Drug nameTamsulosin
DescriptionTamsulosin is a selective antagonist at alpha-1A and alpha-1B-adrenoceptors in the prostate, prostatic capsule, prostatic urethra, and bladder neck. At least three discrete alpha1-adrenoceptor subtypes have been identified: alpha-1A, alpha-1B and alpha-1D; their distribution differs between human organs and tissue. Approximately 70% of the alpha1-receptors in human prostate are of the alpha-1A subtype. Blockage of these receptors causes relaxation of smooth muscles in the bladder neck and prostate.
DrugBankPrimary Accession Number: DB00706
DIN02238123
TypeApproved, Investigational, Small Molecule
IndicationUsed in the treatment of signs and symptoms of benign prostatic hyperplasia.
Mechanism of ActionTamsulosin is a selective antagonist at alpha-1A and alpha-1B-adrenoceptors in the prostate, prostatic capsule, prostatic urethra, and bladder neck. At least three discrete alpha1-adrenoceptor subtypes have been identified: alpha-1A, alpha-1B and alpha-1D; their distribution differs between human organs and tissue. Approximately 70% of the alpha1-receptors in human prostate are of the alpha-1A subtype. Blockage of these receptors causes relaxation of smooth muscles in the bladder neck and prostate.
AbsorptionAbsorption of tamsulosin HCI from capsules 0.4 mg is essentially complete (>90%) following oral administration under fasting conditions.
ToxicityLD50 = 650 mg/kg (in rats)
Protein Binding94%-99%
Interactions
RXListhttp://www.rxlist.com/cgi/generic2/tamsul.htm
KEGGdrug: Not available / compound: C07124
PubChemcompound: 129211 / substance: 668003
PharmGKBNot available
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
Alpha-1-acid glycoprotein 1ORM15004A1AG1_HUMANrs3182041 rs1126801 rs11552135 rs11552130 rs3182034 rs1803077 rs1803076 rs1766074 rs1126810 rs1126746 rs1126724 rs1126721 rs1126718 rs1126712 rs1126708
FilesDB00706.mol | DB00706_2005-10-01.pdf | DB00706_417.pdf | pdb_830247625473-0.pdb | sdf_4026081614996-0.sdf |
Smilesisomeric:
CCOC1=CC=CC=C1OCCN[C@H](C)CC1=CC(=C(OC)C=C1)S(N)(=O)=O
canonical:
CCOC1=CC=CC=C1OCCNC(C)CC1=CC(=C(OC)C=C1)S(N)(=O)=O

© 2010-2020 All rights reserved. King Abdullah University of Science and Technology, All rights reserved