Budesonide

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Budesonide
Budesonide.png
Budesonide ball-and-stick.png
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.
Legal status
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
Budesonide.png
Budesonide ball-and-stick.png
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.
Legal status
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, COPD 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).

A new extended-release formulation of budesonide called "Uceris" has been recently approved by the United States FDA for ulcerative colitis.[1]

It is on the World Health Organization's List of Essential Medicines, a list of the most important medication needed in a basic health system.[2]

Medical uses[edit]

Asthma[edit]

Budesonide is nebulized for maintenance and prophylactic treatment of asthma including patients who require oral corticosteroids and those who may benefit from systemic dose reduction.[3]

Crohn's disease[edit]

Treatment of active Crohn's disease involving the ileum and/or ascending colon; maintenance of remission (for up to 3 months) of Crohn's disease (mild-to-moderate) involving the ileum and/or ascending colon.[4]

Ulcerative colitis[edit]

Budesonide assists in the induction of remission in patients with active ulcerative colitis.[5]

Side-effects[edit]

Budesonide may cause:[6]

In addition, the following symptoms should be reported immediately:

Contraindications[edit]

Budesonide is contraindicated as a primary treatment of status asthmaticus or other acute episode of asthma where intensive measures are required.[7] It is also contraindicated for patients who have hypersensitivity to budesonide.[8]

Mechanism of action[edit]

Budesonide:

Dietary considerations[edit]

Those taking tablets or capsules orally should avoid grapefruit juice and echinacea.

Also, high fat meals delay absorption but do not impede absorption.

Pharmacokinetics[edit]

International brand names[edit]

Aeronide (TH); Aquacort (DE); B Cort (CO); Bronex (PH); Budair (MY); Budecort DP (MY); Budenofalk (DE, GB, HK, KP, PH, SG); Budeson (AR); Budeson Aqua (AR); BudeSpray (TH); Budiair (KP); Budicort Respules (IL); Bunase (TH); Clebudan (CN); Cycortide (HK); Denecort (PH); Duasma (TW); Eltair (MY); Entocort (AR, AT, BE, BR, CH, CZ, DK, FI, FR, GB, HK, IE, IL, IT, KP, NL, NO, PL, PT, SE, TR); Giona Easyhaler (MY, SG, TH); Inflammide (PE); Miflonid (CZ); Miflonide (BE, DE, IL, IT, NZ, PT); Neumocort (PY); Novopulmon (DE, FR); Pulmicon Susp for Nebulizer (KP); Pulmicort (AT, BE, BG, BR, CH, CL, CN, CO, CR, CZ, DE, DK, DO, EE, FI, FR, GB, GR, GT, HN, ID, IN, NI, NL, NO, PA, PK, PL, PT, RU, SE, SV, TR, TW, UY, VE); Pulmicort Nasal Turbohaler (CL, KE, MU, NG); Pulmicort Turbuhaler (KE, MU, NG); Rafton (FR); Rhinocort (AU); Rhinocort Aqua (HK); Rhinoside (GR); Symbicort (FR, US) Uceris (US)

See also[edit]

References[edit]

  1. ^ "Uceris Approved for Active Ulcerative Colitis". empr.com. 2013-01-16. Retrieved 2013-01-16. 
  2. ^ "WHO Model List of EssentialMedicines". World Health Organization. October 2013. Retrieved 22 April 2014. 
  3. ^ Global Strategy for Asthma Management and Prevention, Global Initiative for Asthma (GINA) 2011. Available at http://www.ginasthma.org
  4. ^ Lichtenstein GR, Hanauer SB, and Sandborn WJ, “Management of Crohn's Disease in Adults,” Am J Gastroenterol, 2009, 104(2):465-83. [PubMed 19174807]
  5. ^ Habal FM and Huang VW, "Review Article: A Decision-Making Algorithm For the Management of Pregnancy in the Inflammatory Bowel Disease Patient," Aliment Pharmacol Ther, 2012, 35(5):501-15. [PubMed 22221203]
  6. ^ a b BUDESONIDE - NASAL AEROSOL INHALER (Rhinocort) side effects, medical uses, and drug interactions
  7. ^ Todd GR, Acerini CL, Buck JJ, et al, "Acute Adrenal Crisis in Asthmatics Treated With High-Dose Fluticasone Propionate," Eur Respir J, 2002, 19(6):1207-9. [PubMed 12108877]
  8. ^ Todd GR, Acerini CL, Ross-Russell R, et al, "Survey of Adrenal Crisis Associated With Inhaled Corticosteroids in the United Kingdom," Arch Dis Child, 2002, 87(6):457-61. [PubMed 12456538]

External links[edit]