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Tamsulosin

CHEMBL836 Phase 4 已批准 Small molecule
Half-Life
10-13 hours
Bioavailability
—
Protein Binding
—
Molecular Weight
408.5 g/mol
LogP
2.7
Phase
4

This medication relaxes the muscles in the prostate and bladder neck, making it easier for men with an enlarged prostate (BPH) to urinate. It works by blocking alpha receptors, which reduces the tension in the smooth muscle of the urinary tract. Dizziness upon standing is a common side effect, especially when first starting treatment.

分子量

408.5100 g/mol

LogP

2.70

TPSA

108.00 Ų

Lipinski 五规则

符合

治疗领域

Bladder Cancer Benign Prostatic Hyperplasia Cardiovascular Disease Pain Management Multiple Sclerosis Chronic Kidney Disease Hypertension Chronic Pain Prostate Cancer Colorectal Cancer

药物分类

G — G - Genito-Urinary System and Sex Hormones

作用机制

Selective alpha-1A adrenergic receptor antagonist.

Pharmacokinetics (PK)

Half-Life 10-13 hours

Pharmacodynamics (PD)

机制

Selective alpha-1A adrenergic receptor antagonist.

二维结构

SVG PNG

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SMILES

                    
CCOc1ccccc1OCCN[C@H](C)Cc1ccc(OC)c(S(N)(=O)=O)c1

                

                

                
                

                    
InChI

                    
InChI=1S/C20H28N2O5S/c1-4-26-17-7-5-6-8-18(17)27-12-11-22-15(2)13-16-9-10-19(25-3)20(14-16)28(21,23)24/h5-10,14-15,22H,4,11-13H2,1-3H3,(H2,21,23,24)/t15-/m1/s1

                

                

                

                    
                    

                        
Molecular Formula

                        
C20H28N2O5S

                    

                    
                    

                        
HBD / HBA

                        
2 / 7

                    

                    
                    

                        
可旋转键数

                        
11

                    

                    
                    
                    

                        
重原子数

                        
28

                    

                    
                

            


            
            

                
                

                    
                    

                        

                            ADRB2 (Beta-2 Adrenergic Receptor)
                            Antagonist
                        

                        
                        Primary Target
                        
                    

                    
                

                
            


            
            

                
                

                    
                    
                        

                            

  
  Minor


                            
                                Tamsulosin + Finasteride
                            
                        

                        
                        
Finasteride and tamsulosin are deliberately combined (as Duodart/Jalyn) for BPH treatment; the combination provides additive symptom relief with no significant adverse pharmacokinetic interaction.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Tamsulosin + Fluconazole
                            
                        

                        
                        
Fluconazole inhibits CYP3A4-mediated tamsulosin metabolism, substantially increasing tamsulosin exposure and the risk of hypotension and syncope.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Tamsulosin + Diltiazem
                            
                        

                        
                        
Diltiazem inhibits CYP3A4-mediated tamsulosin metabolism, increasing tamsulosin plasma concentrations by up to 2-fold and heightening the risk of orthostatic hypotension and dizziness.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Tamsulosin + Sildenafil
                            
                        

                        
                        
Combining tamsulosin (alpha-1 blocker) with sildenafil (PDE-5 inhibitor) produces additive vasodilation, substantially increasing the risk of symptomatic hypotension, dizziness, and syncope.

                        
                    
                    
                

                
            


            
            

                
                


    
    
        
    
    
    
No side effects recorded

    
    
Side effect data is not yet available for this drug.

    



                
            


            
            
            

                
常见问题

                

                    
                    

                        
                        

                            
This medication relaxes the muscles in the prostate and bladder neck, making it easier for men with an enlarged prostate (BPH) to urinate. It works by blocking alpha receptors, which reduces the tension in the smooth muscle of the urinary tract. Dizziness upon standing is a common side effect, especially when first starting treatment.

                        

                    

                    

                    

                    
                    

                        
                        

                            
Selective alpha-1A adrenergic receptor antagonist.

                        

                    

                    

                    
                    

                        
                        

                            
Key pharmacokinetic parameters for Tamsulosin: Half-life: 10-13 hours.

                        

                    

                    

                    

                        
                        

                            
Yes, Tamsulosin is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.

                        

                    

                

            

            

            
            

            
            
            

                
Related Drugs


                
                

                    
Same Drug Class

                    

                        
                        
                            Sildenafil
                            Small molecule
                        
                        
                        
                            Finasteride
                            Small molecule
                        
                        
                    

                

                

                
                
                
            

            

            
            
{# References & Data Sources section for drug detail pages.
   Renders standard pharmacological database links plus the drug's data_sources field. #}


    
References & Data Sources

    
    
        
        
  • 
            
            
                ChEMBL — European Bioinformatics Institute (EBI).
                CHEMBL836.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 129211.
                Chemical information database.
            
        
    • 
        
        
        
        
    

    
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.




        


        
        
    


    



    
医疗免责声明

    

        This content is for educational and informational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before making medication decisions.
    

    

        Data sources:
        ChEMBL,
        PubChem,
        DailyMed.