Endralazine - a new hydralazine-like antihypertensive with high systemic bioavailability
| Autor: | I. Cozamanis, R. Zacest, Phillip A. Reece |
|---|---|
| Rok vydání: | 1983 |
| Předmět: |
Drug
Adult Male media_common.quotation_subject Biological Availability Pharmacology Absorption Pharmacokinetics Blood plasma medicine Humans Pharmacology (medical) Volunteer media_common Volume of distribution Chemistry Acetylation General Medicine Hydralazine Bioavailability Pyridazines Kinetics Phenotype Endralazine medicine.drug |
| Zdroj: | European journal of clinical pharmacology. 25(4) |
| ISSN: | 0031-6970 |
| Popis: | Endralazine (E), a new hydralazine-like antihypertensive was given intravenously (0.05 mg/kg) to 10 normal volunteers (5 slow and 5 fast acetylators). Plasma levels were fitted to a 3 compartment model and pharmacokinetic parameters (area under curve [AUC 0 ∞ ], clearance, volume of distribution, half-lives) obtained in the usual way. Bioavailabilities of 5 and 10 mg oral doses of E were determined from the AUC 0 ∞ generated in a previous study of oral E given to the same subjects. E had high system bioavailability (73.5–99.1%) suggesting that it was almost completely absorbed without undergoing appreciable first-pass metabolism. Furthermore, dose size and acetylator phenotype did not significantly affect the bioavailability of E. This behaviour contrasts with that of hydralazine where systemic bioavailability was |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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