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Influence of digitalis and diuretics on ouabain binding sites on human erythrocytes

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Summary

It has been reported that during chronic treatment with digitalis, the number of digitalis binding sites is increased in human erythrocytes [22]. From this finding a tachyphylaxis for cardiac glycosides has been postulated. We reinvestigated this problem in several groups of patients.

The number of3H-ouabain binding sites per erythrocyte in control persons (group I) was 214±60,n=43 (x±SD). The dissociation constant (KD) was 1.8±0.5 nM. Thirteen patients (group II) taking cardiac glycosides only, for at least 6 months, had 281±99 (p<0.05) ouabain binding sites per single red cell, KD=1.8±0.7 nM. Group III (34 patients) took digitalis for more than 6 months and diuretics for at least 3 months (352±126 (p<0.001), KD=1.6±0.6). Twenty-three of these (group IV) were taking a combination with “K+-saving” diuretics (336±194 (p<0.01), KD=1.6±0.5) and (group V, 11 patients) a combination with “K+-losing” diuretics (462±133 (p<0.001), KD=1.4±0.4). Nine patients (group VI) had a chronic hypokalemia, mainly due to taking furosemide (437±98 (p<0.001), KD=1.5±0.4). Four control persons took 50 mg hydrochlorothiazide daily for more than 4 months without measurable K+-losses and without changes in ouabain binding sites.

It is concluded from these findings that diuretic treatment with chronic hypokalemia in addition to digitalis is accompanied by a significant increase in ouabain binding sites in human red cells. Although the difference between control persons and those taking cardiac glycosides only, is statistically significant (p<0.05), the biological relevance is questionable because of considerable overlap of the values. Receptor affinity was unchanged under all circumstances. A change in the number of ouabain binding sites — if occurring also in the heart — may go along with an altered digitalis sensitivity.

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  1. Medizinische Klinik I der Universität München, Klinikum Großhadern, München

    E. Erdmann, K. Werdan & W. Krawietz

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  1. E. Erdmann
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  2. K. Werdan
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  3. W. Krawietz
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Supported by the DFG (Er 65/4-3)

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Erdmann, E., Werdan, K. & Krawietz, W. Influence of digitalis and diuretics on ouabain binding sites on human erythrocytes. Klin Wochenschr 62, 87–92 (1984). https://doi.org/10.1007/BF01769668

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  • DOI: https://doi.org/10.1007/BF01769668

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