Drug/Small Molecule:
terazosin

2D structure

Overview

Generic Names: Abbott 45975; Terazosin HCl; Terazosin hydrochloride; Terazosina [INN-Spanish]; Terazosine; Terazosine [INN-French]; Terazosinum [INN-Latin]; Trazosin HCl
Trade Names: Blavin; Flumarc; Fosfomic; Heitrin; Hytracin; Hytrin; Hytrinex; Itrin; Urodie; Vasocard; Vasomet; Vicard
PharmGKB Accession Id: PA451612

Description

Terazosin is a selective alpha 1 antagonist used for treatment of symptoms of prostate enlargement (BPH). It also acts to lower blood pressure, so it is a drug of choice for men with hypertension and prostate enlargement. It works by blocking the action of adrenaline on smooth muscle of the bladder and the blood vessel walls. (source: Drug Bank)

Indication

For the treatment of symptomatic benign prostatic hyperplasia (BPH) and also for hypertension. (source: Drug Bank)

ATC Therapeutic Category

  • G04CA:Alpha-adrenoreceptor antagonists

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Terazosin selectively and competitively inhibits vascular postsynaptic alpha(1)-adrenergic receptors, resulting in peripheral vasodilation and a reduction of vascular resistance and blood pressure. Unlike the nonselective alph-adrenergic blockers phenoxybenzamine and phentolamine, terazosin does not block presynaptic alpha(2)-receptors and, hence, does not cause reflex activation of norepinephrine release to produce reflex tachycardia. (source: Drug Bank)

Pharmacology

Terazosin, classified as a quinazoline, is similar to doxazosin and prazosin. As an alpha-adrenergic blocking agent, terazosin is used to treat hypertension and benign prostatic hypertrophy (BPH). Terazosin produces vasodilation and reduces peripheral resistance but in general has slight effect on cardiac output. Antihypertensive effect with chronic dosing is usually not accompanied by reflex tachycardia. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic. One of the four metabolites identified (piperazine derivative of terazosin) has antihypertensive activity. (source: Drug Bank)

Protein Binding

90-94% (source: Drug Bank)

Absorption

Essentially completely absorbed in man (90% bioavailability). (source: Drug Bank)

Toxicity

LD<sub>50</sub>=259.3mg/kg (i.v. in mice) (source: Drug Bank)

Isomeric SMILES Code:

COc1cc2c(cc1OC)nc(nc2N)N3CCN(CC3)C(=O)C4CCCO4 (source: Drug Bank)

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Not annotated
CYP3A
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  • PK
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Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A4
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  • PK
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Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A5
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  • PK
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Publications

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)

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB01162
KEGG Compound ID:
C07127
PubChem Compound ID:
5401
PubChem Substance ID:
9337

Common Searches

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Non-Curated Publications

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

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