Digoxin inhibits sodium-potassium ATPase, which increases intracellular sodium concentration leading to increased intracellular calcium concentration. Autonomic effects of this include vagomimetic action and baroreceptor sensitization which lead to positive inotropic action, reduced sympathetic response and decreased renin-angiotensin system output (neurohormonal deactivation)
藥動學
Bioavailability, oral solution: 70% to 85%; Protein binding: 25%; Vd: 475 to 500 L ( hyperthyroidism: Increased, hypothyroidism: Decreased. Metabolism- Hepatic: 13%, not CYP450-dependent; Excretion-Renal: 50% to 70% unchanged, Fecal: 3% to 5%, Biliary: 6% to 8%, Dialyzable: No (hemodialysis, peritoneal); Elimination Half Life: 1.5 to 2 days (Anuric patients: 3.5 to 5 days)
禁忌症
Ventricular fibrillation, digitalis intoxication.
懷孕分類
C Although limited experience, the data is lacking association between the drug and congenital defects.
哺乳分類
Safe; the milk/plasm ratio have varies from 0.6-0.9. No adverse effects in the nursing infant have been reported
副作用
GI disturbance, anorexia (the earliest symptom of digoxin overdose), cardiac arrhythmia, and conduction defect.
劑量和給藥方法
Adults: Oral: rapid digitalization: 0.75-1.5mg, maintenance dose: 0.125-0.25mg; Infants and Children: 10-20ug/kg/day by mouth
Heart failure
(Oral solution) Loading dose, first dose: Give half the total loading dose; for subsequent doses as clinically indicated, give additional fractions of the total loading dose at 4- to 8-hour intervals; total oral loading dose: (premature) 20 to 30 mcg/kg; (full term) 25 to 35 mcg/kg; (1 to 24 months) 35 to 60 mcg/kg; (2 to 5 years) 30 to 45 mcg/kg; (5 to 10 years) 20 to 35 mcg/kg; (older than 10 years) 10 to 15 mcg/kg
(Oral solution) Maintenance dosage, (premature) 2.3 to 3.9 mcg/kg twice daily; (full term) 3.8 to 5.6 mcg/kg twice daily; (1 to 24 months) 5.6 to 9.4 mcg/kg twice daily; (2 to 5 years) 4.7 to 6.6 mcg/kg twice daily; (5 to 10 years) 2.8 to 5.6 mcg/kg twice daily; (older than 10 years) 3 to 4.5 mcg/kg once daily