心律不整、心衰竭 Atrial fibrillation or atrial flutter: Control of ventricular response rate in adults with chronic atrial fibrillation Heart failure with reduced ejection fraction (HFrEF): Mild to moderate (or stage C) heart failure in adults
#仿單變更2021#仿單變更2022
藥理
Antiarrhythmic Agent; Cardiac Glycoside:
1. Supraventricular arrhythmias: Direct suppression of the AV node conduction to increase effective refractory period and decrease conduction velocity.
2. Heart failure: Inhibition of the Na+-K+-ATPase pump in myocardial cells, which in turn promotes calcium influx leading to increased contractility.
藥動學
Distribution
1. Vd: Extensive to peripheral tissues, heart/serum concentration is 70:1
2. Protein binding:~25% Metabolism
only ~16% is metabolized to 3-beta-digoxigenin, 3-keto-digoxigenin, dihydrodigoxin<20220324>, and glucuronide and sulfate conjugates Excretion
Mainly in urine, 50-70% as unchanged drug, by glomerular filtration and active tubular secretion Pharmakodynamics
1. Therapeutic plasma concentrations: (adults) generally 0.5–2 ng/mL.
2. Onset of action: (Heart rate control)5 to 60 minutes
3. Duration: (Adult) 3-4 days
禁忌症
1. Ventricular fibrillation
2. Digitalis intoxication
3. Hypersensitivity to digoxin, other forms of digitalis
懷孕分類
C; Although limited experience, the data is lacking association between the drug and congenital defects.
哺乳分類
The amount of digoxin available to the infant via breast milk is not likely to be clinically significant. WHO considers digoxin to be compatible with breastfeeding
副作用
GI disturbance, anorexia (the earliest symptom of digoxin overdose), cardiac arrhythmia, conduction defect, blurred vision, halos around bright objects, disturbed color vision (yellow vision)
劑量和給藥方法
Administration:
IV preferred, inject slowly ≥5 minutes. Atrial fibrillation/flutter: for rate control
Initial 0.25 to 0.5 mg over several minutes, with repeat doses of 0.25 mg Q6H to a maximum of 1.5 mg over 24 hours Heart failure with reduced ejection fraction (HFrEF):
Loading dose not recommended
小兒調整劑量
Loading dose:(IV)
1. Neonate(<1.5kg): 20 mcg/kg within 24 hours
2. Neonate(1.5-2.5kg): 30 mcg/kg within 24 hours
3. 1-24 months, 2-5 years of age: 35 mcg/kg within 24 hours
4. 5-10 years of age: 25 mcg/kg within 24 hours<2021/8/17> Maintenance dose:
1. Neonate: 20% of loading dose within 24 hours
2. 1 month to 10 years of age: 25% of loading dose within 24 hours<2021/8/17>
腎功能調整劑量
Loading dose:
1. CrCl >15 mL/minute: No dosage adjustment necessary
2. CrCl ≤15 mL/minute: Administer 50% of usual dose
3. Hemodialysis, peritoneal dialysis: Use only when rapid ventricular rate control is necessary, reduce to 50% of usual dose Maintenance dose:
1. CrCl ≥60 mL/minute: No dosage adjustment necessary
2. CrCl 45 to 60 mL/minute: 0.0625 to 0.125 mg once daily
3. CrCl 30 to 45 mL/minute: 0.0625 mg once daily
4. CrCl <30 mL/minute, hemodialysis, peritoneal dialysis: 0.0625 mg every 48 hours or consider alternative agent