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=NC(=NC(N)=C2C=C1OC)N3CCN(CC3)C(=O)C4COC5=CC=CC=C5O4

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 66 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 2778	9.27 null [pKi]
Alpha-1b adrenergic receptor 44 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 2778	9.09 null [pKi]
Alpha-1d adrenergic receptor 36 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 2778	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 8429	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 567 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019668s021lbl.pdf	Primary		Approved 8429	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
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 1737	substrate 1037	substrate 1217	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
OATP2B1 123 P-gp 1461 BCRP 699 NTCP 34 OATP1B1 788 OATP1B3 706 OCT1 512	CYP2C19 991

Drug as perpetrator

Target	Modality	Activity
OATP1B1 803	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/22541068/	no
OATP1B3 715	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/22541068/	no
OATP2B1 126	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/22541068/	no
BCRP 773	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/22355323/	yes
NTCP 35	inhibitor 3277 Sources: https://mospace.umsystem.edu/xmlui/bitstream/handle/10355/43706/KHURANARolMemTra.pdf?sequence=1	yes
OCT1 543	inhibitor 3277 Sources: https://pubmed.ncbi.nlm.nih.gov/18788725/	yes
P-gp 1650	inhibitor 3277 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 1737	substrate 3367 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 991	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021269s011lbl.pdf	minor
CYP2C9 1037	substrate 3367 Sources: https://www.pfizer.ca/sites/default/files/201710/CARDURA_PM_Eng_201486_4Apr2017.pdf	minor
CYP2D6 1217	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021269s011lbl.pdf	minor

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1647	inhibitor 1626 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
Meta-analysis of studies using selective alpha1-blockers in patients with hypertension and type 2 diabetes.	2001 Dec	11777296
5alpha-reductase inhibitors: what role should they play?	2001 Dec	11750255
Terazosin, doxazosin, and prazosin: current clinical experience.	2001 Dec	11750252
Tamsulosin: current clinical experience.	2001 Dec	11750250
Participant recruitment in the Antihypertensive and Lipid-Lowering Treatment to Prevent Heart Attack Trial (ALLHAT).	2001 Dec	11738123
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
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
[Effect of doxazosin on postural changes in blood pressure using a multibiomedical recorder].	2001 Oct	11725558
A random comparison of fosinopril and nifedipine GITS in patients with primary renal disease.	2001 Oct	11593109
Cardiovascular protection and blood pressure reduction: a meta-analysis.	2001 Oct 20	11684211
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
[Doxazosin, of modified liberation, in hemodialyzed patients].	2002 Apr	12090057
Double-blind, placebo-controlled crossover comparison of five classes of antihypertensive drugs.	2002 Apr	11910315
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
Effect of doxazosin on stretch-activated adenosine triphosphate release in bladder urothelial cells from patients with benign prostatic hyperplasia.	2002 Aug	12137852
Critical evaluation of the problem of chronic urinary retention after orthotopic bladder substitution in women.	2002 Aug	12131315
alpha1-Adrenergic blockers in young men with primary bladder neck obstruction.	2002 Aug	12131312
Microalbuminuria reduction with valsartan in patients with type 2 diabetes mellitus: a blood pressure-independent effect.	2002 Aug 6	12163426
Differential actions of naftopidil, doxazosin and nifedipine on platelet thromboxane generation and platelet-derived growth factor efflux in vitro.	2002 Aug-Sep	12189011
Double-blind, crossover, comparative study of doxazosin and enalapril in the treatment of hypertension in renal transplant patients under cyclosporine immunosuppression.	2002 Feb	11959345
Combined oral therapy with sildenafil and doxazosin for the treatment of non-organic erectile dysfunction refractory to sildenafil monotherapy.	2002 Feb	11896478
The use of alpha-adrenoceptor antagonists in lower urinary tract disease.	2002 Feb	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 Feb	11805209
Flow injection analysis of doxazosin mesylate using UV-detection.	2002 Feb 1	11814727
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
Relationship between arterial distensibility and low-frequency power spectrum of blood pressure in spontaneously hypertensive rats.	2002 Jan	11743232
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
Managing benign prostatic hyperplasia.	2002 Jul 1	12126034
Successful blood pressure control in the African American Study of Kidney Disease and Hypertension.	2002 Jul 22	12123409
Doxazosin, an inferior antihypertensive agent?	2002 Jun	12037690
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 Mar	11875314
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 May	12075946
Alpha1-adrenoceptor antagonists radiosensitize prostate cancer cells via apoptosis induction.	2002 May-Jun	12168853
Doxazosin and congestive heart failure.	2002 May-Jun	12045387
Premature termination of clinical trials--lessons learned.	2002 May-Jun	12045375
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).

Substance Class	Chemical Created by `admin` on `Sat Dec 16 17:39:35 GMT 2023` Edited by `admin` on `Sat Dec 16 17:39:35 GMT 2023`
Record UNII	NW1291F1W8
Record Status	`Validated (UNII)`
Record Version

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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

(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

CARDURA XL

Brand Name

English

Classification Tree Code System Code

NDF-RT

N0000175553