DOXAZOSIN

Details

Stereochemistry	RACEMIC
Molecular Formula	C23H25N5O5
Molecular Weight	451.476
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COc1cc2c(cc1OC)nc([nH]c2=N)N3CCN(CC3)C(=O)C4COc5ccccc5O4

InChI

InChIKey=RUZYUOTYCVRMRZ-UHFFFAOYSA-N

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)

HIDE SMILES / InChI

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019668s021lbl.pdf | https://www.drugbank.ca/drugs/DB00590

Doxazosin mesylate is a quinazoline compound sold by Pfizer under the brand name CARDURA. CARDURA is indicated for the treatment of both the urinary outflow obstruction and obstructive and irritative symptoms associated with BPH: obstructive symptoms (hesitation, intermittency, dribbling, weak urinary stream, incomplete emptying of the bladder) and irritative symptoms (nocturia, daytime frequency, urgency, burning). CARDURA may be used in all BPH patients whether hypertensive or normotensive. In patients with hypertension and BPH, both conditions were effectively treated with CARDURA monotherapy. CARDURA provides rapid improvement in symptoms and urinary flow rate in 66–71% of patients. CARDURA is also indicated for the treatment of hypertension. CARDURA may be used alone or in combination with diuretics, beta-adrenergic blocking agents, calcium channel blockers, or angiotensin-converting enzyme inhibitors. Doxazosin acts by inhibiting the postsynaptic alpha(1)-adrenoceptors on vascular smooth muscle. This inhibits the vasoconstrictor effect of circulating and locally released catecholamines (epinephrine and norepinephrine), resulting in peripheral vasodilation.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Alpha-1a adrenergic receptor 33 Target ID: CHEMBL229 Sources: https://www.drugbank.ca/drugs/DB00590 \| https://www.ncbi.nlm.nih.gov/pubmed/16302814 \| https://www.ncbi.nlm.nih.gov/pubmed/1968249	Antagonist 1131	9.27 null [pKi]
Alpha-1b adrenergic receptor 22 Target ID: CHEMBL232 Sources: https://www.drugbank.ca/drugs/DB00590 \| https://www.ncbi.nlm.nih.gov/pubmed/16302814 \| https://www.ncbi.nlm.nih.gov/pubmed/1968249	Antagonist 1131	9.09 null [pKi]
Alpha-1d adrenergic receptor 14 Target ID: CHEMBL223 Sources: https://www.drugbank.ca/drugs/DB00590 \| https://www.ncbi.nlm.nih.gov/pubmed/16302814 \| https://www.ncbi.nlm.nih.gov/pubmed/1968249	Antagonist 1131	9.09 null [pKi]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Benign prostatic hyperplasia 16 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019668s021lbl.pdf	Primary		Approved 4033	CARDURA Approved Use INDICATIONS AND USAGE A. Benign Prostatic Hyperplasia (BPH). CARDURA is indicated for the treatment of both the urinary outflow obstruction and obstructive and irritative symptoms associated with BPH: obstructive symptoms (hesitation, intermittency, dribbling, weak urinary stream, incomplete emptying of the bladder) and irritative symptoms (nocturia, daytime frequency, urgency, burning). CARDURA may be used in all BPH patients whether hypertensive or normotensive. In patients with hypertension and BPH, both conditions were effectively treated with CARDURA monotherapy. CARDURA provides rapid improvement in symptoms and urinary flow rate in 66–71% of patients. Sustained improvements with CARDURA were seen in patients treated for up to 14 weeks in double-blind studies and up to 2 years in open-label studies. B. Hypertension. CARDURA is also indicated for the treatment of hypertension. CARDURA may be used alone or in combination with diuretics, beta-adrenergic blocking agents, calcium channel blockers, or angiotensin-converting enzyme inhibitors. Launch Date 6.5750401E11
Hypertension 235 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019668s021lbl.pdf	Primary		Approved 4033	CARDURA Approved Use INDICATIONS AND USAGE A. Benign Prostatic Hyperplasia (BPH). CARDURA is indicated for the treatment of both the urinary outflow obstruction and obstructive and irritative symptoms associated with BPH: obstructive symptoms (hesitation, intermittency, dribbling, weak urinary stream, incomplete emptying of the bladder) and irritative symptoms (nocturia, daytime frequency, urgency, burning). CARDURA may be used in all BPH patients whether hypertensive or normotensive. In patients with hypertension and BPH, both conditions were effectively treated with CARDURA monotherapy. CARDURA provides rapid improvement in symptoms and urinary flow rate in 66–71% of patients. Sustained improvements with CARDURA were seen in patients treated for up to 14 weeks in double-blind studies and up to 2 years in open-label studies. B. Hypertension. CARDURA is also indicated for the treatment of hypertension. CARDURA may be used alone or in combination with diuretics, beta-adrenergic blocking agents, calcium channel blockers, or angiotensin-converting enzyme inhibitors. Launch Date 6.5750401E11

C_max

Value	Dose	Analyte	Population
9.7 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2139337/	1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered:	DOXAZOSIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
13.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2139337/	1 mg 1 times / day steady-state, oral dose: 1 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DOXAZOSIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
14.3 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2951261/	1 mg 1 times / day steady-state, oral dose: 1 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DOXAZOSIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
151.7 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2951261/	16 mg 1 times / day steady-state, oral dose: 16 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DOXAZOSIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
42.3 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2951261/	4 mg 1 times / day steady-state, oral dose: 4 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DOXAZOSIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
65.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2951261/	8 mg 1 times / day steady-state, oral dose: 8 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DOXAZOSIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
162 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2139337/	1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered:		DOXAZOSIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
268 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2139337/	1 mg 1 times / day steady-state, oral dose: 1 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		DOXAZOSIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
12.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2139337/	1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered:	DOXAZOSIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
15 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2139337/	1 mg 1 times / day steady-state, oral dose: 1 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DOXAZOSIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
11.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2951261/	1 mg 1 times / day steady-state, oral dose: 1 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DOXAZOSIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
11.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2951261/	16 mg 1 times / day steady-state, oral dose: 16 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DOXAZOSIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
12.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2951261/	4 mg 1 times / day steady-state, oral dose: 4 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DOXAZOSIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
8.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2951261/	8 mg 1 times / day steady-state, oral dose: 8 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DOXAZOSIN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
60 mg single, oral Overdose Dose: 60 mg Route: oral Route: single Dose: 60 mg Sources: https://pubmed.ncbi.nlm.nih.gov/16004202/	healthy, 19 years n = 1 Health Status: healthy Age Group: 19 years Sex: F Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/16004202/	Disc. AE: Sinus tachycardia... AEs leading to discontinuation/dose reduction: Sinus tachycardia (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/16004202/
16 mg single, oral (max) Highest studied dose Dose: 16 mg Route: oral Route: single Dose: 16 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019668s028lbl.pdf	unhealthy, adult n = 665 Health Status: unhealthy Condition: Hypertension Age Group: adult Sex: unknown Population Size: 665 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019668s028lbl.pdf	DLT: Postural edema... Dose limiting toxicities: Postural edema (2.7%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019668s028lbl.pdf
4 mg 1 times / day steady, oral Recommended Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/10594469/	healthy, adult n = 35 Health Status: healthy Age Group: adult Sex: unknown Population Size: 35 Sources: https://pubmed.ncbi.nlm.nih.gov/10594469/	Disc. AE: Orthostatic dizziness... AEs leading to discontinuation/dose reduction: Orthostatic dizziness (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/10594469/
16 mg 1 times / day steady, oral (max) Highest studied dose Dose: 16 mg, 1 times / day Route: oral Route: steady Dose: 16 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/19353415/	unhealthy, mean 59 years n = 97 Health Status: unhealthy Condition: Hypertension Age Group: mean 59 years Sex: M+F Population Size: 97 Sources: https://pubmed.ncbi.nlm.nih.gov/19353415/	Disc. AE: Fatigue, Urinary incontinence... Other AEs: Rhinitis... AEs leading to discontinuation/dose reduction: Fatigue (3 patients) Urinary incontinence (2 patients) Other AEs: Rhinitis (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/19353415/
8 mg 1 times / day steady, oral Dose: 8 mg, 1 times / day Route: oral Route: steady Dose: 8 mg, 1 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT01953432	unhealthy n = 22 Health Status: unhealthy Condition: cocaine dependence Population Size: 22 Sources: https://clinicaltrials.gov/ct2/show/NCT01953432	Other AEs: Nausea, Constipation... Other AEs: Nausea (below serious, 2 patients) Constipation (below serious, 1 patient) Allergy (below serious, 1 patient) Dizziness (below serious, 1 patient) Numbness (below serious, 1 patient) Sources: https://clinicaltrials.gov/ct2/show/NCT01953432

AEs

AE	Significance	Dose	Population
Sinus tachycardia	1 patient Disc. AE	60 mg single, oral Overdose Dose: 60 mg Route: oral Route: single Dose: 60 mg Sources: https://pubmed.ncbi.nlm.nih.gov/16004202/	healthy, 19 years n = 1 Health Status: healthy Age Group: 19 years Sex: F Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/16004202/
Postural edema	2.7% DLT	16 mg single, oral (max) Highest studied dose Dose: 16 mg Route: oral Route: single Dose: 16 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019668s028lbl.pdf	unhealthy, adult n = 665 Health Status: unhealthy Condition: Hypertension Age Group: adult Sex: unknown Population Size: 665 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019668s028lbl.pdf
Orthostatic dizziness	1 patient Disc. AE	4 mg 1 times / day steady, oral Recommended Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/10594469/	healthy, adult n = 35 Health Status: healthy Age Group: adult Sex: unknown Population Size: 35 Sources: https://pubmed.ncbi.nlm.nih.gov/10594469/
Rhinitis	1 patient	16 mg 1 times / day steady, oral (max) Highest studied dose Dose: 16 mg, 1 times / day Route: oral Route: steady Dose: 16 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/19353415/	unhealthy, mean 59 years n = 97 Health Status: unhealthy Condition: Hypertension Age Group: mean 59 years Sex: M+F Population Size: 97 Sources: https://pubmed.ncbi.nlm.nih.gov/19353415/
Urinary incontinence	2 patients Disc. AE	16 mg 1 times / day steady, oral (max) Highest studied dose Dose: 16 mg, 1 times / day Route: oral Route: steady Dose: 16 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/19353415/	unhealthy, mean 59 years n = 97 Health Status: unhealthy Condition: Hypertension Age Group: mean 59 years Sex: M+F Population Size: 97 Sources: https://pubmed.ncbi.nlm.nih.gov/19353415/
Fatigue	3 patients Disc. AE	16 mg 1 times / day steady, oral (max) Highest studied dose Dose: 16 mg, 1 times / day Route: oral Route: steady Dose: 16 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/19353415/	unhealthy, mean 59 years n = 97 Health Status: unhealthy Condition: Hypertension Age Group: mean 59 years Sex: M+F Population Size: 97 Sources: https://pubmed.ncbi.nlm.nih.gov/19353415/
Allergy	below serious, 1 patient	8 mg 1 times / day steady, oral Dose: 8 mg, 1 times / day Route: oral Route: steady Dose: 8 mg, 1 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT01953432	unhealthy n = 22 Health Status: unhealthy Condition: cocaine dependence Population Size: 22 Sources: https://clinicaltrials.gov/ct2/show/NCT01953432
Constipation	below serious, 1 patient	8 mg 1 times / day steady, oral Dose: 8 mg, 1 times / day Route: oral Route: steady Dose: 8 mg, 1 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT01953432	unhealthy n = 22 Health Status: unhealthy Condition: cocaine dependence Population Size: 22 Sources: https://clinicaltrials.gov/ct2/show/NCT01953432
Dizziness	below serious, 1 patient	8 mg 1 times / day steady, oral Dose: 8 mg, 1 times / day Route: oral Route: steady Dose: 8 mg, 1 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT01953432	unhealthy n = 22 Health Status: unhealthy Condition: cocaine dependence Population Size: 22 Sources: https://clinicaltrials.gov/ct2/show/NCT01953432
Numbness	below serious, 1 patient	8 mg 1 times / day steady, oral Dose: 8 mg, 1 times / day Route: oral Route: steady Dose: 8 mg, 1 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT01953432	unhealthy n = 22 Health Status: unhealthy Condition: cocaine dependence Population Size: 22 Sources: https://clinicaltrials.gov/ct2/show/NCT01953432
Nausea	below serious, 2 patients	8 mg 1 times / day steady, oral Dose: 8 mg, 1 times / day Route: oral Route: steady Dose: 8 mg, 1 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT01953432	unhealthy n = 22 Health Status: unhealthy Condition: cocaine dependence Population Size: 22 Sources: https://clinicaltrials.gov/ct2/show/NCT01953432

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 882	substrate 530	substrate 610	inhibitor 775

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
OATP2B1 66 P-gp 666 BCRP 303 NTCP 13 OATP1B1 369 OATP1B3 319 OCT1 254	CYP2C19 500

Drug as perpetrator

Target	Modality	Activity
OATP1B1 379	inhibitor 1612 Sources: https://pubmed.ncbi.nlm.nih.gov/22541068/	no
OATP1B3 326	inhibitor 1612 Sources: https://pubmed.ncbi.nlm.nih.gov/22541068/	no
OATP2B1 67	inhibitor 1612 Sources: https://pubmed.ncbi.nlm.nih.gov/22541068/	no
BCRP 346	inhibitor 1612 Sources: https://pubmed.ncbi.nlm.nih.gov/22355323/	yes
NTCP 13	inhibitor 1612 Sources: https://mospace.umsystem.edu/xmlui/bitstream/handle/10355/43706/KHURANARolMemTra.pdf?sequence=1	yes
OCT1 266	inhibitor 1612 Sources: https://pubmed.ncbi.nlm.nih.gov/18788725/	yes
P-gp 754	inhibitor 1612 Sources: https://pubmed.ncbi.nlm.nih.gov/19806783/ \| https://pubmed.ncbi.nlm.nih.gov/11895100/	yes

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP3A4 882	substrate 1689 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021269s011lbl.pdf \| https://pubmed.ncbi.nlm.nih.gov/24092799/	major	likely (co-administration study) Comment: Boceprevir may increase doxazosin concentrations through CYP3A inhibition Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021269s011lbl.pdf \| https://pubmed.ncbi.nlm.nih.gov/24092799/
CYP2C19 500	substrate 1689 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021269s011lbl.pdf	minor
CYP2C9 530	substrate 1689 Sources: https://www.pfizer.ca/sites/default/files/201710/CARDURA_PM_Eng_201486_4Apr2017.pdf	minor
CYP2D6 610	substrate 1689 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021269s011lbl.pdf	minor

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 796	inhibitor 786 Sources: https://pubmed.ncbi.nlm.nih.gov/15098086/

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:4708	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:4708
MolPort	MolPort-001-684-491	https://www.molport.com/shop/molecule-link/MolPort-001-684-491
eMolecules	537813	https://www.emolecules.com/cgi-bin/more?vid=537813

PubMed

Title	Date	PubMed
Quality-of-life assessment in patients with benign prostatic hyperplasia: effects of various interventions.	2001	11735675
Efficacy and tolerability of drugs for treatment of benign prostatic hyperplasia.	2001	11583366
Is postural hypotension a real problem with antihypertensive medication?	2001	11574742
Lower urinary tract symptoms suggestive of benign prostatic obstruction--Triumph: the role of general practice databases.	2001	11275742
Renal hemodynamic effects of captopril and doxazosin during slight physical activity in hypertensive patients with type-1 diabetes mellitus.	2001	11174009
Reduced heat shock proteins: a mechanism to explain higher cardiovascular events associated with doxazosin.	2001 Apr	11319678
Baseline characteristics of the diabetic participants in the Antihypertensive and Lipid-Lowering Treatment to Prevent Heart Attack Trial (ALLHAT).	2001 Apr	11315826
Recent clinical trial highlights in hypertension.	2001 Apr	11276395
Lessons learned from prematurely terminated clinical trials.	2001 Aug	11470019
Apoptotic activity of doxazosin on prostate stroma in vitro is mediated through an autocrine expression of TGF-beta1.	2001 Aug 1	11494328
Meta-analysis of studies using selective alpha1-blockers in patients with hypertension and type 2 diabetes.	2001 Dec	11777296
Clinical Implications of Recent Findings from the Antihypertensive and Lipid-Lowering Treatment To Prevent Heart Attack Trial (ALLHAT) and Other Studies of Hypertension.	2001 Dec 18	11747386
Operational aspects of terminating the doxazosin arm of The Antihypertensive and Lipid Lowering Treatment to Prevent Heart Attack Trial (ALLHAT).	2001 Feb	11165421
Low-dose ACE with alpha- or beta-adrenergic receptor inhibitors have beneficial SHR cardiovascular effects.	2001 Jan	11452337
[Bilateral pheochromocytoma: laparoscopic surgery in 2 cases].	2001 Jan	11265213
A quantitative analysis of antagonism and inverse agonism at wild-type and constitutively active hamster alpha1B-adrenoceptors.	2001 Jan	11191834
Safety and availability of doxazosin in treating hypertensive patients with chronic renal failure.	2001 Jul	11510747
Antihypertensive effect of alpha- and beta-adrenergic blockade in obese and lean hypertensive subjects.	2001 Jul	11465655
Role of alpha1-blockade in congenital long QT syndrome: investigation by exercise stress test.	2001 Jul	11446501
Reduction of human prostate tumor vascularity by the alpha1-adrenoceptor antagonist terazosin.	2001 Jul 1	11433417
Doxazosin added to single-drug therapy in hypertensive patients with benign prostatic hypertrophy.	2001 Jul-Aug	11498652
[Long-term therapy of benign prostatic hyperplasia. Our experience].	2001 Mar	11346714
The release of the substrate for xanthine oxidase in hypertensive patients was suppressed by angiotensin converting enzyme inhibitors and alpha1-blockers.	2001 Mar	11327632
Initiation of nonselective alpha1-antagonist therapy and occurrence of hypotension-related adverse events among men with benign prostatic hyperplasia: a retrospective cohort study.	2001 May	11394731
Effect of antihypertensive therapy on renal artery structure in type 2 diabetic rats with hypertension.	2001 May	11358940
Doxazosin inhibits monocyte chemotactic protein 1-directed migration of human monocytes.	2001 May	11336104
[Alpha-blockers in therapy of arterial hypertension. No longer the drug of first choice].	2001 May 31	11460395
Effects of antihypertensive agents on blood pressure during exercise.	2001 Nov	11768726
Doxazosin for the management of hypertension: implications of the findings of the ALLHAT trial.	2001 Nov	11724218
Doxazosin and congestive heart failure.	2001 Nov 1	11691497
A random comparison of fosinopril and nifedipine GITS in patients with primary renal disease.	2001 Oct	11593109
Heart lines. Cardura update.	2001 Sep	11572810
Effect of doxazosin on rat urinary bladder function after partial outlet obstruction.	2002	11857670
Influence of the alpha-1-adrenergic receptor blocker doxazosin on exercise-induced hyperkalemia in hemodialysis patients.	2002	11834878
Acute effects of serotonin on rat bladder contractility.	2002	11803267
Efficacy and safety of doxazosin for perioperative management of patients with pheochromocytoma.	2002 Aug	12192533
Two-drug therapy is best for symptomatic prostate enlargement: combination should change clinical practice.	2002 Aug	12168985
Medical therapy for benign prostatic hyperplasia progression.	2002 Aug	12149154
Differential actions of naftopidil, doxazosin and nifedipine on platelet thromboxane generation and platelet-derived growth factor efflux in vitro.	2002 Aug-Sep	12189011
The use of alpha-adrenoceptor antagonists in lower urinary tract disease.	2002 Feb	11829730
Stability-indicating methods for the determination of doxazosin mezylate and celecoxib.	2002 Feb 1	11814719
Low-dose doxazosin improved aortic stiffness and endothelial dysfunction as measured by noninvasive evaluation.	2002 Jan	11924726
Stroke associated with alpha blocker therapy for benign prostatic hypertrophy.	2002 Jan	11837346
Quinazoline-derived alpha1-adrenoceptor antagonists induce prostate cancer cell apoptosis via an alpha1-adrenoceptor-independent action.	2002 Jan 15	11809715
Psychological characteristics and responses to antihypertensive drug therapy.	2002 Jan-Feb	11821634
Treatment of hypertension in the elderly.	2002 Jan-Feb	11773711
alpha-Adrenoceptor antagonists in the treatment of benign prostate hyperplasia.	2002 Jul	12037374
Successful blood pressure control in the African American Study of Kidney Disease and Hypertension.	2002 Jul 22	12123409
Alpha1-adrenoceptor antagonists radiosensitize prostate cancer cells via apoptosis induction.	2002 May-Jun	12168853
Relationship of antihypertensive treatment regimens and change in blood pressure to risk for heart failure in hypertensive patients randomly assigned to doxazosin or chlorthalidone: further analyses from the Antihypertensive and Lipid-Lowering treatment to prevent Heart Attack Trial.	2002 Sep 3	12204014

Patents

Sample Use Guides

In Vivo Use Guide

Usual Adult Dose for Hypertension Initial dose: 1 mg orally once a day. Maintenance dose: 1 to 16 mg orally once a day. Usual Adult Dose for Benign Prostatic Hyperplasia Initial dose: Immediate-release: 1 mg orally once a day. Extended-release: 4 mg orally once a day with breakfast Maintenance dose: Immediate-release: 1 to 8 mg orally once a day. Extended-release: 4 to 8 mg orally once a day with breakfast. Depending on the patient's symptomatic response and tolerability, the dose may be increased to 8 mg (the maximum recommended dose). The recommended titration interval is 3 to 4 weeks.

Route of Administration: Oral

In Vitro Use Guide

Ring segments of splanchnic, peripheral, coronary, pulmonary and uterine conduit arteries obtained during surgery were studied in tissue baths. Resistance arteries dissected from various sites were studied in a myograph. Both conduit and resistance vessels contracted in response to the alpha 1-agonist phenylephrine (10(-7) to 10(-4) mol/l), an effect that was antagonized by the alpha 1-antagonist doxazosin (10(-8) to 10(-6) mol/l).

Name

Type

Language

DOXAZOSIN

Official Name

English

DOXAZOSIN [MI]

Common Name

English

C02CA04

Code

English

1-(4-AMINO-6,7-DIMETHOXY-2-QUINAZOLINYL)-4-(1,4-BENZODIOXAN-2-YLCARBONYL)PIPERAZINE

Systematic Name

English

(+/-)-DOXAZOSIN

Common Name

English

DOXAZOSIN [WHO-DD]

Common Name

English

(4-(4-AMINO-6,7-DIMETHOXY-2-QUINAZOLINYL)-1-PIPERAZINYL)(2,3-DIHYDRO-1,4-BENZODIOXIN-2-YL)METHANONE

Systematic Name

English

DOXAZOSIN [INN]

Common Name

English

PIPERAZINE, 1-(4-AMINO-6,7-DIMETHOXY-2-QUINAZOLINYL)-4-((2,3-DIHYDRO-1,4-BENZODIOXIN-2-YL)CARBONYL)-

Systematic Name

English

DOXAZOSIN [VANDF]

Common Name

English

METHANONE, (4-(4-AMINO-6,7-DIMETHOXY-2-QUINAZOLINYL)-1-PIPERAZINYL)(2,3-DIHYDRO-1,4-BENZODIOXIN-2-YL)-

Systematic Name

English

UK-33274

Code

English

CARDURA XL

Brand Name

English

Classification Tree Code System Code

NDF-RT

N0000175553