Disposition of bemitradine, a Renal Vasodilator and Diuretic, in Man
| Autor: | C. W. Vose, A. Gray, N. Lopez, J. A. Steiner, R. D. Brownsill, C. M. Walls, Y. Robinson |
|---|---|
| Rok vydání: | 1988 |
| Předmět: |
Adult
Male medicine.medical_specialty Vasodilator Agents Health Toxicology and Mutagenesis Metabolite medicine.medical_treatment Administration Oral Glucuronates Urine Toxicology Biochemistry Absorption Renal Circulation Excretion chemistry.chemical_compound Pharmacokinetics Oral administration Internal medicine medicine Humans Diuretics Biotransformation Pharmacology General Medicine Middle Aged Triazoles Bioavailability Pyrimidines Endocrinology chemistry Diuretic Glucuronide |
| Zdroj: | Xenobiotica. 18:1413-1423 |
| ISSN: | 1366-5928 0049-8254 |
| DOI: | 10.3109/00498258809042264 |
| Popis: | 1. 14C-Bemitradine (50 mg) was rapidly and efficiently absorbed (approximately 89%) in man following a single oral dose, as a solution in gelatine capsules. Peak 14C levels of 895 +/- 154 ng equiv./ml (mean +/- S.E.M.) were reached within 2 h, and declined with half-lives of 1.07 +/- 0.25 and 13.0 +/- 5.6h. 2. No bemitradine was detected in plasma, but peak concn. (124 +/- 29 ng/ml) of its desethyl metabolite were reached at 1.05 +/- 0.28 h, and declined with a half-life of 1.32 +/- 0.08 h. 3. Desethylbemitradine was rapidly metabolized to its ether glucuronide, a phenol and a dihydrodiol which were also present as glucuronide conjugates. The glucuronides were the major compounds in plasma from 2 h after drug administration. 4. Excretion in 5 days amounted to 88.8 +/- 2.3% and 10.4 +/- 2.1% dose in urine and faeces respectively. No bemitradine or desethylbemitradine were excreted unchanged. 8-(2-Hydroxyethyl)-7-(3,4- dihydroxycyclohexa-1,5-dienyl)-1,2,4-triazolo-1,5c-pyrimidin e-5-amine (E; 17% dose); 8-(2-hydroxyethyl)-7-(4-hydroxyphenyl)-1,2,4-triazolo-1,5c- pyrimidine-5-amine (F; 4% dose), their glucuronides (A, 19% dose and B, 6% dose respectively), desethylbemitradine glucuronide (D, 25% dose) and an unidentified metabolite (C, 12% dose) were excreted in urine. Compound F was the major faecal metabolite. |
| Databáze: | OpenAIRE |
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