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Mechanism of Action
Budesonide¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ 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.
Pharmacology
Budesonide¿¡ ´ëÇÑ Pharmacology Á¤º¸ 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.
Protein Binding
Budesonide¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 85-90%
Half-life
Budesonide¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 2.0 and 3.6 hours
Absorption
Budesonide¿¡ ´ëÇÑ Absorption Á¤º¸ Absorption is complete following oral administration.
Biotransformation
Budesonide¿¡ ´ëÇÑ Biotransformation Á¤º¸ 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.
Toxicity
Budesonide¿¡ ´ëÇÑ Toxicity Á¤º¸ 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.
Drug Interactions
Budesonide¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Itraconazole The imidazole increases levels/effect of budesonideKetoconazole The imidazole increases levels/effect of budesonide
CYP450 Drug Interaction
[CYP450 TableÁ÷Á¢Á¶È¸]
Drug Target
[Drug Target]
SNP Á¤º¸
Name: Budesonide (DB01222)
Interacting Gene/Enzyme: T-box transcription factor TBX21 (Gene symbol = TBX21) Swissprot Q9UL17
SNP(s): rs2240017 (C Allele)
Effect: Improved response for long-term asthma treatment
Reference(s): Tantisira KG, Hwang ES, Raby BA, Silverman ES, Lake SL, Richter BG, Peng SL, Drazen JM, Glimcher LH, Weiss ST: TBX21: a functional variant predicts improvement in asthma with the use of inhaled corticosteroids. Proc Natl Acad Sci U S A. 2004 Dec 28;101(52):18099-104. Epub 2004 Dec 16. [PubMed]
Description
Budesonide¿¡ ´ëÇÑ Description Á¤º¸ A glucocorticoid used in the management of asthma, the treatment of various skin disorders, and allergic rhinitis. [PubChem]
Drug Category
Budesonide¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-inflammatory AgentsBronchodilator AgentsCorticosteroidsGlucocorticoids
Smiles String Canonical
Budesonide¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CCCC1OC2CC3C4CCC5=CC(=O)C=CC5(C)C4C(O)CC3(C)C2(O1)C(=O)CO
Smiles String Isomeric
Budesonide¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CCC[C@H]1O[C@@H]2C[C@H]3[C@@H]4CCC5=CC(=O)C=C[C@]5(C)[C@H]4[C@@H](O)C[C@]3(C)[C@@]2(O1)C(=O)CO
InChI Identifier
Budesonide¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C25H34O6/c1-4-5-21-30-20-11-17-16-7-6-14-10-15(27)8-9-23(14,2)22(16)18(28)12-24(17,3)25(20,31-21)19(29)13-26/h8-10,16-18,20-22,26,28H,4-7,11-13H2,1-3H3/t16-,17-,18-,20+,21-,22+,23-,24-,25+/m0/s1
Chemical IUPAC Name
Budesonide¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ Not Available
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