Bonjour, l'
Oxazepam est surtout metabolisé par glucuronidation. Je ne pense donc pas que le pamplemeousse (inhibiteur du CYP 2A4) change grand chose.
https://paindr.com/wp-content/uploads/2 … _-9-30.pdfhttps://pubchem.ncbi.nlm.nih.gov/compou … -ExcretionRoute of Elimination
Oxazepam is primarily eliminated in the urine as its glucuronide metabolite, with the feces containing approximately 21% of the unchanged drug. The majority of an orally ingested dose of
oxazepam is excreted within 48 hours.
There are three major pathways of
oxazepam metabolism in mice and rats (as in humans): direct conjugation, phenyl ring oxidation and diazepine ring contraction. In mice, conjugation is mainly with glucuronide, predominantly excreted in the urine; in rats, conjugation is mainly with sulfate, which is almost entirely eliminated in the feces. The sulfate conjugate of
oxazepam, which is unstable in acidic media, may be the source of the fecal
oxazepam It has not been detected in mice. Studies with recirculating, perfused male Swiss (CD-1) mouse liver preparations showed that
oxazepam glucuronides are the dominant liver metabolites in this species.
Oxazepam can also be conjugated with glucuronide by the placenta of rabbits, apparently in contrast to the human organ. Phenyl ring oxidation is more important in rats than in mice (or humans) and a dihydrodiol (probably the 3',4'- dihydrodiol, since 2'-hydroxy derivatives are not known) accounts for about 30% of the 72-hr urinary metabolites in Fischer 344 rats. This metabolite, which probably forms via an arene oxide intermediate and has not been found in mice, holds implications for the toxicological properties of
oxazepam. In rats, ring contraction to 6-chloro-4-phenyl- 2(1H)-quinazoline carboxylic acid occurs to roughly one half of the extent seen in mice.
https://en.wikipedia.org/wiki/Glucuronidationhttps://pubmed.ncbi.nlm.nih.gov/7773302/Amicalement
Dernière modification par prescripteur (07 septembre 2021 à 17:41)