The effects of beta‐adrenoceptor antagonists and levomepromazine on the metabolic ratio of debrisoquine

The in vivo inhibitory effect of five beta‐adrenoceptor antagonists and levomepromazine on debrisoquine metabolism was assessed in 37 subjects. The debrisoquine phenotyping test was performed before and after 7 days' treatment with oxprenolol (40 mg three times daily), propranolol (20 mg three...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:British journal of clinical pharmacology 1990-10, Vol.30 (4), p.638-643
Hauptverfasser: Kallio, J, Huupponen, R, Seppala, M, Sako, E, Iisalo, E
Format: Artikel
Sprache:eng
Schlagworte:
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:The in vivo inhibitory effect of five beta‐adrenoceptor antagonists and levomepromazine on debrisoquine metabolism was assessed in 37 subjects. The debrisoquine phenotyping test was performed before and after 7 days' treatment with oxprenolol (40 mg three times daily), propranolol (20 mg three times daily), timolol (10 mg twice daily), pindolol (5 mg twice daily), metoprolol (50 mg twice daily) or levomepromazine (10 mg daily), each of which was given to six‐seven subjects. No clear change in the urinary metabolic ratio of debrisoquine/4‐OH‐debrisoquine (MR) was seen with any of the single beta‐adrenoceptor antagonist treatments, but the MR value increased significantly when all beta‐ adrenoceptor blocker treatments were considered together. Debrisoquine metabolism was clearly impaired after levomepromazine 10 mg daily for 7 days; the mean MR increased from 1.24 +/− 1.6 to 4.70 +/− 5.23 (P = 0.018) and the excretion of 4‐hydroxydebrisoquine decreased from 0.92 +/− 0.46 mg to 0.31 +/− 0.19 mg (P = 0.043). Thus, levomepromazine changes MRs towards those characteristic of phenotypically poor metabolizers, but beta‐adrenoceptor antagonists at the doses examined have only a marginal effect.
ISSN:0306-5251
1365-2125
DOI:10.1111/j.1365-2125.1990.tb03827.x