Budesonide

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Budesonide
Systematic (IUPAC) name
16,17-(butylidenebis(oxy))-11,21-dihydroxy-, (11-β,16-α)-pregna-1,4-diene-3,20-dione
Clinical data
Trade namesRhinocort or Neox
AHFS/Drugs.commonograph
MedlinePlusa608007
Pregnancy cat.B (US)
Legal statusPOM (UK) -only (US)
RoutesOral, Nasal, tracheal, rectal
Pharmacokinetic data
Bioavailability10-20% (first pass effect)
Protein binding85-90%
MetabolismHepatic CYP3A4
Half-life2.0-3.6 hours
ExcretionRenal, Faecal
Identifiers
CAS number51333-22-3 YesY
ATC codeA07EA06 D07AC09, R01AD05, R03BA02
PubChemCID 40000
DrugBankDB01222
ChemSpider36566 YesY
UNIIQ3OKS62Q6X YesY
KEGGD00246 YesY
ChEMBLCHEMBL1370 N
Chemical data
FormulaC25H34O6 
Mol. mass430.534 g/mol
 N (what is this?)  (verify)
 
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Budesonide
Systematic (IUPAC) name
16,17-(butylidenebis(oxy))-11,21-dihydroxy-, (11-β,16-α)-pregna-1,4-diene-3,20-dione
Clinical data
Trade namesRhinocort or Neox
AHFS/Drugs.commonograph
MedlinePlusa608007
Pregnancy cat.B (US)
Legal statusPOM (UK) -only (US)
RoutesOral, Nasal, tracheal, rectal
Pharmacokinetic data
Bioavailability10-20% (first pass effect)
Protein binding85-90%
MetabolismHepatic CYP3A4
Half-life2.0-3.6 hours
ExcretionRenal, Faecal
Identifiers
CAS number51333-22-3 YesY
ATC codeA07EA06 D07AC09, R01AD05, R03BA02
PubChemCID 40000
DrugBankDB01222
ChemSpider36566 YesY
UNIIQ3OKS62Q6X YesY
KEGGD00246 YesY
ChEMBLCHEMBL1370 N
Chemical data
FormulaC25H34O6 
Mol. mass430.534 g/mol
 N (what is this?)  (verify)

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.

A new formulation is in clinical trials for ulcerative colitis.[1]

Contents

Pharmacology

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.[citation needed] Overall, it has a lower incidence of systemic manifestations than similar medications.

Side-effects

Budesonide may cause:[3]

In addition, the following symptoms should be reported immediately:

It was reported in an online news story article posted on Monday, September 3, 2012, by Maggie Fox, on the NBCNEWS.com Vitals blog, that the drug was found by researchers to potentially cause a permanent small decrease in height in certain children taking the medication. The study, presented at a respiratory conference in Vienna, Austria, and appearing in the New England Journal of Medicine, also took into account results from a previous major study showing the same phenomenon, but it was not known then to be permanent. For more information, please see the article.[4]

Misuse

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]

See also

References

External links