Effects of inducers and inhibitors of mixed-function oxidases on the biliary excretion of pentacaine metabolites
| Autor: | Mária Ďurišová, Tomas Trnovec, M. Kukan, V. Ščasnár, Štefan Bezek |
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| Rok vydání: | 1990 |
| Předmět: |
Male
medicine.medical_specialty Pyridines Metabolite Pharmaceutical Science Mixed Function Oxygenases Excretion chemistry.chemical_compound Pharmacokinetics Internal medicine medicine Animals Bile Pharmacology (medical) Cimetidine Enzyme inducer Pharmacology biology Portal Vein Rats Inbred Strains General Medicine Drug interaction Rats Endocrinology chemistry Enzyme inhibitor Enzyme Induction Phenobarbital Injections Intravenous biology.protein Carbamates Methylcholanthrene medicine.drug |
| Zdroj: | Biopharmaceutics & Drug Disposition. 11:395-401 |
| ISSN: | 1099-081X 0142-2782 |
| DOI: | 10.1002/bdd.2510110504 |
| Popis: | The biliary excretion of 3H-pentacaine and its metabolites was studied in rats pretreated with an inducer or inhibitor of mixed-function oxidases. Over one-fourth (25.8 per cent) of a 2 mg kg-1 intraportal dose of 3H-pentacaine was excreted in bile in urethaneanaesthetized control rats within 3 h. The radioactivity appeared in the form of the parent drug, basic metabolites, and metabolite conjugates, 3.1, 86.5, and 10.4 per cent of the total radioactivity excreted, respectively. Pretreatment of rats with phenobarbital enhanced only slightly the biliary excretion of basic metabolites, and pretreatment with 3-methylcholanthrene had no effect. Phenobarbital also increased the initial rate of excretion of conjugates, but this effect was not sustained. 3-Methylcholanthrene had a tendency to impair excretion of conjugates by bile. Pretreatment of rats with SKF 525-A decreased the biliary excretion of both basic metabolites and conjugates while cimetidine did not alter significantly the biliary excretion of pentacaine metabolites. These results suggest that the canalicular transport of metabolites may be the most important factor in controlling pentacaine metabolite excretion in bile. |
| Databáze: | OpenAIRE |
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