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曲唑酮的代谢研究。III 种属差异。

Studies on metabolism of trazodone. III Species differences.

作者信息

Yamato C, Takahashi T, Fujita T

出版信息

Xenobiotica. 1976 May;6(5):295-306. doi: 10.3109/00498257609151641.

DOI:10.3109/00498257609151641
PMID:936649
Abstract
  1. After oral administration of (14C) trazodone HCl (4 mg/kg) to rabbits, the blood level of radioactivity shows a peak at 3 h; unchanged trazodone concentration in brain is higher than that in plasma at 3 h after dosage. 29 The metabolic fate of trazodone in rabbits is different from that in rats and a new, basic metabolite is present in rabbit liver, brain, plasma and urine. 3. The concentration pattern in blood of humans given a single dosage (50 mg) of trazodone HCl is similar to that in rabbits rather than that in rats. 4. The rate of metabolism of trazodone by liver microsomes from mice is approximately 1-5 times higher than that with rat or rabbit liver microsomes.
摘要
  1. 给兔子口服(14C)盐酸曲唑酮(4毫克/千克)后,放射性血药浓度在3小时达到峰值;给药后3小时,脑中未变化的曲唑酮浓度高于血浆中的浓度。29曲唑酮在兔子体内的代谢命运与在大鼠体内不同,一种新的碱性代谢物存在于兔肝、脑、血浆和尿液中。3. 给予单次剂量(50毫克)盐酸曲唑酮的人体血液中的浓度模式与兔子相似,而非与大鼠相似。4. 小鼠肝微粒体对曲唑酮的代谢速率比大鼠或兔肝微粒体高约1 - 5倍。

相似文献

1
Studies on metabolism of trazodone. III Species differences.曲唑酮的代谢研究。III 种属差异。
Xenobiotica. 1976 May;6(5):295-306. doi: 10.3109/00498257609151641.
2
Studies on metabolism of trazodone. IV. Intestinal absorption in rats and rabbits.曲唑酮的代谢研究。IV. 大鼠和兔子的肠道吸收
Xenobiotica. 1976 Sep;6(9):521-9. doi: 10.3109/00498257609151664.
3
Studies on metabolism of trazodone. I. Metabolic fate of (14C)trazodone hydrochloride in rats.曲唑酮的代谢研究。I. 大鼠体内盐酸(14C)曲唑酮的代谢命运。
Xenobiotica. 1974 May;4(5):313-26. doi: 10.3109/00498257409052059.
4
Metabolism of labetalol by animals and man.拉贝洛尔在动物和人体内的代谢。
Br J Clin Pharmacol. 1976 Aug;3(4 Suppl 3):695-710.
5
Effect of dosage and route of administration of trazodone on cerebral concentration of 1-m-chlorophenylpiperazine in rats. Kinetics of trazodone biotransformation in rats.曲唑酮的剂量和给药途径对大鼠脑中1-间氯苯基哌嗪浓度的影响。大鼠曲唑酮生物转化的动力学。
Pol J Pharmacol Pharm. 1983 May-Jun;35(3):241-7.
6
[Pharmacokinetics and metabolism of trazodone in man (author's transl)].曲唑酮在人体中的药代动力学与代谢(作者译)
Arzneimittelforschung. 1976;26(11):2084-9.
7
Species and dose differences in the accumulation of imipramine by mammalian lungs.
Drug Metab Dispos. 1981 Jul-Aug;9(4):322-6.
8
Pharmacokinetics of trazodone after different routes of administration.曲唑酮不同给药途径后的药代动力学。
Pol J Pharmacol Pharm. 1981 Oct;33(3):341-8.
9
NTP Toxicology and Carcinogenesis Studies of 1-Amino-2,4-Dibromoanthraquinone (CAS No. 81-49-2) in F344/N Rats and B6C3F1 Mice (Feed Studies).1-氨基-2,4-二溴蒽醌(CAS编号:81-49-2)在F344/N大鼠和B6C3F1小鼠中的NTP毒理学与致癌性研究(饲料喂养研究)
Natl Toxicol Program Tech Rep Ser. 1996 Aug;383:1-370.
10
Pharmacokinetics and metabolism of zopiclone.佐匹克隆的药代动力学与代谢
Int Pharmacopsychiatry. 1982;17 Suppl 2:76-91.

引用本文的文献

1
Trazodone: a review of its pharmacological properties and therapeutic use in depression and anxiety.曲唑酮:对其药理特性及在抑郁和焦虑治疗中的应用综述
Drugs. 1981 Jun;21(6):401-29. doi: 10.2165/00003495-198121060-00001.
2
Excretion of trazodone in breast milk.曲唑酮在母乳中的排泄情况。
Br J Clin Pharmacol. 1986 Sep;22(3):367-70. doi: 10.1111/j.1365-2125.1986.tb02903.x.