Acigoxin: Full Drug Profile

Acigoxin - General Information

Cardioactive derivative of lanatoside A or of digitoxin used for fast digitalization in congestive heart failure.

Pharmacology of Acigoxin

The main pharmacological effects of acetyldigitoxin are on the heart. Extracardiac effects are responsible for many of the adverse effects. Its main cardiac effects are 1) a decrease of conduction of electrical impulses through the AV node, making it a commonly used drug in controlling the heart rate during atrial fibrillation or atrial flutter, and 2) an increase of force of contraction via inhibition of the Na⁺/K⁺ ATPase pump.

Additional information about Acigoxin

Acigoxin Indication

Used for fast digitalization in congestive heart failure.

Mechanism Of Action

Acigoxin binds to a site on the extracellular aspect of the α-subunit of the Na⁺/K⁺ ATPase pump in the membranes of heart cells (myocytes). This causes an increase in the level of sodium ions in the myocytes, which then leads to a rise in the level of calcium ions. The proposed mechanism is the following: inhibition of the Na⁺/K⁺ pump leads to increased Na⁺ levels, which in turn slows down the extrusion of Ca²⁺ via the Na⁺/Ca²⁺ exchange pump. Increased amounts of Ca²⁺ are then stored in the sarcoplasmic reticulum and released by each action potential, which is unchanged by acetyldigitoxin. This is a different mechanism from that of catecholamines. Acigoxin also increases vagal activity via its central action on the central nervous system, thus decreasing the conduction of electrical impulses through the AV node. This is important for its clinical use in different arrhythmias.

Generic Name

Acetyldigitoxin

Drug Category

Anti-Arrhythmia Agents; Cardiotonic Agents; Enzyme Inhibitors

Drug Type

Small Molecule; Approved

Other Brand Names containing Acetyldigitoxin

Acylanid; Crystodigin; Acigoxin;

Absorption

Bioavailability is 60 to 80% following oral administration.

Toxicity (Overdose)

Toxicity includes ventricular tachycardia or ventricular fibrillation, or progressive bradyarrhythmias, or heart block. LD50 = 7.8 mg/kg (orally in mice).

Dosage Forms of Acigoxin

Injection Intravenous

Chemical IUPAC Name

[(2R,3R,4S,6S)-3-hydroxy-6-[(2R,4S,6S)-4-hydroxy-6-[(2R,3S,4S,6R)-4-hydroxy-6-[[(5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2H-furan-3-yl)-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-3-yl]oxy]-2-methyloxan-3-yl]oxy-2-methyloxan-3-yl]oxy-2-methyloxan-4-yl] acetate

Chemical Formula

C43H66O14

Acetyldigitoxin on Wikipedia

https://en.wikipedia.org/wiki/Acetyldigitoxin

Organisms Affected

Humans and other mammals