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
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	100% (but large 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)
Routes	Oral, Nasal, tracheal, rectal
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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.

[edit] 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.

[edit] 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.

[edit] Recall

Pulmicort inhalers were recalled in 2002 because there was concern that they may not always have provided the full dosage.^{[citation needed]}

[edit] Misuse or Abuse

In its Fiscal Year 2010 Work Plan, the Office of Inspector General (OIG) of the U.S. 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. OIG FY10 Work Plan (p. 26).

[edit] References

1. ^ BUDESONIDE - NASAL AEROSOL INHALER (Rhinocort) side effects, medical uses, and drug interactions

[edit] External links

• Budesonide Pharmacokinetics - PubPK.org
• FDA Label (PDF)
• National Institute of Health's Medline about Budesonide