Budesonide

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 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 Y
ATC code	A07EA06 D07AC09, R01AD05, R03BA02
PubChem	CID 40000
DrugBank	APRD00442
ChemSpider	36566 Y
UNII	Q3OKS62Q6X Y
KEGG	D00246 Y
ChEMBL	CHEMBL1370 N
Chemical data
Formula	C25H34O6
Mol. mass	430.534 g/mol
SMILES	eMolecules & PubChem
InChI InChI=1S/C25H34O6/c1-4-5-21-30-20-11-17-16-7-6-14-10-15(27)8-9-23(14,2)22(16)18(28)12-24(17,3)25(20,31-21)19(29)13-26/h8-10,16-18,20-22,26,28H,4-7,11-13H2,1-3H3/t16-,17-,18-,20+,21+,22+,23-,24-,25+/m0/s1 Y Key:VOVIALXJUBGFJZ-VXKMTNQYSA-N Y
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. Entocort is an expensive drug, costing between 800US and 1500US.

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

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]

• 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
• muscle cramps

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
• on rare occasions, 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.^[4]

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.^[5]

Unlike OTC nasal decongestants, budesonide has not been shown to cause rebound nasal congestion.^[6]

See also

• Fluticasone propionate
• Azelastine

References

1. ^ http://www.genengnews.com/gen-news-highlights/positive-phase-iii-data-mean-cosmo-and-santarus-plan-2011-nda-for-ulcerative-colitis-drug/81244010/
2. ^ http://www.pharmgkb.org/do/serve?objId=PA448681
3. ^ BUDESONIDE - NASAL AEROSOL INHALER (Rhinocort) side effects, medical uses, and drug interactions
4. ^ AstraZeneca Pulmicort recall
5. ^ OIG FY10 Work Plan Office of the Inspector General (p. 26).
6. ^ http://www.drugs.com/rhinocort.html

External links

• Budesonide Pharmacokinetics - PubPK.org
• Entocort EC Prescribing information Prometheus Laboratories (PDF)
• Budesonide Oral (Entocort EC) MedlinePlus, National Institutes of Health (NIH), U.S. National Library of Medicine
• Budesonide Nasal Spray (Rhinocort) MedlinePlus, National Institutes of Health (NIH), U.S. National Library of Medicine
• Budesonide Oral Inhalation (Symbicort) MedlinePlus, National Institutes of Health (NIH), U.S. National Library of Medicine