Product Name

Budesonide

CAS Number

51333-22-3

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Product Name:
Budesonide
CAS Number:
51333-22-3
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.
Mode of Action:

The exact mechanism of action of budesonide in the treatment of Crohn’s disease is not fully understood. However, being a glucocorticosteroid, budesonide has a high local anti-inflammatory effect.

Pharmacodynamics:

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.

Metabolism:

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 (

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.

IUPAC:
(1S, 2S, 4R, 8S, 9S, 11S, 12S, 13R)-11-hydroxy-8-(2-hydroxyacetyl)-9, 13-dimethyl-6-propyl-5, 7-dioxapentacyclo[10.8.0.0, {2, 9}.0, {4, 8}.0, {13, 18}]icosa-14, 17-dien-16-one
ATC:
A07EA06 D07AC09 R01AD05 R03BA02
PubChem:
63006
DrugBank:
DB01222 (APRD00442)
Formula:
C6H12N2O4Pt
Molecular Mass:
430.5339
SMILES:
[H][C@@]12C[C@H]3OC(CCC)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@H](O)[C@@]1([H])[C@@]2([H])CCC2=CC(=O)C=C[C@]12C
AHFS Code:
52:08.08 68:04.00
InChi:
VOVIALXJUBGFJZ-KWVAZRHASA-N

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