Ouabain is a highly toxic compound, however, it has a low bioavailability and is absorbed poorly from the alimentary tract as so much of the oral dose is destroyed. Intravenous administration results in greater available concentrations. After intravenous administration, the onset of action occurs within 2–10 minutes in humans with the maximum effect enduring for 1.5 hours.
Ouabain is eliminated by renal excretion, largely unchanged.