Effect of Drug Pre-Treatment on The Metabolism of Methyrapone .

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dc.contributor.authorOkereke, Samuel Emeka
dc.date.accessioned2023-05-13T18:03:40Z
dc.date.available2023-05-13T18:03:40Z
dc.date.issued1985
dc.description135Pen_US
dc.description.abstractMetyrapone (SU 488), an inhibitor of 11β - hydroxylase used an a diagnostic and therapeutic agent in the treatment of Cushing's disease, has been found to be metabolised in vivo in rats mainly to metyrapol via reductive mechanism and to the N.-oxides in oxidative mechanism. A significant sex difference as to the production of metyrapol was observed; being higher in the male rats (94 ± 1%) than in the female (64 ± 2%). The influence of drug pretreatment on the metabolism of metyrapone was inventigated in the rats. It was observed that phenobarbital, ethanol and pregnenolone significantly (P< 0.05) caused an induction of the metyrapone N-oxide (B) in the male rats while anthracene did not cause any significant induction. Only ethanol significantly (P<0.05) induced the production of N-oxide A. On the other hand cimetidine a cytochrome P- 450 inhibitor and methimazole, an FAD (flavine Adenine dinucleotide) mediated inhibitor of cytochrome P-450, inhibited the formation of Noxide (13) and slight increase in metyropol formation ccmpared to that produced in the inducers. In the female rats, only phenobarbital significantly (P < 0.05) induced the production of both Noxides with a significant decrease in amount of metyrapol formed. While anthracene has no effect on the formation of both N-oxides of metyrapone, (though with increase in amount of metyrapol formed), ethanol, cimetidine and methimazole inhibited the production of metyrapone N-oxide (B) and (A) with a preferential increase in the amount of metyrapol formed. These then suggest a possibility of both FAD and cytochrome P-450 influence in the oxidative metabolism of metyraponen_US
dc.identifier.citationOkereke,S.E ( 1985) Effect of drug pre-treatment on the metabolism of methyraponeen_US
dc.identifier.urihttps://ir.oauife.edu.ng/123456789/5636
dc.language.isoenen_US
dc.publisherObafemi Awolowo Universityen_US
dc.subjectDrugen_US
dc.subjectMetyraponeen_US
dc.subjectCimetidineen_US
dc.subjectN-oxidesen_US
dc.titleEffect of Drug Pre-Treatment on The Metabolism of Methyrapone .en_US
dc.typeThesisen_US
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