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Namespace Prefixes

PrefixIRI
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Statements

Subject Item
n2:DB01162
rdf:type
n3:Drug
n3:description
Terazosin is a selective alpha1-antagonist used for treatment of symptoms of benign prostatic hyperplasia (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.
n3:dosage
n13:271B4C48-363D-11E5-9242-09173F13E4C5 n13:271B4C43-363D-11E5-9242-09173F13E4C5 n13:271B4C44-363D-11E5-9242-09173F13E4C5 n13:271B4C45-363D-11E5-9242-09173F13E4C5 n13:271B4C46-363D-11E5-9242-09173F13E4C5 n13:271B4C47-363D-11E5-9242-09173F13E4C5 n13:271B4C49-363D-11E5-9242-09173F13E4C5 n13:271B4C4A-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Cushman WC, Ford CE, Cutler JA, Margolis KL, Davis BR, Grimm RH, Black HR, Hamilton BP, Holland J, Nwachuku C, Papademetriou V, Probstfield J, Wright JT Jr, Alderman MH, Weiss RJ, Piller L, Bettencourt J, Walsh SM: Success and predictors of blood pressure control in diverse North American settings: the antihypertensive and lipid-lowering treatment to prevent heart attack trial (ALLHAT). J Clin Hypertens (Greenwich). 2002 Nov-Dec;4(6):393-404. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/12461301
n3:group
approved
n3:halfLife
12 hours
n3:indication
For the treatment of symptomatic BPH and mild to moderate hypertension.
owl:sameAs
n10:DB01162 n12:DB01162
dcterms:title
Terazosin
adms:identifier
n6:Terazosin n21:46509129 n22:PA451612 n23:5401 n25:C07127 n26:0904-6126-61 n27:DB01162 n28:9445 n29:5208
n3:mechanismOfAction
In general, &alpha;<sub>1</sub>-adrenergic receptors mediate contraction and hypertrophic growth of smooth muscle cells. &alpha;<sub>1</sub>-Receptors are 7-transmembrane domain receptors coupled to G proteins, G<sub>q/11</sub>. Three &alpha;<sub>1</sub>-receptor subtypes, which share approximately 75% homology in their transmembrane domains, have been identified: &alpha;<sub>1A</sub> (chromosome 8), &alpha;<sub>1B</sub> (chromosome 5), and &alpha;<sub>1D</sub> (chromosome 20). Terazosin is the first &alpha;<sub>1</sub>-receptor antagonist to demonstrate selectivity for the &alpha;<sub>1A</sub>-receptor. All three receptor subtypes appear to be involved in maintaining vascular tone. The &alpha;<sub>1A</sub>-receptor maintains basal vascular tone while the &alpha;<sub>1B</sub>-receptor mediates the vasocontrictory effects of exogenous &alpha;<sub>1</sub>-agonists. Activation of &alpha;<sub>1</sub>-receptors activates G<sub>q</sub>-proteins, which results in intracellular stimulation of phospholipases C, A<sub>2</sub>, and D. This results in mobilization of Ca<sup>2+</sup> from intracellular stores, activation of mitogen-activated kinase and PI<sub>3</sub> kinase pathways and subsequent vasoconstriction. Terozosin produces its pharmacological effects by inhibiting &alpha;<sub>1A</sub>-receptor activation. Inhibition of these receptors in the vasculature and prostate results in muscle relaxation, decreased blood pressure and improved urinary outflow in symptomatic benign prostatic hyperplasia.
n3:packager
n7:271B4C11-363D-11E5-9242-09173F13E4C5 n7:271B4C12-363D-11E5-9242-09173F13E4C5 n7:271B4C10-363D-11E5-9242-09173F13E4C5 n7:271B4C0C-363D-11E5-9242-09173F13E4C5 n7:271B4C15-363D-11E5-9242-09173F13E4C5 n7:271B4C0D-363D-11E5-9242-09173F13E4C5 n7:271B4C16-363D-11E5-9242-09173F13E4C5 n7:271B4C0A-363D-11E5-9242-09173F13E4C5 n7:271B4C13-363D-11E5-9242-09173F13E4C5 n7:271B4C0B-363D-11E5-9242-09173F13E4C5 n7:271B4C14-363D-11E5-9242-09173F13E4C5 n7:271B4C0E-363D-11E5-9242-09173F13E4C5 n7:271B4C0F-363D-11E5-9242-09173F13E4C5 n7:271B4C04-363D-11E5-9242-09173F13E4C5 n7:271B4C05-363D-11E5-9242-09173F13E4C5 n7:271B4C02-363D-11E5-9242-09173F13E4C5 n7:271B4C03-363D-11E5-9242-09173F13E4C5 n7:271B4C08-363D-11E5-9242-09173F13E4C5 n7:271B4C09-363D-11E5-9242-09173F13E4C5 n7:271B4C06-363D-11E5-9242-09173F13E4C5 n7:271B4C07-363D-11E5-9242-09173F13E4C5 n7:271B4C19-363D-11E5-9242-09173F13E4C5 n7:271B4C1A-363D-11E5-9242-09173F13E4C5 n7:271B4C17-363D-11E5-9242-09173F13E4C5 n7:271B4C18-363D-11E5-9242-09173F13E4C5 n7:271B4C1B-363D-11E5-9242-09173F13E4C5 n7:271B4C1C-363D-11E5-9242-09173F13E4C5 n7:271B4C1E-363D-11E5-9242-09173F13E4C5 n7:271B4C1F-363D-11E5-9242-09173F13E4C5 n7:271B4C1D-363D-11E5-9242-09173F13E4C5 n7:271B4C00-363D-11E5-9242-09173F13E4C5 n7:271B4C01-363D-11E5-9242-09173F13E4C5 n7:271B4BFE-363D-11E5-9242-09173F13E4C5 n7:271B4BFF-363D-11E5-9242-09173F13E4C5 n7:271B4C22-363D-11E5-9242-09173F13E4C5 n7:271B4C23-363D-11E5-9242-09173F13E4C5 n7:271B4C20-363D-11E5-9242-09173F13E4C5 n7:271B4C21-363D-11E5-9242-09173F13E4C5 n7:271B4C26-363D-11E5-9242-09173F13E4C5 n7:271B4C24-363D-11E5-9242-09173F13E4C5 n7:271B4C25-363D-11E5-9242-09173F13E4C5
n3:patent
n8:5212176 n8:5294615
n3:routeOfElimination
Approximately 10% of an orally administered dose is excreted as parent drug in the urine and approximately 20% is excreted in the feces.
n3:synonym
1-(4-Amino-6,7-dimethoxy-2-quinazolinyl)-4-((tetrahydro-2-furanyl)carbonyl)piperazine Terazosina Terazosine Terazosin Terazosinum
n3:toxicity
LD<sub>50</sub>=259.3mg/kg (IV in mice)
n19:hasAHFSCode
n20:24-20-00
n3:proteinBinding
90-94%
n3:salt
n3:synthesisReference
K. S. Keshava Murthy, Gamini Weeratunga, Tianhao Zhou, Bhaskar Reddy Guntoori, "Process for the manufacture of intermediates suitable to make doxazosin, terazosin, prazosin, tiodazosin and related antihypertensive medicines." U.S. Patent US5919931, issued September, 1986.
n17:hasConcept
n18:M0528343
foaf:page
n16:terazosin.html n24:teraz.htm
n3:IUPAC-Name
n4:271B4C4F-363D-11E5-9242-09173F13E4C5
n3:InChI
n4:271B4C55-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n4:271B4C54-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n4:271B4C51-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n4:271B4C52-363D-11E5-9242-09173F13E4C5
n3:SMILES
n4:271B4C53-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n4:271B4C4D-363D-11E5-9242-09173F13E4C5 n4:271B4C65-363D-11E5-9242-09173F13E4C5
n3:logP
n4:271B4C4B-363D-11E5-9242-09173F13E4C5 n4:271B4C4E-363D-11E5-9242-09173F13E4C5 n4:271B4C67-363D-11E5-9242-09173F13E4C5
n3:logS
n4:271B4C4C-363D-11E5-9242-09173F13E4C5
n19:hasATCCode
n30:G04CA03
n3:H-Bond-Acceptor-Count
n4:271B4C5B-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n4:271B4C5C-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n4:271B4C56-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n4:271B4C57-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n4:271B4C59-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n4:271B4C58-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n4:271B4C5A-363D-11E5-9242-09173F13E4C5
n3:absorption
Essentially completely absorbed in man (90% bioavailability).
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
63590-64-7
n3:category
n3:containedIn
n11:271B4C36-363D-11E5-9242-09173F13E4C5 n11:271B4C37-363D-11E5-9242-09173F13E4C5 n11:271B4C34-363D-11E5-9242-09173F13E4C5 n11:271B4C35-363D-11E5-9242-09173F13E4C5 n11:271B4C3A-363D-11E5-9242-09173F13E4C5 n11:271B4C3B-363D-11E5-9242-09173F13E4C5 n11:271B4C38-363D-11E5-9242-09173F13E4C5 n11:271B4C39-363D-11E5-9242-09173F13E4C5 n11:271B4C2E-363D-11E5-9242-09173F13E4C5 n11:271B4C2F-363D-11E5-9242-09173F13E4C5 n11:271B4C2C-363D-11E5-9242-09173F13E4C5 n11:271B4C2D-363D-11E5-9242-09173F13E4C5 n11:271B4C32-363D-11E5-9242-09173F13E4C5 n11:271B4C33-363D-11E5-9242-09173F13E4C5 n11:271B4C30-363D-11E5-9242-09173F13E4C5 n11:271B4C31-363D-11E5-9242-09173F13E4C5 n11:271B4C3E-363D-11E5-9242-09173F13E4C5 n11:271B4C3F-363D-11E5-9242-09173F13E4C5 n11:271B4C3C-363D-11E5-9242-09173F13E4C5 n11:271B4C3D-363D-11E5-9242-09173F13E4C5 n11:271B4C42-363D-11E5-9242-09173F13E4C5 n11:271B4C40-363D-11E5-9242-09173F13E4C5 n11:271B4C41-363D-11E5-9242-09173F13E4C5 n11:271B4C27-363D-11E5-9242-09173F13E4C5 n11:271B4C2A-363D-11E5-9242-09173F13E4C5 n11:271B4C2B-363D-11E5-9242-09173F13E4C5 n11:271B4C28-363D-11E5-9242-09173F13E4C5 n11:271B4C29-363D-11E5-9242-09173F13E4C5
n3:Bioavailability
n4:271B4C61-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n4:271B4C63-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n4:271B4C64-363D-11E5-9242-09173F13E4C5
n3:Melting-Point
n4:271B4C66-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n4:271B4C60-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n4:271B4C5F-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n4:271B4C62-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n4:271B4C50-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n4:271B4C5D-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n4:271B4C5E-363D-11E5-9242-09173F13E4C5