Clinical Use of Digitalis: A State of the Art Review

Thomas F. Whayne Jr


Am J Cardiovasc Drugs. 2018;18(6):427-440. 

In This Article

Clinically Relevant Digitalis Glycosides

Multiple cardiac glycosides exist and can also be classified as cardiotonic steroids, including digitalis leaf, digitoxin, digoxin, and ouabain (Table 1).[12] Cardiac glycosides, such as peruvoside, have even shown promise in the management of cancer, especially ovarian cancer and leukemia.[12] The cardiac glycosides all have a specific affinity to sodium–potassium adenosine triphosphatase ( Na+/K+-ATPase).[12] These cardiac glycosides, after binding, are highly specific inhibitors of cellular membrane Na+/K+-ATPase, which makes up the so-called cellular sodium pump and which couples membrane ion translocation to high-energy ATP hydrolysis.[13] Cardiac glycosides display functional variability, with different behaviors and therapeutic doses.[12] Digitalis leaf (prepared digitalis) is a raw mix of glycosides obtained from powdered foxglove leaves that requires biological standardization, but activity may still vary from one preparation of tablets to the next.[14] Digoxin, which is the most widely used digitalis derivative, comes from Digitalis lanata (the white foxglove), as does lanatoside-C, which is the glycoside precursor of digoxin.[14] Digitoxin is a pure glycoside obtained from D. purpurea; digitoxin has a slower onset of action than digoxin or lanatoside-C and its much longer half-life means accumulation in the body is greater.[14] Ouabain (strophanthin-G), which is also a pure glycoside, is usually obtained from Strophanthus gratus but can be derived from other vegetable sources.[14] Some clinicians consider ouabain uniquely valuable because of its rapid onset of action when such an effect has been considered advantageous.[14]