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The metabolic fate of $[^{3}$H]econazole in man
| Content Provider | Scilit |
|---|---|
| Author | Midgley, I. Biggs, S. R. Hawkins, D. R. Chasseaud, L. F. Darragh, A. Brodie, R. R. Walmsley, L. M. |
| Copyright Year | 1981 |
| Description | 1. Following single oral doses of $[^{3}$H]econazole base (500 mg) to two human subjects, excretion of radioactivity was prolonged, and incomplete after five days (means of 40% and 27% dose in urine and faeces respectively). 2. Plasma concn. of unchanged econazole and total radioactivity attained peak values at approx. the same time for each subject (1±5-3 h), but the former declined much faster than the latter. Most of the$ ^{3}$H in early plasma samples was present as unchanged drug and extractable metabolites, but after 24h concn. of econazole were close to the limit of detection (0±4μg/ml) and very little plasma$ ^{3}$H was extractable, whereas $total^{3}$H concn. were still measurable after five days (mean 1±54μg/ml). Thus, plasma contained metabolites with much longer half-lives than econazole. 3. The main route of biotransformation of econazole in man involved multiple oxidation of the imidazole ring carbons followed by O-dealkylation and conjugation of the resulting alcohols, probably with glucuronic acid. |
| Related Links | http://www.tandfonline.com/doi/pdf/10.3109/00498258109045871 |
| Ending Page | 608 |
| Page Count | 14 |
| Starting Page | 595 |
| ISSN | 00498254 |
| e-ISSN | 13665928 |
| DOI | 10.3109/00498258109045871 |
| Journal | Xenobiotica |
| Issue Number | 9 |
| Volume Number | 11 |
| Language | English |
| Publisher | Informa UK Limited |
| Publisher Date | 1981-01-01 |
| Access Restriction | Open |
| Subject Keyword | Journal: Xenobiotica Legal Medicine Toxicology Sup Radioactivity Concn Econazole in Man Metabolites Unchanged Plasma Days |
| Content Type | Text |
| Resource Type | Article |
| Subject | Health, Toxicology and Mutagenesis Medicine Biochemistry Toxicology Pharmacology |
