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(Circulation. 1972;45:1176.)
© 1972 American Heart Association, Inc.

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Ouabain Pharmacokinetics in Dog and Man

Determination by Radioimmunoassay

RICHARD SELDEN M.D.¹; THOMAS W. SMITH M.D.¹; William Findley B.A.¹

¹ From the Cardiac Unit, Department of Medicine, Massachusetts General Hospital and Harvard Medical School, Boston, Massachusetts 02114.

The pharmacokinetics of the relatively polar and rapidly acting cardiac glycoside ouabain (G-strophanthin) were studied in dogs and human subjects by the use of a newly devised radioimmunoassay technic. This method had high specificity and a sensitivity of less than 0.1 ng of ouabain per ml of plasma or urine. After administration of a single intravenous dose, the plasma ouabain concentration fell rapidly in both dogs and humans. After 7 hours, a phase of exponential decline was reached which had a half-life of 18 hours in dogs and 21 hours in normal human subjects. Repeated intravenous administration of ouabain to human subjects for 9 consecutive days resulted in the establishment of a plateau of plasma concentration and urinary excretion after 4-5 days, confirming plasma and urinary half-lives in the 19-24-hour range. The mean ratio of renal clearance of ouabain to that of creatinine was 0.81 in the human subjects. The plasma half-life of ouabain determined in these studies is in good agreement with previous observations of the half-life of dissipation of positive inotropy and of slowing of ventricular response to atrial fibrillation after ouabain administration.

Key Words: Cardiac glycoside • Ouabain-specific antibody • Digitalis glycoside • Tritiated ouabain • G-Strophanthin

Submitted on October 27, 1971
Accepted on January 7, 1972

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