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
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 11:41
Dernière modification de la notice
20/08/2019 17:10