Drug intelligence / Profile preview

acetyldigitoxin

Development stage
Unknown
Lead developer
Sandoz
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Acetyldigitoxin is a cardenolide glycoside derived from digitoxin, used primarily as a cardiotonic and anti-arrhythmic agent in the management of congestive heart failure and certain cardiac arrhythmias. It acts by inhibiting the sodium/potassium-transporting ATPase (Na+/K+ ATPase) pump on the membranes of cardiac myocytes. This inhibition increases intracellular sodium, which subsequently raises intracellular calcium via reduced activity of the Na+/Ca2+ exchanger. The increased calcium enhances myocardial contractility (positive inotropic effect). Additionally, acetyldigitoxin increases vagal tone through central nervous system effects, slowing conduction through the atrioventricular node—an important mechanism for controlling ventricular rate in atrial fibrillation or flutter. Acetyldigitoxin is well absorbed orally and has been used for rapid digitalization due to its pharmacokinetic properties[1][2][4][5][6].

Other names
3'''-O-acetyldigitoxinAcylanid
02

Targets

ATP1A1 (Sodium/potassium-transporting ATPase subunit alpha-1)

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