Trade names Rhinocort or Neox
Pregnancy cat. B
POM ( UK) ℞ -only ( US)
Routes Oral, Nasal, tracheal, rectal
Bioavailability 10-20% (first pass effect)
Protein binding 85-90%
Half-life 2.0-3.6 hours
Excretion Renal, Faecal
A07 EA06 D07 , AC09 R01 , AD05 R03 BA02
C 25 H 34 O 6
Mol. mass 430.534 g/mol
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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 ]
nebulized for maintenance and prophylactic treatment of asthma including patients who require oral corticosteroids and those who may benefit from systemic dose reduction. [2 ]
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. [3 ]
Ulcerative colitis [ edit ]
Budesonide assists in the induction of remission in patients with active ulcerative colitis.
Contraindications [ edit ]
Budesonide is contraindicated as a primary treatment of status asthmaticus or other acute episode of asthma where intensive measures are required.
It is also contraindicated for patients who have hypersensitivity to budesonide. [5 ] [6 ]
Mechanism of action [ edit ]
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
Grapefruit juice may double absorption of oral budesonide.
Echinacea diminishes absorption.
Also, high fat meals delay absorption but don't 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.
Side-effects [ edit ]
Budesonide may cause:
nose irritation or burning
bleeding or sores in the nose
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
on rare occasions, behavioral changes — when these do occur, they seem to mostly affect children.
International brand names [ edit ]
Aeronide (TH); Aquacort (DE); B Cort (CO); Bronex (PH); Budair (MY); Budecort DP (MY); Budenofalk (DE, 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
See also [ edit ]
References [ edit ]
^ "Uceris Approved for Active Ulcerative Colitis". empr.com. 2013-01-16 . Retrieved 2013-01-16.
^ Global Strategy for Asthma Management and Prevention, Global Initiative for Asthma (GINA) 2011. Available at http://www.ginasthma.org
^ Lichtenstein GR, Hanauer SB, and Sandborn WJ, “Management of Crohn's Disease in Adults,” Am J Gastroenterol, 2009, 104(2):465-83. [PubMed 19174807]
^ 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]
^ 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]
^ 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]
^ a b BUDESONIDE - NASAL AEROSOL INHALER (Rhinocort) side effects, medical uses, and drug interactions
External links [ edit ]
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