Pharmacology and pharmacokinetics of 5-aminosalicylic acid
| Autor: | K E Maier, Ulrich Klotz |
|---|---|
| Rok vydání: | 1987 |
| Předmět: |
Aminosalicylic acid
Physiology Lumen (anatomy) Pharmacology Inflammatory bowel disease chemistry.chemical_compound Pharmacokinetics Intestinal mucosa Crohn Disease Sulfasalazine medicine Humans Mesalamine Clinical Trials as Topic business.industry Gastroenterology medicine.disease digestive system diseases Aminosalicylic Acids surgical procedures operative chemistry Renal physiology Liberation Colitis Ulcerative business medicine.drug |
| Zdroj: | Digestive diseases and sciences. 32 |
| ISSN: | 0163-2116 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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