DOI: 10.1111/j.1600-0773.1980.tb02463.x. Pharmacokinetic Studies of 5‐Fluorouracil after Oral and Intravenous Administration in Man

Pharmacokinetic Studies of 5‐Fluorouracil after Oral and Intravenous Administration in Man

10.1111/j.1600-0773.1980.tb02463.x

Crossref journal-article

Wiley

Acta Pharmacologica et Toxicologica (311)

Abstract

Abstract The pharmacokinetic conditions for oral administration of 5‐fluorouracil (5‐FU) were investigated in 16 patients with malignant liver tumours. The concentration of 5‐FU in portal and systemic blood was determined by a microbiologic method every 10 min. during 2 hours after oral or intravenous administration of a standard dose of 250 mg 5‐FU (∼ 4 mg/kg b.wt.) or 15 mg 5‐FU/kg b.wt. The drug was rapidly absorbed after oral administration with peak values within 10–30 min. 25% of the lower and 40% of the higher oral dose reached the systemic circulation. The reduction of systemic bio‐availability was partly accomplished by a loss in the gastrointestinal tract and partly by extraction by the liver. The hepatic extraction ratio was calculated to 0.56 and 0.26 after the lower and the higher dose respectively indicating a saturable process. The availability of 5‐FU was significantly higher in portal blood than in systemic blood after oral administration. The opposite conditions were found after intravenous administration. Thus, oral administration of 5‐FU to patients with malignant liver tumours seems rational.

Bibliography

AlmersjÃ¶, O. E., Gustavsson, B. G., RegÃ¥rdh, C. âG., & WÃ¥hlÃ©n, P. (1980). Pharmacokinetic Studies of 5âFluorouracil after Oral and Intravenous Administration in Man. Acta Pharmacologica et Toxicologica, 46(5), 329â336. Portico.

Authors 4

O. E. Almersjö (first)
B. G. Gustavsson (additional)
C.‐G. Regårdh (additional)
P. Wåhlén (additional)

References 30 Referenced 35

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{'key': 'e_1_2_2_3_1', 'first-page': '131', 'article-title': 'Results of liver dearterialization combined with regional perfusion of 5‐Fluorouracil for liver cancer', 'volume': '142', 'author': 'Almersjö O.', 'year': '1976', 'journal-title': 'Acta Chir. Scand.'} / Acta Chir. Scand. / Results of liver dearterialization combined with regional perfusion of 5‐Fluorouracil for liver cancer by Almersjö O. (1976)
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{'key': 'e_1_2_2_6_1', 'first-page': '227', 'article-title': 'Methodological aspects on an agar plate technique for determination of biologically active 5‐fluorouracil in blood, urine and bile', 'volume': '85', 'author': 'Almersjö O.', 'year': '1977', 'journal-title': 'Acta Pathol. Microbiol. Scand.'} / Acta Pathol. Microbiol. Scand. / Methodological aspects on an agar plate technique for determination of biologically active 5‐fluorouracil in blood, urine and bile by Almersjö O. (1977)
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{'key': 'e_1_2_2_12_1', 'first-page': '1045', 'article-title': 'The physiological disposition of 5‐fluorouracil in mice bearing SOL Li210 lymphocytic leukemia', 'volume': '32', 'author': 'Chadwick M.', 'year': '1972', 'journal-title': 'Cancer Res.'} / Cancer Res. / The physiological disposition of 5‐fluorouracil in mice bearing SOL Li210 lymphocytic leukemia by Chadwick M. (1972)
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{'key': 'e_1_2_2_26_1', 'first-page': '1109', 'article-title': 'Question and answers: Oral vs intravenous administration of fluorouracil', 'volume': '229', 'author': 'Moertel C. G.', 'year': '1974', 'journal-title': 'JAMA'} / JAMA / Question and answers: Oral vs intravenous administration of fluorouracil by Moertel C. G. (1974)
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{'key': 'e_1_2_2_30_1', 'first-page': '749', 'article-title': 'The blood supply of colorectal liver metastases', 'volume': '39', 'author': 'Taylor J.', 'year': '1979', 'journal-title': 'Brit. J. Cancer'} / Brit. J. Cancer / The blood supply of colorectal liver metastases by Taylor J. (1979)
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Dates

Type	When
Created	15 years, 1 month ago (July 29, 2010, 5:37 p.m.)
Deposited	1 year, 9 months ago (Nov. 7, 2023, 4:55 p.m.)
Indexed	1 year, 6 months ago (Feb. 6, 2024, 7:48 a.m.)
Issued	45 years, 3 months ago (May 1, 1980)
Published	45 years, 3 months ago (May 1, 1980)
Published Online	16 years, 5 months ago (March 13, 2009)
Published Print	45 years, 3 months ago (May 1, 1980)

Funders 0

None

BibTeX

@article{Almersj__1980, title={Pharmacokinetic Studies of 5‐Fluorouracil after Oral and Intravenous Administration in Man}, volume={46}, ISSN={0001-6683}, url={http://dx.doi.org/10.1111/j.1600-0773.1980.tb02463.x}, DOI={10.1111/j.1600-0773.1980.tb02463.x}, number={5}, journal={Acta Pharmacologica et Toxicologica}, publisher={Wiley}, author={Almersjö, O. E. and Gustavsson, B. G. and Regårdh, C.‐G. and Wåhlén, P.}, year={1980}, month=may, pages={329–336} }

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