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四种磺胺类药物在奶牛体内的代谢

The metabolism of four sulphonamides in cows.

作者信息

Nielsen P

出版信息

Biochem J. 1973 Dec;136(4):1039-45. doi: 10.1042/bj1361039.

DOI:10.1042/bj1361039
PMID:4786525
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1166054/
Abstract
  1. The metabolism of sulphanilamide, sulphadimidine (4,6-dimethyl-2-sulphanilamidopyrimidine), sulphamethoxazole (5-methyl-3-sulphanilamidoisoxazole) and sulphadoxine (5,6-dimethoxy-4-sulphanilamidopyrimidine) given by intravenous injection has been examined in cows. 2. The sulphonamides were present mainly as unchanged drugs in blood samples collected 2h after administration. 3. The sulphonamides were excreted in the milk partly as unchanged drugs and partly as conjugated metabolites whereas only small amounts were excreted as the N(4)-acetyl derivatives. 4. The unchanged drug and the N(4)-acetyl derivative were the major constituents in urine samples after administration of sulphanilamide, sulphamethoxazole and sulphadoxine. 5. Besides the unchanged drug, the N(4)-acetyl derivative and the conjugated metabolites, three further metabolites of sulphadimidine were isolated from urine samples and identified. They were 5-hydroxy-4,6-dimethyl-2-sulphanilamidopyrimidine, 4-hydroxymethyl-6-methyl-2-sulphanilamidopyrimidine and sulphaguanidine.
摘要
  1. 已对静脉注射磺胺、磺胺二甲嘧啶(4,6 - 二甲基 - 2 - 磺胺嘧啶)、磺胺甲恶唑(5 - 甲基 - 3 - 磺胺异恶唑)和磺胺多辛(5,6 - 二甲氧基 - 4 - 磺胺嘧啶)在奶牛体内的代谢情况进行了研究。2. 在给药后2小时采集的血样中,磺胺类药物主要以原形存在。3. 磺胺类药物在牛奶中的排泄,部分以原形,部分以结合代谢物的形式,而仅有少量以N(4)-乙酰衍生物的形式排泄。4. 给予磺胺、磺胺甲恶唑和磺胺多辛后,尿样中的主要成分是原形药物和N(4)-乙酰衍生物。5. 除了原形药物、N(4)-乙酰衍生物和结合代谢物外,还从尿样中分离并鉴定出了磺胺二甲嘧啶的另外三种代谢物。它们是5 - 羟基 - 4,6 - 二甲基 - 2 - 磺胺嘧啶、4 - 羟甲基 - 6 - 甲基 - 2 - 磺胺嘧啶和磺胺胍。

相似文献

1
The metabolism of four sulphonamides in cows.四种磺胺类药物在奶牛体内的代谢
Biochem J. 1973 Dec;136(4):1039-45. doi: 10.1042/bj1361039.
2
[Mammary excretion in goats of sulphadoxine and sulphamethoxazole compared with sulphanilamide and sulphadimidine].[山羊中磺胺多辛和磺胺甲恶唑与磺胺嘧啶和磺胺二甲嘧啶的乳腺排泄情况比较]
Nord Vet Med. 1972 Jan;24(1):1-10.
3
[Renal excretion of sulphanilamide, sulphadimidine, sulphadoxine and sulphamethoxazole in goats].[山羊体内磺胺、磺胺二甲嘧啶、磺胺多辛和磺胺甲恶唑的肾脏排泄情况]
Nord Vet Med. 1972 Dec;24(12):601-11.
4
Renal excretion of N4-acetyl sulphanilamide and N4-acetyl sulphadimidine in goats.山羊体内N4-乙酰磺胺和N4-乙酰磺胺二甲嘧啶的肾脏排泄情况。
Acta Vet Scand. 1974;15(2):188-97. doi: 10.1186/BF03547480.
5
Metabolism of sulphonamides in goats.山羊体内磺胺类药物的代谢
Acta Vet Scand. 1973;14(4):647-9.
6
Sulphamethoxazole acetylation in fast and slow acetylators.快速和慢速乙酰化者体内的磺胺甲恶唑乙酰化作用
Int J Clin Pharmacol Ther Toxicol. 1990 Apr;28(4):164-6.
7
Species differences in the metabolism and excretion of sulphasomidine and sulphamethomidine.磺胺索嘧啶和磺胺甲嘧啶在代谢及排泄方面的种属差异。
Biochem J. 1969 Jan;111(2):173-9. doi: 10.1042/bj1110173.
8
Clinical pharmacokinetics of sulphonamides and their N4-acetyl derivatives.磺胺类药物及其N4-乙酰衍生物的临床药代动力学。
Antibiot Chemother (1971). 1982;31:22-118. doi: 10.1159/000400131.
9
Structure and species as factors affecting the metabolism of some methoxy-6-sulphanilamidopyrimidines.结构与物种作为影响某些甲氧基-6-磺胺嘧啶代谢的因素
Biochem J. 1969 Jan;111(2):167-72. doi: 10.1042/bj1110167.
10
Pharmacokinetics and renal clearance of sulphadimidine, sulphamerazine and sulphadiazine and their N4-acetyl and hydroxy metabolites in pigs.磺胺二甲嘧啶、磺胺甲嘧啶和磺胺嘧啶及其N4-乙酰和羟基代谢产物在猪体内的药代动力学和肾清除率
Vet Q. 1989 Apr;11(2):78-86. doi: 10.1080/01652176.1989.9694203.

引用本文的文献

1
Serum and milk concentrations of several sulphonamides and their N4-acetyl metabolites following oral administration to cows.给奶牛口服给药后几种磺胺类药物及其N4-乙酰代谢物的血清和乳汁浓度。
Acta Vet Scand. 1983;24(4):374-83. doi: 10.1186/BF03546711.
2
Isolation and identification of 4-hydroxysulfamerazine and preliminary studies on its pharmacokinetics in dogs.4-羟基磺胺甲基嘧啶的分离鉴定及其在犬体内的药代动力学初步研究
Pharm Weekbl Sci. 1984 Apr 27;6(2):80-7. doi: 10.1007/BF01953959.
3
Renal excretion of N4-acetyl sulphanilamide and N4-acetyl sulphadimidine in goats.山羊体内N4-乙酰磺胺和N4-乙酰磺胺二甲嘧啶的肾脏排泄情况。
Acta Vet Scand. 1974;15(2):188-97. doi: 10.1186/BF03547480.
4
N1-glucosides as urinary metabolites of sulphadimidine, sulphamerazine and sulphamethoxazole.N1-葡萄糖苷作为磺胺嘧啶、磺胺甲嘧啶和磺胺甲恶唑的尿液代谢产物。
Eur J Drug Metab Pharmacokinet. 1988 Jul-Sep;13(3):177-83. doi: 10.1007/BF03189937.
5
Concentrations of trimethoprim and sulphadoxine in tissues from goats and a cow.山羊和一头奶牛组织中甲氧苄啶和磺胺多辛的浓度。
Acta Vet Scand. 1975;16(3):405-10. doi: 10.1186/BF03546658.
6
Model ecosystem evaluation of the environmental impacts of the veterinary drugs phenothiazine, sulfamethazine, clopidol, and diethylstilbestrol.兽药吩噻嗪、磺胺二甲嘧啶、氯羟吡啶和己烯雌酚对环境影响的模型生态系统评估
Environ Health Perspect. 1976 Dec;18:167-79. doi: 10.1289/ehp.7618167.

本文引用的文献

1
The metabolism of sulphonamides: 5. A study of the oxidation and acetylation of sulphonamide drugs and related compounds in the rabbit.磺胺类药物的代谢:5. 家兔体内磺胺类药物及相关化合物的氧化和乙酰化研究
Biochem J. 1948;42(3):351-6. doi: 10.1042/bj0420351.
2
The metabolism of sulphamezathine, 4:6-dimethylpyrimidine and 2-amino-4:6-dimethylpyrimidine in the rabbit with observations on the hydroxylation of some other sulphonamides.磺胺甲嘧啶、4:6-二甲基嘧啶和2-氨基-4:6-二甲基嘧啶在兔体内的代谢以及对其他一些磺胺类药物羟基化作用的观察
Biochem J. 1951 Apr;48(4):400-6. doi: 10.1042/bj0480400.
3
The preparation and properties of beta-glucuronidase. IV. Inhibition by sugar acids and their lactones.β-葡萄糖醛酸酶的制备及其性质。IV. 糖酸及其内酯的抑制作用。
Biochem J. 1952 Nov;52(3):464-72. doi: 10.1042/bj0520464.
4
Active mammary excretion of N4-acetylated sulphanilamide.N4-乙酰化磺胺的乳腺主动排泄
Acta Vet Scand. 1969;10(4):402-3. doi: 10.1186/BF03548272.
5
Comparative toxicological, chemotherapeutic and pharmacokinetic studies with sulphormethoxine and other sulphonamides in animals and man.磺胺甲氧嗪与其他磺胺类药物在动物和人体中的比较毒理学、化疗学及药代动力学研究。
Chemotherapy. 1969;14(4):195-226. doi: 10.1159/000220630.
6
Species differences in the metabolism and excretion of sulphasomidine and sulphamethomidine.磺胺索嘧啶和磺胺甲嘧啶在代谢及排泄方面的种属差异。
Biochem J. 1969 Jan;111(2):173-9. doi: 10.1042/bj1110173.
7
Structure and species as factors affecting the metabolism of some methoxy-6-sulphanilamidopyrimidines.结构与物种作为影响某些甲氧基-6-磺胺嘧啶代谢的因素
Biochem J. 1969 Jan;111(2):167-72. doi: 10.1042/bj1110167.
8
Species differences in the metabolism of sulphadimethoxine.磺胺二甲氧嘧啶代谢的种属差异。
Biochem J. 1968 Oct;109(5):851-6. doi: 10.1042/bj1090851.
9
[Renal excretion of sulphanilamide, sulphadimidine, sulphadoxine and sulphamethoxazole in goats].[山羊体内磺胺、磺胺二甲嘧啶、磺胺多辛和磺胺甲恶唑的肾脏排泄情况]
Nord Vet Med. 1972 Dec;24(12):601-11.
10
The metabolism of sulphadimethoxypyrimidine.磺胺二甲氧嘧啶的代谢
Xenobiotica. 1972 Jan;2(1):69-75. doi: 10.3109/00498257209036235.