JPET xPharm- The Comprehensive Pharmacology Reference

Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
QUICK SEARCH:   [advanced]


     

This Article
Right arrow Full Text (PDF)
Right arrow Submit a response
Right arrow Alert me when this article is cited
Right arrow Alert me when eLetters are posted
Right arrow Alert me if a correction is posted
Services
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Download to citation manager
Citing Articles
Right arrow Citing Articles via HighWire
Right arrow Citing Articles via Google Scholar
Google Scholar
Right arrow Articles by Burns, J. J.
Right arrow Articles by Brodie, B. B.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Burns, J. J.
Right arrow Articles by Brodie, B. B.
Journal of Pharmacology And Experimental Therapeutics, Vol. 109, Issue 3, 346-357, 1953
Copyright © 1953 by American Society for Pharmacology and Experimental Therapeutics

THE PHYSIOLOGICAL DISPOSITION OF PHENYLBUTAZONE (BUTAZOLIDIN) IN MAN AND A METHOD FOR ITS ESTIMATION IN BIOLOGICAL MATERIAL

J. J. Burns 1, Rose K. Rose 1, Theodore Chenkin 1, A. Goldman 1, Arthur Schulert 1, and Bernard B. Brodie 2

1 Third (New York University) Medical Division, Goldwater Memorial Hospital, New York, New York
2 Laboratory of Chemical Pharmacology, National Heart Institute, National Institutes of Health, Public Health Service, Department of Health, Education, and Welfare, Bethesda 14, Maryland

1. A method is described for the estimation of phenylbutazone in biological fluids and tissues.

2. Phenylbutazone is rapidly and completely absorbed from the gastrointestinal tract of man. Intramuscular absorption, on the other hand, is relatively slow, because of localization of the drug at the site of the injection.

3. Phenylbutazone at therapeutic concentrations is highly bound to plasma proteins. About one-third of a single dose of the drug is localized in plasma.

4. The drug is almost completely metabolized in the body. After discontinuance of dosage, the rate of biotransformation in man is slow, averaging about 20 per cent per day, but varies considerably in different subjects. Subjects with Laennec's cirrhosis of the liver metabolize the drug as readily as normal subjects.

5. Plasma levels of phenylbutazone are not proportional to dosage. Plasma levels achieved on doses of 1600 mgm. per day are only a few per cent higher than those obtained on doses of 800 mgm. per day. On both dosage regimens, absorption is complete and urinary excretion of the drug is negligible.

6. Different species vary markedly in the rates at which they metabolize phenylbutazone. The biologic half-life of the drug is about 72 hours in man, 6 hours in dog and rat, 5 hours in guinea pig, and 3 hours in rabbit.

Submitted on July 1, 1953




This article has been cited by other articles:


Home page
 ScienceHome page
E. S. Vesell and J. G. Page
Genetic Control of Drug Levels in Man: Antipyrine
Science, July 5, 1968; 161(3836): 72 - 73.
[Abstract] [PDF]

Home page
 ScienceHome page
E. S. Vesell and J. G. Page
Genetic Control of Drug Levels in Man: Phenylbutazone
Science, March 29, 1968; 159(3822): 1479 - 1480.
[Abstract] [PDF]


Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
All ASPET Journals Molecular Pharmacology Pharmacological Reviews
Molecular Interventions Drug Metabolism and Disposition

Copyright © 1953 by the American Society for Pharmacology and Experimental Therapeutics.