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Digoxin

CHEMBL1751 Phase 4 承認済み Small molecule
Half-Life
36-48 hours
Bioavailability
—
Protein Binding
—
Molecular Weight
780.9 g/mol
LogP
1.3
Phase
4

Extracted from the foxglove plant, digoxin is a cardiac glycoside used to strengthen the failing heart's contraction and to slow the ventricular rate in atrial fibrillation and flutter. It inhibits the sodium-potassium ATPase pump in heart muscle, which indirectly raises intracellular calcium and increases the force of each beat, while its effects on the vagus nerve slow conduction through the atrioventricular node. A large steroidal glycoside (C41H64O14) with a long half-life of roughly 36 to 48 hours, it is notable for a narrow therapeutic window: concentrations only modestly above the effective range can provoke dangerous rhythm disturbances, so blood levels are monitored. One of the oldest heart medicines still in use, digoxin remains an approved option for selected patients with heart failure and rate control.

A cardiac glycoside derived from the foxglove plant used to treat heart failure and control heart rate in atrial fibrillation and flutter. It works by inhibiting the sodium-potassium ATPase pump, increasing the calcium available for heart muscle contraction. It has a narrow therapeutic window and blood levels must be monitored to avoid toxicity, which can cause dangerous heart rhythm disturbances.

分子量

780.9430 g/mol

LogP

1.30

TPSA

203.00 Ų

リピンスキーの五則

不適合

治療領域

Pancreatic Cancer Endometriosis Cardiovascular Disease Pain Management Non-Small Cell Lung Cancer Rheumatoid Arthritis Chronic Obstructive Pulmonary Disease Epilepsy Schizophrenia Bipolar Disorder Melanoma Non-Alcoholic Fatty Liver Disease Stroke Obesity Type 2 Diabetes Hypertension Major Depressive Disorder Breast Cancer Chronic Pain Hepatitis C Tuberculosis Heart Failure Atrial Fibrillation Prostate Cancer Leukemia

薬物分類

C — C - Cardiovascular System

作用機序

Inhibits Na+/K+-ATPase, increasing intracellular calcium.

Pharmacokinetics (PK)

Half-Life 36-48 hours

Pharmacodynamics (PD)

機序

Inhibits Na+/K+-ATPase, increasing intracellular calcium.

2D構造

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
Embed this structure

                        

                        

                            
                            
                        

                    

                

                

                
                

                    
SMILES

                    
C[C@H]1O[C@@H](O[C@H]2[C@@H](O)C[C@H](O[C@H]3[C@@H](O)C[C@H](O[C@H]4CC[C@@]5(C)[C@H](CC[C@@H]6[C@@H]5C[C@@H](O)[C@]5(C)[C@@H](C7=CC(=O)OC7)CC[C@]65O)C4)O[C@@H]3C)O[C@@H]2C)C[C@H](O)[C@@H]1O

                

                

                
                

                    
InChI

                    
InChI=1S/C41H64O14/c1-19-36(47)28(42)15-34(50-19)54-38-21(3)52-35(17-30(38)44)55-37-20(2)51-33(16-29(37)43)53-24-8-10-39(4)23(13-24)6-7-26-27(39)14-31(45)40(5)25(9-11-41(26,40)48)22-12-32(46)49-18-22/h12,19-21,23-31,33-38,42-45,47-48H,6-11,13-18H2,1-5H3/t19-,20-,21-,23-,24+,25-,26-,27+,28+,29+,30+,31-,33+,34+,35+,36-,37-,38-,39+,40+,41+/m1/s1

                

                

                

                    
                    

                        
Molecular Formula

                        
C41H64O14

                    

                    
                    

                        
HBD / HBA

                        
6 / 14

                    

                    
                    

                        
回転可能結合数

                        
7

                    

                    
                    
                    

                        
重原子数

                        
55

                    

                    
                

            


            
            

                
                

                    
                    

                        

                            ABCB1 (P-glycoprotein)
                            Substrate
                        

                        
                        Primary Target
                        
                    

                    
                    

                        

                            ADRB1 (Beta-1 Adrenergic Receptor)
                            Other
                        

                        
                    

                    
                

                
            


            
            

                
                

                    
                    
                        

                            

  
  Minor


                            
                                Digoxin + Valsartan
                            
                        

                        
                        
Valsartan may slightly increase digoxin plasma levels by reducing its renal clearance; the interaction is generally modest.

                        
                    
                    
                    
                        

                            

  
  Minor


                            
                                Digoxin + Sitagliptin
                            
                        

                        
                        
Sitagliptin modestly increases digoxin exposure through inhibition of P-glycoprotein-mediated renal tubular secretion, though the effect is unlikely to be clinically significant at therapeutic digoxin doses.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Digoxin + Spironolactone
                            
                        

                        
                        
Spironolactone can increase digoxin levels by reducing its renal clearance and may cross-react with some digoxin immunoassays, confounding monitoring.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Digoxin + Diltiazem
                            
                        

                        
                        
Diltiazem significantly increases digoxin plasma levels through P-gp inhibition and may additionally slow AV nodal conduction, exacerbating bradycardia or heart block.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Digoxin + Furosemide
                            
                        

                        
                        
Furosemide-induced hypokalemia and hypomagnesemia increase the risk of digoxin toxicity even when digoxin levels remain within the conventional therapeutic range.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Digoxin + Metoprolol
                            
                        

                        
                        
Metoprolol adds to digoxin's rate-slowing effect at the AV node, increasing the risk of bradycardia and AV block in susceptible patients.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Digoxin + Albuterol
                            
                        

                        
                        
Albuterol-induced hypokalaemia can potentiate digoxin toxicity by increasing myocardial sensitivity to digoxin at any given plasma concentration.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Digoxin + Carvedilol
                            
                        

                        
                        
Carvedilol increases digoxin plasma concentrations through P-gp inhibition and adds negative chronotropic and dromotropic effects, increasing the risk of bradycardia and AV block.

                        
                    
                    
                

                
            


            
            

                
                


    
    
        
    
    
    
No side effects recorded

    
    
Side effect data is not yet available for this drug.

    



                
            


            
            
            

                
よくある質問

                

                    
                    

                        
                        

                            
A cardiac glycoside derived from the foxglove plant used to treat heart failure and control heart rate in atrial fibrillation and flutter. It works by inhibiting the sodium-potassium ATPase pump, increasing the calcium available for heart muscle contraction. It has a narrow therapeutic window and blood levels must be monitored to avoid toxicity, which can cause dangerous heart rhythm disturbances.

                        

                    

                    

                    

                    
                    

                        
                        

                            
Inhibits Na+/K+-ATPase, increasing intracellular calcium.

                        

                    

                    

                    
                    

                        
                        

                            
Key pharmacokinetic parameters for Digoxin: Half-life: 36-48 hours.

                        

                    

                    

                    

                        
                        

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

                        

                    

                

            

            

            
            

            
            
            

                
Related Drugs


                
                

                    
Same Drug Class

                    

                        
                        
                            Atorvastatin
                            Small molecule
                        
                        
                        
                            Amlodipine
                            Small molecule
                        
                        
                        
                            Lisinopril
                            Small molecule
                        
                        
                        
                            Metoprolol
                            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).
                CHEMBL1751.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 2724385.
                Chemical information database.
            
        
    • 
        
        
        
        
    

    
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-04.




        


        
        
    


    



    
医学的免責事項

    

        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.