PharmGKB: The Pharmacogenomics Knowledge Base

Drug/Small Molecule:
doxazosin

2D structure

Overview

Trade Names: Alfadil; Cardenalin; Cardular; Cardura; Cardura-1; Cardura-2; Cardura-4; Carduran; Diblocin; Doxazosin mesylate; Normothen; Supressin
PharmGKB Accession Id: PA449407

Description

A selective alpha-1-adrenergic blocker that lowers serum cholesterol. It is also effective in the treatment of hypertension. PubChem (source: Drug Bank)

Indication

For treatment and management of Hypertension and urinary obstruction symptoms of BPH. (source: Drug Bank)

ATC Therapeutic Category

  • C02CA:Alpha-adrenoreceptor antagonists

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

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. (source: Drug Bank)

Pharmacology

Doxazosin is an alpha-adrenergic blocking agent used to treat hypertension and benign prostatic hyperplasia. Accordingly, Doxazosin is a selective inhibitor of the alpha1 subtype of alpha adrenergic receptors. In the human prostate, Doxazosin antagonizes phenylephrine (alpha1 agonist)-induced contractions, <i>in vitro</i>, and binds with high affinity to the alpha1c adrenoceptor, which is thought to be the predominant functional type in the prostate. Studies in normal human subjects have shown that Doxazosin competitively antagonized the pressor effects of phenylephrine (an alpha1 agonist) and the systolic pressor effect of norepinephrine. The antihypertensive effect of Doxazosin results from a decrease in systemic vascular resistance and the parent compound Doxazosin is primarily responsible for the antihypertensive activity. (source: Drug Bank)

Food Interactions

Avoid alcohol.
Avoid natural licorice.
Take without regard to meals. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic. (source: Drug Bank)

Protein Binding

98% (source: Drug Bank)

Absorption

65% (source: Drug Bank)

Toxicity

Symptoms of overdose include hypotension. Oral LD<sub>50</sub> is greater than 1000 mg/kg in mice and rats. (source: Drug Bank)

Isomeric SMILES Code:

COc1cc2c(cc1OC)nc(nc2N)N3CCN(CC3)C(=O)C4COc5ccccc5O4 (source: Drug Bank)

Curated Annotations (Curated Annotation)

  1. rs5065 at chr1:11828655 in CLCN6, NPPA
    This variant has been associated with modification of antihypertensive medication effects on blood pressure and cardiovascular disease.
    Variant Name:
    NPPA:T2238C
    Related Drugs:
    amlodipine, chlorthalidone, doxazosin, lisinopril
    Related Diseases:
    Cardiovascular Diseases, Coronary Disease, Stroke
    Evidence:
    PMID:18212314
Variant names are different names that have been used in the literature and other resources to refer to the same variant.

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Has annotations
ACE
  •   
  • PD
  •   
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
ADD1
  • CO
  •   
  •   
  •   
  • GN
Publications
No phenotype data Genotype Data Available No literature annotations Not annotated
CLCN6
  •   
  •   
  •   
  •   
  •   
Variants
No phenotype data No genotype data Literature annotations available Not annotated
NPPA
  • CO
  •   
  •   
  •   
  • GN
Publications, Variants

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
ADRA1A Uncurated Annotation (source: Drug Bank)
ADRA1B Uncurated Annotation (source: Drug Bank)
ADRA1D Uncurated Annotation (source: Drug Bank)

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
tadalafil Uncurated Annotation Risk of significant hypotension with this association (source: Drug Bank)
vardenafil Uncurated Annotation Risk of significant hypotension with this association (source: Drug Bank)

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Cardiovascular Diseases
  • CO
  •   
  •   
  •   
  • GN
Publications, Variants
No phenotype data No genotype data Literature annotations available Not annotated
Coronary Disease
  • CO
  •   
  •   
  •   
  • GN
Publications, Variants
No phenotype data No genotype data Literature annotations available Not annotated
Death
  • CO
  •   
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Heart Failure
  • CO
  •   
  •   
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Hypertension
  • CO
  • PD
  •   
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Myocardial Infarction
  • CO
  •   
  •   
  •   
  • GN
Publications
Phenotype data available No genotype data Literature annotations available Not annotated
Stroke
  • CO
  •   
  •   
  •   
  • GN
Publications, Variants

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

Additional Datasets

These datasets are minimally curated and are sorted alphabetically by title.

  1. The Connectivity Map: using gene-expression signatures to connect small molecules, genes, and disease

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00590
KEGG Compound ID:
C06970
PubChem Compound ID:
3157
PubChem Substance ID:
9184

Common Searches

Search PubMed
Search Medline Plus
Search PubChem
Search CTD

Non-Curated Publications

A list of non-curated publications that mention this drug is available.

PharmGKB integrates drug information from different sources: DrugBank, Open Eye Scientific Software.
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