digoxin Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
882 20830-75-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • digoxin
  • cardiogoxin
  • digoxine
A cardiotonic glycoside obtained mainly from Digitalis lanata; it consists of three sugars and the aglycone DIGOXIGENIN. Digoxin has positive inotropic and negative chronotropic activity. It is used to control ventricular rate in ATRIAL FIBRILLATION and in the management of congestive heart failure with atrial fibrillation. Its use in congestive heart failure and sinus rhythm is less certain. The margin between toxic and therapeutic doses is small. (From Martindale, The Extra Pharmacopoeia, 30th ed, p666)
  • Molecular weight: 780.95
  • Formula: C41H64O14
  • CLOGP: 1.42
  • LIPINSKI: 3
  • HAC: 14
  • HDO: 6
  • TPSA: 203.06
  • ALOGS: -3.79
  • ROTB: 7

Drug dosage:

DoseUnitRoute
0.25 mg O
0.25 mg P

Approvals:

DateAgencyCompanyOrphan
Oct. 24, 1975 FDA EUROHLTH INTL SARL

FDA Adverse Event Reporting System

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Toxicity to various agents 4136.96 55.05 1041 2990 46013 3335815
Bradycardia 3177.03 55.05 697 3334 15972 3365856
Cardioactive drug level increased 2159.30 55.05 302 3729 209 3381619
Acute kidney injury 996.38 55.05 359 3672 49324 3332504
Nausea 931.78 55.05 449 3582 129196 3252632
Atrial fibrillation 919.54 55.05 283 3748 23658 3358170
Vomiting 852.91 55.05 378 3653 89153 3292675
Hyperkalaemia 812.26 55.05 218 3813 11076 3370752
Dizziness 775.74 55.05 338 3693 76174 3305654
Drug interaction 715.60 55.05 278 3753 46534 3335294
Hypotension 637.65 55.05 260 3771 49254 3332574
Asthenia 598.84 55.05 270 3761 65395 3316433
Overdose 497.03 55.05 196 3835 33782 3348046
Decreased appetite 485.96 55.05 204 3827 41286 3340542
Heart rate decreased 416.73 55.05 110 3921 5168 3376660
Renal failure 415.65 55.05 171 3860 32769 3349059
Dehydration 375.14 55.05 160 3871 33489 3348339
International normalised ratio increased 371.77 55.05 127 3904 14488 3367340
Dyspnoea 368.90 55.05 227 3804 102707 3279121
Ventricular tachycardia 363.48 55.05 101 3930 5761 3376067
Syncope 350.13 55.05 141 3890 25492 3356336
Atrioventricular block 342.99 55.05 79 3952 2085 3379743
Confusional state 334.16 55.05 153 3878 37845 3343983
Atrioventricular block complete 312.99 55.05 75 3956 2357 3379471
Fatigue 305.77 55.05 205 3826 107035 3274793
Cardioactive drug level above therapeutic 299.84 55.05 41 3990 16 3381812
Cardiac failure 289.57 55.05 115 3916 19990 3361838
Arrhythmia 278.44 55.05 94 3937 10303 3371525
Medication error 273.90 55.05 96 3935 11775 3370053
Bradyarrhythmia 271.19 55.05 52 3979 539 3381289
Blood creatinine increased 263.48 55.05 110 3921 21708 3360120
Nodal rhythm 255.84 55.05 50 3981 577 3381251
Drug level increased 252.87 55.05 72 3959 4473 3377355
Completed suicide 241.25 55.05 115 3916 30999 3350829
Product quality issue 232.50 55.05 107 3924 26628 3355200
Cardiac arrest 230.29 55.05 107 3924 27212 3354616
Fall 222.89 55.05 135 3896 58748 3323080
Sinus bradycardia 222.04 55.05 61 3970 3318 3378510
Malaise 220.27 55.05 139 3892 65038 3316790
Blood potassium increased 215.79 55.05 62 3969 3974 3377854
Foetal exposure during pregnancy 203.11 55.05 83 3948 15468 3366360
Renal impairment 200.09 55.05 86 3945 18175 3363653
Ventricular extrasystoles 197.33 55.05 56 3975 3431 3378397
Diarrhoea 195.26 55.05 155 3876 104193 3277635
Visual impairment 193.29 55.05 78 3953 14068 3367760
Torsade de pointes 191.23 55.05 53 3978 2976 3378852
Atrioventricular block second degree 186.27 55.05 43 3988 1141 3380687
Premature baby 180.01 55.05 62 3969 7191 3374637
Atrioventricular block first degree 177.68 55.05 44 3987 1584 3380244
Cardiac murmur 169.26 55.05 47 3984 2656 3379172
Vision blurred 168.84 55.05 78 3953 19511 3362317
Lethargy 166.70 55.05 70 3961 13945 3367883
Ventricular fibrillation 164.03 55.05 51 3980 4282 3377546
Nodal arrhythmia 162.06 55.05 32 3999 390 3381438
Cardiac failure congestive 159.92 55.05 86 3945 29736 3352092
General physical health deterioration 152.92 55.05 74 3957 20515 3361313
Adverse drug reaction 150.45 55.05 58 3973 9253 3372575
Loss of consciousness 147.62 55.05 80 3951 28067 3353761
Xanthopsia 141.71 55.05 23 4008 78 3381750
Atrial flutter 135.19 55.05 39 3992 2529 3379299
Hypokalaemia 131.58 55.05 59 3972 13746 3368082
Abdominal pain 129.85 55.05 88 3943 46137 3335691
Blood urea increased 128.95 55.05 49 3982 7511 3374317
Palpitations 127.98 55.05 64 3967 19019 3362809
Electrocardiogram QT prolonged 118.61 55.05 51 3980 10744 3371084
Venous pressure jugular increased 118.35 55.05 21 4010 135 3381693
Cardioactive drug level decreased 118.09 55.05 17 4014 17 3381811
Condition aggravated 118.09 55.05 78 3953 39155 3342673
Hyponatraemia 115.56 55.05 59 3972 18300 3363528
Cardiogenic shock 115.42 55.05 38 3993 3828 3378000
Mental status changes 111.67 55.05 48 3983 10099 3371729
Heart rate increased 110.30 55.05 53 3978 14433 3367395
Electrocardiogram ST segment depression 110.27 55.05 27 4004 925 3380903
Electrocardiogram abnormal 104.08 55.05 31 4000 2246 3379582
Left ventricular dysfunction 100.71 55.05 29 4002 1866 3379962
Weight decreased 99.96 55.05 71 3960 40040 3341788
Tachycardia 99.54 55.05 58 3973 23313 3358515
Cardiomegaly 99.52 55.05 35 3996 4303 3377525
Cardioactive drug level below therapeutic 98.34 55.05 13 4018 1 3381827
Blood pressure decreased 97.44 55.05 48 3983 13788 3368040
Atrial tachycardia 97.40 55.05 22 4009 527 3381301
Bundle branch block right 96.93 55.05 28 4003 1822 3380006
Heart rate irregular 96.52 55.05 32 3999 3292 3378536
Chronic kidney disease 93.25 55.05 37 3994 6355 3375473
Death 93.15 55.05 124 3907 152200 3229628
Hypophagia 91.63 55.05 36 3995 6025 3375803
Oedema peripheral 88.31 55.05 62 3969 34299 3347529
Bundle branch block left 88.23 55.05 25 4006 1517 3380311
Supraventricular extrasystoles 84.07 55.05 23 4008 1226 3380602
Cardiac disorder 83.13 55.05 43 3988 13676 3368152
Intentional overdose 81.71 55.05 44 3987 15181 3366647
Somnolence 80.17 55.05 57 3974 32147 3349681
Disorientation 80.10 55.05 38 3993 10041 3371787
Hypersensitivity myocarditis 79.17 55.05 12 4019 22 3381806
Electrocardiogram QRS complex prolonged 77.81 55.05 22 4009 1324 3380504
Cardio-respiratory arrest 75.60 55.05 42 3989 15398 3366430
Ejection fraction decreased 74.73 55.05 28 4003 4119 3377709
Suicide attempt 74.58 55.05 42 3989 15805 3366023
Dyspnoea exertional 73.84 55.05 32 3999 6854 3374974
Maternal exposure during pregnancy 73.38 55.05 36 3995 10235 3371593
Oedema 72.05 55.05 40 3991 14640 3367188
Supraventricular tachycardia 69.85 55.05 25 4006 3231 3378597
Incorrect dose administered 68.52 55.05 38 3993 13876 3367952
Presyncope 68.42 55.05 28 4003 5203 3376625
Feeling abnormal 64.54 55.05 47 3984 27478 3354350
Myocardial infarction 64.29 55.05 57 3974 44076 3337752
Hypomagnesaemia 63.09 55.05 24 4007 3678 3378150
Orthostatic hypotension 62.62 55.05 26 4005 5010 3376818
Hallucination, visual 62.11 55.05 25 4006 4451 3377377
Blood pressure diastolic decreased 61.83 55.05 19 4012 1528 3380300
Chromatopsia 60.86 55.05 13 4018 238 3381590
Metabolic acidosis 60.41 55.05 30 4001 8748 3373080
Diabetic metabolic decompensation 59.02 55.05 11 4020 96 3381732
Chest pain 56.63 55.05 51 3980 40224 3341604
Drug ineffective 56.62 55.05 85 3946 116005 3265823
Hallucination 56.45 55.05 33 3998 13307 3368521
Low birth weight baby 56.26 55.05 18 4013 1652 3380176
Pulmonary hypertension 56.20 55.05 26 4005 6484 3375344

Pharmacologic Action:

SourceCodeDescription
ATC C01AA05 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
CARDIAC GLYCOSIDES
Digitalis glycosides
FDA EPC N0000175568 Cardiac Glycoside
FDA Chemical/Ingredient N0000008157 Cardiac Glycosides
MeSH PA D000889 Anti-Arrhythmia Agents
MeSH PA D002316 Cardiotonic Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D020011 Protective Agents
CHEBI has role CHEBI:38070 anti-arrhythmia drug
CHEBI has role CHEBI:38147 cardiotonic drug

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Poisoning by digitalis glycoside indication 12876009
Chronic heart failure indication 48447003
Atrial fibrillation indication 49436004 DOID:0060224
Senile cardiac amyloidosis contraindication 16573007
Myocardial infarction contraindication 22298006 DOID:5844
Sick sinus syndrome contraindication 36083008 DOID:13884
Myxedema contraindication 43153006 DOID:11634
Hypokalemia contraindication 43339004
Sinus bradycardia contraindication 49710005
Myocarditis contraindication 50920009 DOID:820
Acute nephropathy contraindication 58574008
Hypercalcemia contraindication 66931009 DOID:12678
Ventricular fibrillation contraindication 71908006
Wolff-Parkinson-White pattern contraindication 74390002 DOID:384
Cor pulmonale contraindication 83291003 DOID:8515
Constrictive pericarditis contraindication 85598007 DOID:11481
Kidney disease contraindication 90708001 DOID:2527
Hypomagnesemia contraindication 190855004
Atrioventricular block contraindication 233917008 DOID:0050820
Idiopathic hypertrophic subaortic stenosis contraindication 360465008
Restrictive cardiomyopathy contraindication 415295002 DOID:397

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Sodium/potassium-transporting ATPase Transporter INHIBITOR IC50 6.40 CHEMBL CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 4.14 WOMBAT-PK
Signal transducer and activator of transcription 3 Transcription factor IC50 5.73 CHEMBL
Nuclear receptor ROR-gamma Nuclear hormone receptor IC50 5.70 CHEMBL
Sodium/potassium-transporting ATPase subunit alpha-1 Transporter IC50 6.30 CHEMBL
Sodium/potassium-transporting ATPase subunit alpha-2 Ion channel IC50 5.78 DRUG MATRIX
Nuclear receptor ROR-gamma Unclassified IC50 5.70 CHEMBL

External reference:

IDSource
DB00390 DRUGBANK_ID
4726 IUPHAR_LIGAND_ID
4018047 VUID
N0000146388 NUI
C0012265 UMLSCUI
D00298 KEGG_DRUG
73K4184T59 UNII
389 INN_ID
1413 MMSL
3407 RXNORM
387461009 SNOMEDCT_US
796001 SNOMEDCT_US
4597 MMSL
d00210 MMSL
4018047 VANDF
N0000005903 NDFRT
N0000146388 NDFRT
000593 NDDF
CHEMBL1751 ChEMBL_ID
D004077 MESH_DESCRIPTOR_UI
2724385 PUBCHEM_CID
CHEBI:4551 CHEBI
DGX PDB_CHEM_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Digoxin HUMAN PRESCRIPTION DRUG LABEL 1 0054-0057 SOLUTION 0.05 mg ORAL NDA 16 sections
Digoxin HUMAN PRESCRIPTION DRUG LABEL 1 0115-9811 TABLET 125 ug ORAL ANDA 17 sections
Digoxin HUMAN PRESCRIPTION DRUG LABEL 1 0115-9822 TABLET 250 ug ORAL ANDA 17 sections
Digoxin HUMAN PRESCRIPTION DRUG LABEL 1 0143-1240 TABLET 125 ug ORAL ANDA 16 sections
Digoxin HUMAN PRESCRIPTION DRUG LABEL 1 0143-1241 TABLET 250 ug ORAL ANDA 16 sections
DIGITEK HUMAN PRESCRIPTION DRUG LABEL 1 0378-6155 TABLET 0.13 mg ORAL ANDA 16 sections
DIGITEK HUMAN PRESCRIPTION DRUG LABEL 1 0378-6156 TABLET 0.25 mg ORAL ANDA 16 sections
DIGOX HUMAN PRESCRIPTION DRUG LABEL 1 0527-1324 TABLET 125 ug ORAL ANDA 11 sections
DIGOX HUMAN PRESCRIPTION DRUG LABEL 1 0527-1325 TABLET 250 ug ORAL ANDA 11 sections
Digoxin HUMAN PRESCRIPTION DRUG LABEL 1 0615-0518 TABLET 250 ug ORAL ANDA 12 sections
Digoxin HUMAN PRESCRIPTION DRUG LABEL 1 0615-0547 TABLET 0.13 mg ORAL ANDA 12 sections
Digoxin HUMAN PRESCRIPTION DRUG LABEL 1 0615-7729 TABLET 125 ug ORAL ANDA 11 sections
Digoxin HUMAN PRESCRIPTION DRUG LABEL 1 0615-7730 TABLET 250 ug ORAL ANDA 11 sections
DIGOXIN HUMAN PRESCRIPTION DRUG LABEL 1 0615-7935 TABLET 0.13 mg ORAL NDA AUTHORIZED GENERIC 17 sections
Digoxin HUMAN PRESCRIPTION DRUG LABEL 1 0641-1410 INJECTION 0.25 mg INTRAMUSCULAR ANDA 16 sections
Digoxin HUMAN PRESCRIPTION DRUG LABEL 1 0641-6184 INJECTION 0.25 mg INTRAMUSCULAR ANDA 16 sections
Digoxin HUMAN PRESCRIPTION DRUG LABEL 1 0781-3059 INJECTION, SOLUTION 250 ug INTRAMUSCULAR ANDA 16 sections
Digoxin HUMAN PRESCRIPTION DRUG LABEL 1 0904-5921 TABLET 125 ug ORAL ANDA 16 sections
Digoxin HUMAN PRESCRIPTION DRUG LABEL 1 0904-5922 TABLET 250 ug ORAL ANDA 16 sections
Digoxin HUMAN PRESCRIPTION DRUG LABEL 1 16714-590 TABLET 125 ug ORAL ANDA 16 sections
Digoxin HUMAN PRESCRIPTION DRUG LABEL 1 16714-591 TABLET 250 ug ORAL ANDA 16 sections
Digoxin HUMAN PRESCRIPTION DRUG LABEL 1 17856-0057 SOLUTION 0.05 mg ORAL NDA 15 sections
Digoxin HUMAN PRESCRIPTION DRUG LABEL 1 21695-678 TABLET 0.13 mg ORAL ANDA 17 sections
LANOXIN HUMAN PRESCRIPTION DRUG LABEL 1 24987-240 TABLET 0.06 mg ORAL NDA 17 sections
LANOXIN HUMAN PRESCRIPTION DRUG LABEL 1 24987-242 TABLET 0.13 mg ORAL NDA 17 sections
LANOXIN HUMAN PRESCRIPTION DRUG LABEL 1 24987-245 TABLET 0.19 mg ORAL NDA 17 sections
LANOXIN HUMAN PRESCRIPTION DRUG LABEL 1 24987-249 TABLET 0.25 mg ORAL NDA 17 sections
LANOXIN HUMAN PRESCRIPTION DRUG LABEL 1 24987-260 INJECTION, SOLUTION 250 ug INTRAMUSCULAR NDA 16 sections
LANOXIN HUMAN PRESCRIPTION DRUG LABEL 1 24987-262 INJECTION, SOLUTION 100 ug INTRAMUSCULAR NDA 11 sections
DIGITEK HUMAN PRESCRIPTION DRUG LABEL 1 42292-002 TABLET 0.25 mg ORAL ANDA 16 sections