Prazepamの代謝に関する研究(第4報)Prazepamのサルにおける体内動態

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Metabolism of orally administered [5-^<14>C] prazepam was investigated in cynomolgus monkeys. The radioactivity in the plasma reached a peak level at 3-6 hr after dosing, and thereafter declined gradually with a half-life of about 21 hr. Major metabolites in the plasma were desalkylprazepam (DPZ), 3-hydroxyprazepam (3-HPZ) glucuronide and oxazepam (OX) glucuronide. These glucuronides were rapidly excreted, and DPZ accounted for more that 70% of the total plasma metabolites after 12 hr. More than 70% of the radioactivity were excreted mostly in the urine within 3 days. Major metabolites in the urine were OX glucuronide and 3-HPZ glucuronide. The amount of these glucuronides did not decrease markedly until 48 hr after dosing. 4'-Hydroxydesalkylprazepam sulfate accounted for only 2-4% of the total urinary metabolites. In addition, a very small amount of prazepam (PZ) was detected in the plasma and urine. Most of fecal metabolites was unabsorbed PZ, which indicates that the fecal excretion via bile has little significance in monkeys. These results suggest that the PZ metabolism in the monkey resembles that in man, though the rate of metabolism in the monkey is faster than that in man.
社団法人日本薬学会の論文
1978-07-25