Crystodigin - General Information
Cardioactive derivative of lanatoside A or of digitoxin used for fast digitalization in congestive heart failure.
Pharmacology of Crystodigin
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 Crystodigin
Crystodigin Indication: Used for fast digitalization in congestive heart failure.
Mechanism Of Action: Crystodigin 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. Crystodigin 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.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Acetyldigitoxin
Synonyms: Not Available
Drug Category: Anti-Arrhythmia Agents; Cardiotonic Agents; Enzyme Inhibitors
Drug Type: Small Molecule; Approved
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).
Protein Binding: Not Available
Biotransformation: Not Available
Half Life: Not Available
Dosage Forms of Crystodigin: 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