT, Randall OS, Golden JS, Haywood LJ (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". Current Controlled Trials in Cardiovascular Medicine. 3 (1): 10. doi:10.1186/1468-6708-3-10. PMC 149403. PMID 12459039.
  11. Goldacre, Ben (2012) Bad Pharma How drug companies mislead doctors and harm patients, Fourth Estate, ISBN 0007350740.
  12. Lenzer J (2003-01-18). "Spin doctors soft pedal data on antihypertensives". BMJ. 326 (7381): 170. doi:10.1136/bmj.326.7381.170. PMC 1128917.
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