出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/10/22 00:49:46」(JST)[Wiki en表示]
|Systematic (IUPAC) name|
|Trade names||Rhinocort or Neox|
|Oral, nasal, tracheal, rectal|
|Bioavailability||10-20% (first pass effect)|
|Biological half-life||2.0-3.6 hours|
|CAS Registry Number||Y|
|ATC code||A07D07 , R01 , R03|
|Molecular mass||430.534 g/mol|
|N (what is this?)|
Budesonide is a glucocorticoid steroid used in inhaled formulations for the treatment of asthma, COPD and non-infectious rhinitis (including hay fever and other allergies), and for treatment and prevention of nasal polyposis. It is also used in a delayed-release oral formulations for inflammatory bowel disease including Crohn's disease and ulcerative colitis.
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.
- 1 Medical uses
- 1.1 Asthma
- 1.2 Crohn's disease
- 1.3 Ulcerative colitis
- 2 Side-effects
- 3 Contraindications
- 4 Mechanism of action
- 5 Dietary considerations
- 6 Pharmacokinetics
- 7 International brand names
- 8 See also
- 9 References
- 10 External links
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.
Formulations of delayed-release Budesonide can be effective treatment for mild-to-moderately active Crohn's disease involving the ileum and/or ascending colon. A Cochrane review found evidence for up to 3 months (but not longer) of maintenance of remission Crohn's disease.
Budesonide assists in the induction of remission in patients with active ulcerative colitis.
Budesonide may cause:
- Nose irritation or burning
- Bleeding or sores in the nose
- Upset stomach
- Dry mouth
- 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 (mostly affecting children)
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.
Mechanism of action
- 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.
Those taking tablets or capsules orally should avoid grapefruit juice and echinacea.
- Grapefruit juice may double bioavailability of oral budesonide.
- Echinacea diminishes bioavailability.
Also, high fat meals delay absorption but do not impede absorption.
- 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
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)
- Fluticasone propionate
- 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.
- "WHO Model List of EssentialMedicines" (PDF). World Health Organization. October 2013. Retrieved 22 April 2014.
- 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]
- 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.
- 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]
- BUDESONIDE - NASAL AEROSOL INHALER (Rhinocort) side effects, medical uses, and drug interactions
- 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]
- 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
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- 1. Budesonide in the treatment of inflammatory bowel disease in adults
- 2. 原発性胆汁性肝硬変の治療の概要 overview of the treatment of primary biliary cirrhosis
- 3. 小児および思春期におけるクローン病マネージメントの概要 overview of the management of crohn disease in children and adolescents
- 4. 好酸球性食道炎の治療 treatment of eosinophilic esophagitis
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- Liu YH1, Wu SZ1, Wang G2, Huang NW1, Liu CT1.
- Molecular medicine reports.Mol Med Rep.2015 Jun;11(6):4121-8. doi: 10.3892/mmr.2015.3307. Epub 2015 Feb 5.
- The persistent administration of β2‑adrenergic (β2AR) agonists has been demonstrated to increase the risk of severe asthma, partly due to the induction of tolerance to bronchoprotection via undefined mechanisms. The present study investigated the potential effect of the long‑acting β2‑adren
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- Formulation and characterization of ORMOSIL particles loaded with budesonide for local colonic delivery.
- Petrovska-Jovanovska V1, Geskovski N2, Crcarevska MS2, Memed O1, Petruševski G3, Chachorovska M3, Petrusevska M4, Poceva-Panovska A5, Mladenovska K2, Ugarkovic S3, Glavas-Dodov M6.
- International journal of pharmaceutics.Int J Pharm.2015 Apr 30;484(1-2):75-84. doi: 10.1016/j.ijpharm.2015.02.044. Epub 2015 Feb 20.
- In this study, hybrid silica xerogel particles were developed as carriers of budesonide (BDS) for efficient local treatment of inflammatory bowel diseases (IBD). Organically modified silica particles (ORMOSILs) were prepared by co-condensation of 3-aminopropyltriethoxysilane (APTES) and tetraethyl o
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- Diagnosis and pharmacotherapy of stable chronic obstructive pulmonary disease: the finnish guidelines.
- Kankaanranta H1, Harju T, Kilpeläinen M, Mazur W, Lehto JT, Katajisto M, Peisa T, Meinander T, Lehtimäki L.
- Basic & clinical pharmacology & toxicology.Basic Clin Pharmacol Toxicol.2015 Apr;116(4):291-307. doi: 10.1111/bcpt.12366. Epub 2015 Jan 22.
- The Finnish Medical Society Duodecim initiated and managed the update of the Finnish national guideline for chronic obstructive pulmonary disease (COPD). The Finnish COPD guideline was revised to acknowledge the progress in diagnosis and management of COPD. This Finnish COPD guideline in English lan
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