Metabolites of methohexitone do not contribute to its prolonged action on the central nervous system
| Autor: | M M Ghoneim, C K Chiang, L J Fischer, E Nuotto, K. Korttila |
|---|---|
| Rok vydání: | 1990 |
| Předmět: |
Male
Drug Chromatography Gas Magnetic Resonance Spectroscopy Time Factors Chemical Phenomena media_common.quotation_subject Metabolite Central nervous system Urine Pharmacology Mass Spectrometry Mice chemistry.chemical_compound Dogs medicine Animals Humans Postural Balance ED50 media_common Chemistry Physical business.industry Brain General Medicine Anesthesiology and Pain Medicine medicine.anatomical_structure Mechanism of action chemistry Methohexital Anesthetic medicine.symptom business Psychomotor Performance medicine.drug |
| Zdroj: | Acta Anaesthesiologica Scandinavica. 34:55-58 |
| ISSN: | 1399-6576 0001-5172 |
| DOI: | 10.1111/j.1399-6576.1990.tb03041.x |
| Popis: | Methohexitone has been reported to have a prolonged action on the central nervous system (CNS) despite its relatively short elimination half-life. A hydroxy metabolite of methohexitone was identified, purified and isolated from the urine collected from eight surgical patients and five mongrel dogs anaesthetized with methohexitone. Using a rotarod device, the CNS-activity of the human and canine metabolites was tested in mice and compared to that of methohexitone. In this test, the metabolites showed CNS-depressant activity, but the ED50 (dose needed to affect 50% of the animals) of the metabolites was ten times higher than the ED50 of the parent drug. Because in patients, no traces of the hydroxy metabolite could be found in blood, and in dogs the plasma concentration of the metabolite was about two-thirds of that of the parent compound, it is unlikely that the residual CNS-effects of methohexitone are due to its major metabolite, hydroxymethohexitone. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Plný text