Abstract |
The disposition of 5-aminosalicylic acid (5-AS), the therapeutically active metabolite of sulphasalazine (SZ), has been studied in patients with active inflammatory bowel disease, in patients with biliary tract disease and post-operative T-tube drainage, and in healthy volunteers. Subjects were treated 3 times a day either with 5-AS 0.5 g suppositories and a slow-release preparation or with SZ 1 g tid (equivalent to 5-AS 1.14 g/day). Plasma and urine concentrations of 5-AS and its acetylated major metabolite (AcAS) were monitored during one dosing interval. In a cross-over trial in 5 patients with ulcerative colitis no difference, was found in the dose-corrected mean (+/- SD) steady state plasma levels (Css) of 5-AS and AcAS between treatment with 5-AS suppositories (0.10 +/- 0.07 and 0.50 +/- 0.20 micrograms/ml, respectively) and SZ (0.12 +/- 0.14 and 0.67 +/- 0.14 micrograms/ml, respectively). Urinary excretion of total AS (5-AS + AcAS), too, was similar (192 +/- 70 and 179 +/- 79 mg/day) with both forms of treatment. The oral slow-release form of 5-AS produced slightly higher Css in 5 patients with Crohn's disease (5-AS 0.21 +/- 0.22 micrograms/ml; AcAS 0.83 +/- 0.40 micrograms/ml) and in 5 healthy volunteers (5-AS 0.28 +/- 0.14 micrograms/ml; AcAS 1.10 +/- 0.43 micrograms/ml). Urinary recovery of total AS averaged 20 +/- 6% (patients) and 27 +/- 10% (volunteers).(ABSTRACT TRUNCATED AT 250 WORDS)
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Authors | C Fischer, K Maier, E Stumpf, U von Gaisberg, U Klotz |
Journal | European journal of clinical pharmacology
(Eur J Clin Pharmacol)
Vol. 25
Issue 4
Pg. 511-5
( 1983)
ISSN: 0031-6970 [Print] Germany |
PMID | 6140167
(Publication Type: Clinical Trial, Journal Article, Randomized Controlled Trial, Research Support, Non-U.S. Gov't)
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Chemical References |
- Aminosalicylic Acids
- Sulfasalazine
- Mesalamine
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Topics |
- Adult
- Aged
- Aminosalicylic Acids
(metabolism, therapeutic use)
- Bile
(analysis)
- Biliary Tract Diseases
(drug therapy, metabolism)
- Colitis, Ulcerative
(drug therapy, metabolism)
- Crohn Disease
(drug therapy, metabolism)
- Humans
- Kinetics
- Mesalamine
- Middle Aged
- Sulfasalazine
(metabolism, therapeutic use)
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