Digoxin is one of the primitive cardiovascular medications for congestive heart failure (CHF) and atrial arrhythmias (heart rhythm problems). It is approved by the FDA in 1954 as a cardiac glycoside. Digoxin uses enhance blood flow and force of muscle contraction by inhibiting the reaction of ATPase, an enzyme that regulates the action of calcium, potassium, and sodium in the muscles of the heart. It also treats edema or swelling in the hands and ankles that are caused due to a weak heart.

In the case of pediatric patients, it is used for treating myocardial contractility or heart failure.

This drug is derived from the foxglove plant, also known as Digitalis plant. Hence, it is nomenclature as Digitalis. It is one of the ancient cardiac glycosides prescribed to patients since the 1250s. The therapeutic benefit of this medicinal plant was first discovered by William Withering.

Chemical Formulae – C₄₁H₆₄O₁₄

Weight – 780.9385 mg

Mechanism of Action

Effects of Digoxin in heart failure are as follows:

• Hemodynamic – Dynamics of blood flow.
• Electrophysiologic – Electric system or activity of the heart.
• Neurohormonal – Nerve and hormonal mechanism effective on the heart.

Digoxin is used toreversibly inhibit the sodium-potassium enzyme, which provides beneficial effects. The Na-K ATPase enzyme (sodium pump) maintains the intracellular environment by balancing the entry and exit of Na, K & Ca. Digitalis restricts the sodium pump that enhances intracellular calcium and sodium level inside the myocardial cells. This increases the contractile force of the heart and left ventricular ejection fraction, which is an important cardiac function.

Pathophysiology of heart failure treatmentincludes neurohormonal activation. Digoxin stimulates the parasympathetic nervous system through the vagus nerve, which leads to the SA node (Sinoatrial) or AV node (Atrioventricular). This decreases the heart rate and norepinephrine by activating the parasympathetic nervous system. (2)

Digitalization & Toxicity

Digoxin requires several days of consistent intake to reach a stable therapeutic plasma level, hence, an extra special dosing regimen is required. Loading dosages are required to increase the plasma level. This process is called as Digitalization.

The therapeutic plasma concentration estimation is 0.5 to 1.5ng/ml. However, it is essential to keep a check that the optimum level is crossed as Digitalis compounds have a narrow safety window. Anything above 2.0ng/ml is digital toxicity. It takes a great many days to drop to a safe level due to long-time action. Potassium supplements can reverse the toxic effect. (3)

Side Effects

Digoxin side effects are as follows:

• Nausea, vomiting, and loss of appetite.
• Drowsiness.
• Vision problem.
• Confusion.
• Headache.
• Slow or irregular heartbeat.
• Muscle cramp.

Drug Interaction

If someone is on the following drugs, then they must inform a doctor about their medical history:

• Antibiotics.
• Antiarrhythmic drug.
• Ca⁺channel blockers.
• Drugs related to cardiac diseases.
• Anti-anxiety drugs.
• Antifungal drugs.
• Ulcer related medicines.
• Antacids.
• Diuretic
• Cancer related medicines.
• Colitis and cholesterol related drugs.

Consult a doctor before taking any medicine.

Digoxin, an API

Active Pharmaceutical Ingredients (API) is the main medicinal and therapeutic constituent in medicine. Along with it, other non-medicinal components make a drug or medicine. Anzen Exports is one of the leading API exporters, procuring superior quality of API from the Indian market, and exporting to international companies. We are serving this industry for the last 29 years. Place your inquiry regarding API and educe the best deal.

Disclaimer:

Anzen Exports’ blog posts are based just on our research from cited websites. To be best informed, we advise consulting a doctor about an ingredient or medicine prior to taking it.

 

Sources:

1. Drug Bank
   Website – https://go.drugbank.com/drugs/DB00390
2. Drug Bank
   Website – https://go.drugbank.com/drugs/DB00390
3. Cardiovascular Pharmacology Concept
   Website – https://www.cvpharmacology.com/cardiostimulatory/digitalis
4. Texas Heart Institute
   Website – https://www.texasheart.org/heart-health/heart-information-center/topics/digitalis-medicines/