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犬单次服用异戊巴比妥后的酶诱导作用。

Enzyme induction following a single dose of amobarbital in dogs.

作者信息

Reilly P A, Inaba T, Kadar D, Endrenyi L

出版信息

J Pharmacokinet Biopharm. 1978 Aug;6(4):305-13. doi: 10.1007/BF01060094.

DOI:10.1007/BF01060094
PMID:702272
Abstract

The elimination of amobarbital in dogs was investigated by injecting various doses of amobarbital into a given animal. At low doses (3 mg/kg) serum levels declined in a first-order fashion. Superficially, at high doses (20 mg/kg) the relationship between serum concentration and time could be quantitatively characterized by simple one-compartment saturable kinetics. Indeed, qualitatively, saturation of the amobarbital-metabolizing enzymes was indicated by a shallower initial slope of the semilogarithmic concentration--time profile at the high than at the low dose. However, in addition, an acute enzyme induction phenomenon was observed which was indicated by a shorter terminal half-life of amobarbital at the high dose than after the low dose and also by a shortening in antipyrine half-life.

摘要

通过给特定动物注射不同剂量的异戊巴比妥来研究其在犬体内的消除情况。低剂量(3毫克/千克)时,血清水平呈一级动力学下降。表面上看,高剂量(20毫克/千克)时,血清浓度与时间的关系可用简单的单室饱和动力学进行定量表征。实际上,定性来看,高剂量时半对数浓度-时间曲线的初始斜率比低剂量时更平缓,这表明异戊巴比妥代谢酶出现了饱和。然而,此外还观察到一种急性酶诱导现象,这表现为高剂量时异戊巴比妥的终末半衰期比低剂量时更短,同时安替比林半衰期也缩短。

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1
Enzyme induction following a single dose of amobarbital in dogs.犬单次服用异戊巴比妥后的酶诱导作用。
J Pharmacokinet Biopharm. 1978 Aug;6(4):305-13. doi: 10.1007/BF01060094.
2
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4
[Pharmacokinetics of amobarbital].[异戊巴比妥的药代动力学]
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本文引用的文献

1
The metabolism of amytal labeled with N15 in dogs.狗体内用N15标记的异戊巴比妥的代谢
J Pharmacol Exp Ther. 1950 Feb;98(2):180-3.
2
Ethyl (3-hydroxyisoamyl) barbituric acid as the principal metabolite of amytal.乙基(3-羟基异戊基)巴比妥酸作为异戊巴比妥的主要代谢产物。
J Biol Chem. 1952 Mar;195(1):397-402.
3
The kinetics of amylobarbitone metabolism in healthy men and women.健康男性和女性中异戊巴比妥代谢的动力学
Br J Pharmacol. 1970 Jul;39(3):564-72. doi: 10.1111/j.1476-5381.1970.tb10364.x.
4
Metabolism of amylobarbitone in patients with chronic liver disease.慢性肝病患者中异戊巴比妥的代谢
Br J Pharmacol. 1972 Mar;44(3):549-60. doi: 10.1111/j.1476-5381.1972.tb07292.x.
5
Implications of enzyme induction in drug toxicity studies.酶诱导在药物毒性研究中的意义。
Toxicol Appl Pharmacol. 1967 Mar;10(2):340-51. doi: 10.1016/0041-008x(67)90116-0.
6
Abnormal drug metabolism after barbiturate and paracetamol overdose.巴比妥类药物和对乙酰氨基酚过量后的药物代谢异常。
Br Med J. 1974 Nov 30;4(5943):499-502. doi: 10.1136/bmj.4.5943.499.
7
(2-14C) amobarbital metabolism in tolerant rats.(2-14C)异戊巴比妥在耐受性大鼠体内的代谢。
Xenobiotica. 1974 Jul;4(7):409-23. doi: 10.3109/00498257409052105.
8
Gas chromatographic assessment of the reproducibility of phenazone plasma half-life in young healthy volunteers.气相色谱法评估年轻健康志愿者中非那宗血浆半衰期的重现性。
Eur J Clin Pharmacol. 1974 Aug 23;7(5):381-5. doi: 10.1007/BF00558211.
9
Genetic study of amobarbital elimination based on its kinetics in twins.
Clin Pharmacol Ther. 1976 Dec;20(6):701-14. doi: 10.1002/cpt1976206701.
10
Amobarbital--a probe of hepatic drug oxidation in man.异戊巴比妥——人体肝脏药物氧化的一种探针。
Clin Pharmacol Ther. 1976 Oct;20(4):439-44. doi: 10.1002/cpt1976204439.