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 Pulmicort, Rhinocort, other
AHFS/Drugs.com Monograph
MedlinePlus a608007
Pregnancy
category
  • US: B (No risk in non-human studies)
Routes of
administration
Oral, nasal, tracheal, rectal
Legal status
Legal status
  • UK: POM (Prescription only)
  • US: Over the counter and Rx
Pharmacokinetic data
Bioavailability 10-20% (first pass effect)
Protein binding 85-90%
Metabolism Hepatic CYP3A4
Biological half-life 2.0-3.6 hours
Excretion Renal, faecal
Identifiers
CAS Number 51333-22-3 YesY
ATC code A07EA06 (WHO) D07AC09 (WHO), R01AD05 (WHO), R03BA02 (WHO)
PubChem CID 40000
DrugBank DB01222 YesY
ChemSpider 4444479 N
UNII Q3OKS62Q6X YesY
KEGG D00246 YesY
ChEMBL CHEMBL1370 N
Chemical data
Formula C25H34O6
Molar mass 430.534 g/mol
 NYesY (what is this?)  (verify)

Budesonide (BUD), sold under the brand name Pulmicort among others, is a steroid medication.[1] It is available as an inhaler, pill, and nasal spray.[1][2] The inhaled form is used in the long term management of asthma and chronic obstructive pulmonary disease (COPD).[1][3] The nasal spray is used for allergic rhinitis and nasal polyps.[2][4] The pills in a delayed release form may be used for inflammatory bowel disease including Crohn's disease, ulcerative colitis and microscopic colitis.[5][6]

Common side effects with the inhaled form include respiratory infections, cough, and headaches. Common side effects with the pills include feeling tired, vomiting, and joint pains. Serious side effects include an increased risk of infection, loss of bone strength, and cataracts. Long term use of the pill form may cause adrenal insufficiency. Stopping the pills suddenly following long term use may therefore be dangerous. The inhaled form is generally safe in pregnancy. Budesonide is mainly a glucocorticoid.[1]

Budesonide was initially patented in 1973.[7] Commercial use as an asthma medication began in 1981.[8] It is on the World Health Organization's List of Essential Medicines, the most important medication needed in a basic health system.[9] Some forms are available as a generic medication.[10] The wholesale price in the developing world for an inhaler containing 200 doses is about 5 to 7 USD as of 2014.[11] As of 2015 the cost for a typical month of medication in the United States is 100 to 200 USD.[10]

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 a systemic dose reduction.[12]

Inflammatory bowel disease[edit]

Formulations of delayed-release Budesonide can be effective treatment for mild-to-moderately active Crohn's disease involving the ileum and/or ascending colon.[13] A Cochrane review found evidence for up to 3 months (but not longer) of maintenance of remission Crohn's disease.[14]

Budesonide assists in the induction of remission in people with active ulcerative colitis.[15]

Allergic rhinitis[edit]

Nasal spray budesonide is a treatment for allergic rhinitis.[16]

Side-effects[edit]

Budesonide may cause:[17]

  • 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

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 (mostly affecting children)[17]

Contraindications[edit]

Budesonide is contraindicated as a primary treatment of status asthmaticus or other acute episode of asthma where intensive measures are required.[18] It is also contraindicated for patients who have hypersensitivity to budesonide.[19]

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.

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.

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, ZA); 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. ^ a b c d "Budesonide". The American Society of Health-System Pharmacists. Retrieved Dec 2, 2015. 
  2. ^ a b "Budesonide eent". The American Society of Health-System Pharmacists. Retrieved Dec 2, 2015. 
  3. ^ De Coster, DA; Jones, M (2014). "Tailoring of corticosteroids in COPD management.". Current respiratory care reports. 3: 121–132. doi:10.1007/s13665-014-0084-2. PMID 25089228. 
  4. ^ Rudmik, L; Schlosser, RJ; Smith, TL; Soler, ZM (July 2012). "Impact of topical nasal steroid therapy on symptoms of nasal polyposis: a meta-analysis.". The Laryngoscope. 122 (7): 1431–7. doi:10.1002/lary.23259. PMID 22410935. 
  5. ^ Silverman J, Otley A (2011). "Budesonide in the treatment of inflammatory bowel disease.". Expert Rev Clin Immunol. 7 (4): 419–28. doi:10.1586/eci.11.34. PMID 21790284. 
  6. ^ Pardi DS, Tremaine WJ, Carrasco-Labra A (2016). "American Gastroenterological Association Institute Technical Review on the Medical Management of Microscopic Colitis". Gastroenterology. 150 (1): 247–274.e11. doi:10.1053/j.gastro.2015.11.006. PMID 26584602. 
  7. ^ Domeij, Bengt (2000). Pharmaceutical patents in Europe. The Hague: Kluwer Law International. p. 278. ISBN 9789041113481. 
  8. ^ Hamley, Peter (2015). Small Molecule Medicinal Chemistry: Strategies and Technologies. John Wiley & Sons. p. 390. ISBN 9781118771693. 
  9. ^ "WHO Model List of EssentialMedicines" (PDF). World Health Organization. October 2013. Retrieved 22 April 2014. 
  10. ^ a b Hamilton, Richart (2015). Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. p. 451. ISBN 9781284057560. 
  11. ^ "Budesonide". International Drug Price Indicator Guide. Retrieved 5 December 2015. 
  12. ^ Global Strategy for Asthma Management and Prevention, Global Initiative for Asthma (GINA) 2011. Available at http://www.ginasthma.org
  13. ^ Lichtenstein GR, Hanauer SB, Sandborn WJ (2009). "Management of Crohn's Disease in Adults". Am J Gastroenterol. 104 (2): 465–83. doi:10.1038/ajg.2008.168. PMID 19174807. 
  14. ^ Kuenzig ME, Rezaie A, Seow CH, Otley AR, Steinhart AH, Griffiths AM, et al. (2014). "Budesonide for maintenance of remission in Crohn's disease.". Cochrane Database Syst Rev. 8: CD002913. doi:10.1002/14651858.CD002913.pub3. PMID 25141071. 
  15. ^ Habal FM, Huang VW (2012). "Review Article: A Decision-Making Algorithm For the Management of Pregnancy in the Inflammatory Bowel Disease Patient". Aliment Pharmacol Ther. 35 (5): 501–15. doi:10.1111/j.1365-2036.2011.04967.x. PMID 22221203. 
  16. ^ Stanaland, BE (April 2004). "Once-daily budesonide aqueous nasal spray for allergic rhinitis: a review.". Clinical therapeutics. 26 (4): 473–92. doi:10.1016/s0149-2918(04)90050-1. PMID 15189745. 
  17. ^ a b BUDESONIDE - NASAL AEROSOL INHALER (Rhinocort) side effects, medical uses, and drug interactions
  18. ^ Todd GR, Acerini CL, Buck JJ, Murphy NP, Ross-Russell R, Warner JT, McCance DR (2002). "Acute Adrenal Crisis in Asthmatics Treated With High-Dose Fluticasone Propionate". Eur Respir J. 19 (6): 1207–9. doi:10.1183/09031936.02.00274402. PMID 12108877. 
  19. ^ Todd GR, Acerini CL, Ross-Russell R, Zahra S, Warner JT, McCance D (2002). "Survey of Adrenal Crisis Associated With Inhaled Corticosteroids in the United Kingdom". Arch Dis Child. 87 (6): 457–61. doi:10.1136/adc.87.6.457. PMC 1755820free to read. PMID 12456538. 

External links[edit]