Doxazosin

alpha-Adrenergic Blocker — CARDIOVASCULAR SYSTEM

Key facts

Doxazosin is an ofp drug in the alpha-Adrenergic Blocker class catalogued in DrugCentral. It was first approved by the FDA in 1990. Its mechanism of action is classified as Adrenergic alpha-Antagonists. DrugCentral lists 17 molecular targets, including Adra1b, ADRA1B and ADRA1D. Recorded indications include Benign prostatic hyperplasia and Hypertensive disorder.

• Approval status: ofp (first approved 1990 by the FDA).
• Drug class: alpha-Adrenergic Blocker.
• Mechanism of action: Adrenergic alpha-Antagonists.
• Molecular targets: Adra1b, ADRA1B, ADRA1D and Adra1a (17 listed in DrugCentral).
• Indications: Benign prostatic hyperplasia and Hypertensive disorder.
• ATC code: C02CA04 (Alpha-adrenoreceptor antagonists).
• Molecular formula: C23H25N5O5; molecular weight 451.48 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (2)

• Benign prostatic hyperplasia
• Hypertensive disorder

Contraindications (11)

• Cataract surgery
• Chronic idiopathic constipation
• Disease of liver
• Hepatic failure
• Intraoperative floppy iris syndrome
• Low blood pressure
• Orthostatic hypotension
• Priapism
• Pyloric obstruction
• Stenosis of intestine
• Syncope

Mechanism & targets

• Mechanism of action (MoA): Adrenergic alpha-Antagonists
• Established pharmacologic class: alpha-Adrenergic Blocker

Molecular targets (17)

Target	Gene	Action	Activity
Alpha-1B adrenergic receptor	Adra1b	unknown	Ki 9.38
Alpha-1B adrenergic receptor	ADRA1B	antagonist	Ki 9.10
Alpha-1D adrenergic receptor	ADRA1D	antagonist	Ki 8.85
Alpha-1A adrenergic receptor	Adra1a	unknown	IC50 8.81
Alpha-1A adrenergic receptor	ADRA1A	antagonist	Ki 8.80
5-hydroxytryptamine receptor 4	HTR4	unknown	Ki 6.90
Sodium-dependent dopamine transporter	SLC6A3	unknown	Ki 6.83
5-hydroxytryptamine receptor 2B	HTR2B	unknown	Ki 6.63
Alpha-2C adrenergic receptor	ADRA2C	unknown	Ki 6.55
5-hydroxytryptamine receptor 2C	HTR2C	unknown	Ki 6.54
Potassium voltage-gated channel subfamily H member 2	KCNH2	unknown	IC50 6.23
Alpha-2A adrenergic receptor	ADRA2A	unknown	Ki 6.14
Sodium-dependent serotonin transporter	SLC6A4	unknown	Ki 5.84
Beta-2 adrenergic receptor	ADRB2	unknown	Ki 5.72
Interstitial collagenase	MMP1	unknown	IC50 5.24
Multidrug resistance protein 1	ABCB1	unknown	Ki 5.00
HLA class I histocompatibility antigen, A-3 alpha chain	HLA-A	unknown	Kd 4.80

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1990-11-02	FDA	—	PFIZER

ATC classification

ATC code	Therapeutic hierarchy
C02CA04	CARDIOVASCULAR SYSTEM › ANTIHYPERTENSIVES › ANTIADRENERGIC AGENTS, PERIPHERALLY ACTING › Alpha-adrenoreceptor antagonists
G04CA55	GENITO URINARY SYSTEM AND SEX HORMONES › UROLOGICALS › DRUGS USED IN BENIGN PROSTATIC HYPERTROPHY › Alpha-adrenoreceptor antagonists

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Syncope	426.8
Spirometry abnormal	413.5
Conjunctivitis allergic	410.8
Mite allergy	401.7
Dust allergy	397.5
Mycotic allergy	394.4
Arteriosclerosis	354.0
Normochromic normocytic anaemia	332.6
Hyperkalaemia	299.8
Arteriosclerosis coronary artery	281.1
Pulmonary vasculitis	280.4
Hypertensive crisis	276.4

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Doxazosin is on its molecule page.

• Molecular formula: C₂₃H₂₅N₅O₅
• Molecular weight: 451.48 g/mol
• CAS number: 74191-85-8
• InChIKey: RUZYUOTYCVRMRZ-UHFFFAOYSA-N
• PubChem CID: 3157

COC1=C(OC)C=C2C(N)=NC(=NC2=C1)N1CCN(CC1)C(=O)C1COC2=C(O1)C=CC=C2

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Doxazosin used for?

DrugCentral lists the following indications for Doxazosin: Benign prostatic hyperplasia and Hypertensive disorder.

How does Doxazosin work?

Doxazosin is classified as Adrenergic alpha-Antagonists; its molecular targets in DrugCentral include Adra1b, ADRA1B (antagonist), ADRA1D (antagonist) and Adra1a.

When was Doxazosin first approved?

Doxazosin was first approved by the FDA in 1990.

What drug class does Doxazosin belong to?

Doxazosin is in the alpha-Adrenergic Blocker class.

What is the chemical formula of Doxazosin?

Doxazosin has the molecular formula C23H25N5O5 and a molecular weight of 451.48 g/mol.

Sources

• DrugCentral drug card 954 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1200561 — compound record and bioactivity
• PubChem CID 3157 — chemical identifiers
• DrugBank DB00590 — drug record
• FDA UNII NW1291F1W8 — substance identity
• DailyMed: FDA labels for Doxazosin — current prescribing information (label search)
• UniProt P35368 (ADRA1B) — target protein
• UniProt P25100 (ADRA1D) — target protein
• UniProt P35348 (ADRA1A) — target protein
• UniProt Q01959 (SLC6A3) — target protein
• UniProt P41595 (HTR2B) — target protein
• UniProt P18825 (ADRA2C) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.