Overview of Newer Glucocorticosteroid Preparations for Inflammatory Bowel Disease
Because the glucocorticosteroid receptor seems to be uniform in the human body, there is currently no support for a possibility of separating the therapeutic and adverse glucocorticosteroid actions at the receptor level. However, based on a new generation of glucocorticosteroids characterized by a h...
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| Main Author: | |
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| Format: | Article |
| Language: | English |
| Published: |
Wiley
1990-01-01
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| Series: | Canadian Journal of Gastroenterology |
| Online Access: | http://dx.doi.org/10.1155/1990/708916 |
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| Summary: | Because the glucocorticosteroid receptor seems to be uniform in the human body, there is currently no support for a possibility of separating the
therapeutic and adverse glucocorticosteroid actions at the receptor level. However,
based on a new generation of glucocorticosteroids characterized by a high
first pass metabolism in the liver, it seems possible today co reach a more selective
topical therapy of inflammatory bowel disease. The properties of three new
glucocorticosteroids are presented: the highly potent budesonide, fluticasone
propionate and tixocortol pivalate - the latter with only low topical potency.
Their properties can be exemplified by budesonide, which is currently the best
documented compound. The topical potency of budesonide is 200 and 15 times
higher than chose of hydrocortisone and prednisolone, respectively. This means
that there is a high potential for anti-inflammatory and immunosuppressive
actions on rectal and bowel mucosa. The compound is metabolically stable in
the bowel compartment, which allows full retention of glucocorticosteroid
activity in the target organ. However, when absorbed and distributed to the liver,
there is a 90% first pass hepatic metabolism co metabolites of very low potency.
This suggests that after topical application to rectal or bowel mucosa, glucocorticosteroid
activity in the systemic circulation is low. This is in contrast to
prednisolone, which has a hepatic first pass metabolism of just 20%. |
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| ISSN: | 0835-7900 |