| Item |
Information |
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Drug Groups
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approved; investigational |
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Description
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A glucocorticoid used in the management of asthma, the treatment of various skin disorders, and allergic rhinitis. [PubChem] |
| Indication |
For the treatment of mild to moderate active Crohn's disease. Also for the treatment of asthma, non-infectious rhinitis (including hay fever and other allergies), and for treatment and prevention of nasal polyposis. |
| Pharmacology |
Budesonide is a synthetic corticosteroid used in Crohn's disease to decrease the symptoms and inflammation associated with the disease, especially at times of flare up. Budesonide has a high topical glucocorticosteroid (GCS) activity and a substantial first pass elimination. The formulation contains granules which are coated to protect dissolution in gastric juice, but which dissolve at pH >5.5, ie, normally when the granules reach the duodenum. Thereafter, a matrix of ethylcellulose with budesonide controls the release of the drug into the intestinal lumen in a time-dependent manner. |
| Toxicity |
Single oral doses of 200 and 400 mg/kg were lethal in female and male mice, respectively. The signs of acute toxicity were decreased motor activity, piloerection and generalized edema. |
| Affected Organisms |
| • |
Humans and other mammals |
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| Biotransformation |
Following absorption, budesonide is subject to high first pass metabolism (80-90%). In vitro experiments in human liver microsomes demonstrate that budesonide is rapidly and extensively biotransformed, mainly by CYP3A4, to its 2 major metabolites, 6b-hydroxy budesonide and 16a- hydroxy prednisolone. The glucocorticoid activity of these metabolites is negligible (<1/100) in relation to that of the parent compound. |
| Absorption |
Absorption is complete following oral administration. |
| Half Life |
2.0 and 3.6 hours |
| Protein Binding |
85-90% |
| Elimination |
Budesonide is excreted in urine and feces in the form of metabolites. |
| Distribution |
* 3 L/kg [asthmatic children 4 to 6 years of age] |
| Clearance |
* 0.5 L/min [Athmatic children 4 to 6 years of age] |
| External Links |
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