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猫单剂量研究中地高辛和二氢地高辛药代动力学的比较。

Comparison of the pharmacokinetics of digoxin and dihydrodigoxin in cats in single-dose studies.

作者信息

Heinz N, Flasch H

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1978 Jun;303(2):181-7. doi: 10.1007/BF00508066.

DOI:10.1007/BF00508066
PMID:673023
Abstract

Pharmacokinetics of 3H-dihydrodigoxin and 3H-digoxin after single intravenous and intraduodenal administration in cats are compared. Data could be described by an open two compartment body model. The beta half-life in plasma of dihydrodigoxin after initial rapid distribution is 4.6h compared to 10.4 h after digoxin administration. The volume of tissue distribution of dihydrodigoxin is 7 times smaller than that of digoxin (0.311 versus 2.051). The "specific uptake" of dihydrodigoxin into myocardium and some other tissues is very low. Over 5.5h the cumulative biliary and urinary elimination of dihydrodigoxin is definitely higher (45.7% versus 14.4%). An unexpected peak in TLC plates after dihydrodigoxin administration in blood, bile and urine was identified to be the sodium salt of the opened lactone structure: dihydrodigoxin acid.

摘要

比较了猫单次静脉注射和十二指肠给药后3H-二氢地高辛和3H-地高辛的药代动力学。数据可用开放二室模型描述。二氢地高辛初始快速分布后血浆中的β半衰期为4.6小时,而地高辛给药后为10.4小时。二氢地高辛的组织分布容积比地高辛小7倍(分别为0.311和2.051)。二氢地高辛进入心肌和其他一些组织的“特异性摄取”非常低。在5.5小时内,二氢地高辛经胆汁和尿液的累积消除量明显更高(分别为45.7%和14.4%)。在血液、胆汁和尿液中给予二氢地高辛后,薄层色谱板上出现一个意外峰,鉴定为开环内酯结构的钠盐:二氢地高辛酸。

相似文献

1
Comparison of the pharmacokinetics of digoxin and dihydrodigoxin in cats in single-dose studies.猫单剂量研究中地高辛和二氢地高辛药代动力学的比较。
Naunyn Schmiedebergs Arch Pharmacol. 1978 Jun;303(2):181-7. doi: 10.1007/BF00508066.
2
The development and application of a radioimmunoassay for dihydrodigoxin, a digoxin metabolite.地高辛代谢产物二氢地高辛放射免疫测定法的开发与应用。
J Pharmacol Exp Ther. 1982 Apr;221(1):123-31.
3
The measurement of urinary digoxin and dihydrodigoxin by radioimmunoassay and by mass spectroscopy.采用放射免疫分析法和质谱分析法测定尿中地高辛和二氢地高辛。
Clin Chim Acta. 1975 Jul 23;62(2):213-24. doi: 10.1016/0009-8981(75)90230-2.
4
Increased metabolism to dihydrodigoxin after intake of a microencapsulated formulation of digoxin.摄入地高辛微囊制剂后二氢地高辛的代谢增加。
Eur J Clin Pharmacol. 1984;27(2):197-202. doi: 10.1007/BF00544045.
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Determination of tritiated digoxin and metabolites in urine by liquid chromatography.用液相色谱法测定尿中氚标记地高辛及其代谢物
J Chromatogr. 1981 May 8;223(2):401-8. doi: 10.1016/s0378-4347(00)80113-9.
6
Reduction of digoxin to 20R-dihydrodigoxin by cultures of Eubacterium lentum.迟缓真杆菌培养物将地高辛还原为20R-二氢地高辛。
Appl Environ Microbiol. 1986 Jun;51(6):1300-3. doi: 10.1128/aem.51.6.1300-1303.1986.
7
Biotransformation and elimination of digoxin with normal and minimal renal function.地高辛在肾功能正常和轻度受损时的生物转化与消除。
Clin Pharmacol Ther. 1979 May;25(5 Pt 1):499-513. doi: 10.1002/cpt1979255part1499.
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Pharmacokinetics of beta-methyldigoxin in healthy humans I: intravenous studies.健康人体中β-甲基地高辛的药代动力学I:静脉注射研究
J Pharm Sci. 1977 Feb;66(2):242-53. doi: 10.1002/jps.2600660228.
9
Pharmacokinetics of digoxin in the rat.地高辛在大鼠体内的药代动力学
Drug Metab Dispos. 1976 Jan-Feb;4(1):88-93.
10
Evidence for presence of a reduced form of digoxin-like immunoreactive factor (dihydro-DLIF) in mammalian tissues.哺乳动物组织中存在还原形式的地高辛样免疫反应因子(二氢-DLIF)的证据。
Clin Chem. 1996 Jul;42(7):1092-9.

引用本文的文献

1
Reduction of digoxin to 20R-dihydrodigoxin by cultures of Eubacterium lentum.迟缓真杆菌培养物将地高辛还原为20R-二氢地高辛。
Appl Environ Microbiol. 1986 Jun;51(6):1300-3. doi: 10.1128/aem.51.6.1300-1303.1986.
2
Pharmacokinetics of dihydrodigitoxin in the cat. A comparison with digitoxin.猫体内二氢地高辛的药代动力学。与地高辛的比较。
Naunyn Schmiedebergs Arch Pharmacol. 1979 Dec;310(2):147-53. doi: 10.1007/BF00500279.

本文引用的文献

1
THE DIFFERENCE IN VELOCITY BETWEEN THE LETHAL AND INOTROPIC ACTION OF DIHYDRODIGOXIN.双氢地高辛致死作用与变力作用的速度差异。
Naunyn Schmiedebergs Arch Exp Pathol Pharmakol. 1964 Jul 20;248:437-49. doi: 10.1007/BF00246890.
2
DISTRIBUTION AND EXCRETION OF OUABAIN-H3 AND DIHYDRO-OUABAIN-H3 IN RATS AND SHEEP.哇巴因 - H3和二氢哇巴因 - H3在大鼠和绵羊体内的分布与排泄
J Pharmacol Exp Ther. 1963 Nov;142:223-30.
3
Chemical structure and pharmacological activity of some derivatives of digitoxigenin and digoxigenin.洋地黄毒苷配基和地高辛配基某些衍生物的化学结构与药理活性
Br J Pharmacol Chemother. 1962 Apr;18(2):311-24. doi: 10.1111/j.1476-5381.1962.tb01411.x.
4
Effects of dihydro-ouabain, dihydrodigoxin and dihydrodigitoxin on the heart-lung preparation of the dog.双氢哇巴因、双氢地高辛和双氢毛花苷丙对狗心肺标本的作用。
J Pharmacol Exp Ther. 1957 Nov;121(3):330-9.
5
Structure-activity correlation of the lethality and central effects of selected cardiac glycosides.所选强心苷的致死性与中枢作用的构效关系
J Pharmacol Exp Ther. 1966 Jun;152(3):501-8.
6
Metabolism of digoxin: role of the liver in tritiated digoxin degradation.地高辛的代谢:肝脏在氚标记地高辛降解中的作用。
J Pharmacol Exp Ther. 1965 Dec;150(3):463-8.
7
Concept of a volume of distribution and possible errors in evaluation of this parameter.分布容积的概念以及该参数评估中可能存在的误差。
J Pharm Sci. 1968 Jan;57(1):128-33. doi: 10.1002/jps.2600570125.
8
The clinical pharmacology of digitalis glycosides: a review.洋地黄苷类的临床药理学:综述
Am J Med Sci. 1968 Jun;255:382-414. doi: 10.1097/00000441-196806000-00006.
9
Identification by gas chromatography-mass spectroscopy of dihydrodigoxin--a metabolite of digoxin in man.通过气相色谱-质谱联用技术鉴定人体内地高辛的代谢产物二氢地高辛。
J Pharmacol Exp Ther. 1973 Feb;184(2):424-31.
10
The uptake of cardiac glycosides in relation to their actions in isolated cardiac muscle.强心苷在离体心肌中的摄取与其作用的关系。
Br J Pharmacol. 1972 Nov;46(3):488-97. doi: 10.1111/j.1476-5381.1972.tb08146.x.