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Sign up to Get Early Access ( 5/25/2017 Digoxin ­ DrugBank ID Pharmacology Interactions References Trials Economics Properties Spectra Taxonomy Targets (1) Enzymes (2) Transporters (12) Biointeractions (17) (/drugs/DB00390/biointeractions) Show Drugs with Similar Structures Get DrugBank to go! The DrugBank app for iOS and Android is coming soon. (http://eepurl.com/bZh6g9) Sign up to get early access (http://eepurl.com/bZh6g9) Identication Name Digoxin Accession Number DB00390 (APRD00098) Type Small Molecule Groups Approved Description 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 brillation and in the management of congestive heart failure with atrial brillation. 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) Structure O O O H CH CH CH CH HO HO O O O (/structures/DB00390/image.svg) O H O HO O HO O CH MOL (/structures/small_molecule_drugs/DB00390.mol) SDF (/structures/small_molecule_drugs/DB00390.sdf) PDB (/structures/small_molecule_drugs/DB00390.pdb) SMILES (/structures/small_molecule_drugs/DB00390.smiles) InChI (/structures/small_molecule_drugs/DB00390.inchi) https://www.drugbank.ca/drugs/DB00390 1/25 5/25/2017 Digoxin ­ DrugBank Synonyms 12beta-Hydroxydigitoxin 12β-hydroxydigitoxin 4-[(3S,5R,8R,9S,10S,12R,13S,14S)-3-[(2S,4S,5R,6R)-5-[(2S,4S,5R,6R)-5-[(2S,4S,5R,6R)-4,5-dihydroxy-6-methyl-oxan-2-yl]oxy-4-hydroxy-6-methyl-oxan-2-yl]oxy-4-hydroxy-6-methyl- oxan-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]-5H-furan-2-one Digazolan Digossina Digoxin Digoxina Digoxine Digoxinum Lanadicor External IDs Not Available Product Not Available Ingredients Approved Show 10 entries Prescription Products Search Name Dosage Strength Route Labeller Marketing Start Marketing End Digoxin Tablet .25 mg/1 Oral Par Pharmaceutical 2014-01-14 Not applicable Digoxin Tablet .125 mg/1 Oral Remedy Repack 2016-09-12 2017-03-04 Digoxin Solution .05 mg/mL Oral Precision Dose, Inc. 2017-01-19 Not applicable Digoxin Tablet .125 mg/1 Oral Par Pharmaceutical 2014-01-14 Not applicable Digoxin Tablet .25 mg/1 Oral Remedy Repack 2016-09-21 2017-03-04 Digoxin Tablet .125 mg/1 Oral State of Florida DOH Central Pharmacy 2014-11-01 Not applicable Digoxin Tablet .125 mg/1 Oral Nucare Pharmaceuticals, Inc. 2014-01-14 Not applicable Digoxin Tablet .25 mg/1 Oral Remedy Repack 2017-03-09 Not applicable Digoxin Tablet .125 mg/1 Oral Ncs Health Care Of Ky, Inc Dba Vangard Labs 2014-01-14 Not applicable Digoxin Tablet .25 mg/1 Oral Nucare Pharmaceuticals, Inc. 2014-01-14 Not applicable Showing 1 to 10 of 57 entries Previous 1 2 3 4 5 6 Next https://www.drugbank.ca/drugs/DB00390 2/25 5/25/2017 Digoxin ­ DrugBank Approved Generic Show 10 entries Prescription Products Search Name Dosage Strength Route Labeller Marketing Start Marketing End Apo- Tablet 0.25 mg Oral Apotex Corporation 2006-06-22 Not applicable digoxin Apo- Tablet 0.125 mg Oral Apotex Corporation 2006-06-22 Not applicable digoxin Apo- Tablet 0.0625 mg Oral Apotex Corporation 2006-06-22 Not applicable digoxin Digitek Tablet .125 mg/1 Oral Mylan Institutional 2015-05-06 Not applicable Digitek Tablet .125 mg/1 Oral Mylan Pharmaceuticals 2014-11-17 Not applicable Digitek Tablet .25 mg/1 Oral Mylan Institutional 2015-05-06 Not applicable Digitek Tablet .25 mg/1 Oral Mylan Pharmaceuticals 2014-11-17 Not applicable Digox Tablet 250 ug/1 Oral Aidarex Pharmaceuticals LLC 2002-07-26 Not applicable Digox Tablet 125 ug/1 Oral TYA Pharmaceuticals 2002-07-26 Not applicable Digox Tablet 125 ug/1 Oral Carilion Materials Management 2002-07-26 Not applicable Showing 1 to 10 of 76 entries Previous 1 2 3 4 5 … 8 Next Approved Over the Not Available Counter Products Unapproved/Other Not Available Products https://www.drugbank.ca/drugs/DB00390 3/25 5/25/2017 Digoxin ­ DrugBank International Show 10 entries Brands Search Name Company Agoxin Aristopharma Cardiacin Center Cardiogoxin Medipharma Cardioxin Oboi Cardoxin Not Available Celoxin Celon Centoxin Opsonin Digacin mibe Digocard-G Klonal Digoxina GlaxoSmithKline Showing 1 to 10 of 16 entries Previous 1 2 Next Brand mixtures Not Available Categories Anti-Arrhythmia Agents (/categories/DBCAT000520) Bradycardia-Causing Agents (/categories/DBCAT002703) Carbohydrates (/categories/DBCAT000085) Cardanolides (/categories/DBCAT000822) Cardenolides (/categories/DBCAT000823) Cardiac Glycosides (/categories/DBCAT000821) Cardiac Therapy (/categories/DBCAT002210) Cardiotonic Agents (/categories/DBCAT000589) Cardiovascular Agents (/categories/DBCAT000010) Cardiovascular System (/categories/DBCAT002169) Cytochrome P-450 CYP3A4 Substrates (/categories/DBCAT002646) Digitalis Glycosides (/categories/DBCAT000820) Enzyme Inhibitors (/categories/DBCAT000003) Glycosides (/categories/DBCAT000257) OATP1B1/SLCO1B1 Substrates (/categories/DBCAT002658) P-glycoprotein/ABCB1 Inducers (/categories/DBCAT002666) P-glycoprotein/ABCB1 Inhibitors (/categories/DBCAT002667) P-glycoprotein/ABCB1 Substrates (/categories/DBCAT002668) Protective Agents (/categories/DBCAT000367) Steroids (/categories/DBCAT000309) https://www.drugbank.ca/drugs/DB00390 4/25 5/25/2017 Digoxin ­ DrugBank UNII 73K4184T59 (http://fdasis.nlm.nih.gov/srs/srsdirect.jsp?regno=73K4184T59) CAS number 20830-75-5 Weight Average: 780.9385 Monoisotopic: 780.429606756 Chemical Formula C41H64O14 InChI Key LTMHDMANZUZIPE-PUGKRICDSA-N 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 IUPAC Name 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[8.7.0.0²,⁷.0¹¹,¹⁵]heptadecan-14-yl]-2,5-dihydrofuran-2-one SMILES [H][C@]12CC[C@]3([H])[C@]([H])(C[C@@H](O)[C@]4(C)[C@H](CC[C@]34O)C3=CC(=O)OC3)[C@@]1(C)CC[C@@H](C2)O[C@H]1C[C@H](O)[C@H](O[C@H]2C[C@H](O) [C@H](O[C@H]3C[C@H](O)[C@H](O)[C@@H](C)O3)[C@@H](C)O2)[C@@H](C)O1 Pharmacology Indication For the treatment and management of congestive cardiac insufciency, arrhythmias and heart failure. Structured Chronic Atrial Fibrillation (/indications/DBCOND0065022) Indications NYHA Class I or II heart failure (/indications/DBCOND0025082) NYHA Class III Heart Failure (/indications/DBCOND0048244) Pharmacodynamics Digoxin, a cardiac glycoside similar to digitoxin, is used to treat congestive heart failure and supraventricular arrhythmias due to reentry mechanisms, and to control ventricular rate in the treatment of chronic atrial brillation. Mechanism of Digoxin inhibits the Na-K-ATPase membrane pump, resulting in an increase in intracellular sodium. The sodium calcium exchanger (NCX)in turn tries to extrude the sodium action and in so doing, pumps in more calcium. Increased intracellular concentrations of calcium may promote activation of contractile proteins (e.g., actin, myosin). Digoxin also acts on the electrical activity of the heart, increasing the slope of phase 4 depolarization, shortening the action potential duration, and decreasing the maximal diastolic potential. Pharmacological Target Kind action Actions Organism UniProt ID Sodium/potassium-transporting ATPase subunit alpha- Protein yes Not Human P05023 (http://www.uniprot.org/uniprot/P05023) details 1 Available Related Articles Absorption Absorption of digoxin from the elixir pediatric formulation has been demonstrated to be 70% to 85% complete (90% to 100% from the capsules, and 60% to 80% for tablets). Volume of Not Available distribution Protein binding 25% https://www.drugbank.ca/drugs/DB00390 5/25 5/25/2017 Digoxin ­ DrugBank Metabolism Hepatic (but not dependent upon the cytochrome P-450 system). The end metabolites, which include 3 b-digoxigenin, 3-keto-digoxigenin, and their glucuronide and sulfate conjugates, are polar in nature and are postulated to be formed via hydrolysis, oxidation, and conjugation. Substrate Enzymes Product Digoxin 3 b-digoxigenin (/metabolites/DBMET00697) Details (/reactions/718) Not Available Digoxin 3-keto-digoxigenin (/metabolites/DBMET00716) Details (/reactions/737) Not Available Route of Following intravenous administration to healthy volunteers, 50% to 70% of a digoxin dose is excreted unchanged in the urine. elimination Half life 3.5 to 5 days Clearance Not Available Toxicity Toxicity includes ventricular tachycardia or ventricular brillation, or progressive bradyarrhythmias, or heart block. LD50 = 7.8 mg/kg (orally in mice). Affected organisms Humans and other mammals Pathways Not Available Pharmacogenomic Not Available Effects/ADRs Interactions https://www.drugbank.ca/drugs/DB00390 6/25 5/25/2017 Digoxin ­ DrugBank Drug Interactions Show 10 entries Search Drug Interaction Drug group 1,10-Phenanthroline The serum concentration of Digoxin can be increased when it is combined with 1,10-Phenanthroline. Experimental (/drugs/DB02365) 2-(4-Chlorophenyl)-5- Digoxin may decrease the cardiotoxic activities of 2-(4-Chlorophenyl)-5-Quinoxalinecarboxamide. Experimental Quinoxalinecarboxamide (/drugs/DB03509) 2-Methoxyestradiol Digoxin may decrease the cardiotoxic activities of 2-Methoxyestradiol. Investigational (/drugs/DB02342) 3-Methoxybenzamide Digoxin may decrease the cardiotoxic activities of 3-Methoxybenzamide. Experimental (/drugs/DB03073) 3,4-Dichloroisocoumarin The serum concentration of Digoxin can be increased when it is combined with 3,4- Experimental (/drugs/DB04459) Dichloroisocoumarin.
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