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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)

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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.^[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

Asthma

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

Formulations of delayed-release Budesonide can be effective treatment for mild-to-moderately active Crohn's disease involving the ileum and/or ascending colon.^[4] A Cochrane review found evidence for up to 3 months (but not longer) of maintenance of remission Crohn's disease.^[5]

Ulcerative colitis

Budesonide assists in the induction of remission in patients with active ulcerative colitis.^[6]

Side-effects

Budesonide may cause:^[7]

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 (mostly affecting children)^[7]

Contraindications

Budesonide is contraindicated as a primary treatment of status asthmaticus or other acute episode of asthma where intensive measures are required.^[8] It is also contraindicated for patients who have hypersensitivity to budesonide.^[9]

Mechanism of action

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

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.

Pharmacokinetics

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)

References

^ 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]
^ ^a ^b 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]

External links

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

UpToDate Contents

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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
5. クループ：薬剤および補助治療 croup pharmacologic and supportive interventions

English Journal

A long-acting β2-adrenergic agonist increases the expression of muscarine cholinergic subtype‑3 receptors by activating the β2-adrenoceptor cyclic adenosine monophosphate signaling pathway in airway smooth muscle cells.

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
PMID 25672589

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
PMID 25708004

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
PMID 25515181

Japanese Journal

研究・症例喘息コントロールに対するSMART療法の検討

日本胸部臨床 = The Japanese journal of chest diseases 75(12), 1405-1412, 2016-12
NAID 40021019945

咳喘息におけるブデソニド/ホルモテロール配合剤と吸入ステロイド薬の治療効果の比較

アレルギー・免疫 23(2), 278-285, 2016-02
NAID 40020715971

Caregiver treatment satisfaction is improved together with children's asthma control: Prospective study for budesonide monotherapy in school-aged children with uncontrolled asthma symptoms

Allergology International 64(4), 371-376, 2015
NAID 130005290320

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★リンクテーブル★

リンク元

「ブデソニド」

Budesonide
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; category	US: B (No risk in non-human studies);
Legal status	UK: Prescription-only (POM); US: ℞-only;
Routes of; administration	Oral, nasal, tracheal, rectal
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 Registry Number	51333-22-3
ATC code	A07EA06 D07AC09, R01AD05, R03BA02
PubChem	CID: 40000
DrugBank	DB01222
ChemSpider	36566
UNII	Q3OKS62Q6X
KEGG	D00246
ChEMBL	CHEMBL1370
Chemical data
Formula	C25H34O6
Molecular mass	430.534 g/mol
	SMILES O=C(CO)[C@]25O[C@@H](O[C@@H]5C[C@H]1[C@H]4[C@H]([C@@H](O)C[C@@]12C)[C@]/3(/C=C\C(=O)\C=C\3CC4)C)CCC ;
	InChI InChI=1S/C25H34O6/c1-4-5-21-30-20-11-17-16-7-6-14-10-15(27)8-9-23(14,2)22(16)18(28)12-24(17,3)25(20,31-21)19(29)13-26/h8-10,16-18,20-22,26,28H,4-7,11-13H2,1-3H3/t16-,17-,18-,20+,21+,22+,23-,24-,25+/m0/s1 ; Key:VOVIALXJUBGFJZ-VXKMTNQYSA-N ;
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　　[★]

英: budesonide
商: シムビコート、パルミコート、ブデソン、Rhinocort

[pmid21790284-1] 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.

[2] "WHO Model List of EssentialMedicines" (PDF). 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]

[pmid25141071-5] 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.

[6] 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]

[emedicinehealth-7] BUDESONIDE - NASAL AEROSOL INHALER (Rhinocort) side effects, medical uses, and drug interactions

[8] 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]

[9] 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]

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budesonide