Literature DB >> 6783058

The in vitro metabolism of ethinyloestradiol, mestranol and levonorgestrel by human jejunal mucosa.

D J Back, M Bates, A M Breckenridge, A Ellis, J M Hall, M Maciver, M L Orme, P H Rowe.   

Abstract

1 Ethinyloestradiol was extensively metabolised in vitro by human jejunal mucosa to form ethinyloestradiol sulphate. 2 The amount of conjugation was directly related to the weight of biopsy tissue. 3 The degree of conjugation of mestranol and levonorgestrel was much lower than for ethinyloestradiol suggesting that the 17-position of the steroid nucleus is relatively inaccessible for conjugation. 4 No Phase I metabolism of ethinyloestradiol or levonorgestrel was apparent in the conditions used in these experiments.

Entities:  

Keywords:  Clinical Research; Contraception; Contraceptive Agents; Contraceptive Agents, Estrogen; Contraceptive Agents, Female; Contraceptive Agents, Progestin; Ethinyl Estradiol; Examinations And Diagnoses; Family Planning; In Vitro; Laboratory Examinations And Diagnoses; Laboratory Procedures; Mestranol; Metabolic Effects; Norgestrel; Research Methodology

Mesh:

Substances:

Year:  1981        PMID: 6783058      PMCID: PMC1401625          DOI: 10.1111/j.1365-2125.1981.tb00534.x

Source DB:  PubMed          Journal:  Br J Clin Pharmacol        ISSN: 0306-5251            Impact factor:   4.335


  10 in total

1.  ENZYMES AND DRUG SENSITIVITY. ACETYLATION POLYMORPHISMS.

Authors:  D A EVANS
Journal:  Proc R Soc Med       Date:  1964-06

2.  A chemical method for the determination of oestriol, oestrone and oestradiol in human urine.

Authors:  J B BROWN
Journal:  Biochem J       Date:  1955-06       Impact factor: 3.857

3.  Formation of oestrone glucosiduronate by the human intestinal tract.

Authors:  E DICZFALUSY; C FRANKSSON; B P LISBOA; B MARTINSEN
Journal:  Acta Endocrinol (Copenh)       Date:  1962-08

4.  Oestrogen conjugation by the human intestinal tract.

Authors:  E DICZFALUSY; C FRANKSSON; B MARTINSEN
Journal:  Acta Endocrinol (Copenh)       Date:  1961-09

Review 5.  Metabolism of hormones, drugs and other substances by the gut.

Authors:  K Hartiala
Journal:  Physiol Rev       Date:  1973-04       Impact factor: 37.312

6.  Metabolism of tetrahydrocannabinol by the small intestine.

Authors:  M L Greene; D R Saunders
Journal:  Gastroenterology       Date:  1974-03       Impact factor: 22.682

7.  Plasma levels of ethynyloestradiol after administration of ethynyloestradiol or mestranol to human subjects.

Authors:  R J Warren; K Fotherby
Journal:  J Endocrinol       Date:  1973-11       Impact factor: 4.286

8.  Investigations of pharmacokinetics of levonorgestrel to specific consideration of a possible first-pass effect in women.

Authors:  M Hümpel; H Wendt; G Pommerenke; C Weiss; U Speck
Journal:  Contraception       Date:  1978-03       Impact factor: 3.375

9.  Metabolism of flurazepam by the small intestine.

Authors:  W A Mahon; T Inaba; R M Stone
Journal:  Clin Pharmacol Ther       Date:  1977-08       Impact factor: 6.875

10.  An investigation of the pharmacokinetics of ethynylestradiol in women using radioimmunoassay.

Authors:  D J Back; A M Breckenridge; F E Crawford; M MacIver; M L Orme; P H Rowe; M J Watts
Journal:  Contraception       Date:  1979-09       Impact factor: 3.375

  10 in total
  12 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

2.  Loss of orally administered drugs in GI tract.

Authors:  Yogeshkumar Nanasaheb Gavhane; Adhikrao Vyankatrao Yadav
Journal:  Saudi Pharm J       Date:  2012-04-20       Impact factor: 4.330

Review 3.  Pharmacokinetic drug interactions with oral contraceptives.

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

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

Review 5.  The third S.K. & F. Prize lecture, University of London, December 1981. The clinical pharmacology of oral contraceptive steroids.

Authors:  M L Orme
Journal:  Br J Clin Pharmacol       Date:  1982-07       Impact factor: 4.335

Review 6.  Pharmacokinetic interactions with antiepileptic drugs.

Authors:  E Perucca
Journal:  Clin Pharmacokinet       Date:  1982 Jan-Feb       Impact factor: 6.447

Review 7.  Extrahepatic metabolism of drugs in humans.

Authors:  D R Krishna; U Klotz
Journal:  Clin Pharmacokinet       Date:  1994-02       Impact factor: 6.447

8.  First pass biotransformation of ethinylestradiol in rat small intestine in situ.

Authors:  M Schwenk; C Schiemenz; V L del Pino; H Remmer
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1982-12       Impact factor: 3.000

9.  The gut wall metabolism of ethinyloestradiol and its contribution to the pre-systemic metabolism of ethinyloestradiol in humans.

Authors:  D J Back; A M Breckenridge; M MacIver; M Orme; H S Purba; P H Rowe; I Taylor
Journal:  Br J Clin Pharmacol       Date:  1982-03       Impact factor: 4.335

Review 10.  Individual variation in first-pass metabolism.

Authors:  Y K Tam
Journal:  Clin Pharmacokinet       Date:  1993-10       Impact factor: 6.447

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