Metabolic disposition and cardiovascular effects of methyldopate in unanesthetized rhesus monkeys.
Methyldopate, the ethyl ester hydrochloride salt of alpha-methyldopa (alpha-MD), is used extensively in the treatment of severe hypertension. We have developed a high-pressure liquid chromatographic assay to determine the plasma-time concentrations of alpha-MD after intravenous administration of methyldopate and alpha-MD in the monkey in an effort to evaluate the bioavailability of alpha-MD and the extent of in vivo hydrolysis of the amino ester to the amino acid. The results establish that in this experimental situation methyldopate is not metabolically equivalent to alpha-MD.
D000818:Animals; D001682:Biological Availability; D001794:Blood Pressure / Q000187:drug effects; D002849:Chromatography, Gas; D000882:Haplorhini; D006439:Hemodynamics / Q000187:drug effects*; D008253:Macaca mulatta; D008297:Male; D013058:Mass Spectrometry; D008750:Methyldopa / Q000031:analogs & derivatives* / Q000097:blood / Q000494:pharmacology; D011674:Pulse / Q000187:drug effects; D013997:Time Factors
D008750:Methyldopa