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  • Title: Metabolic disposition and cardiovascular effects of methyldopate in unanesthetized rhesus monkeys.
    Author: Walson PD, Marshall KS, Forsyth RP, Rapoport R, Melmon KL, Castagnoli N.
    Journal: J Pharmacol Exp Ther; 1975 Oct; 195(1):151-8. PubMed ID: 810574.
    Abstract:
    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.
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