DOXAZOSIN

Details

Stereochemistry	RACEMIC
Molecular Formula	C23H25N5O5
Molecular Weight	451.4751
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COC1=CC2=C(C=C1OC)C(N)=NC(=N2)N3CCN(CC3)C(=O)C4COC5=C(O4)C=CC=C5

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

Molecular Formula	C23H25N5O5
Molecular Weight	451.4751
Charge	0
Count

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

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 67 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 2849	9.27 null [pKi]
Alpha-1b adrenergic receptor 45 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 2849	9.09 null [pKi]
Alpha-1d adrenergic receptor 37 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 2849	9.09 null [pKi]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Benign prostatic hyperplasia 28 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019668s021lbl.pdf	Primary		Approved 8583	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 1990
Hypertension 575 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019668s021lbl.pdf	Primary		Approved 8583	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 1990

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
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
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

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
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
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

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 Health Status: healthy Age Group: 19 years Sex: F 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 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 Health Status: unhealthy Age Group: adult Sex: unknown 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 Health Status: healthy Age Group: adult Sex: unknown 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 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 Health Status: unhealthy Age Group: mean 59 years Sex: M+F 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 Health Status: unhealthy 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 Health Status: healthy Age Group: 19 years Sex: F Sources: https://pubmed.ncbi.nlm.nih.gov/16004202/
Postural edema	2.7% DLT	16 mg single, oral 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 Health Status: unhealthy Age Group: adult Sex: unknown 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 Health Status: healthy Age Group: adult Sex: unknown Sources: https://pubmed.ncbi.nlm.nih.gov/10594469/
Rhinitis	1 patient	16 mg 1 times / day steady, oral 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 Health Status: unhealthy Age Group: mean 59 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/19353415/
Urinary incontinence	2 patients Disc. AE	16 mg 1 times / day steady, oral 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 Health Status: unhealthy Age Group: mean 59 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/19353415/
Fatigue	3 patients Disc. AE	16 mg 1 times / day steady, oral 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 Health Status: unhealthy Age Group: mean 59 years Sex: M+F 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy 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 Health Status: unhealthy Sources: https://clinicaltrials.gov/ct2/show/NCT01953432

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946	substrate 1193	substrate 1388	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
OATP2B1 157 P-gp 1741 BCRP 910 NTCP 39 OATP1B1 1079 OATP1B3 961 OCT1 620	CYP2C19 1119

Drug as perpetrator

Target	Modality	Activity
OATP1B1 1095	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/22541068/	no
OATP1B3 970	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/22541068/	no
OATP2B1 162	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/22541068/	no
BCRP 985	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/22355323/	yes
NTCP 40	inhibitor 4027 Sources: https://mospace.umsystem.edu/xmlui/bitstream/handle/10355/43706/KHURANARolMemTra.pdf?sequence=1	yes
OCT1 656	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/18788725/	yes
P-gp 1932	inhibitor 4027 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 1946	substrate 4014 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 1119	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021269s011lbl.pdf	minor
CYP2C9 1193	substrate 4014 Sources: https://www.pfizer.ca/sites/default/files/201710/CARDURA_PM_Eng_201486_4Apr2017.pdf	minor
CYP2D6 1388	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021269s011lbl.pdf	minor

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 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
eMolecules	537813	https://www.emolecules.com/cgi-bin/more?vid=537813
MolPort	MolPort-001-684-491	https://www.molport.com/shop/molecule-link/MolPort-001-684-491

PubMed

Title	Date	PubMed
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.	2002-09-03	12204014
Differential actions of naftopidil, doxazosin and nifedipine on platelet thromboxane generation and platelet-derived growth factor efflux in vitro.	2002-08-22	12189011
Alpha1-adrenoceptor antagonists radiosensitize prostate cancer cells via apoptosis induction.	2002-08-10	12168853
Microalbuminuria reduction with valsartan in patients with type 2 diabetes mellitus: a blood pressure-independent effect.	2002-08-06	12163426
Efficacy and safety of doxazosin for perioperative management of patients with pheochromocytoma.	2002-08	12192533
Two-drug therapy is best for symptomatic prostate enlargement: combination should change clinical practice.	2002-08	12168985
Medical therapy for benign prostatic hyperplasia progression.	2002-08	12149154
Effect of doxazosin on stretch-activated adenosine triphosphate release in bladder urothelial cells from patients with benign prostatic hyperplasia.	2002-08	12137852
Critical evaluation of the problem of chronic urinary retention after orthotopic bladder substitution in women.	2002-08	12131315
alpha1-Adrenergic blockers in young men with primary bladder neck obstruction.	2002-08	12131312
Successful blood pressure control in the African American Study of Kidney Disease and Hypertension.	2002-07-22	12123409
Managing benign prostatic hyperplasia.	2002-07-01	12126034
alpha-Adrenoceptor antagonists in the treatment of benign prostate hyperplasia.	2002-07	12037374
Doxazosin and congestive heart failure.	2002-06-05	12045387
Premature termination of clinical trials--lessons learned.	2002-06-05	12045375
Doxazosin, an inferior antihypertensive agent?	2002-06	12037690
A postmarketing, open-label study to evaluate the tolerability and effectiveness of replacing standard-formulation doxazosin with doxazosin in the gastrointestinal therapeutic system formulation in adult patients with hypertension.	2002-05	12075946
[Doxazosin, of modified liberation, in hemodialyzed patients].	2002-04	12090057
Double-blind, placebo-controlled crossover comparison of five classes of antihypertensive drugs.	2002-04	11910315
Reduction of the soluble cyclic GMP vasorelaxing system in the vascular wall of stroke-prone spontaneously hypertensive rats: effect of the alpha1 -receptor blocker doxazosin.	2002-03	11875314
Psychological characteristics and responses to antihypertensive drug therapy.	2002-02-01	11821634
Flow injection analysis of doxazosin mesylate using UV-detection.	2002-02-01	11814727
Stability-indicating methods for the determination of doxazosin mezylate and celecoxib.	2002-02-01	11814719
Double-blind, crossover, comparative study of doxazosin and enalapril in the treatment of hypertension in renal transplant patients under cyclosporine immunosuppression.	2002-02	11959345
Combined oral therapy with sildenafil and doxazosin for the treatment of non-organic erectile dysfunction refractory to sildenafil monotherapy.	2002-02	11896478
The use of alpha-adrenoceptor antagonists in lower urinary tract disease.	2002-02	11829730
Modeling of relationships between pharmacokinetics and blockade of agonist-induced elevation of intraurethral pressure and mean arterial pressure in conscious dogs treated with alpha(1)-adrenoceptor antagonists.	2002-02	11805209
Quinazoline-derived alpha1-adrenoceptor antagonists induce prostate cancer cell apoptosis via an alpha1-adrenoceptor-independent action.	2002-01-15	11809715
Treatment of hypertension in the elderly.	2002-01-05	11773711
Low-dose doxazosin improved aortic stiffness and endothelial dysfunction as measured by noninvasive evaluation.	2002-01	11924726
Stroke associated with alpha blocker therapy for benign prostatic hypertrophy.	2002-01	11837346
Relationship between arterial distensibility and low-frequency power spectrum of blood pressure in spontaneously hypertensive rats.	2002-01	11743232
The choice of antihypertensive drugs in patients with erectile dysfunction.	2002	12017207
Effect of doxazosin on rat urinary bladder function after partial outlet obstruction.	2002	11857670
Observational multicentric trial performed with doxazosin: evaluation of sexual effects on patients with diagnosed benign prostatic hyperplasia.	2002	11834898
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
Clinical Implications of Recent Findings from the Antihypertensive and Lipid-Lowering Treatment To Prevent Heart Attack Trial (ALLHAT) and Other Studies of Hypertension.	2001-12-18	11747386
Meta-analysis of studies using selective alpha1-blockers in patients with hypertension and type 2 diabetes.	2001-12	11777296
5alpha-reductase inhibitors: what role should they play?	2001-12	11750255
Terazosin, doxazosin, and prazosin: current clinical experience.	2001-12	11750252
Tamsulosin: current clinical experience.	2001-12	11750250
Participant recruitment in the Antihypertensive and Lipid-Lowering Treatment to Prevent Heart Attack Trial (ALLHAT).	2001-12	11738123
Doxazosin and congestive heart failure.	2001-11-01	11691497
Effects of antihypertensive agents on blood pressure during exercise.	2001-11	11768726
Doxazosin for the management of hypertension: implications of the findings of the ALLHAT trial.	2001-11	11724218
Effects of blood pressure lowering with amlodipine or lisinopril on vascular structure of the common carotid artery.	2001-11	11672450
Cardiovascular protection and blood pressure reduction: a meta-analysis.	2001-10-20	11684211
[Effect of doxazosin on postural changes in blood pressure using a multibiomedical recorder].	2001-10	11725558
Quality-of-life assessment in patients with benign prostatic hyperplasia: effects of various interventions.	2001	11735675

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).

Substance Class	Chemical Created by `admin` on `Wed Apr 02 09:25:14 GMT 2025` Edited by `admin` on `Wed Apr 02 09:25:14 GMT 2025`
Record UNII	NW1291F1W8
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

DOXAZOSIN

Official Name

English

CARDURA XL

Preferred 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

(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

Doxazosin [WHO-DD]

Common Name

English

UK-33274

Code

English

Classification Tree Code System Code

NDF-RT

N0000175553