Abstract
1 Five patients have been studied to determine the contribution of the gut wall to the pre-systemic metabolism of ethinyloestradiol. All patients had a catheter inserted into their hepatic portal vein as part of their surgical management. 2 After an oral dose of 50 micrograms (65 microCi) ethinyloestradiol, blood samples were taken from the hepatic portal vein and from a peripheral vein at intervals for 1 h. 3 In each patient the concentration of conjugated ethinyloestradiol in the portal vein was considerably higher than in the peripheral vein. 4 Although a number of assumptions have been made, calculations showed that the gut wall appeared to be twice as effective as the liver in conjugating ethinyloestradiol on the first pass. 5 In two patients there was no evidence of major uptake or metabolism of ethinyloestradiol in the lung.
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- Andersson K. E., Bergdahl B., Dencker H., Wettrell G. Proscillaridin activity in portal and peripheral venous blood after oral administration to man. Eur J Clin Pharmacol. 1977 Apr 20;11(4):277–281. doi: 10.1007/BF00607677. [DOI] [PubMed] [Google Scholar]
- Back D. J., Bates M., Breckenridge A. M., Ellis A., Hall J. M., Maciver M., Orme M. L., Rowe P. H. The in vitro metabolism of ethinyloestradiol, mestranol and levonorgestrel by human jejunal mucosa. Br J Clin Pharmacol. 1981 Mar;11(3):275–278. doi: 10.1111/j.1365-2125.1981.tb00534.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Back D. J., Breckenridge A. M., Crawford F. E., MacIver M., Orme M. L., Rowe P. H., Watts M. J. An investigation of the pharmacokinetics of ethynylestradiol in women using radioimmunoassay. Contraception. 1979 Sep;20(3):263–273. doi: 10.1016/0010-7824(79)90098-2. [DOI] [PubMed] [Google Scholar]
- DICZFALUSY E., FRANKSSON C., LISBOA B. P., MARTINSEN B. Formation of oestrone glucosiduronate by the human intestinal tract. Acta Endocrinol (Copenh) 1962 Aug;40:537–551. doi: 10.1530/acta.0.0400537. [DOI] [PubMed] [Google Scholar]
- DICZFALUSY E., FRANKSSON C., MARTINSEN B. Oestrogen conjugation by the human intestinal tract. Acta Endocrinol (Copenh) 1961 Sep;38:59–72. doi: 10.1530/acta.0.0380059. [DOI] [PubMed] [Google Scholar]
- Levy G., Matsuzawa T. Pharmacokinetics of salicylamide elimination in man. J Pharmacol Exp Ther. 1967 May;156(2):285–293. [PubMed] [Google Scholar]
- Mahon W. A., Inaba T., Stone R. M. Metabolism of flurazepam by the small intestine. Clin Pharmacol Ther. 1977 Aug;22(2):228–233. doi: 10.1002/cpt1977222228. [DOI] [PubMed] [Google Scholar]
- Routledge P. A., Shand D. G. Presystemic drug elimination. Annu Rev Pharmacol Toxicol. 1979;19:447–468. doi: 10.1146/annurev.pa.19.040179.002311. [DOI] [PubMed] [Google Scholar]