| Pharmacology and pharmacokinetics of 5-aminosalicylic acid. | |
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MedLine Citation:
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PMID: 3319458 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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There is accumulating clinical evidence that 5-aminosalicylic acid (5-ASA), a primary metabolite of sulfasalazine (SAS), represents the therapeutic active moiety of the azo-compound SAS in the treatment of chronic inflammatory bowel disease (IBD). Since it is presumed that 5-ASA acts from the lumen of the intestine, it is important to know how much 5-ASA is released from its special galenic formulations. After liberation of 5-ASA in the terminal ileum (only slow release oral preparations of 5-ASA) and colon (5-ASA suppositories and enemas), 5-ASA is only partly absorbed. A major part of this 5-ASA is presystemically eliminated, eg, N-acetylated during its first passage through the intestinal mucosa and liver. Mean steady state plasma levels of unchanged 5-ASA are rather low (range 0.02 to 1.2 microgram/ml) whereas those of Ac-5-ASA are always higher (range 0.1 to 2.9 micrograms/ml). This is due to the rapid elimination of 5-ASA (t1/2 = 0.4 to 2.4h) and the slightly slower renal excretion of the Ac-5-ASA (t1/2 = 6 to 9 h, renal clearance = 200 to 300 ml/min). The knowledge of the pharmacokinetic properties of 5-ASA from different drug formulations might contribute to a better understanding of its mode of action in IBD. |
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Authors:
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U Klotz; K E Maier |
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Publication Detail:
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Type: Clinical Trial; Journal Article; Research Support, Non-U.S. Gov't; Review |
Journal Detail:
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Title: Digestive diseases and sciences Volume: 32 ISSN: 0163-2116 ISO Abbreviation: Dig. Dis. Sci. Publication Date: 1987 Dec |
Date Detail:
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Created Date: 1988-02-02 Completed Date: 1988-02-02 Revised Date: 2007-11-15 |
Medline Journal Info:
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Nlm Unique ID: 7902782 Medline TA: Dig Dis Sci Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 46S-50S Citation Subset: AIM; IM |
Affiliation:
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Dr. Margarete Fischer-Bosch Institut fuer Klinische Pharmakologie, Stuttgart, Federal Republic of Germany. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Aminosalicylic Acids
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pharmacokinetics*,
pharmacology*,
therapeutic use Clinical Trials as Topic Colitis, Ulcerative / drug therapy* Crohn Disease / drug therapy* Humans Mesalamine |
| Chemical | |
Reg. No./Substance:
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0/Aminosalicylic Acids; 89-57-6/Mesalamine |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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