rhinocort

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	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
ATC code	A07EA06 (WHO) D07AC09 (WHO), R01AD05 (WHO), R03BA02 (WHO)
PubChem	CID 40000
DrugBank	DB01222
ChemSpider	4444479
UNII	Q3OKS62Q6X
KEGG	D00246
ChEMBL	CHEMBL1370
Chemical data
Formula	C25H34O6
Molar mass	430.534 g/mol
	SMILES CCCC1O[C@@H]2C[C@H]3[C@@H]4CCC5=CC(=O)C=C[C@@]5([C@H]4[C@H](C[C@@]3([C@@]2(O1)C(=O)CO)C)O)C ;
	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-KWVAZRHASA- ;
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関: Budesonide

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/06/18 12:52:04」(JST)

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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 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

Asthma

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

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

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

Side-effects

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

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

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.

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

^ ^a ^b ^c ^d "Budesonide". The American Society of Health-System Pharmacists. Retrieved Dec 2, 2015.
^ ^a ^b "Budesonide eent". The American Society of Health-System Pharmacists. Retrieved Dec 2, 2015.
^ 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.
^ 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.
^ 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.
^ 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.
^ Domeij, Bengt (2000). Pharmaceutical patents in Europe. The Hague: Kluwer Law International. p. 278. ISBN 9789041113481.
^ Hamley, Peter (2015). Small Molecule Medicinal Chemistry: Strategies and Technologies. John Wiley & Sons. p. 390. ISBN 9781118771693.
^ "WHO Model List of EssentialMedicines" (PDF). World Health Organization. October 2013. Retrieved 22 April 2014.
^ ^a ^b Hamilton, Richart (2015). Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. p. 451. ISBN 9781284057560.
^ "Budesonide". International Drug Price Indicator Guide. Retrieved 5 December 2015.
^ 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]
^ Stanaland, BE (April 2004). "Once-daily budesonide aqueous nasal spray for allergic rhinitis: a review.". Clinical therapeutics 26 (4): 473–92. PMID 15189745.
^ ^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. Overview of the treatment of primary biliary cholangitis (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

Dry powder nasal drug delivery: challenges, opportunities and a study of the commercial Teijin Puvlizer Rhinocort device and formulation.

Pozzoli M1, Rogueda P2, Zhu B3, Smith T4, Young PM3, Traini D3, Sonvico F1,5.
Drug development and industrial pharmacy.Drug Dev Ind Pharm.2016 Oct;42(10):1660-8. doi: 10.3109/03639045.2016.1160110. Epub 2016 Mar 22.
PURPOSE: To discuss the challenges and opportunities for dry powder nasal medications and to put this in to perspective by evaluating and characterizing the performance of the Teijin beclomethasone dipropionate (BDP) dry powder nasal inhaler; providing a baseline for future nasal products developmen
PMID 26953090

Quality by design approach for development of suspension nasal spray products: a case study on budesonide nasal suspension.

Chudiwal SS1, Dehghan MH2.
Drug development and industrial pharmacy.Drug Dev Ind Pharm.2016 Oct;42(10):1643-52. doi: 10.3109/03639045.2016.1160108. Epub 2016 Mar 27.
The objective of this study was to provide quality by design (QbD) approach for development of suspension type nasal spray products. Quality target product profile (QTPP) of test product budesonide nasal suspension (B-NS) was defined and critical quality attributes (CQAs) were identified. Critical f
PMID 26943653

The glucocorticoid budesonide has protective and deleterious effects in experimental colitis in mice.

Ocón B1, Aranda CJ2, Gámez-Belmonte R1, Suárez MD2, Zarzuelo A1, Martínez-Augustin O2, Sánchez de Medina F3.
Biochemical pharmacology.Biochem Pharmacol.2016 Sep 15;116:73-88. doi: 10.1016/j.bcp.2016.07.010. Epub 2016 Jul 16.
Glucocorticoids are widely used for the management of inflammatory bowel disease, albeit with known limitations for long-term use and relevant adverse effects. In turn, they have harmful effects in experimental colitis. We aimed to explore the mechanism and possible implications of this phenomenon.
PMID 27431777

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

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[AHFS2015-1] "Budesonide". The American Society of Health-System Pharmacists. Retrieved Dec 2, 2015.

[AHFS2015ENT-2] "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.

[Sil2011-5] 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.

[Ric2015-10] 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, and Sandborn WJ, “Management of Crohn's Disease in Adults,” Am J Gastroenterol, 2009, 104(2):465-83. [PubMed 19174807]

[pmid25141071-14] 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 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]

[16] Stanaland, BE (April 2004). "Once-daily budesonide aqueous nasal spray for allergic rhinitis: a review.". Clinical therapeutics 26 (4): 473–92. PMID 15189745.

[emedicinehealth-17] BUDESONIDE - NASAL AEROSOL INHALER (Rhinocort) side effects, medical uses, and drug interactions

[18] 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]

[19] 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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