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Budesonide
drug data and news
Budesonide drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Budesonide | ||
| Brand Names/Synonyms | Bidien; Budeson; Budesonide; Budesonide, Pharma; BudesonideÊ; Cortivent; Desonide; Desowen; Entocort; Entocort Ec; Micronyl; Preferid; Pulmicort; Pulmicort Nebuamp; Pulmicort Respules; Pulmicort Turbuhaler; Rhinocort; Rhinocort Aqua; Rhinocort Turbuhaler; Spirocort; Tridesilon | ||
| Indication | For the treatment of mild to moderate active Crohn's disease. | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Budesonide is a synthetic corticosteroid indicated for the treatment of mild to moderate active Crohn's disease involving the ileum and/or the ascending colon. Budesonide is 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. | ||
| Mechanism 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. | ||
| Budesonide News (When available) |
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| Dosage Forms | CAPSULE (SUSTAINED-RELEASE); METERED-DOSE (AEROSOL); SUSPENSION | ||
| Drug_Category | Bronchodilator Agents; Anti-inflammatory Agents; Corticosteroids; ATC:A07EA06; ATC:D07AC09; ATC:R01AD05; ATC:R03BA02 | ||
| Absorption | Complete | ||
| Interactions |
Interactions for Budesonide: Concomitant oral administration of ketoconazole (a known inhibitor of CYP3A4 activity in the liver and in the intestinal mucosa) caused an eight-fold increase of the systemic exposure to oral budesonide. If treatment with inhibitors of CYP3A4 activity (such as ketoconazole, intraconazole, ritonavir, indinavir, saquinavir, erythromycin, etc.) is indicated, reduction of the budesonide dose should be considered. After extensive intake of grapefruit juice (which inhibits CYP3A4 activity predominantly in the intestinal mucosa), the systemic exposure for oral budesonide increased about two times. As with other drugs primarily being metabolized through CYP3A4, ingestion of grapefruit or grapefruit juice should be avoided in connection with budesonide administration. | ||
| Toxicity | Side effects include headache, respiratory infection, nausea, back pain, dyspepsia, dizziness, abdominal pain, flatulence, vomiting, fatigue | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | Not Available | ||
| Chemical Formula | C25H34O6 | ||
| Molecular Weight | 430.534 g/mol | ||
| Smiles String | CCCC1OC2CC3C4CCC5=CC(=O)C=CC5(C4C(CC3(C2(O1)C(=O)CO)C)O)C | ||
| Melting Point | 221-232 oC | ||
| Water Solubility | insoluble | ||
| State | Solid | ||
| LogP/Hphobicity | 3.145 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | rapidly and extensively biotransformed, mainly by CYP3A4 | ||
| Half Life | 2.0 and 3.6 hours | ||
| Protein Binding [%] | 85-90% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/cx1621.shtml http://www.drugs.com/cons/Budesonide.html http://www.rxlist.com/cgi/generic/entocort.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00442 | ||
| CAS Registry Number | 51333-22-3 | ||
| KEGG Compound ID | C06858 | ||
| PubChem ID | SID:63577 | ||
| PharmGKB ID | PA448681 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2241003 |
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