Plasma level of the prodrug midodrine and its active metabolite in comparison with the alpha-mimetic action in dogs.
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.
D000316:Adrenergic alpha-Agonists; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D004285:Dogs; D004983:Ethanolamines / Q000494:pharmacology*; D006339:Heart Rate / Q000187:drug effects; D006439:Hemodynamics / Q000187:drug effects; D008297:Male; D008879:Midodrine / Q000097:blood / Q000378:metabolism / Q000494:pharmacology*; D013997:Time Factors
D000316:Adrenergic alpha-Agonists; D004983:Ethanolamines; D008879:Midodrine