Pharmacokinetics of a new angiotensin I converting enzyme inhibitor (alacepril) after oral dosing in fasting or fed states
| Autor: | Hideki Hirakata, Nobuaki Ohchi, Kenichi Motomura, Kaoru Onoyama, Kouji Hayashi, Hiroshi Tsuruda, Masatoshi Fujishima, Teruo Omae, Suguru Tomooka |
|---|---|
| Rok vydání: | 1985 |
| Předmět: |
Adult
Male medicine.medical_specialty Captopril Alacepril Administration Oral Blood Pressure Pharmacology Pharmacokinetics Heart Rate Oral administration Internal medicine medicine Humans Pharmacology (medical) cardiovascular diseases Dosing Biotransformation Chromatography High Pressure Liquid Meal biology Chemistry Angiotensin-converting enzyme Fasting Middle Aged Kinetics Endocrinology Enzyme inhibitor biology.protein Drug Evaluation hormones hormone substitutes and hormone antagonists circulatory and respiratory physiology medicine.drug |
| Zdroj: | Clinical Pharmacology and Therapeutics. 38:462-468 |
| ISSN: | 1532-6535 0009-9236 |
| DOI: | 10.1038/clpt.1985.205 |
| Popis: | The plasma concentration and urinary excretion of a newly developed angiotensin I converting enzyme inhibitor, alacepril (which is converted to captopril after absorption), were investigated in seven normal healthy subjects. Fifty milligrams of the drug was administered orally either in the fasting or in the fed state. In the fasting state, the time of maximal plasma concentration (tmax) was 1 hour for free captopril, 1.7 hours for protein-conjugated captopril, and 1.6 hours for total captopril. The biologic t1/2 of free, protein-conjugated, and total captopril was 1.9, 4.2, and 5 hours, respectively. In the fed state, neither tmax nor t1/2 changed, except that the tmax of free captopril was prolonged to 1.9 hours (P less than 0.01). Cumulative urinary excretion of free captopril at 8 hours was 35% of the drug administered in the fasting state and that of total captopril at 24 hours was 59%. These data did not differ significantly from those obtained after food intake. The biologic t1/2 of free captopril after alacepril dosing was longer than in previous studies of captopril per se. Because biologic or clinical effects have not been studied, it should be left conjectural whether alacepril is a longer-acting angiotensin I converting enzyme inhibitor. A prolonged effect of the drug can be expected by its administration after a meal. |
| Databáze: | OpenAIRE |
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