QuickView for digoxin (compound)

Summary
General Info

PubChem

PubChem Compound 2724385

Name:	Digoxin
PubChem Compound ID:	2724385
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 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 formula:	C₄₁H₆₄O₁₄
Molecular weight:	780.938 g/mol
Synonyms:	MLS000069819; SMR000059217; NCGC00090797-01; Digoxin; 20830-75-5; SPBio_002393; Prestwick_170; Prestwick0_000437; Prestwick1_000437

DrugBank

Identification

Name:	Digoxin
Name (isomeric):	DB00390
Drug Type:	small molecule
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 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)
Synonyms:	Digitalis Glycoside
Brand:	Neodioxanin, Digoxin Pediatric, Eudigox, Cogoxin, Rougoxin, Dixina, Stillacor, Dilanacin, Dynamos, Dokim, Longdigox, Lanacrist, Davoxin, Cardoxin, Cordioxil, Lanacordin, Homolle's Digitalin, Neo-Lanicor, Digitekt, Lanoxin, Lanicor, Lenoxin, Lanoxicaps, Vanoxin, Digacin, Lenoxicaps, SK-Digoxin
Category:	Cardiotonic Agents, Antiarrhythmic Agents, Enzyme Inhibitors, Anti-Arrhythmia Agents
CAS number:	20830-75-5

Pharmacology

Indication:	For the treatment and management of congestive cardiac insufficiency, arrhythmias and heart failure.
Pharmacology:	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 fibrillation.
Mechanism of Action:	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 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 t... show more » 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 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. show less «
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).
Protein binding:	25%
Biotransformation:	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.
Route of elimination:	Following intravenous administration to healthy volunteers, 50% to 70% of a digoxin dose is excreted unchanged in the urine.
Half Life:	3.5 to 5 days
Toxicity:	Toxicity includes ventricular tachycardia or ventricular fibrillation, or progressive bradyarrhythmias, or heart block. LD₅₀ = 7.8 mg/kg (orally in mice).
Affected organisms:	Humans and other mammals

Interactions

Food interaction:

Avoid avocado.

Limit garlic, ginger, gingko, and horse chestnut.

Avoid milk, calcium containing dairy products, iron, antacids, or aluminum salts 2 hours before or 6 hours after using antacids while on this medication.

Avoid salt substitutes containing potassium.

Avoid bran and high fiber foods within 2 hours of taking this medication.

Drug interaction:

Dextrothyroxine	The thyroid hormone, dextrothyroxine, decreases the effect of digoxin.
Gatifloxacin	Gatifloxacin increases the effect of digoxin
Hydrochlorothiazide	Possible electrolyte variations and arrhythmias
Verapamil	Verapamil may increase the serum concentration of Digoxin by decreasing its metabolism and clearance. Monitor for changes in the therapeutic/adverse effects of Digoxin if Verpamail is initiated, discontinued or dose changed.
Colestipol	The resin decreases the effect of digoxin

Dextrothyroxine	The thyroid hormone, dextrothyroxine, decreases the effect of digoxin.
Gatifloxacin	Gatifloxacin increases the effect of digoxin
Hydrochlorothiazide	Possible electrolyte variations and arrhythmias
Verapamil	Verapamil may increase the serum concentration of Digoxin by decreasing its metabolism and clearance. Monitor for changes in the therapeutic/adverse effects of Digoxin if Verpamail is initiated, discontinued or dose changed.
Colestipol	The resin decreases the effect of digoxin
Metolazone	Possible electrolyte variations and arrhythmias
Doxorubicin	The antineoplasic agent decreases the effect of digoxin
Propafenone	Propafenone increases the effect of digoxin
Ticlopidine	Ticlopidine may decrease Digoxin levels. Monitor for Digoxin levels with Ticlopidine is initiated, discontinued or dose changed.
Clarithromycin	The macrolide, clarithromycin, may increase the effect of digoxin in 10% of patients.
Cyclophosphamide	The antineoplasic agent decreases the effect of digoxin
Chlorthalidone	Possible electrolyte variations and arrhythmias
Bumetanide	Possible electrolyte variations and arrhythmias
Erythromycin	The macrolide, erythromycin, may increase the effect of digoxin in 10% of patients.
Chlorothiazide	Possible electrolyte variations and arrhythmias
Polythiazide	Possible electrolyte variations and arrhythmias
Spironolactone	Increased digoxin levels and decreased effect in presence of spironolactone
Quinidine barbiturate	Quinine/quinidine increases the effect of digoxin
Bleomycin	The antineoplasic agent decreases the effect of digoxin
Hydroxychloroquine	Hydroxychloroquine increases the effect of digoxin
Liotrix	The thyroid hormone, liotrix, decreases the effect of digoxin.
Methyclothiazide	Possible electrolyte variations and arrhythmias
Quinine	Quinine/quinidine increases the effect of digoxin
Indapamide	Possible electrolyte variations and arrhythmias
Alprazolam	The benzodiazepine, alprazolam, may increase the effect of digoxin.
Vincristine	The antineoplasic agent decreases the effect of digoxin
Cyclosporine	Cyclosporine may increase the effect of digoxin.
Bendroflumethiazide	Possible electrolyte variations and arrhythmias
Furosemide	Possible electrolyte variations and arrhythmias
Cholestyramine	The resin decreases the effect of digoxin
Amiodarone	Amiodarone may increase the effect of digoxin.
St. John's Wort	St. John's Wort decreases the effect of digoxin
Benzthiazide	Possible electrolyte variations and arrhythmias
Methotrexate	The antineoplasic agent decreases the effect of digoxin
Trichlormethiazide	Possible electrolyte variations and arrhythmias
Carmustine	The antineoplasic agent decreases the effect of digoxin
Ethacrynic acid	Possible electrolyte variations and arrhythmias
Voriconazole	Voriconazole may increase the serum concentration of digoxin. Monitor for increased serum concentrations and toxic effects of digoxin if voriconazole is initiated or dose increased.
Prazosin	Prazosin increases the effect of digoxin
Ritonavir	Ritonavir increases levels/effect of digoxin
Propylthiouracil	The antithyroid agent may increase the effect of digoxin.
Telmisartan	Telmisartan may increase plasma Digoxin concentrations. Monitor Digoxin levels and adjust dose as required if Telmisartan is initiated, discontinued or dose changed.
Liothyronine	The thyroid hormone, liothyronine, decreases the effect of digoxin.
Quinethazone	Possible electrolyte variations and arrhythmias
Rabeprazole	Rabeprazole increases the effect of digoxin
Quinidine	Quinine/quinidine increases the effect of digoxin
Acarbose	Acarbose may decrease the serum levels of digoin. It is thought that acarbose reduces digoin absorption. Monitor for changes in digoxin serum levels and therapeutic and adverse effects if acarbose is initiated, discontinued or dose changed.
Thyroglobulin	The thyroid hormone, thyroglobulin, decreases the effect of digoxin.
Levothyroxine	The thyroid hormone, levothyroxine, decreases the effect of digoxin.
Penicillamine	Penicillamine decreases the effect of digoxin
Trimetrexate	The absorption of Digoxin, a cardiac glycoside, may be decreased by antineoplastic agents such as Trimetrexate. Liquid forms of Digoxin do not appear to be significantly affected. Monitor Digoxin tablet efficacy if Trimetrexate therapy is initiated, discontinued or if the dose is altered.
Telithromycin	Telithromycin may increase the plasma concentration of Digoxin. Monitor for changes in Digoxin efficacy/toxicity if Telithromycin is initiated, discontinued or dose changed.
Procarbazine	The antineoplasic agent decreases the effect of digoxin
Cyclothiazide	Possible electrolyte variations and arrhythmias
Carvedilol	Carvedilol may increase the serum levels and effect of digoxin.
Methimazole	The antithyroid agent increases the effect of digoxin
Hydroflumethiazide	Possible electrolyte variations and arrhythmias
Diazepam	The benzodiazepine, diazepam, may increase the effect of digoxin.
Ginseng	Changes in digoxin serum levels
Tolbutamide	Tolbutamide increases the effect of digoxin
Ranolazine	Ranolazine may increase the serum level of digoxin. Monitor for changes in the serum level and therapeutic and adverse effects of digoxin if ranolazine is initiated, discontinued or dose changed.
Josamycin	The macrolide, josamycin, may increase the effect of digoxin in 10% of patients.
Penciclovir	The multivalent agent decreases the effect of penicillamine
Dihydroquinidine barbiturate	Quinine/quinidine increases the effect of digoxin
Cytarabine	The antineoplasic agent decreases the effect of digoxin
Itraconazole	Itraconazole increases the effect of digoxin
Sulfasalazine	Sulfasalazine may decrease the effect of digoxin.
Cinitapride	Cinitapride can alter the absorption of digoxin as it simulates gastric emptying.