Enalapril maleate and a lysine analogue (MK-521): disposition in man

Détails

ID Serval
serval:BIB_E80FAA4D7EBB
Type
Article: article d'un périodique ou d'un magazine.
Collection
Publications
Institution
Titre
Enalapril maleate and a lysine analogue (MK-521): disposition in man
Périodique
British Journal of Clinical Pharmacology
Auteur(s)
Ulm  E. H., Hichens  M., Gomez  H. J., Till  A. E., Hand  E., Vassil  T. C., Biollaz  J., Brunner  H. R., Schelling  J. L.
ISSN
0306-5251 (Print)
Statut éditorial
Publié
Date de publication
09/1982
Volume
14
Numéro
3
Pages
357-62
Notes
Journal Article --- Old month value: Sep
Résumé
1 The disposition of two angiotensin converting-enzyme inhibitor drugs was studied in normal volunteers. One drug was enalapril maleate (MK-421), which requires in vivo esterolysis to yield active inhibitor (MK-422). The other was a lysine analogue of MK-422 (MK-521), which requires no bioactivation. 2 Absorption of enalapril maleate (10 mg, p.o.) was rapid, with peak serum concentrations of enalapril observed 0.5-1.5 h after administration. Based upon urinary recovery of total drug (enalapril plus MK-422), absorption was at least 61%. Bioactivation appeared to be largely post-absorptive. From the ratio of MK-422 to total drug in urine, the minimum extent of bioactivation was estimated at 0.7. 3 A similar dose of MK-521 was absorbed more slowly, reaching peak serum concentrations 6-8 h following drug administration. Minimum absorption, based upon urinary recovery, was 29%. 4 Serum concentration v time profiles for both drugs were polyphasic and exhibited prolonged terminal phases. 5 Recovery in urine and faeces of administered enalapril maleate (intact and as MK-422) was 94%. Recovery of MK-521 was 97%. These results indicate lack of significant metabolism of these agents, apart from the bioactivation of enalapril.
Mots-clé
*Angiotensin-Converting Enzyme Inhibitors Biotransformation Dipeptides/*metabolism Enalapril Humans Intestinal Absorption Lisinopril Male
Pubmed
Web of science
Création de la notice
25/01/2008 10:41
Dernière modification de la notice
20/08/2019 16:10
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