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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
Identifiers
CAS number 51333-22-3
ATC code A07EA06 D07AC09, R01AD05, R03BA02
PubChem 40000
DrugBank APRD00442
ChemSpider 36566
Chemical data
Formula C25H34O6 
Mol. mass 430.534 g/mol
SMILES eMolecules & PubChem
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
Therapeutic considerations
Pregnancy cat. C(US)
Legal status POM (UK) -only (US)
Routes Oral, Nasal, tracheal, rectal
 Yes check.svgY(what is this?)  (verify)

Budesonide is a glucocorticoid steroid for the treatment of asthma, non-infectious rhinitis (including hay fever and other allergies), and for treatment and prevention of nasal polyposis. Additionally, 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's marketed by Eurofarma under the brand name Noex. Entocort EC is an oral capsule marketed in the United States by Prometheus Laboratories.

Contents

Pharmacology

Budesonide has a high first-pass metabolism. 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.

Side Effects

Budesonide may cause:[1]

  • nose irritation or burning
  • bleeding or sores in the nose
  • lightheadedness
  • upset stomach
  • cough
  • hoarseness
  • dry mouth
  • rash
  • sore throat
  • bad taste in mouth
  • change in mucus color

In addition the following symptoms should be reported immediately:

  • difficulty breathing or swelling of the face
  • white patches in the throat, mouth, or nose
  • irregular menstrual periods
  • severe acne
  • rarely, behavioral changes—when these do occur, they seem to mostly affect children. For citation, see reference above.

Recall

Pulmicort inhalers were recalled by AstraZeneca in 2004 because there was concern that they may not always have provided the full dosage.[2]

Misuse or Abuse

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.[3]

Unlike OTC nasal decongestants, budesonide has not been shown to cause rebound nasal congestion.[4]

References

External links








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