Digitaline Nativelle

In the U.S.

• Digitek
• Digox
• Lanoxicaps
• Lanoxin
• Lanoxin Pediatric

In Canada

• Digitaline Nativelle

Available Dosage Forms:

• Tablet
• Capsule, Liquid Filled
• Solution
• Elixir

Therapeutic Class: Cardiovascular Agent

Pharmacologic Class: Cardiac Glycoside

Chemical Class: Digitalis Glycoside

You should not use digoxin if you have ventricular fibrillation (a heart rhythm disorder of the ventricles, or lower chambers of the heart that allow blood to flow out of the heart).

Avoid becoming overheated or dehydrated during exercise, in hot weather, or by not drinking enough fluids. Digoxin overdose can occur more easily if you are dehydrated.

Get emergency medical help if you have signs of an allergic reaction to digoxin: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

• nausea, vomiting, loss of appetite;

• fast, slow, or uneven heart rate;

• bloody or black, tarry stools;

• blurred vision, yellowed vision; or

• confusion, hallucinations, unusual thoughts or behavior.

Serious side effects may be more likely in older adults and those who are ill or debilitated.

Common digoxin side effects may include:

• nausea, diarrhea;

• feeling weak or dizzy;

• headache, weakness, anxiety, depression;

• enlarged breasts in men; or

• mild skin rash.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Other drugs may interact with digoxin, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.

Total loading dose: Administer one-half the total loading dose initially (all formulations), then give one-fourth the total loading dose every 6 to 8 hours for two doses (IV and tablets), or give additional fractions every 4 to 8 hours (oral solution).
-IV: 8 to 12 mcg/kg
-Tablets: 10 to 15 mcg/kg
-Oral solution: 10 to 15 mcg/kg

Maintenance dose:
-IV: 2.4 to 3.6 mcg/kg once a day
-Tablets: 3.4 to 5.1 mcg/kg once a day
-Oral solution: 3.0 to 4.5 mcg/kg once a day

Comments:
-IM administration is not recommended due to associated pain and muscle necrosis. If IM administration is required, no more than 500 mcg of the injectable formulation should be injected into a single site.
-If rapid titration is desired, initiate with a loading dose followed by maintenance dosing; otherwise, initiate with maintenance dosing without a loading dose.
-Maintenance dose may also be estimated by the following formula: Total maintenance dose = loading dose x (% daily loss/100). For recommended maintenance doses according to lean body weight and renal function and additional definitions regarding maintenance dose calculation, the manufacturer product information should be consulted.
-Reduce dose in patients whose lean weight is an abnormally small fraction of total body mass (e.g., obesity, edema).
-Doses may be increased every 2 weeks according to clinical response, serum drug levels, and toxicity.

Uses:
-Treatment of mild to moderate heart failure in adults. Where possible, this drug should be used in combination with a diuretic and an angiotensin-converting enzyme (ACE) inhibitor.
-Control of ventricular response rate in patients with chronic atrial fibrillation.

Data not available

Animal studies have not been reported. In humans, adverse fetal effects have been reported at doses that produced maternal toxicity. There are no controlled data in human pregnancy. AU TGA pregnancy category A: Drugs which have been taken by a large number of pregnant women and women of childbearing age without any proven increase in the frequency of malformations or other direct or indirect harmful effects on the fetus having been observed. US FDA pregnancy category C: Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.

Use is recommended only if clearly needed and the benefit outweighs the risk. AU TGA pregnancy category: A US FDA pregnancy category: C

Summary of Use during Lactation

Because of the low levels of digoxin in breastmilk, amounts ingested by the infant are small and would not be expected to cause any adverse effects in breastfed infants. If the mother is to receive digoxin intravenously, avoidance of breastfeeding for 2 hours after the dose will lessen the dose the infant receives.

Drug Levels

Maternal Levels. In 11 women taking digoxin 0.25 mg daily orally, milk digoxin levels obtained on days 3 to 7 postpartum were relatively constant at 0.644 mcg/L.[1] The amounts in milk represent an infant dosage of about 2.3% of the maternal weight-adjusted dosage or 0.097 mcg/kg daily, which is about 1% of the neonatal maintenance dosage.

Milk digoxin levels were 0.41 and 0.78 mcg/L in two mothers taking oral digoxin 0.25 mg daily.[2]

Milk digoxin levels ranged from undetectable (<0.5 mcg/L) to 1 mcg/L in 5 women treated with unspecified doses of digoxin. Milk and serum levels were similar.[3]

A milk digoxin level of 1.9 mcg/L was measured in a mother taking 0.75 mg daily of digoxin during pregnancy and postpartum.[4]

After an intravenous bolus dose of digoxin 0.5 mg in 11 women, digoxin serum and milk levels rapidly equilibrated, with high levels occurring rapidly, dropping to low levels by about 2 hours after the dose. A pharmacokinetic simulation using data from these mothers indicate that a fully breastfed infant would obtain a serum level of only about 3% of a therapeutic level with maternal intake of 0.5 mg daily of digoxin.[5]

Infant Levels. In two breastfed infants whose mothers were taking oral digoxin 0.25 mg daily, digoxin was undetectable (< 0.1 mcg/L) in their serum after 10 days of maternal therapy.[2]

A mother took 0.75 mg daily of digoxin during pregnancy and postpartum. Her infant had a serum level of 0.2 mcg/L after nursing for 7 days, having decreased from a level of 0.6 mcg/L at birth.[4]

Effects in Breastfed Infants

At least 4 infants have been reported to have been breastfed in studies on digoxin in breastmilk. None had any detectable digoxin effect.[2][4][6]

Effects on Lactation and Breastmilk

Relevant published information was not found as of the revision date.

References

1. Chan V, Tse TF, and Wong V. Transfer of digoxin across the placenta and into breast milk. Br J Obstet Gynaecol. 78;85:605-9. PMID: 687540

2. Loughnan PM. Digoxin excretion in human breast milk. J Pediatr. 78;92:1019-20. PMID: 660341

3. Levy M, Granit L, Laufer N. Excretion of drugs in human milk. N Engl J Med. 1977;297:789. Letter. PMID: 895815

4. Finley JP, Waxman MB, Wong PY et al. Digoxin excretion in human milk. J Pediatr. 1979;94:339-40. Letter. PMID: 762640

5. Reinhardt D, Richter O, Genz T et al. Kinetics of the transplacental passage of digoxin from breast feeding mothers to their infants. Eur J Pediatr. 1982;138:49-52. PMID: 7075628

6. Miller MR, Withers R, Bhamra R et al. Verapamil and breast-feeding. Eur J Clin Pharmacol. 1986;30:125-6. PMID: 3709626

Substance Name

Digoxin

CAS Registry Number

20830-75-5

Drug Class

Antiarrhythmics

Cardiac Glycosides