Details of the Drug

General Information of Drug (ID: DMQCTIH)

Drug Name
Digoxin
Synonyms
digoxin; 20830-75-5; 12beta-Hydroxydigitoxin; Digoxine; Lanoxin; Lanoxicaps; Digossina; Digoxina; Digoxinum; Digosin; Lanicor; Digacin; Dilanacin; CHEBI:4551; MLS000069819; Lanacordin; Cardiogoxin; Eudigox; Davoxin; SMR000059217; Rougoxin; Mapluxin; Lenoxin; Lanacrist; Dynamos; Vanoxin; Neo-Lanicor; Lanoxin PG; Digoxin Pediatric; Digoxin Nativelle; SK-Digoxin; UNII-73K4184T59; Homolle's digitalin; Hemigoxine Nativelle; MFCD00003674; Digitek (TN); Lanoxicaps (TN); Lanoxin (TN); Digoxin (JP15/USP); (3beta,5beta,12beta)-3-{[2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl]oxy}-12,14-dihydroxycard-20(22)-enolide; 4-[(1S,2S,5S,7R,10R,11S,14R,15S,16R)-5-{[(2R,4S,5S,6R)-5-{[(2S,4S,5S,6R)-5-{[(2S,4S,5S,6R)-4,5-dihydroxy-6-methyloxan-2-yl]oxy}-4-hydroxy-6-methyloxan-2-yl]oxy}-4-hydroxy-6-methyloxan-2-yl]oxy}-11,16-dihydroxy-2,15-dimethyltetracyclo[8700^{2,7}; [3H]digoxin
Indication
Disease Entry ICD 11 Status REF
Arrhythmia BC9Z Approved [1], [2]
Congestive cardiac insufficiency BD1Z Approved [1], [2]
Heart failure BD10-BD13 Approved [1], [2]
Therapeutic Class
Antiarrhythmic Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 3 Molecular Weight (mw) 780.9
Topological Polar Surface Area (xlogp) 1.3
Rotatable Bond Count (rotbonds) 7
Hydrogen Bond Donor Count (hbonddonor) 6
Hydrogen Bond Acceptor Count (hbondacc) 14
ADMET Property
Absorption Cmax
The maximum plasma concentration (Cmax) of drug is 1.32 +/- 0.18 mcg/L [3]
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 1.0 h [3]
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 3: high solubility and low permeability [4]
Bioavailability
The bioavailability of drug is 50-90% [3]
Clearance
The drug present in the plasma can be removed from the body at the rate of 1.7 mL/min/kg [5]
Elimination
After intravenous (IV) administration to healthy subjects, 50-70% of the dose is measured excreted as unchanged digoxin in the urine [3]
Half-life
The concentration or amount of drug in body reduced by one-half in 1.5 - 2 days (in healthy subjects) [6]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.0000128 micromolar/kg/day [7]
Unbound Fraction
The unbound fraction of drug in plasma is 0.7% [5]
Vd
The volume of distribution (Vd) of drug is 475-500 L [6]
Water Solubility
The ability of drug to dissolve in water is measured as 0.986 mg/mL [4]
Chemical Identifiers
Formula
C41H64O14
IUPAC Name
3-[(3S,5R,8R,9S,10S,12R,13S,14S,17R)-3-[(2R,4S,5S,6R)-5-[(2S,4S,5S,6R)-5-[(2S,4S,5S,6R)-4,5-dihydroxy-6-methyloxan-2-yl]oxy-4-hydroxy-6-methyloxan-2-yl]oxy-4-hydroxy-6-methyloxan-2-yl]oxy-12,14-dihydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]-2H-furan-5-one
Canonical SMILES
C[C@@H]1[C@H]([C@H](C[C@@H](O1)O[C@@H]2[C@H](O[C@H](C[C@@H]2O)O[C@@H]3[C@H](O[C@H](C[C@@H]3O)O[C@H]4CC[C@]5([C@@H](C4)CC[C@@H]6[C@@H]5C[C@H]([C@]7([C@@]6(CC[C@@H]7C8=CC(=O)OC8)O)C)O)C)C)C)O)O
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
InChIKey
LTMHDMANZUZIPE-PUGKRICDSA-N
Cross-matching ID
PubChem CID
2724385
ChEBI ID
CHEBI:4551
CAS Number
20830-75-5
DrugBank ID
DB00390
TTD ID
D02OZE
VARIDT ID
DR00148
INTEDE ID
DR0498
ACDINA ID
D00198

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Organic anion transporter M1 (SLCO4C1) TTACFNR SO4C1_HUMAN Modulator [8]
Sodium/potassium-transporting ATPase (SPT ATPase) TTQ38E9 AT1A1_HUMAN; AT1A2_HUMAN; AT1A3_HUMAN; AT1B1_HUMAN; AT1B2_HUMAN; AT1B3_HUMAN Inhibitor [9]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Multidrug resistance protein 3 (ABCB4) DTZRMK5 MDR3_HUMAN Substrate [10]
Organic solute transporter subunit alpha (SLC51A) DTMEQ32 OSTA_HUMAN Substrate [11]
Organic solute transporter subunit beta (SLC51B) DT1V9AJ OSTB_HUMAN Substrate [11]
Organic anion transporting polypeptide 4C1 (SLCO4C1) DTY0QMU SO4C1_HUMAN Substrate [12]
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTPFTEQ SO2B1_HUMAN Substrate [13]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Substrate [14]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [15]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [16]
Cardiac glycoside reductase 2 (cgr2) DE9VSLW CGR2_EGGLE Substrate [17]
Cardiac glycoside reductase 1 (cgr1) DE84PFW CGR1_EGGLE Substrate [17]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Digoxin
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Furosemide DMMQ8ZG Moderate Increased risk of hypokalemia by the combination of Digoxin and Furosemide. Heart failure [BD10-BD1Z] [63]
Bumetanide DMRV7H0 Moderate Increased risk of hypokalemia by the combination of Digoxin and Bumetanide. Heart failure [BD10-BD1Z] [63]
Hydroflumethiazide DMVPUQI Moderate Increased risk of hypomagnesemia by the combination of Digoxin and Hydroflumethiazide. Heart failure [BD10-BD1Z] [63]
Coadministration of a Drug Treating the Disease Different from Digoxin (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Sodium bicarbonate DMMU6BJ Minor Decreased absorption of Digoxin due to formation of complexes caused by Sodium bicarbonate. Acidosis [5C73] [64]
Midostaurin DMI6E0R Moderate Decreased clearance of Digoxin due to the transporter inhibition by Midostaurin. Acute myeloid leukaemia [2A60] [65]
Arn-509 DMT81LZ Moderate Accelerated clearance of Digoxin due to the transporter induction by Arn-509. Acute myeloid leukaemia [2A60] [65]
Gilteritinib DMWQ4MZ Moderate Decreased clearance of Digoxin due to the transporter inhibition by Gilteritinib. Acute myeloid leukaemia [2A60] [66]
Scopolamine DMOM8AL Minor Altered absorption of Digoxin due to GI dynamics variation caused by Scopolamine. Addictive disorder [6C50-6C5Z] [67]
Framycetin DMF8DNE Minor Altered absorption of Digoxin caused by Framycetin. Alcoholic liver disease [DB94] [68]
Paromomycin DM1AGXN Minor Altered absorption of Digoxin caused by Paromomycin. Amoebiasis [1A36] [68]
Nifedipine DMSVOZT Moderate Decreased renal excretion of Digoxin caused by Nifedipine. Angina pectoris [BA40] [69]
Clorazepate DMC3JST Moderate Increased plasma concentration of Digoxin and Clorazepate due to competitive binding of plasma proteins. Anxiety disorder [6B00-6B0Z] [70]
Alprazolam DMC7XDN Moderate Increased plasma concentration of Digoxin and Alprazolam due to competitive binding of plasma proteins. Anxiety disorder [6B00-6B0Z] [71]
Halazepam DMPFWO6 Moderate Increased plasma concentration of Digoxin and Halazepam due to competitive binding of plasma proteins. Anxiety disorder [6B00-6B0Z] [71]
Chlordiazepoxide DMTN5XI Moderate Increased plasma concentration of Digoxin and Chlordiazepoxide due to competitive binding of plasma proteins. Anxiety disorder [6B00-6B0Z] [71]
Oxazepam DMXNZM4 Moderate Increased plasma concentration of Digoxin and Oxazepam due to competitive binding of plasma proteins. Anxiety disorder [6B00-6B0Z] [71]
Levalbuterol DM5YBO1 Moderate Interference of cell/tissue uptake of Digoxin by Levalbuterol. Asthma [CA23] [72]
Salbutamol DMN9CWF Moderate Interference of cell/tissue uptake of Digoxin by Salbutamol. Asthma [CA23] [72]
Kanamycin DM2DMPO Minor Altered absorption of Digoxin caused by Kanamycin. Bacterial infection [1A00-1C4Z] [68]
Rabeprazole DMMZXIW Moderate Increased risk of hypomagnesemia by the combination of Digoxin and Rabeprazole. Bacterial infection [1A00-1C4Z] [73]
Oxytetracycline DMOVH1M Moderate Altered absorption of Digoxin due to GI flora changes caused by Oxytetracycline. Bacterial infection [1A00-1C4Z] [74]
Troleandomycin DMUZNIG Moderate Decreased clearance of Digoxin due to the transporter inhibition by Troleandomycin. Bacterial infection [1A00-1C4Z] [75]
Minocycline DMVN5OH Moderate Altered absorption of Digoxin due to GI flora changes caused by Minocycline. Bacterial infection [1A00-1C4Z] [74]
Tetracycline DMZA017 Moderate Altered absorption of Digoxin due to GI flora changes caused by Tetracycline. Bacterial infection [1A00-1C4Z] [74]
Erdafitinib DMI782S Moderate Decreased clearance of Digoxin due to the transporter inhibition by Erdafitinib. Bladder cancer [2C94] [76]
Tucatinib DMBESUA Moderate Decreased clearance of Digoxin due to the transporter inhibition by Tucatinib. Breast cancer [2C60-2C6Y] [77]
Mannitol DMSCDY9 Moderate Increased risk of hypokalemia by the combination of Digoxin and Mannitol. Bronchiectasis [CA24] [63]
Demeclocycline DMZEPFJ Moderate Altered absorption of Digoxin due to GI flora changes caused by Demeclocycline. Bronchitis [CA20] [74]
Atorvastatin DMF28YC Moderate Decreased clearance of Digoxin due to the transporter inhibition by Atorvastatin. Cardiovascular disease [BA00-BE2Z] [78]
PF-04449913 DMSB068 Moderate Decreased clearance of Digoxin due to the transporter inhibition by PF-04449913. Chronic myelomonocytic leukaemia [2A40] [65]
Ardeparin DMYRX8B Minor Increased plasma concentration of Digoxin and Ardeparin due to competitive binding of plasma proteins. Coronary thrombosis [BA43] [79]
Mifepristone DMGZQEF Moderate Decreased clearance of Digoxin due to the transporter inhibition by Mifepristone. Cushing syndrome [5A70] [80]
Pasireotide DMHM7JS Moderate Increased risk of atrioventricular block by the combination of Digoxin and Pasireotide. Cushing syndrome [5A70] [81]
Ivacaftor DMZC1HS Moderate Decreased clearance of Digoxin due to the transporter inhibition by Ivacaftor. Cystic fibrosis [CA25] [82]
Hyoscyamine DM804UR Minor Altered absorption of Digoxin due to GI dynamics variation caused by Hyoscyamine. Digestive system disease [DE2Z] [67]
Mepenzolate DM8YU2F Minor Altered absorption of Digoxin due to GI dynamics variation caused by Mepenzolate. Digestive system disease [DE2Z] [67]
SODIUM CITRATE DMHPD2Y Minor Decreased absorption of Digoxin due to formation of complexes caused by SODIUM CITRATE. Discovery agent [N.A.] [64]
Oxybutynine DMJPBAX Minor Altered absorption of Digoxin due to GI dynamics variation caused by Oxybutynine. Discovery agent [N.A.] [67]
Diazepam DM08E9O Moderate Increased plasma concentration of Digoxin and Diazepam due to competitive binding of plasma proteins. Epilepsy/seizure [8A61-8A6Z] [71]
Clonazepam DMTO13J Moderate Increased plasma concentration of Digoxin and Clonazepam due to competitive binding of plasma proteins. Epilepsy/seizure [8A61-8A6Z] [71]
Rufinamide DMWE60C Moderate Increased metabolism of Digoxin caused by Rufinamide mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [65]
Ethacrynic acid DM60QMR Moderate Increased risk of hypomagnesemia by the combination of Digoxin and Ethacrynic acid. Essential hypertension [BA00] [83]
Bendroflumethiazide DM7EVLC Moderate Increased risk of hypomagnesemia by the combination of Digoxin and Bendroflumethiazide. Essential hypertension [BA00] [63]
Benzthiazide DMQWZ0H Moderate Increased risk of hypomagnesemia by the combination of Digoxin and Benzthiazide. Essential hypertension [BA00] [63]
Solifenacin DMG592Q Minor Altered absorption of Digoxin due to GI dynamics variation caused by Solifenacin. Functional bladder disorder [GC50] [67]
Tolterodine DMSHPW8 Minor Altered absorption of Digoxin due to GI dynamics variation caused by Tolterodine. Functional bladder disorder [GC50] [67]
Darifenacin DMWXLYZ Minor Altered absorption of Digoxin due to GI dynamics variation caused by Darifenacin. Functional bladder disorder [GC50] [67]
Itraconazole DMCR1MV Major Decreased clearance of Digoxin due to the transporter inhibition by Itraconazole. Fungal infection [1F29-1F2F] [84]
Propantheline DM2EN6G Minor Altered absorption of Digoxin due to GI dynamics variation caused by Propantheline. Gastric ulcer [DA60] [67]
Dexlansoprazole DM1DBV5 Moderate Decreased clearance of Digoxin due to the transporter inhibition by Dexlansoprazole. Gastro-oesophageal reflux disease [DA22] [73]
Acetazolamide DM1AF5U Moderate Increased risk of hypomagnesemia by the combination of Digoxin and Acetazolamide. Glaucoma [9C61] [63]
Methazolamide DM7J2TA Moderate Increased risk of hypokalemia by the combination of Digoxin and Methazolamide. Glaucoma [9C61] [63]
Dichlorphenamide DMH7IDQ Moderate Increased risk of hypomagnesemia by the combination of Digoxin and Dichlorphenamide. Glaucoma [9C61] [83]
Colchicine DM2POTE Moderate Decreased clearance of Digoxin due to the transporter inhibition by Colchicine. Gout [FA25] [85]
GS-5885 DMSL3DX Moderate Decreased clearance of Digoxin due to the transporter inhibition by GS-5885. Hepatitis virus infection [1E50-1E51] [86]
Procarbazine DMIK367 Moderate Decreased absorption of Digoxin due to intestinal mucosa variation caused by Procarbazine. Hodgkin lymphoma [2B30] [87]
Etravirine DMGV8QU Moderate Decreased clearance of Digoxin due to the transporter inhibition by Etravirine. Human immunodeficiency virus disease [1C60-1C62] [81]
BMS-201038 DMQTAGO Moderate Decreased clearance of Digoxin due to the transporter inhibition by BMS-201038. Hyper-lipoproteinaemia [5C80] [88]
Nisoldipine DM7ISKJ Moderate Decreased renal excretion of Digoxin caused by Nisoldipine. Hypertension [BA00-BA04] [69]
Indapamide DMGN1PW Moderate Increased risk of hypomagnesemia by the combination of Digoxin and Indapamide. Hypertension [BA00-BA04] [63]
Trichlormethiazide DMHAQCO Moderate Increased risk of hypokalemia by the combination of Digoxin and Trichlormethiazide. Hypertension [BA00-BA04] [63]
Hydrochlorothiazide DMUSZHD Moderate Increased risk of hypomagnesemia by the combination of Digoxin and Hydrochlorothiazide. Hypertension [BA00-BA04] [63]
Levothyroxine DMHN027 Moderate Increased renal excretion of Digoxin caused by Levothyroxine. Hypo-thyroidism [5A00] [89]
Belladonna DM2RBWK Minor Altered absorption of Digoxin due to GI dynamics variation caused by Belladonna. Infectious gastroenteritis/colitis [1A40] [67]
Suvorexant DM0E6S3 Moderate Decreased clearance of Digoxin due to the transporter inhibition by Suvorexant. Insomnia [7A00-7A0Z] [90]
Flurazepam DMAL4G0 Moderate Increased plasma concentration of Digoxin and Flurazepam due to competitive binding of plasma proteins. Insomnia [7A00-7A0Z] [71]
Triazolam DMETYK5 Moderate Increased plasma concentration of Digoxin and Triazolam due to competitive binding of plasma proteins. Insomnia [7A00-7A0Z] [71]
Quazepam DMY4D87 Moderate Increased plasma concentration of Digoxin and Quazepam due to competitive binding of plasma proteins. Insomnia [7A00-7A0Z] [71]
Estazolam DMZGXUM Moderate Increased plasma concentration of Digoxin and Estazolam due to competitive binding of plasma proteins. Insomnia [7A00-7A0Z] [71]
Clidinium DMUMQZ0 Minor Altered absorption of Digoxin due to GI dynamics variation caused by Clidinium. Irritable bowel syndrome [DD91] [67]
Dicyclomine DMZSDGX Minor Altered absorption of Digoxin due to GI dynamics variation caused by Dicyclomine. Irritable bowel syndrome [DD91] [67]
Remimazolam DMLVSYX Moderate Increased plasma concentration of Digoxin and Remimazolam due to competitive binding of plasma proteins. Labour/delivery anaesthesia complication [JB0C] [71]
Methotrexate DM2TEOL Moderate Decreased absorption of Digoxin due to intestinal mucosa variation caused by Methotrexate. Leukaemia [2A60-2B33] [87]
Capmatinib DMYCXKL Moderate Decreased clearance of Digoxin due to the transporter inhibition by Capmatinib. Lung cancer [2C25] [91]
Quinine DMSWYF5 Moderate Decreased elimination of Digoxin caused by Quinine mediated competitive inhibition of bile excretion. Malaria [1F40-1F45] [92]
Fludarabine DMVRLT7 Moderate Decreased absorption of Digoxin due to intestinal mucosa variation caused by Fludarabine. Malignant haematopoietic neoplasm [2B33] [87]
Ibrutinib DMHZCPO Moderate Decreased clearance of Digoxin due to the transporter inhibition by Ibrutinib. Mature B-cell lymphoma [2A85] [65]
Vincristine DMINOX3 Moderate Decreased absorption of Digoxin due to intestinal mucosa variation caused by Vincristine. Mature B-cell lymphoma [2A85] [87]
Cytarabine DMZD5QR Moderate Decreased absorption of Digoxin due to intestinal mucosa variation caused by Cytarabine. Mature B-cell lymphoma [2A85] [87]
Lanthanum carbonate DMMJQSH Moderate Decreased absorption of Digoxin due to formation of complexes caused by Lanthanum carbonate. Mineral absorption/transport disorder [5C64] [81]
Midazolam DMXOELT Moderate Increased plasma concentration of Digoxin and Midazolam due to competitive binding of plasma proteins. Mood/affect symptom [MB24] [71]
Carfilzomib DM48K0X Moderate Decreased clearance of Digoxin due to the transporter inhibition by Carfilzomib. Multiple myeloma [2A83] [65]
Thalidomide DM70BU5 Moderate Increased risk of ventricular arrhythmias by the combination of Digoxin and Thalidomide. Multiple myeloma [2A83] [66]
Siponimod DM2R86O Major Increased risk of atrioventricular block by the combination of Digoxin and Siponimod. Multiple sclerosis [8A40] [66]
Fingolimod DM5JVAN Major Increased risk of bradycardia by the combination of Digoxin and Fingolimod. Multiple sclerosis [8A40] [93]
Ozanimod DMT6AM2 Moderate Increased risk of bradycardia by the combination of Digoxin and Ozanimod. Multiple sclerosis [8A40] [94]
Rolapitant DM8XP26 Moderate Decreased clearance of Digoxin due to the transporter inhibition by Rolapitant. Nausea/vomiting [MD90] [95]
Metoclopramide DMFA5MY Minor Altered absorption of Digoxin due to GI dynamics variation caused by Metoclopramide. Nausea/vomiting [MD90] [96]
Metolazone DMB39LO Moderate Increased risk of hypomagnesemia by the combination of Digoxin and Metolazone. Oedema [MG29] [63]
Polythiazide DMCH80F Moderate Increased risk of hypokalemia by the combination of Digoxin and Polythiazide. Oedema [MG29] [63]
Olaparib DM8QB1D Moderate Decreased metabolism of Digoxin caused by Olaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [66]
Flavoxate DMKV4NL Minor Altered absorption of Digoxin due to GI dynamics variation caused by Flavoxate. Pain [MG30-MG3Z] [67]
Biperiden DME78OA Minor Altered absorption of Digoxin due to GI dynamics variation caused by Biperiden. Parkinsonism [8A00] [67]
Methylscopolamine DM5VWOB Minor Altered absorption of Digoxin due to GI dynamics variation caused by Methylscopolamine. Peptic ulcer [DA61] [67]
Esomeprazole DM7BN0X Moderate Decreased clearance of Digoxin due to the transporter inhibition by Esomeprazole. Peptic ulcer [DA61] [73]
Lonafarnib DMGM2Z6 Moderate Decreased clearance of Digoxin due to the transporter inhibition by Lonafarnib. Premature ageing appearance [LD2B] [97]
Enzalutamide DMGL19D Moderate Accelerated clearance of Digoxin due to the transporter induction by Enzalutamide. Prostate cancer [2C82] [98]
Amisulpride DMSJVAM Moderate Increased risk of ventricular arrhythmias by the combination of Digoxin and Amisulpride. Schizophrenia [6A20] [65]
Cyclophosphamide DM4O2Z7 Moderate Decreased absorption of Digoxin due to intestinal mucosa variation caused by Cyclophosphamide. Solid tumour/cancer [2A00-2F9Z] [87]
Vandetanib DMRICNP Moderate Decreased clearance of Digoxin due to the transporter inhibition by Vandetanib. Solid tumour/cancer [2A00-2F9Z] [66]
Doxorubicin DMVP5YE Moderate Decreased absorption of Digoxin due to intestinal mucosa variation caused by Doxorubicin. Solid tumour/cancer [2A00-2F9Z] [87]
Pitolisant DM8RFNJ Moderate Increased metabolism of Digoxin caused by Pitolisant mediated induction of UGT. Somnolence [MG42] [65]
Fostamatinib DM6AUHV Moderate Decreased metabolism of Digoxin caused by Fostamatinib mediated inhibition of CYP450 enzyme. Thrombocytopenia [3B64] [99]
Albiglutide DM1JEGF Minor Altered absorption of Digoxin due to GI dynamics variation caused by Albiglutide. Type 2 diabetes mellitus [5A11] [100]
Liraglutide DM3FXPS Minor Altered absorption of Digoxin due to GI dynamics variation caused by Liraglutide. Type 2 diabetes mellitus [5A11] [101]
Atropine DMEN6X7 Minor Altered absorption of Digoxin due to GI dynamics variation caused by Atropine. Unspecific substance harmful effect [NE6Z] [67]
Amiodarone DMUTEX3 Major Increased plasma concentration of Digoxin and Amiodarone due to competitive binding of plasma proteins. Ventricular tachyarrhythmia [BC71] [102]
⏷ Show the Full List of 104 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
D&C green no. 5 E00265 20431 Colorant
Hydrazine yellow E00409 164825 Colorant
Quinoline yellow WS E00309 24671 Colorant
Stearic acid E00079 5281 Emulsifying agent; Solubilizing agent; Viscosity-controlling agent; lubricant
Sunset yellow FCF E00255 17730 Colorant
Beta-D-lactose E00099 6134 Diluent; Dry powder inhaler carrier; Lyophilization aid
Carmellose sodium E00625 Not Available Disintegrant
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate E00208 11177 lubricant
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
⏷ Show the Full List of 10 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Digoxin 0.125 mg tablet 0.125 mg Oral Tablet Oral
Digoxin 0.25 mg tablet 0.25 mg Oral Tablet Oral
Digoxin 125 mcg tablet 125 mcg Oral Tablet Oral
Digoxin 0.0625 mg tablet 0.0625 mg Oral Tablet Oral
Digoxin 0.1875 mg tablet 0.1875 mg Oral Tablet Oral
Digoxin 250 mcg tablet 250 mcg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4726).
2 FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 021648.
3 Iisalo E: Clinical pharmacokinetics of digoxin. Clin Pharmacokinet. 1977 Jan-Feb;2(1):1-16. doi: 10.2165/00003088-197702010-00001.
4 BDDCS applied to over 900 drugs
5 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
6 FDA Approved Drug Products: Lanoxin (digoxin) oral tablets
7 Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
8 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1227).
9 Fab antibody fragments: some applications in clinical toxicology. Drug Saf. 2004;27(14):1115-33.
10 MDR3 P-glycoprotein, a phosphatidylcholine translocase, transports several cytotoxic drugs and directly interacts with drugs as judged by interference with nucleotide trapping. J Biol Chem. 2000 Aug 4;275(31):23530-9.
11 Functional complementation between a novel mammalian polygenic transport complex and an evolutionarily ancient organic solute transporter, OSTalpha-OSTbeta. J Biol Chem. 2003 Jul 25;278(30):27473-82.
12 Isolation and characterization of a digoxin transporter and its rat homologue expressed in the kidney. Proc Natl Acad Sci U S A. 2004 Mar 9;101(10):3569-74.
13 Drug Interactions in Infectious Diseases.
14 Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33.
15 MDR1 function is sensitive to the phosphorylation state of myosin regulatory light chain. Biochem Biophys Res Commun. 2010 Jul 16;398(1):7-12.
16 Omeprazole-associated digoxin toxicity. South Med J. 2007 Apr;100(4):400-2.
17 Mechanistic insight into digoxin inactivation by Eggerthella lenta augments our understanding of its pharmacokinetics. Gut Microbes. 2014 Mar-Apr;5(2):233-8.
18 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
19 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
20 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
21 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
22 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
23 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
24 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
25 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
26 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
27 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
28 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
29 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
30 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
31 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
32 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
33 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
34 Pharmacokinetics and disposition of silodosin (KMD-3213)]. Yakugaku Zasshi. 2006 Mar;126 Spec no.:237-45.
35 LST-2, a human liver-specific organic anion transporter, determines methotrexate sensitivity in gastrointestinal cancers. Gastroenterology. 2001 Jun;120(7):1689-99.
36 Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clin Cancer Res. 2013 Mar 15;19(6):1458-66.
37 Effect of pregnane X receptor ligands on transport mediated by human OATP1B1 and OATP1B3. Eur J Pharmacol. 2008 Apr 14;584(1):57-65.
38 Influence of non-steroidal anti-inflammatory drugs on organic anion transporting polypeptide (OATP) 1B1- and OATP1B3-mediated drug transport. Drug Metab Dispos. 2011 Jun;39(6):1047-53.
39 Relevance of conserved lysine and arginine residues in transmembrane helices for the transport activity of organic anion transporting polypeptide 1B3. Br J Pharmacol. 2010 Feb 1;159(3):698-708.
40 Influence of SLCO1B1, 1B3, 2B1 and ABCC2 genetic polymorphisms on mycophenolic acid pharmacokinetics in Japanese renal transplant recipients. Eur J Clin Pharmacol. 2007 Dec;63(12):1161-9.
41 FDA Drug Development and Drug Interactions
42 Impact of OATP transporters on pharmacokinetics. Br J Pharmacol. 2009 Oct;158(3):693-705.
43 Molecular identification and characterization of novel members of the human organic anion transporter (OATP) family. Biochem Biophys Res Commun. 2000 Jun 24;273(1):251-60.
44 The Transporter Classification Database (TCDB): recent advances. Nucleic Acids Res. 2016 Jan 4;44(D1):D372-9. (ID: 2.A.60.1.20)
45 Small-Dosing Clinical Study: Pharmacokinetic, Pharmacogenomic (SLCO2B1 and ABCG2), and Interaction (Atorvastatin and Grapefruit Juice) Profiles of 5 Probes for OATP2B1 and BCRP. J Pharm Sci. 2017 Sep;106(9):2688-2694.
46 Identification of drugs and drug metabolites as substrates of multidrug resistance protein 2 (MRP2) using triple-transfected MDCK-OATP1B1-UGT1A1-MRP2 cells. Br J Pharmacol. 2012 Mar;165(6):1836-1847.
47 Functional characterization of pH-sensitive organic anion transporting polypeptide OATP-B in human. J Pharmacol Exp Ther. 2004 Feb;308(2):438-45.
48 Human platelets express organic anion-transporting peptide 2B1, an uptake transporter for atorvastatin. Drug Metab Dispos. 2009 May;37(5):1129-37.
49 pH-sensitive interaction of HMG-CoA reductase inhibitors (statins) with organic anion transporting polypeptide 2B1. Mol Pharm. 2011 Aug 1;8(4):1303-13.
50 Drug-drug interaction between pitavastatin and various drugs via OATP1B1. Drug Metab Dispos. 2006 Jul;34(7):1229-36.
51 Involvement of multiple transporters in the hepatobiliary transport of rosuvastatin. Drug Metab Dispos. 2008 Oct;36(10):2014-23.
52 Substrate-dependent drug-drug interactions between gemfibrozil, fluvastatin and other organic anion-transporting peptide (OATP) substrates on OATP1B1, OATP2B1, and OATP1B3. Drug Metab Dispos. 2007 Aug;35(8):1308-14.
53 OSTalpha-OSTbeta: a major basolateral bile acid and steroid transporter in human intestinal, renal, and biliary epithelia. Hepatology. 2005 Dec;42(6):1270-9.
54 Comparative clinical pharmacokinetics of dipeptidyl peptidase-4 inhibitors. Clin Pharmacokinet. 2012 Aug 1;51(8):501-14.
55 Transport of estrone 3-sulfate mediated by organic anion transporter OATP4C1: estrone 3-sulfate binds to the different recognition site for digoxin in OATP4C1. Drug Metab Pharmacokinet. 2010;25(3):314-7.
56 Treatment of congestive heart failure--current status of use of digitoxin. Eur J Clin Invest. 2001;31 Suppl 2:10-7.
57 Medicinal plants in therapy. Bull World Health Organ. 1985;63(6):965-81.
58 Rostafuroxin: an ouabain antagonist that corrects renal and vascular Na+-K+- ATPase alterations in ouabain and adducin-dependent hypertension. Am J Physiol Regul Integr Comp Physiol. 2006 Mar;290(3):R529-35.
59 First-in-human study of pbi-05204, an oleander-derived inhibitor of akt, fgf-2, nf- beta and p70s6k, in patients with advanced solid tumors. Invest New Drugs. 2014 Dec;32(6):1204-12.
60 ClinicalTrials.gov (NCT03646071) A Study of RX108 in Patients With Locally Advanced or Metastatic Solid Tumors. U.S. National Institutes of Health.
61 Novel analogues of istaroxime, a potent inhibitor of Na+,K+-ATPase: synthesis and structure-activity relationship. J Med Chem. 2008 Aug 14;51(15):4601-8.
62 WO patent application no. 1995,0085,58, Novel deoxy and oxygen-substituted sugar-containing 14-aminosteroid compounds.
63 Brown DD, Dormois JC, Abraham GN, et al "Effect of furosemide on the renal excretion of digoxin." Clin Pharmacol Ther 20 (1976): 395-400. [PMID: 975715]
64 Allen MD, Greenblatt DJ, Harmatz JS, Smith TW "Effect of magnesium--aluminum hydroxide and kaolin--pectin on absorption of digoxin from tablets and capsules." J Clin Pharmacol 21 (1981): 26-30. [PMID: 7012189]
65 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
66 Cerner Multum, Inc. "Australian Product Information.".
67 Binnion PF, McDermott M, LeSher D "Bioavailability of digoxin." Lancet 1 (1973): 1118. [PMID: 4122032]
68 Lindenbaum J, Maulitz RM, Butler VP "Inhibition of digoxin absorption by neomycin." Gastroenterology 71 (1976): 399-404. [PMID: 950089]
69 Belz GG, Aust PE, Munkes R "Digoxin plasma concentrations and nifedipine ." Lancet 1 (1981): 844-5. [PMID: 6111709]
70 Ochs HR, Greenblatt DJ, Verburg-Ochs B "Effect of alprazolam on digoxin kinetics and creatinine clearance." Clin Pharmacol Ther 38 (1985): 595-8. [PMID: 2865030]
71 Castillo-Ferrando JR, Garcia M, Carmona J "Digoxin levels and diazepam." Lancet 2 (1980): 368. [PMID: 6105500]
72 Agencia Espaola de Medicamentos y Productos Sanitarios Healthcare "Centro de informacion online de medicamentos de la AEMPS - CIMA.".
73 Andersson T "Omeprazole drug interaction studies." Clin Pharmacokinet 21 (1991): 195-212. [PMID: 1764870]
74 Lindenbaum J, Rund DG, Butler VP Jr, Tse-Eng D, Saha JR "Inactivation of digoxin by the gut flora: reversal by antibiotic therapy." N Engl J Med 305 (1981): 789-94. [PMID: 7266632]
75 Hughes J, Crowe A. Inhibition of P-glycoprotein-mediated efflux of digoxin and its metabolites by macrolide antibiotics.?J Pharmacol Sci. 2010;113(4):315-324. [PMID: 20724802]
76 Product Information. Balversa (erdafitinib). Janssen Products, LP, Horsham, PA.
77 Product Information. Tukysa (tucatinib). Seattle Genetics Inc, Bothell, WA.
78 Boyd RA, Stern RH, Stewart BH, et al. "Atorvastatin coadministration may increase digoxin concentrations by inhibition of intestinal P-glycoprotein-mediated secretion." J Clin Pharmacol 40 (2000): 91-8. [PMID: 10631627]
79 Storstein L, Janssen H "Studies on digitalis VI: the effect of heparin on serum protein binding of digitoxin and digoxin." Clin Pharmacol Ther 20 (1976): 15-23. [PMID: 1277722]
80 Product Information. Korlym (mifepristone). Corcept Therapeutics Incorporated, Menlo Park, CA.
81 Canadian Pharmacists Association.
82 Product Information. Kalydeco (ivacaftor). Vertex Pharmaceuticals, Cambridge, MA.
83 Semple P, Tilstone WJ, Lawson DH "Furosemide and urinary digoxin clearance." N Engl J Med 293 (1975): 612-3. [PMID: 902451]
84 Alderman CP, Allcroft PD "Digoxin-itraconazole interaction: possible mechanisms." Ann Pharmacother 31 (1997): 438-40. [PMID: 9101006]
85 Product Information. Colcrys (colchicine). AR Scientific Inc, Philadelphia, PA.
86 Becquemont L, Verstuyft C, Kerb R, et al. "Effect of grapefruit juice on digoxin pharmacokinetics in humans." Clin Pharmacol Ther 70 (2001): 311-6. [PMID: 11673746]
87 Bjornsson TD, Huang AT, Roth P, Jacob DS, Christenson R "Effects of high-dose cancer chemotherapy on the absorption of digoxin in two different formulations." Clin Pharmacol Ther 39 (1986): 25-8. [PMID: 3943266]
88 Product Information. Juxtapid (lomitapide). Aegerion Pharmaceuticals Inc, Cambridge, MA.
89 Frye RL, Braunwald E "Studies on digitalis. III: The influence of triiodothyronine on digitalis requirements." Circulation 23 (1961): 376-82. [PMID: 13702336]
90 Product Information. Belsomra (suvorexant). Merck & Company Inc, Whitehouse Station, NJ.
91 Product Information. Tabrecta (capmatinib). Novartis Pharmaceuticals, East Hanover, NJ.
92 Brater DC, Morrelli HF "Systemic alkalosis and digitalis related arrhythmias." Acta Med Scand Suppl 647 (1981): 79-85. [PMID: 6942644]
93 Product Information. Gilenya (fingolimod). Novartis Pharmaceuticals, East Hanover, NJ.
94 Product Information. Zeposia (ozanimod). Celgene Corporation, Summit, NJ.
95 Product Information. Varubi (rolapitant). Tesaro Inc., Waltham, MA.
96 Fraser EJ, Leach RH, Poston JW, Bold AM, Culank LS, Lipede AB "Dissolution-rates and bioavailability of digoxin tablets." Lancet 1 (1973): 1393. [PMID: 4122785]
97 Product Information. Zokinvy (lonafarnib). Eiger BioPharmaceuticals, Palo Alto, CA.
98 Benoist G, van Oort I, et al "Drug-drug interaction potential in men treated with enzalutamide: Mind the gap." Br J Clin Pharmacol 0 (2017): epub. [PMID: 28881501]
99 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
100 EMEA. European Medicines Agency "EPARs. European Union Public Assessment Reports.".
101 Product Information. Victoza (liraglutide). Novo Nordisk Pharmaceuticals Inc, Princeton, NJ.
102 Bajaj BP, Baig MW, Perrins EJ "Amiodarone-induced torsades de pointes: the possible facilitatory role of digoxin." Int J Cardiol 33 (1991): 335-7. [PMID: 1743800]