Drug nameTerazosin
DescriptionTerazosin 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.
DrugBankPrimary Accession Number: DB01162
DIN02243749
TypeApproved, Small Molecule
IndicationFor the treatment of symptomatic benign prostatic hyperplasia (BPH) and also for hypertension.
Mechanism of ActionTerazosin 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.
AbsorptionEssentially completely absorbed in man (90% bioavailability).
ToxicityLD50=259.3mg/kg (i.v. in mice)
Protein Binding90-94%
Interactions
RXListhttp://www.rxlist.com/cgi/generic/teraz.htm
KEGGdrug: Not available / compound: C07127
PubChemcompound: 5401 / substance: 9337
PharmGKBPA451612
Metabolizing Enzymes
NameGeneEntrezIDUniprotSNP
Target
NameGeneEntrezIDSwissprotSNP
Alpha-1A adrenergic receptorADRA1A148ADA1A_HUMANrs56318220 rs56233953 rs59765666 rs1048101 rs56394436 rs7833704 rs3730287 rs3730247 rs2229126 rs2229125 rs2229124 rs1496121 rs1383914 rs1048102
Alpha-1B adrenergic receptorADRA1B147ADA1B_HUMANrs34322837 rs8192450 rs8192448 rs3730284 rs3729604 rs2229181
Alpha-1D adrenergic receptorADRA1D146ADA1D_HUMANrs55915202 rs55926349 rs35105284 rs3803964
FilesDB01162.mol | DB01162_2004-06-01.pdf | pdb_9401250824834-0.pdb | sdf_9003649514996-0.sdf |
Smilesisomeric:
COC1=C(OC)C=C2C(N)=NC(=NC2=C1)N1CCN(CC1)C(=O)[C@H]1CCCO1
canonical:
COC1=C(OC)C=C2C(N)=NC(=NC2=C1)N1CCN(CC1)C(=O)C1CCCO1

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