Plasma level of the prodrug midodrine and its active metabolite in comparison with the alpha-mimetic action in dogs

Kolassa, N.; Schützenberger, W.G.; Wiener, H.; Krivanek, P.

Archives Internationales de Pharmacodynamie et de Therapie 238(1): 96-104

1979


ISSN/ISBN: 0003-9780
PMID: 90492
Document Number: 3655
Midodrine, i.v. or orally administered, causes a prolonged elevation of blood pressure and a reduction in heart rate. These cardiovascular changes are not correlated to the plasma levels of the intact drug. On administration of either midodrine or its metabolite, ST-1059, formed by cleavage of the glycine residue, the elevation of blood pressure and the reduction in heart rate were significantly correlated to the plasma level of ST-1059. The results are in agreement with the assumption that the pressor activity of midodrine is mainly exerted by its metabolite ST-1059.

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Plasma level of the prodrug midodrine and its active metabolite in comparison with the alpha-mimetic action in dogs