| Autor: |
Ulm, EH, Hichens, M, Gomez, HJ, Till, AE, Hand, E, Vassil, TC, Biollaz, J, Brunner, HR, Schelling, JL |
| Zdroj: |
British Journal of Clinical Pharmacology; 1982, Vol. 14 Issue 3, p357-362, 6p |
| Abstrakt: |
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. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
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