评估的吸收、排泄和代谢[14 c] etoperidone男人。
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考德威尔吉瓦,吴WN Masucci农协
评估的吸收、排泄和代谢[14 c] etoperidone男人。
Xenobiotica。2001年11月,31 (11):823 - 39。doi: 10.1080 / 00498250110091758。
- PubMed ID
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11765144 (在PubMed]
- 文摘
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1。吸收、排泄和代谢2 - [3 - (4 - (3-chlorophenyl) 1-piperazinyl)丙基)4,5-diethyl-2, 4-dihydro-3H-1, 2, 4 -盐酸triazole-3-one(盐酸etoperidone)六个健康男性调查。受试者之前尝过一夜之间接受单剂量口服100毫克的解决方案[14 c] etoperidone盐酸。2。等离子体(0-48 h) (0 - 120 h)和尿液粪便(0 - 120 h)样本收集。终端的总放射性半衰期等离子体为21.7 + / - 2.8 h明显间隙为1.01 + / - 0.08毫升min (1)。复苏总辐射的尿液和粪便是78.8 + / - 3.6%和9.6 + / - 4.1%的剂量,分别。3所示。Etoperidone和21代谢物是孤立和等离子体中标识,尿液和粪便提取物。不变etoperidone占< 0.01%剂量的排泄物样本。 Nine metabolites were identified in the plasma extracts and 21 urinary metabolites were identified. Seven faecal metabolites were identified. 4. Five proposed pathways were used to describe the formation of the metabolites: alkyl oxidation, piperazinyl oxidation, N-dealkylation, phenyl hydroxylation and conjugation. Alkyl oxidation of etoperidone resulted in the formation of 2-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-4-ethyl-2,4-dihydro-5- (1-hydroxyethyl)-3H-1,2,4-triazole-3-one. Piperazinyl oxidation of this metabolite leads to the formation of its N-oxide. N-dealkylation of the piperazinyl group led to the formation of 1-(3-chlorophenyl) piperazine and triazole propionic acid. Phenyl hydroxylation led to three important metabolites in the urine and faeces.
