Systematic (IUPAC) name | |
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16,17-(butylidenebis(oxy))-11,21-dihydroxy-, (11-β,16-α)-pregna-1,4-diene-3,20-dione | |
Clinical data | |
Trade names | Rhinocort |
AHFS/Drugs.com | monograph |
MedlinePlus | a608007 |
Pregnancy cat. | C(US) |
Legal status | POM (UK) ℞-only (US) |
Routes | Oral, Nasal, tracheal, rectal |
Pharmacokinetic data | |
Bioavailability | 10-20% (first pass effect) |
Protein binding | 85-90% |
Metabolism | Hepatic CYP3A4 |
Half-life | 2.0-3.6 hours |
Excretion | Renal, Faecal |
Identifiers | |
CAS number | 51333-22-3 |
ATC code | A07EA06 D07AC09, R01AD05, R03BA02 |
PubChem | CID 40000 |
DrugBank | APRD00442 |
ChemSpider | 36566 |
UNII | Q3OKS62Q6X |
KEGG | D00246 |
ChEMBL | CHEMBL1370 |
Chemical data | |
Formula | C25H34O6 |
Mol. mass | 430.534 g/mol |
SMILES | eMolecules & PubChem |
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Budesonide is a glucocorticoid steroid for the treatment of asthma and non-infectious rhinitis (including hay fever and other allergies), and for treatment and prevention of nasal polyposis. In addition, it is used for Crohn's disease (inflammatory bowel disease).
It is marketed by AstraZeneca as a nasal inhalant under the brand name Rhinocort (in Denmark, as Rhinosol), as an oral inhalant under the brand name Pulmicort (in Israel, Budicort), and as either an enema or a modified-release oral capsule under the brand name Entocort. It is also sold in combination with formoterol (Oxis) in a single inhaler, under the brand name Symbicort. In Brazil it is marketed by Eurofarma under the brand name Noex. Entocort EC is an oral capsule marketed in the United States by Prometheus Laboratories. Entocort is an expensive drug, costing between 800US and 1500US.
A new formulation is in clinical trials for ulcerative colitis.[1]
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Budesonide has a high first-pass metabolism.[2] It has efficacy in the terminal ileum and the right colon.
Budesonide in comparison with prednisolone has been associated with fewer bone density losses, and, unlike other corticosteroids, has little influence on the hypothalamic-pituitary-adrenal axis, which also limits the need of tapering before discontinuation. Overall, it has a lower incidence of systemic manifestations than similar medications.
Budesonide may cause:[3]
In addition, the following symptoms should be reported immediately:
Pulmicort inhalers were recalled by AstraZeneca in 2004 because there was concern that they may not always have provided the full dosage.[4]
In its Fiscal Year 2010 Work Plan, the Office of the Inspector General (OIG) of the United States Department of Health and Human Services, stated that it would be investigating whether the number of units of budesonide billed and paid for by Medicare in South Florida exceeds the amount of the drug actually distributed in the area. The OIG noted that its previous work had revealed "aberrant billing patterns" for inhaled budesonide in South Florida, and stated that it believes many of these billings may be fraudulent.[5]
Unlike OTC nasal decongestants, budesonide has not been shown to cause rebound nasal congestion.[6]
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