Literature DB >> 941195

Human urinary and liver conjugates of 17alpha-ethnylestradiol.

E D Helton, M C Williams, J W Goldzieher.   

Abstract

Chromatographic profiles of the conjugates of 17alpha-ethynylestradiol (EE2) were obtained from the urine of castrate and normal women given tritium labeled EE2 orally. Five distinct radioactive peaks were observed, with considerable quantitative variation between individuals. Glucosiduronate fractions comprised the dominant excreted radioactivity. In vitro incubation of normal human liver also produced five conjugate types. Simultaneous intravenous/oral (14C/3H) administration of EE2 demonstrated conversion to identical urinary conjugate and free steroid products, with a greater excretion of the intravenous material. Authentic 3-glucuronide of EE2 was synthesized and its position in the chromatographic system relative to the urinary conjugate peaks demonstrated.

Entities:  

Keywords:  Biology; Castration; Clinical Research; Contraception; Contraceptive Agents, Estrogen--administraction and dosage; Contraceptive Agents, Estrogen--analysis; Contraceptive Agents, Estrogen--side effects; Contraceptive Agents, Female--administraction and dosage; Contraceptive Agents, Female--analysis; Contraceptive Agents, Female--side effects; Contraceptive Agents--administraction and dosage; Contraceptive Agents--analysis; Contraceptive Agents--side effects; Enzymatic Effects; Enzymes And Enzyme Inhibitors; Estrogens; Ethinyl Estradiol--administraction and dosage; Ethinyl Estradiol--analysis; Ethinyl Estradiol--side effects; Examinations And Diagnoses; Family Planning; Hepatic Effects; Hormones; Human Volunteers; Hysterectomy; In Vitro; Laboratory Examinations And Diagnoses; Laboratory Procedures; Metabolic Effects; Physiology; Research Methodology; Steroid Metabolic Effects; Women

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Substances:

Year:  1976        PMID: 941195     DOI: 10.1016/0039-128x(76)90144-6

Source DB:  PubMed          Journal:  Steroids        ISSN: 0039-128X            Impact factor:   2.668


  6 in total

Review 1.  Pharmacokinetic drug interactions involving 17alpha-ethinylestradiol: a new look at an old drug.

Authors:  Hongjian Zhang; Donghui Cui; Bonnie Wang; Yong-Hae Han; Praveen Balimane; Zheng Yang; Michael Sinz; A David Rodrigues
Journal:  Clin Pharmacokinet       Date:  2007       Impact factor: 6.447

Review 2.  Pharmacokinetic drug interactions with oral contraceptives.

Authors:  D J Back; M L Orme
Journal:  Clin Pharmacokinet       Date:  1990-06       Impact factor: 6.447

3.  Metabolic oxidation of the ethynyl group in 4-ethynylbiphenyl.

Authors:  A Wade; A M Symons; L Martin; D V Parke
Journal:  Biochem J       Date:  1979-12-15       Impact factor: 3.857

Review 4.  Clinical pharmacokinetics of oral contraceptive steroids.

Authors:  M L Orme; D J Back; A M Breckenridge
Journal:  Clin Pharmacokinet       Date:  1983 Mar-Apr       Impact factor: 6.447

5.  Interindividual variability in the glucuronidation and sulphation of ethinyloestradiol in human liver.

Authors:  A Temellini; L Giuliani; G M Pacifici
Journal:  Br J Clin Pharmacol       Date:  1991-06       Impact factor: 4.335

6.  Risk-Benefit Assessment of Ethinylestradiol Using a Physiologically Based Pharmacokinetic Modeling Approach.

Authors:  Udoamaka Ezuruike; Helen Humphries; Maurice Dickins; Sibylle Neuhoff; Iain Gardner; Karen Rowland Yeo
Journal:  Clin Pharmacol Ther       Date:  2018-04-27       Impact factor: 6.875

  6 in total

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