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Studies on the metabolism of guanethidine in hypertensive patients
Authors:K H Rahn  P G Dayton
Affiliation:1. Department of Excellence-Biomedical Sciences and Public Health, Università Politecnica delle Marche, 60121 Ancona, Italy;2. Servei de Farmacologia Clínica, Hospital Universitari Germans Trias i Pujol (HUGTiP, IGTP)- Universitat Aut`onoma de Barcelona, Unitat Docent HUGTiP, Badalona, Spain;3. National Centre on Addiction and Doping, Istituto Superiore di Sanit`a, Rome, Italy;4. Tbilisi State University, Institute of Physical and Analytical Chemistry, School of Exact and Natural Sciences, 0179 Tbilisi, Georgia;5. Phenomenex Inc., 411 Madrid Ave., Torrance 90501, CA, USA;1. Bydgoszcz University of Science and Technology, Faculty of Chemical Technology and Engineering, Seminaryjna 3, 85-326, Bydgoszcz, Poland;2. Nicolaus Copernicus University in Toruń, Faculty of Pharmacy, Jurasza 2, 85-089, Bydgoszcz, Poland;1. Unit of Forensic Toxicology, Department of Anatomical, Histological, Forensic, and Orthopedic Sciences, Università la Sapienza, V. Le Regina Elena 366, 00161 Rome, Italy;2. Department of Excellence of Biomedical Science and Public Health, University “Politecnica delle Marche” of Ancona, Via Tronto 10/a, 60124, Ancona, Italy;3. National Centre on Addiction and Doping, Istituto Superiore di Sanità, V. Le Regina Elena 299, 00161 Rome, Italy;4. Institute of Emerging Health Professions, Thomas Jefferson University, Philadelphia, PA, USA
Abstract:The urinary excretion of guanethidine (G) and its metabolites was studied in seven subjects with essential hypertension after a single oral dose of 14C-G and after long-term treatment with oral doses ranging from 10 to 141 mg daily.One metabolite (M1) could be adsorbed on and eluted from cationic exchange resin in the same way as G itself. However, G was extractable into ether from alkaline solutions, whereas M1 remained in the aqueous phase. Both G and M1 were measured by a specific fluorometric method and by radioassay. The urine of patients treated with 14C-G contained more radioactivity than could be accounted for by G and M1, indicating the presence of at least one more metabolite of the drug.
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