Biotransformation of bromperidol in rat, dog, and man.
Biotransformation of bromperidol in rat, dog, and man.
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溴哌啶醇在大鼠、狗和人体内的生物转化。
DOI：
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发表时间：
1983
期刊：
影响因子：
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通讯作者：
J. Patrick
中科院分区：
文献类型：
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作者：
F. Wong;C. P. Bateman;C. Shaw;J. Patrick
本文研究了14C-溴哌利多口服给药后在大鼠、狗和人体内的代谢规律。给雌性Wistar大鼠服用14C-溴哌利多7天后，尿中排泄23%-29%，粪便中排泄38%-45%。在狗身上，39%-74%的给药剂量在同一时期从尿液中排泄，26%-43%从粪便中排泄。在大鼠和狗中，溴哌利多被广泛代谢；与代谢物相关的大部分尿放射性来自于通过氧化N-脱烷基化裂解溴哌利多分子。在给志愿者服用14C-溴哌利多后，在13天的时间里，28%-50%的剂量从尿液中消除，18%-46%的剂量从粪便中消除。虽然溴哌利多在人体内被广泛代谢，但尿液中的大部分放射性(70-75%)与完整药物的O-葡萄糖醛酸化物结合物有关。因此，氧化N-脱烷基似乎不是药物在人体内的主要尿代谢途径。
The metabolic fate of 14C-bromperidol after po administration was studied in rat, dog, and man. When 14C-bromperidol was given to female Wistar rats, 23-29% of the dose was excreted in the urine and 38-45% in the feces over a 7-day period. In dogs, 39-74% of the administered dose was excreted in the urine and 26-43% in the feces over the same period. In both rats and dogs, bromperidol was extensively metabolized; most of the urinary radioactivity associated with metabolites arose from cleavage of the bromperidol molecule via oxidative N-dealkylation. After administration of 14C-bromperidol to human volunteers, 28-50% of the dose was eliminated in the urine while 18-46% was eliminated in the feces over a 13-day period. Although bromperidol appeared to be extensively metabolized in man, the major portion of the urinary radioactivity (70-75%) was associated with the O-glucuronide conjugate of intact drug. Thus, oxidative N-dealkylation does not appear to be the major urinary metabolic pathway of the drug in man.