Document Detail


Pharmacokinetics of pyrazinoyl-guanidine, 3-aminopyrazinoyl-guanidine and their corresponding pyrazinoic acid metabolites in humans and dogs.
MedLine Citation:
PMID:  1438523     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Pyrazinoylguanidine (PZG), 3-aminopyrazinoylguanidine (NH2PZG) and their pyrazinoic acid metabolites were measured by a new reverse-phase HPLC method in the serum of dogs and humans after administration of PZG, NH2PZG or 2-pyrazinoic acid (PZA). Kinetic properties of PZG and its principal metabolite, PZA, were studied in normal humans and also in azotemic patients, since PZG acts on renal tubules of patients with kidney failure to increase urea elimination. In humans and dogs, PZG was rapidly hydrolyzed to PZA. The serum half-life (t1/2) of PZG was 1 h. In turn, PZA was metabolized to 5-hydroxy-PZA, but no evidence appeared for conjugation of PZA with glycine. The apparent volume of distribution of PZG and its 3-amino analog, NH2PZG, exceeded that of total body water. In the dog the serum t1/2 for NH2PZG was twice that of PZG. Compared to PZG, NH2PZG and its metabolite, 3-aminopyrazinoic acid, were much stabler in vitro in serum and water.
Authors:
G T Passananti; E S Vesell; E V Jeszenka; R T Gelarden; K H Beyer
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Publication Detail:
Type:  Comparative Study; Journal Article    
Journal Detail:
Title:  Pharmacology     Volume:  45     ISSN:  0031-7012     ISO Abbreviation:  Pharmacology     Publication Date:  1992  
Date Detail:
Created Date:  1992-12-17     Completed Date:  1992-12-17     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0152016     Medline TA:  Pharmacology     Country:  SWITZERLAND    
Other Details:
Languages:  eng     Pagination:  129-41     Citation Subset:  IM    
Affiliation:
Department of Pharmacology, Pennsylvania State University, College of Medicine, Hershey 17033.
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MeSH Terms
Descriptor/Qualifier:
Animals
Chromatography, High Pressure Liquid
Dogs
Dose-Response Relationship, Drug
Drug Stability
Guanidines / pharmacokinetics*
Half-Life
Humans
Hydrolysis
Molecular Structure
Pyrazinamide / analogs & derivatives*,  blood
Pyrazines / pharmacokinetics*
Uremia / blood
Chemical
Reg. No./Substance:
0/Guanidines; 0/Pyrazines; 14559-68-3/3-amino-2-pyrazinoylguanidine; 60398-24-5/2-pyrazinoylguanidine; 98-96-4/Pyrazinamide; 98-97-5/pyrazinoic acid

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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