- Overview
- Properties
- Genetics
- Related Genes
- Related Drugs
- Related Diseases
- Datasets
- Downloads/LinkOuts
Overview
| IUPAC Name: | [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-(2,3-dihydro-1,4-benzodioxin-2-yl)methanone |
|---|---|
| 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]
Indication
For treatment and management of Hypertension and urinary obstruction symptoms of BPH.
ATC Therapeutic Category
- C02CA:Alpha-adrenoreceptor antagonists
Pharmacology and Interactions
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.
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, in vitro, 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.
Food Interactions
Avoid alcohol. Avoid natural licorice. Take without regard to meals.
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic.
Protein Binding
98%
Absorption
65%
Half Life
22 hours
Toxicity
Symptoms of overdose include hypotension. Oral LD50 is greater than 1000 mg/kg in mice and rats.
Chemical Properties
Chemical Formula:
C23H25N5O5
SMILES Code:
COc1cc2c(cc1OC)nc(nc2N)N3CCN(CC3)C(=O)C4COc5ccccc5O4
(Format: OpenEye Isomeric)
Molecular Weight ( average / monoisotopic )
451.4751 / 451.1856
Curated Annotations (
)
-
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
Curated Information
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
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ACE |
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Publications |
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ADD1 |
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Publications |
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CLCN6 |
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Variants |
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NPPA |
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Publications, Variants |
Non-Curated Information
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
Non-Curated Information
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| tadalafil | Risk of significant hypotension with this association |
| vardenafil | Risk of significant hypotension with this association |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
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Cardiovascular Diseases |
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Publications, Variants |
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Coronary Disease |
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Publications, Variants |
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Death |
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Publications |
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Heart Failure |
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Publications |
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Hypertension |
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Publications |
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Myocardial Infarction |
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Publications |
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Stroke |
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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.
LinkOuts
Common Searches
Search PubMed
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.
