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 names Rhinocort or Neox
AHFS/Drugs.com monograph
MedlinePlus a608007
Pregnancy cat.
Legal status
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 YesY
ATC code A07EA06 D07AC09, R01AD05, R03BA02
PubChem CID 40000
DrugBank DB01222
ChemSpider 36566 YesY
UNII Q3OKS62Q6X YesY
KEGG D00246 YesY
ChEMBL CHEMBL1370 N
Chemical data
Formula C25H34O6 
Mol. mass 430.534 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]

  • 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.[6]

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:

  • Controls the rate of protein synthesis.
  • Depresses the migration of polymorphonuclear leukocytes and fibroblasts.
  • Reverses capillary permeability and lysosomal stabilization at the cellular level to prevent or control inflammation.
  • Has a potent glucocorticoid activity and weak mineralocorticoid activity.

Dietary considerations[edit]

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

  • Grapefruit juice may double absorption of oral budesonide.
  • Echinacea diminishes absorption.

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

Pharmacokinetics[edit]

  • Onset of action: Nebulization: 2-8 days; Inhalation: 24 hours
  • Peak effect: Nebulization: 4-6 weeks; Inhalation: 1-2 weeks
  • Distribution: 2.2-3.9 L/kg
  • Protein binding: 85% to 90%
  • Metabolism: Hepatic via CYP3A4 to two metabolites: 16 alpha-hydroxyprednisolone and 6 beta-hydroxybudesonide; minor activity
  • Bioavailability: Limited by high first-pass effect; Capsule: 9% to 21%; Nebulization: 6%; Inhalation: 6% to 13%
  • Half-life elimination: 2-3.6 hours
  • Time to peak: Capsule: 0.5-10 hours (variable in Crohn's disease); Nebulization: 10-30 minutes; Inhalation: 1-2 hours; Tablet: 7.4-19.2 hours
  • Excretion: Urine (60%) and feces as metabolites.

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 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]