DOXAZOSIN HYDROCHLORIDE

Details

Stereochemistry	RACEMIC
Molecular Formula	C23H25N5O5.ClH
Molecular Weight	487.936
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

Cl.COC1=CC2=NC(=NC(N)=C2C=C1OC)N3CCN(CC3)C(=O)C4COC5=CC=CC=C5O4

InChI

InChIKey=AQAZIYFEPYHLHC-UHFFFAOYSA-N

InChI=1S/C23H25N5O5.ClH/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);1H

HIDE SMILES / InChI

Molecular Formula	ClH
Molecular Weight	36.461
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

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 2760	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 2760	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 2760	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 8360	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 549 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019668s021lbl.pdf	Primary		Approved 8360	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 1709	substrate 1010	substrate 1193	inhibitor 1599

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
OATP2B1 122 P-gp 1437 BCRP 691 NTCP 34 OATP1B1 781 OATP1B3 700 OCT1 506	CYP2C19 985

Drug as perpetrator

Target	Modality	Activity
OATP1B1 796	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/22541068/	no
OATP1B3 709	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/22541068/	no
OATP2B1 125	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/22541068/	no
BCRP 765	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/22355323/	yes
NTCP 35	inhibitor 3240 Sources: https://mospace.umsystem.edu/xmlui/bitstream/handle/10355/43706/KHURANARolMemTra.pdf?sequence=1	yes
OCT1 523	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/18788725/	yes
P-gp 1626	inhibitor 3240 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 1709	substrate 3326 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 985	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021269s011lbl.pdf	minor
CYP2C9 1010	substrate 3326 Sources: https://www.pfizer.ca/sites/default/files/201710/CARDURA_PM_Eng_201486_4Apr2017.pdf	minor
CYP2D6 1193	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021269s011lbl.pdf	minor

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1632	inhibitor 1613 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
Effects of two atypical neuroleptics, olanzapine and risperidone, on the function of the urinary bladder and the external urethral sphincter in anesthetized rats.	2001	11580866
Is postural hypotension a real problem with antihypertensive medication?	2001	11574742
A comparison of selected antihypertensives and the use of conventional vs ambulatory blood pressure in the detection and treatment of hypertension.	2001	11574740
Discontinuation of alpha-blockade after initial treatment with finasteride and doxazosin in men with lower urinary tract symptoms and clinical evidence of benign prostatic hyperplasia.	2001 Aug	11489700
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
5alpha-reductase inhibitors: what role should they play?	2001 Dec	11750255
Low-dose ACE with alpha- or beta-adrenergic receptor inhibitors have beneficial SHR cardiovascular effects.	2001 Jan	11452337
On call. I'm a 76-year-old man with an enlarged prostate. I've been taking Cardura and it's helped a lot, but my doctor stopped it because he said a study found the drug could cause heart failure. Now I'm getting up three or four times a night again. Is Cadura safe?	2001 Jul	11511462
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
[Doxazosin and soluble guanylate cyclase in a rat model of hypertension].	2001 Jul	11446964
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
Low-dose alpha/beta blockade in the treatment of essential hypertension.	2001 Jun	11411735
Voltammetric determination of doxazosin in tablets using rotating platinum electrode.	2001 Jun	11377017
US FDA weighs options for warning on antihypertensive drug.	2001 Jun 2	11403832
Structure-activity studies for a novel series of bicyclic substituted hexahydrobenz[e]isoindole alpha1A adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia.	2001 Jun 7	11384242
[Long-term therapy of benign prostatic hyperplasia. Our experience].	2001 Mar	11346714
Update in pharmacologic treatment of hypertension.	2001 May	11407110
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
Reversible renal impairment induced by treatment with the angiotensin II receptor antagonist candesartan in a patient with bilateral renal artery stenosis.	2001 May 17	11388887
[Alpha-blockers in therapy of arterial hypertension. No longer the drug of first choice].	2001 May 31	11460395
[Doksazozin "Cardura" in acute urinary retention caused by benign prostatic hyperplasia].	2001 May-Jun	11505534
Effects of antihypertensive agents on blood pressure during exercise.	2001 Nov	11768726
Doxazosin and congestive heart failure.	2001 Nov 1	11691497
Ventricular production of natriuretic peptides and ventricular structural remodeling in hypertensive heart failure.	2001 Oct	11593113
A random comparison of fosinopril and nifedipine GITS in patients with primary renal disease.	2001 Oct	11593109
Warning for antihypertensive drug?	2001 Oct 6	11597701
Doxazosin reduces prevalence of small dense low density lipoprotein and remnant-like particle cholesterol levels in nondiabetic and diabetic hypertensive patients.	2001 Sep	11587157
Heart lines. Cardura update.	2001 Sep	11572810
The choice of antihypertensive drugs in patients with erectile dysfunction.	2002	12017207
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
[Doxazosin, of modified liberation, in hemodialyzed patients].	2002 Apr	12090057
Efficacy and safety of doxazosin for perioperative management of patients with pheochromocytoma.	2002 Aug	12192533
Medical therapy for benign prostatic hyperplasia progression.	2002 Aug	12149154
Critical evaluation of the problem of chronic urinary retention after orthotopic bladder substitution in women.	2002 Aug	12131315
Double-blind, crossover, comparative study of doxazosin and enalapril in the treatment of hypertension in renal transplant patients under cyclosporine immunosuppression.	2002 Feb	11959345
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
Psychological characteristics and responses to antihypertensive drug therapy.	2002 Jan-Feb	11821634
Treatment of hypertension in the elderly.	2002 Jan-Feb	11773711
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
Premature termination of clinical trials--lessons learned.	2002 May-Jun	12045375

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 `Thu Jul 06 17:03:23 UTC 2023` Edited by `admin` on `Thu Jul 06 17:03:23 UTC 2023`
Record UNII	Y9EDC2483R
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

DOXAZOSIN HYDROCHLORIDE

Common Name

English

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

Common Name

English

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

Systematic Name

English

Code System Code Type Description

EPA CompTox

DTXSID00469077