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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/07/09 20:36:14」(JST)

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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]

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

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

Budesonide assists in the induction of remission in patients with active ulcerative colitis.^[5]

Side-effects

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 (mostly affecting children)^[6]

Contraindications

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

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); 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

^ "Uceris Approved for Active Ulcerative Colitis". empr.com. 2013-01-16. Retrieved 2013-01-16.
^ "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]
^ 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. クローン病治療におけるブデソニド budesonide in the treatment of crohn disease
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

Evaluation of an in vitro faecal degradation method for early assessment of the impact of colonic degradation on colonic absorption in humans.

Tannergren C1, Borde A2, Boreström C1, Abrahamsson B1, Lindahl A1.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.Eur J Pharm Sci.2014 Jun 16;57:200-6. doi: 10.1016/j.ejps.2013.10.001. Epub 2013 Oct 24.
The objective of this study was to develop and evaluate an in vitro method to investigate bacterial-mediated luminal degradation of drugs in colon in humans. This would be a valuable tool for the assessment of drug candidates during early drug development, especially for compounds intended to be dev
PMID 24514453
PMID 24685705
PMID 24487458

Japanese Journal

リノコートパウダースプレー鼻用25μg : 粘膜付着性をもったドライパウダー鼻噴霧用ステロイド薬

阪野典子
Drug delivery system 25(6), 617-621, 2010-11-25
NAID 10027642968

舌に限局性に生じた増殖性天疱瘡の1例

小田島潤一,瀬川清,関克典,中山温史,降旗球司,武田泰典
日本口腔外科学会雑誌 46(4), 226-228, 2000-04-20
… Spray steroid (Rhinocort<SUP>®</SUP>) therapy of the affected site was initiated (150μg/day), and 7 months later there was considerable improvement of the tongue. …
NAID 10006381628

Effect of pre-seasonal and seasonal treatment with budesonide topical nasal powder in patients with seasonal allergic rhinitis

, , , ,
Allergology International 45(3), 151-157, 1996
… The efficacy and safety of budesonide nasal powder (Rhinocort Turbuhaler®) in seasonal allergic rhinitis when given only at the onset of symptoms during the pollen season or when also given before the pollen season, were compared. …
NAID 130004476632

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★リンクテーブル★

リンク元	「ブデソニド」
関連記事	「rhinocort」

「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

「rhinocort」

　　[★]

同: Rhinocort
関: Budesonide

[1] "Uceris Approved for Active Ulcerative Colitis". empr.com. 2013-01-16. Retrieved 2013-01-16.

[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]

[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]

[emedicinehealth-6] 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]

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Rhinocort