Digitoxin is a naturally occurring cardiac glycoside and pharmaceutical active ingredient belonging to the digitalis group of compounds. It acts primarily on the Na⁺/K⁺-ATPase enzyme and has positive inotropic effects on cardiac muscle.
Digitoxin is identified by CAS No. 71-63-6. Its molecular formula is C41H64O13 and its molecular weight is approximately 764.94 g/mol.
Digitoxin is a steroidal cardiac glycoside structurally related to digoxin. It contains a steroid nucleus, a lactone ring and three digitoxose sugar residues. Its pharmacological activity is associated with inhibition of the sodium-potassium ATPase pump.
Digitoxin inhibits Na⁺/K⁺-ATPase, increasing intracellular sodium concentration in cardiac cells. This indirectly increases intracellular calcium availability and enhances myocardial contractility.
Digitoxin also influences cardiac conduction and autonomic activity, which contributes to its therapeutic and pharmacological effects.
Digitoxin binds to and inhibits the Na⁺/K⁺-ATPase pump in cardiac muscle cells. Increased intracellular sodium reduces the activity of the sodium-calcium exchanger, resulting in increased intracellular calcium.
The increased calcium availability enhances cardiac muscle contraction, producing a positive inotropic effect.
Digitoxin has historically been used in pharmaceutical preparations for certain cardiac conditions, including:
Its use is highly dependent on current clinical guidelines and regulatory approval in the intended market.
Digitoxin is relevant to pharmaceutical manufacturers and formulation-development organizations working with cardiac glycoside and cardiovascular pharmaceutical products.
Because cardiac glycosides have a narrow therapeutic index, stringent control of identity, assay, purity and related substances is particularly important during pharmaceutical development and manufacturing.
Digitoxin API quality evaluation may include:
Testing should be performed using validated analytical methods appropriate for the API.
Digitoxin intended for pharmaceutical manufacturing should comply with applicable GMP, quality-control and regulatory requirements.
Because Digitoxin is a potent cardiac glycoside, manufacturing and handling should follow appropriate occupational safety, containment and quality-control procedures.
A batch-specific Certificate of Analysis (CoA) should provide relevant analytical results and acceptance criteria.
Digitoxin API should be stored in tightly closed, appropriately labelled containers under the manufacturer's specified storage conditions. Protection from excessive heat, moisture and unsuitable environmental exposure should be maintained.
Digitoxin is relevant to pharmaceutical companies developing cardiovascular and cardiac glycoside formulations.
For commercial pharmaceutical applications, customers should verify the API grade, identity, assay, purity, impurity profile, specification, regulatory documentation and batch-specific CoA before use.
Consistent Digitoxin API quality is essential for reliable pharmaceutical formulation and manufacturing. Control of identity, potency, purity and related substances supports reproducible product quality.
Appropriate documentation may include a Certificate of Analysis, specification sheet, safety documentation and applicable regulatory information.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | NLT 98.0% by HPLC |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.2% |
| Heavy Metals | NMT 10 ppm |
| pH (1% Solution) | 2.0 – 4.0 |
| Individual Impurity | ≤ 0.5% |
| Water Content | NMT 0.5% |
| Melting Point | 150°C – 154°C |