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CARDIOVASCULAR SYSTEM › CARDIAC THERAPY › CARDIAC GLYCOSIDES › Digitalis glycosides
digitoxin
C01AA04
Forms & Strengths
- Oral tablets: 0.1 mg
- Oral tablets: 0.2 mg
Adult Dosing
- Digitalization (rapid): 0.6 to 1.2 mg divided in doses over 24 hours
- Digitalization (slow): 0.2 mg daily for 4 days, then maintenance
- Maintenance: 0.05 to 0.15 mg orally once daily
Pediatric Dosing
- Safety and efficacy not well established in pediatric patients; use is generally avoided
- Neonates/Infants (if used): Total digitalisizing dose 0.02 to 0.03 mg/kg divided over 24 hours
Indications
- Heart failure with reduced ejection fraction
- Atrioventricular nodal tachyarrhythmias (e.g., rate control in atrial fibrillation)
Mechanism of Action
- Inhibition of the Na+/K+-ATPase membrane pump in myocardial cells
- Increases intracellular sodium, leading to increased intracellular calcium via Na+/Ca2+ exchanger
- Enhances myocardial contractility (positive inotrope)
- Decreases conduction velocity through the AV node and increases vagal tone
Contraindications
- Ventricular fibrillation
- Second- or third-degree atrioventricular block without a pacemaker
- Wolff-Parkinson-White syndrome associated with atrial fibrillation
- Known hypersensitivity to digitoxin or other digitalis glycosides
- Hypertrophic obstructive cardiomyopathy (unless coexisting heart failure/atrial fibrillation)
Adverse Reactions
- Cardiac arrhythmias (PVCs, bigeminy, trigeminy, AV block)
- Nausea, vomiting, anorexia, diarrhea
- Visual disturbances (blurred vision, yellow-green halos/xanthopsia)
- Central nervous system effects (fatigue, dizziness, headache, confusion)
Drug Interactions
- Potassium-depleting diuretics (thiazides, loop diuretics) increase risk of digitalis toxicity
- Amiodarone, quinidine, and verapamil increase serum digitoxin levels
- Inducers of CYP3A4 (e.g., rifampin, barbiturates) decrease digitoxin efficacy
- Beta-blockers and non-dihydropyridine calcium channel blockers enhance AV nodal blockade
Curated Content: Needs Vetting Before Put to Clinical Use