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词条 Budesonide
释义

  1. Medical uses

     Asthma  Inflammatory bowel disease  Allergic rhinitis  Eosinophilic esophagitis 

  2. Side effects

  3. Contraindications

  4. Interactions

  5. Pharmacology

  6. Pharmacokinetics

  7. Chemistry

     Stereoisomerism 

  8. Society and culture

     Brand names 

  9. See also

  10. References

  11. External links

{{Drugbox
| Verifiedfields = changed
| Watchedfields = changed
| verifiedrevid = 459985202
| IUPAC_name = 11β,21-Dihydroxy-16α,17α-[butane-1,1-diylbis(oxy)]pregna-1,4-diene-3,20-dione
| image = Budesonid Grundstruktur V4.svg
| width = 250
| image2 = Budesonide ball-and-stick.png
| width2 = 250
| tradename = Pulmicort, Rhinocort, Entocort, others
| Drugs.com = {{drugs.com|monograph|budesonide}}
| MedlinePlus = a608007
| pregnancy_AU =
| pregnancy_US = B
| pregnancy_category =
| licence_EU = yes
| legal_AU = S2
| legal_CA = Rx-only
| legal_UK = POM
| legal_US = OTC
| legal_US_comment = and Rx-only
| routes_of_administration = By mouth, nasal, tracheal, rectal
| bioavailability = 10-20% (first pass effect)
| protein_bound = 85-90%
| metabolism = Hepatic CYP3A4
| elimination_half-life = 2.0-3.6 hours
| excretion = Urine, feces
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 51333-22-3
| ATC_prefix = A07
| ATC_suffix = EA06
| ATC_supplemental = {{ATC|D07|AC09}}, {{ATC|R01|AD05}}, {{ATC|R03|BA02}}
| PubChem = 40000
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank = DB01222
| ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}}
| ChemSpiderID = 4444479
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = Q3OKS62Q6X
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D00246
| ChEMBL_Ref = {{ebicite|changed|EBI}}
| ChEMBL = 1370
| PDB_ligand = 8W5
| C=25 | H=34 | O=6
| molecular_weight = 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
| StdInChI_Ref = {{stdinchicite|changed|chemspider}}
| StdInChI = 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
| StdInChIKey_Ref = {{stdinchicite|changed|chemspider}}
| StdInChIKey = VOVIALXJUBGFJZ-KWVAZRHASA
| synonyms =
}}Budesonide (BUD), sold under the brand name Pulmicort among others, is a medication of the corticosteroid type.[1] It is available as an inhaler, pill, nasal spray, and rectal forms.[1][2] The inhaled form is used in the long-term management of asthma and chronic obstructive pulmonary disease (COPD).[1][3][4] The nasal spray is used for allergic rhinitis and nasal polyps.[2][5] The pills in a delayed release form and rectal forms may be used for inflammatory bowel disease including Crohn's disease, ulcerative colitis and microscopic colitis.[6][7][8]

Common side effects with the inhaled form include respiratory infections, cough, and headaches.[1] Common side effects with the pills include feeling tired, vomiting, and joint pains.[1] Serious side effects include an increased risk of infection, loss of bone strength, and cataracts.[1] Long-term use of the pill form may cause adrenal insufficiency.[1] Stopping the pills suddenly following long-term use may therefore be dangerous.[1] The inhaled form is generally safe in pregnancy.[1] Budesonide is mainly acting as a glucocorticoid.[1]

Budesonide was initially patented in 1973.[9] Commercial use as an asthma medication began in 1981.[10] It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.[11] Some forms are available as a generic medication.[12] The wholesale price in the developing world for an inhaler containing 200 doses is about US$5 to US$7 as of 2014.[13] As of 2015 the cost for a typical month of the inhaler medication in the United States is US$100 to US$200.[14] In 2016 it was the 207th most prescribed medication in the United States with more than 2 million prescriptions.[15]

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.[16]

Inflammatory bowel disease

Formulations of delayed-release Budesonide are an effective treatment for mild-to-moderately active Crohn's disease involving the ileum and/or ascending colon.[17] A Cochrane review found evidence for up to 3 months (but not longer) of maintenance of remission Crohn's disease.[18]

Budesonide assists in the induction of remission in people with active ulcerative colitis.[19]

Budesonide is highly effective and recommended as the drug of choice in microscopic colitis, for induction and maintenance of remission, and for both the lymphocytic colitis and collagenous colitis forms.[20]

Allergic rhinitis

Nasal spray budesonide is a treatment for allergic rhinitis.[21]

Eosinophilic esophagitis

Topical budesonide has considerable effects in eosinophilic esophagitis.[22]

Side effects

Budesonide may cause:[23]

  • 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
  • Blurred vision [24]

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)[23]

Contraindications

Budesonide is contraindicated as a primary treatment of status asthmaticus or other acute episode of asthma where intensive measures are required.[25] It is also contraindicated for patients who have hypersensitivity to budesonide.[26]

Interactions

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.{{cn|date=April 2019}}

Pharmacology

Budesonide is an agonist of glucocorticoid receptors. Among its effects are:

  • 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.{{cn|date=April 2019}}

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.{{cn|date=April 2019}}

Chemistry

{{See also|List of corticosteroids|List of corticosteroid cyclic ketals}}

Budesonide, also known as 11β,21-dihydroxy-16α,17α-(butylidenebis(oxy))pregna-1,4-diene-3,20-dione, is a synthetic pregnane steroid and non-halogenated cyclic ketal corticosteroid.[27][28] It is the C16α hydroxyl, C16α,17α cyclic ketal with butyraldehyde derivative of prednisolone (11β,17α,21-trihydroxypregna-1,4-diene-3,20-dione).[27][28]

Stereoisomerism

Budesonide
(2 stereoisomers)

(22R)-configuration
(22S)-configuration

Society and culture

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); Budinide (KSA); 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, ZA) Uceris (US)

See also

  • Azelastine
  • Fluticasone propionate

References

1. ^1 2 3 4 5 6 7 8 9 {{cite web|title=Budesonide|url=https://www.drugs.com/monograph/budesonide.html|publisher=The American Society of Health-System Pharmacists|accessdate=Dec 2, 2015|deadurl=no|archiveurl=https://web.archive.org/web/20151128150235/http://www.drugs.com/monograph/budesonide.html|archivedate=2015-11-28|df=}}
2. ^1 {{cite web|title=Budesonide eent|url=https://www.drugs.com/monograph/budesonide-eent.html|publisher=The American Society of Health-System Pharmacists|accessdate=Dec 2, 2015|deadurl=no|archiveurl=https://web.archive.org/web/20151208195318/http://www.drugs.com/monograph/budesonide-eent.html|archivedate=2015-12-08|df=}}
3. ^{{cite journal|last1=De Coster|first1=DA|last2=Jones|first2=M|title=Tailoring of corticosteroids in COPD management.|journal=Current Respiratory Care Reports|date=2014|volume=3|issue=3|pages=121–132|pmid=25089228|doi=10.1007/s13665-014-0084-2|pmc=4113685}}
4. ^{{cite journal|last1=Christophi|first1=GP|last2=Rengarajan|first2=A|last3=Ciorba|first3=MA|title=Rectal budesonide and mesalamine formulations in active ulcerative proctosigmoiditis: efficacy, tolerance, and treatment approach.|journal=Clinical and Experimental Gastroenterology|date=2016|volume=9|pages=125–30|pmid=27274301|doi=10.2147/CEG.S80237|pmc=4876845}}
5. ^{{cite journal|last1=Rudmik|first1=L|last2=Schlosser|first2=RJ|last3=Smith|first3=TL|last4=Soler|first4=ZM|title=Impact of topical nasal steroid therapy on symptoms of nasal polyposis: a meta-analysis.|journal=The Laryngoscope|date=July 2012|volume=122|issue=7|pages=1431–7|pmid=22410935|doi=10.1002/lary.23259}}
6. ^{{cite journal|vauthors=Silverman J, Otley A | title=Budesonide in the treatment of inflammatory bowel disease. | journal=Expert Rev Clin Immunol | year= 2011 | volume= 7 | issue= 4 | pages= 419–28 | pmid=21790284 | doi=10.1586/eci.11.34 | pmc= }}
7. ^{{cite journal |vauthors=Pardi DS, Tremaine WJ, Carrasco-Labra A |title=American Gastroenterological Association Institute Technical Review on the Medical Management of Microscopic Colitis |journal=Gastroenterology |volume=150 |issue=1 |pages=247–274.e11 |year=2016 |pmid=26584602 |doi=10.1053/j.gastro.2015.11.006 |url=}}
8. ^{{cite book|title=British national formulary : BNF 58|date=2009|publisher=British Medical Association|isbn=9780857111562|pages=56–57|edition=58}}
9. ^{{cite book|last1=Domeij|first1=Bengt|title=Pharmaceutical patents in Europe|date=2000|publisher=Kluwer Law International|location=The Hague|isbn=9789041113481|page=278|url=https://books.google.ca/books?id=KZfvZN2WfjcC&pg=PA278|deadurl=no|archiveurl=https://web.archive.org/web/20151208072850/https://books.google.ca/books?id=KZfvZN2WfjcC&pg=PA278|archivedate=2015-12-08|df=}}
10. ^{{cite book|last1=Hamley|first1=Peter|title=Small Molecule Medicinal Chemistry: Strategies and Technologies|date=2015|publisher=John Wiley & Sons|isbn=9781118771693|page=390|url=https://books.google.ca/books?id=LOudCgAAQBAJ&pg=PA390|deadurl=no|archiveurl=https://web.archive.org/web/20151208062120/https://books.google.ca/books?id=LOudCgAAQBAJ&pg=PA390|archivedate=2015-12-08|df=}}
11. ^{{cite web|title=WHO Model List of Essential Medicines (19th List)|url=http://www.who.int/medicines/publications/essentialmedicines/EML_2015_FINAL_amended_NOV2015.pdf?ua=1|work=World Health Organization|accessdate=8 December 2016|date=April 2015|deadurl=no|archiveurl=https://web.archive.org/web/20161213052708/http://www.who.int/medicines/publications/essentialmedicines/EML_2015_FINAL_amended_NOV2015.pdf?ua=1|archivedate=13 December 2016|df=}}
12. ^{{cite book|last1=Hamilton|first1=Richart|title=Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition|date=2015|publisher=Jones & Bartlett Learning|isbn=9781284057560|page=451}}
13. ^{{cite web|title=Budesonide|url=http://mshpriceguide.org/en/single-drug-information/?DMFId=1406&searchYear=2014|website=International Drug Price Indicator Guide|accessdate=5 December 2015}}
14. ^{{cite book|last1=Hamilton|first1=Richart|title=Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition|date=2015|publisher=Jones & Bartlett Learning|isbn=9781284057560|page=451}}
15. ^{{cite web |title=The Top 300 of 2019 |url=https://clincalc.com/DrugStats/Top300Drugs.aspx |website=clincalc.com |accessdate=22 December 2018}}
16. ^Global Strategy for Asthma Management and Prevention, Global Initiative for Asthma (GINA) 2011. Available at http://www.ginasthma.org {{webarchive|url=https://web.archive.org/web/20131014032230/http://www.ginasthma.org/ |date=2013-10-14 }}
17. ^{{cite journal | vauthors = Lichtenstein GR, Hanauer SB, Sandborn WJ | year = 2009 | title = Management of Crohn's Disease in Adults | url = | journal = Am J Gastroenterol | volume = 104 | issue = 2| pages = 465–83 | pmid = 19174807 | doi=10.1038/ajg.2008.168}}
18. ^{{cite journal | vauthors=Kuenzig ME, Rezaie A, Seow CH, Otley AR, Steinhart AH, Griffiths AM, etal | title=Budesonide for maintenance of remission in Crohn's disease. | journal=Cochrane Database Syst Rev | year=2014 | volume=8 | issue= 8| pages=CD002913 | doi=10.1002/14651858.CD002913.pub3 | pmc= | pmid=25141071 }}
19. ^{{cite journal | author = Habal FM, Huang VW | year = 2012 | title = Review Article: A Decision-Making Algorithm For the Management of Pregnancy in the Inflammatory Bowel Disease Patient | url = | journal = Aliment Pharmacol Ther | volume = 35 | issue = 5| pages = 501–15 | pmid = 22221203 | doi=10.1111/j.1365-2036.2011.04967.x}}
20. ^{{Cite web|url=http://www.gastrojournal.org/article/S0016-5085(15)01623-6/pdf|title=American Gastroenterological Association Institute Technical Review on the Medical Management of Microscopic Colitis|last=Pardi|first=Darrell|date=2016|website=www.gastrojournal.org|access-date=}}
21. ^{{cite journal|last1=Stanaland|first1=BE|title=Once-daily budesonide aqueous nasal spray for allergic rhinitis: a review.|journal=Clinical Therapeutics|date=April 2004|volume=26|issue=4|pages=473–92|pmid=15189745|doi=10.1016/s0149-2918(04)90050-1}}
22. ^{{cite journal |last1=Rawla |first1=P |last2=Sunkara |first2=T |last3=Thandra |first3=KC |last4=Gaduputi |first4=V |title=Efficacy and Safety of Budesonide in the Treatment of Eosinophilic Esophagitis: Updated Systematic Review and Meta-Analysis of Randomized and Non-Randomized Studies. |journal=Drugs in R&D |date=December 2018 |volume=18 |issue=4 |pages=259-269 |doi=10.1007/s40268-018-0253-9 |pmid=30387081}}
23. ^1 BUDESONIDE - NASAL AEROSOL INHALER (Rhinocort) side effects, medical uses, and drug interactions {{webarchive |url=https://web.archive.org/web/20081106080137/http://www.emedicinehealth.com/budesonide-nasal_aerosol_inhaler/article.htm |date=November 6, 2008 }}
24. ^{{cite web|title=Budesonide: CMDh scientific conclusions and grounds for variation, amendments to the product information and timetable for the implementation - PSUSA/00000449/201604|url=http://www.ema.europa.eu/docs/en_GB/document_library/Periodic_safety_update_single_assessment/2017/03/WC500223322.pdf|publisher=European Medicines Agency (EMA)|accessdate=19 May 2017|date=March 10, 2017|deadurl=no|archiveurl=https://web.archive.org/web/20170908174615/http://www.ema.europa.eu/docs/en_GB/document_library/Periodic_safety_update_single_assessment/2017/03/WC500223322.pdf|archivedate=8 September 2017|df=}}
25. ^{{cite journal | vauthors=Todd GR, Acerini CL, Buck JJ, Murphy NP, Ross-Russell R, Warner JT, McCance DR | year = 2002 | title = Acute Adrenal Crisis in Asthmatics Treated With High-Dose Fluticasone Propionate | url = | journal = Eur Respir J | volume = 19 | issue = 6| pages = 1207–9 | pmid = 12108877 | doi=10.1183/09031936.02.00274402}}
26. ^{{cite journal |vauthors=Todd GR, Acerini CL, Ross-Russell R, Zahra S, Warner JT, McCance D | year = 2002 | title = Survey of Adrenal Crisis Associated With Inhaled Corticosteroids in the United Kingdom | url = | journal = Arch Dis Child | volume = 87 | issue = 6| pages = 457–61 | pmid = 12456538 | pmc=1755820 | doi=10.1136/adc.87.6.457}}
27. ^1 {{cite book|author=J. Elks|title=The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies|url=https://books.google.com/books?id=0vXTBwAAQBAJ&pg=PA186|date=14 November 2014|publisher=Springer|isbn=978-1-4757-2085-3|pages=186, 1011|deadurl=no|archiveurl=https://web.archive.org/web/20170908174614/https://books.google.com/books?id=0vXTBwAAQBAJ&pg=PA186|archivedate=8 September 2017|df=}}
28. ^1 {{cite book|author1=Thomas L. Lemke|author2=David A. Williams|title=Foye's Principles of Medicinal Chemistry|url=https://books.google.com/books?id=R0W1ErpsQpkC&pg=PA1253|year=2008|publisher=Lippincott Williams & Wilkins|isbn=978-0-7817-6879-5|pages=1253–|deadurl=no|archiveurl=https://web.archive.org/web/20170908174614/https://books.google.com/books?id=R0W1ErpsQpkC&pg=PA1253|archivedate=2017-09-08|df=}}

External links

  • [https://web.archive.org/web/20100216094309/http://www.entocortec.com/PDF/ENTOCORT_PI.pdf Entocort EC Prescribing information] Prometheus Laboratories (PDF)
  • [https://www.nlm.nih.gov/medlineplus/druginfo/meds/a608007.html Budesonide Oral (Entocort EC)] MedlinePlus, National Institutes of Health (NIH), U.S. National Library of Medicine
  • [https://www.nlm.nih.gov/medlineplus/druginfo/meds/a601030.html Budesonide Nasal Spray (Rhinocort)] MedlinePlus, National Institutes of Health (NIH), U.S. National Library of Medicine
  • [https://www.nlm.nih.gov/medlineplus/druginfo/meds/a601030.html Budesonide Oral Inhalation (Symbicort)] MedlinePlus, National Institutes of Health (NIH), U.S. National Library of Medicine
{{Glucocorticoids}}{{Antidiarrheals, intestinal anti-inflammatory/anti-infective agents}}{{Nasal preparations}}{{Asthma_and_copd_rx}}{{Glucocorticoidics}}{{AstraZeneca}}

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