View source for Biology:Budesonide

{{Short description|Type of corticosteroid medication; group of stereoisomers}}
{{Infobox drug
| Verifiedfields = changed
| Watchedfields = changed
| verifiedrevid = 459985202
| image = Budesonide skeletal.svg
| width = 250
| alt = 
| image2 = Budesonide ball-and-stick.png
| width2 = 250
| alt2 = 
| caption = 

<!-- Clinical data -->
| pronounce = 
| tradename = Pulmicort, Rhinocort, Entocort, others
| Drugs.com = {{drugs.com|monograph|budesonide}}
| MedlinePlus = a608007
| licence_EU = yes
| DailyMedID = Budesonide
| pregnancy_AU = A
| pregnancy_AU_comment = /{{nbsp}}B3
| pregnancy_category = 
| routes_of_administration = [[Medicine:Oral administration|By mouth]], [[Medicine:Nasal administration|nasal]], [[Medicine:Tracheal intubation|tracheal]], [[Medicine:Rectal administration|rectal]], [[Biology:Inhalation|inhalation]]
| class = 
| ATC_prefix = A07
| ATC_suffix = EA06
| ATC_supplemental = {{ATC|D07|AC09}}, {{ATC|R01|AD05}}, {{ATC|R03|BA02}}

<!-- Legal status -->
| legal_AU = S2
| legal_AU_comment = /{{nbsp}}S4
| legal_BR = <!-- OTC, A1, A2, A3, B1, B2, C1, C2, C3, C4, C5, D1, D2, E, F -->
| legal_BR_comment = 
| legal_CA = Rx-only
| legal_CA_comment = <ref>{{cite web | title=Regulatory Decision Summary - Uceris | website=Health Canada | date=23 October 2014 | url=https://hpr-rps.hres.ca/reg-content/regulatory-decision-summary-detail.php?linkID=RDS00675 | access-date=4 June 2022 | archive-date=5 June 2022 | archive-url=https://web.archive.org/web/20220605060335/https://hpr-rps.hres.ca/reg-content/regulatory-decision-summary-detail.php?linkID=RDS00675 | url-status=live }}</ref>
| legal_DE = <!-- Anlage I, II, III or Unscheduled -->
| legal_DE_comment = 
| legal_NZ = <!-- Class A, B, C -->
| legal_NZ_comment = 
| legal_UK = POM
| legal_UK_comment = 
| legal_US = OTC
| legal_US_comment = /&nbsp;Rx-only<ref name="Tarpeyo FDA label">{{cite web | title=Tarpeyo- budesonide capsule, delayed release | website=DailyMed | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=938cada4-d6bf-4252-836f-dd40f9eadb4d | access-date=24 December 2021 | archive-date=25 December 2021 | archive-url=https://web.archive.org/web/20211225032829/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=938cada4-d6bf-4252-836f-dd40f9eadb4d | url-status=live }}</ref><ref>{{cite web | title=Pulmicort Flexhaler- budesonide aerosol, powder | website=DailyMed | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=54234b7d-3bcc-4809-1881-1d21484856a0 | access-date=24 December 2021 | archive-date=19 September 2021 | archive-url=https://web.archive.org/web/20210919024400/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=54234b7d-3bcc-4809-1881-1d21484856a0 | url-status=live }}</ref>
| legal_EU = Rx-only
| legal_EU_comment = <ref name="Jorveza EPAR">{{cite web | title=Jorveza EPAR | website=[[Organization:European Medicines Agency|European Medicines Agency]] (EMA) | date=17 September 2018 | url=https://www.ema.europa.eu/en/medicines/human/EPAR/jorveza | access-date=3 March 2023 | archive-date=4 March 2023 | archive-url=https://web.archive.org/web/20230304065613/https://www.ema.europa.eu/en/medicines/human/EPAR/jorveza | url-status=live }}</ref><ref name="Kinpeygo EPAR" />
| legal_UN = <!-- N I, II, III, IV / P I, II, III, IV -->
| legal_UN_comment = 
| legal_status = <!-- For countries not listed above -->

<!-- Pharmacokinetic data -->
| bioavailability = 10-20% (first pass effect)
| protein_bound = 85-90%
| metabolism = [[Biology:Liver|Liver]] [[Biology:CYP3A4|CYP3A4]]
| metabolites = 
| onset = 
| elimination_half-life = 2.0-3.6 hours
| duration_of_action = 
| excretion = [[Biology:Urine|Urine]], [[Biology:Feces|feces]]

<!-- Identifiers -->
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 51333-22-3
| CAS_supplemental = 
| PubChem = 40000
| IUPHAR_ligand = 
| 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
| ChEBI = 
| ChEMBL_Ref = {{ebicite|changed|EBI}}
| ChEMBL = 1370
| NIAID_ChemDB = 
| PDB_ligand = 8W5
| synonyms = BUD

<!-- Chemical and physical data -->
| IUPAC_name = 11β,21-Dihydroxy-16α,17α-[butane-1,1-diylbis(oxy)]pregna-1,4-diene-3,20-dione
| C=25 | H=34 | O=6
| 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
| StdInChI_comment = 
| StdInChIKey_Ref = {{stdinchicite|changed|chemspider}}
| StdInChIKey = VOVIALXJUBGFJZ-KWVAZRHASA
| density = 
| density_notes = 
| melting_point = 
| melting_high = 
| melting_notes = 
| boiling_point = 
| boiling_notes = 
| solubility = 
| sol_units = 
| specific_rotation = 
}}

<!-- Definition and medical uses -->
'''Budesonide''', sold under the brand name '''Pulmicort''' among others, is a [[Chemistry:Medication|medication]] of the [[Biology:Corticosteroid|corticosteroid]] type.<ref name=AHFS2015/> It is available as an [[Medicine:Metered-dose inhaler|inhaler]], nebulization solution, pill, [[Medicine:Nasal spray|nasal spray]], and rectal forms.<ref name=AHFS2015>{{cite web|title=Budesonide|url=https://www.drugs.com/monograph/budesonide.html|publisher=The American Society of Health-System Pharmacists|access-date=2 December 2015|url-status=live|archive-url=https://web.archive.org/web/20151128150235/http://www.drugs.com/monograph/budesonide.html|archive-date=28 November 2015}}</ref><ref name=AHFS2015ENT>{{cite web|title=Budesonide eent|url=https://www.drugs.com/monograph/budesonide-eent.html|publisher=The American Society of Health-System Pharmacists|access-date=2 December 2015|url-status=live|archive-url=https://web.archive.org/web/20151208195318/http://www.drugs.com/monograph/budesonide-eent.html|archive-date=8 December 2015}}</ref> The inhaled form is used in the long-term management of [[Medicine:Asthma|asthma]] and [[Medicine:Chronic obstructive pulmonary disease|chronic obstructive pulmonary disease]] (COPD).<ref name=AHFS2015 /><ref>{{cite journal | vauthors = De Coster DA, Jones M | title = Tailoring of corticosteroids in COPD management | journal = Current Respiratory Care Reports | volume = 3 | issue = 3 | pages = 121–132 | date = 2014 | pmid = 25089228 | pmc = 4113685 | doi = 10.1007/s13665-014-0084-2 }}</ref><ref>{{cite journal | vauthors = Christophi GP, Rengarajan A, Ciorba MA | title = Rectal budesonide and mesalamine formulations in active ulcerative proctosigmoiditis: efficacy, tolerance, and treatment approach | journal = Clinical and Experimental Gastroenterology | volume = 9 | pages = 125–30 | date = 2016 | pmid = 27274301 | pmc = 4876845 | doi = 10.2147/CEG.S80237 | doi-access = free }}</ref> The nasal spray is used for [[Medicine:Allergic rhinitis|allergic rhinitis]] and [[Medicine:Nasal polyp|nasal polyp]]s.<ref name=AHFS2015ENT/><ref>{{cite journal | vauthors = Rudmik L, Schlosser RJ, Smith TL, Soler ZM | title = Impact of topical nasal steroid therapy on symptoms of nasal polyposis: a meta-analysis | journal = The Laryngoscope | volume = 122 | issue = 7 | pages = 1431–7 | date = July 2012 | pmid = 22410935 | doi = 10.1002/lary.23259 | s2cid = 25637461 }}</ref> The pills in a delayed release form and rectal forms may be used for [[Medicine:Inflammatory bowel disease|inflammatory bowel disease]] including [[Medicine:Crohn's disease|Crohn's disease]], [[Medicine:Ulcerative colitis|ulcerative colitis]], and [[Medicine:Microscopic colitis|microscopic colitis]].<ref name=Sil2011>{{cite journal | vauthors = Silverman J, Otley A | title = Budesonide in the treatment of inflammatory bowel disease | journal = Expert Review of Clinical Immunology | volume = 7 | issue = 4 | pages = 419–28 | date = July 2011 | pmid = 21790284 | doi = 10.1586/eci.11.34 | s2cid = 32892611 }}</ref><ref name = "Pardi_2016">{{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 | date = January 2016 | pmid = 26584602 | doi = 10.1053/j.gastro.2015.11.006 }}</ref><ref name=BNF58>{{cite book|title=British national formulary: BNF 58|date=2009|publisher=British Medical Association|isbn=9780857111562|pages=56–57|edition=58}}</ref>

<!-- Side effects and mechanism -->
Common [[Medicine:Side effect|side effect]]s with the inhaled form include respiratory infections, cough, and headaches.<ref name=AHFS2015/> Common side effects with the pills include feeling tired, vomiting, and joint pains.<ref name=AHFS2015/> Serious side effects include an increased risk of infection, loss of bone strength, and cataracts.<ref name=AHFS2015/> Long-term use of the pill form may cause adrenal insufficiency.<ref name=AHFS2015/> Stopping the pills suddenly following long-term use may therefore be dangerous.<ref name=AHFS2015/> The inhaled form is generally safe in [[Medicine:Pregnancy|pregnancy]].<ref name=AHFS2015/> Budesonide chiefly acts as a [[Chemistry:Glucocorticoid|glucocorticoid]].<ref name=AHFS2015/>

<!-- Society and culture -->
Budesonide was initially patented in 1973.<ref>{{cite book| vauthors = Domeij B |title=Pharmaceutical patents in Europe|date=2000|publisher=Kluwer Law International|location=The Hague|isbn=9789041113481|page=278|url=https://books.google.com/books?id=KZfvZN2WfjcC&pg=PA278|url-status=live|archive-url=https://web.archive.org/web/20151208072850/https://books.google.ca/books?id=KZfvZN2WfjcC&pg=PA278|archive-date=8 December 2015}}</ref> Commercial use as an asthma medication began in 1981.<ref>{{cite book| vauthors = Hamley P |title=Small Molecule Medicinal Chemistry: Strategies and Technologies|date=2015|publisher=John Wiley & Sons|isbn=9781118771693|page=390|url=https://books.google.com/books?id=LOudCgAAQBAJ&pg=PA390|url-status=live|archive-url=https://web.archive.org/web/20151208062120/https://books.google.ca/books?id=LOudCgAAQBAJ&pg=PA390|archive-date=8 December 2015}}</ref> It is on the [[Medicine:WHO Model List of Essential Medicines|World Health Organization's List of Essential Medicines]].<ref name="WHO21st">{{cite book | vauthors = ((World Health Organization)) | title = World Health Organization model list of essential medicines: 21st list 2019 | year = 2019 | hdl = 10665/325771 |  publisher = World Health Organization | location = Geneva | id = WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO | hdl-access=free}}</ref> Some forms are available as a generic medication.<ref name=Ric2015>{{cite book| vauthors = Hamilton R |title=Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition|date=2015|publisher=Jones & Bartlett Learning|isbn=9781284057560|page=451}}</ref><ref>{{cite web | title=First Generic Drug Approvals 2023 | website=U.S. [[Organization:Food and Drug Administration|Food and Drug Administration]] (FDA) | date=30 May 2023 | url=https://www.fda.gov/drugs/drug-and-biologic-approval-and-ind-activity-reports/first-generic-drug-approvals | archive-url=https://web.archive.org/web/20230630003621/https://www.fda.gov/drugs/drug-and-biologic-approval-and-ind-activity-reports/first-generic-drug-approvals | archive-date=30 June 2023 | url-status=live | access-date=30 June 2023}}</ref> In 2019, generic budesonide was listed as being involved in [[Company:Teva Pharmaceuticals|Teva]]'s [[Social:Price fixing|price fixing]] scheme in the United States.<ref>{{Cite news|vauthors=Murphy H|date=11 May 2019|title=Teva and Other Generic Drugmakers Inflated Prices Up to 1,000%, State Prosecutors Say|work=The New York Times|url=https://www.nytimes.com/2019/05/11/health/teva-price-fixing-lawsuit.html|access-date=27 May 2020|archive-date=30 May 2020|archive-url=https://web.archive.org/web/20200530154338/https://www.nytimes.com/2019/05/11/health/teva-price-fixing-lawsuit.html|url-status=live}}</ref> In 2020, it was the 207th most commonly prescribed medication in the United States, with more than 2{{nbsp}}million prescriptions.<ref>{{cite web | title = The Top 300 of 2020 | url = https://clincalc.com/DrugStats/Top300Drugs.aspx | website = ClinCalc | access-date = 7 October 2022 | archive-date = 18 March 2020 | archive-url = https://web.archive.org/web/20200318234059/https://clincalc.com/DrugStats/Top300Drugs.aspx | url-status = live }}</ref><ref>{{cite web | title = Budesonide - Drug Usage Statistics | website = ClinCalc | url = https://clincalc.com/DrugStats/Drugs/Budesonide | access-date = 7 October 2022 | archive-date = 29 April 2017 | archive-url = https://web.archive.org/web/20170429130248/https://clincalc.com/DrugStats/Drugs/Budesonide | url-status = live }}</ref>

==Medical uses==
===Asthma===
Budesonide is given by [[Medicine:Metered-dose inhaler|metered-dose inhaler]] or nebulizer for maintenance and prophylactic treatment of [[Medicine:Asthma|asthma]], including patients who require oral corticosteroids and those who may benefit from a systemic dose reduction.<ref>Global Strategy for Asthma Management and Prevention, Global Initiative for Asthma (GiNA) 2011. Available at https://www.ginasthma.org {{webarchive|url=https://web.archive.org/web/20131014032230/http://www.ginasthma.org/ |date=14 October 2013}}</ref>

===Inflammatory bowel disease===
Formulations of delayed-release budesonide are an effective treatment for mild-to-moderately active [[Medicine:Crohn's disease|Crohn's disease]] involving the [[Biology:Ileum|ileum]] and/or [[Biology:Ascending colon|ascending colon]].<ref>{{cite journal | vauthors = Lichtenstein GR, Hanauer SB, Sandborn WJ | year = 2009 | title = Management of Crohn's Disease in Adults | journal = Am J Gastroenterol | volume = 104 | issue = 2| pages = 465–83 | pmid = 19174807 | doi=10.1038/ajg.2008.168| s2cid = 10176441| doi-access = free }}</ref> A [[Cochrane Library|Cochrane]] review found evidence for up to three months (but not longer) of maintenance of remission in Crohn's disease.<ref name="pmid25141071">{{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=7133546 | pmid=25141071 }}</ref>

Budesonide assists in the induction of [[Medicine:Remission|remission]] in people with active [[Medicine:Ulcerative colitis|ulcerative colitis]].<ref>{{cite journal | vauthors = Habal FM, Huang VW | year = 2012 | title = Review Article: A Decision-Making Algorithm For the Management of Pregnancy in the Inflammatory Bowel Disease Patient | journal = Aliment Pharmacol Ther | volume = 35 | issue = 5| pages = 501–15 | pmid = 22221203 | doi=10.1111/j.1365-2036.2011.04967.x| s2cid = 34662981 | doi-access = free }}</ref>

Budesonide is highly effective and recommended as the drug of choice in [[Medicine:Microscopic colitis|microscopic colitis]], for induction and maintenance of remission, and for both the [[Medicine:Lymphocytic colitis|lymphocytic colitis]] and [[Medicine:Collagenous colitis|collagenous colitis]] forms.<ref name = "Pardi_2016" /><ref>{{cite journal | vauthors = Miehlke S, Guagnozzi D, Zabana Y, Tontini GE, Kanstrup Fiehn AM, Wildt S, Bohr J, Bonderup O, Bouma G, D'Amato M, Heiberg Engel PJ, Fernandez-Banares F, Macaigne G, Hjortswang H, Hultgren-Hörnquist E, Koulaouzidis A, Kupcinskas J, Landolfi S, Latella G, Lucendo A, Lyutakov I, Madisch A, Magro F, Marlicz W, Mihaly E, Munck LK, Ostvik AE, Patai ÁV, Penchev P, Skonieczna-Żydecka K, Verhaegh B, Münch A | display-authors = 6 | title = European guidelines on microscopic colitis: United European Gastroenterology and European Microscopic Colitis Group statements and recommendations | journal = United European Gastroenterology Journal | volume = 9 | issue = 1 | pages = 13–37 | date = February 2021 | pmid = 33619914 | pmc = 8259259 | doi = 10.1177/2050640620951905}}</ref>

===Allergic rhinitis===
Budesonide in the form of nasal sprays is a treatment for [[Medicine:Allergic rhinitis|allergic rhinitis]].<ref>{{cite journal | vauthors = Stanaland BE | title = Once-daily budesonide aqueous nasal spray for allergic rhinitis: a review | journal = Clinical Therapeutics | volume = 26 | issue = 4 | pages = 473–92 | date = April 2004 | pmid = 15189745 | doi = 10.1016/s0149-2918(04)90050-1}}</ref>

===Eosinophilic esophagitis===
Topical budesonide has considerable effects in eosinophilic esophagitis.<ref>{{cite journal | vauthors = Rawla P, Sunkara T, Thandra KC, Gaduputi 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 | volume = 18 | issue = 4 | pages = 259–269 | date = December 2018 | pmid = 30387081 | pmc = 6277325 | doi = 10.1007/s40268-018-0253-9}}</ref> For this use, it is formulated as a tablet that [[Chemistry:Dispersion|disperses]] in the mouth, and sold under the brand name Jorveza.<ref>{{drugs.com|uk|jorveza}}</ref>

=== Berger's disease ===
Budesonide (Tarpeyo (US); Kinpeygo (EU, UK)) is indicated to reduce proteinuria (increased protein levels in the urine) in adults with primary [[Medicine:IgA nephropathy|immunoglobulin A (IgA) nephropathy]] (Berger's disease) at risk of rapid disease progression.<ref name="Tarpeyo FDA label" /><ref>{{cite web | title=FDA approves first drug to decrease urine protein in IgA nephropathy, a rare kidney disease | website=U.S. [[Organization:Food and Drug Administration|Food and Drug Administration]] (FDA) | date=17 December 2021 | url=https://www.fda.gov/drugs/fda-approves-first-drug-decrease-urine-protein-iga-nephropathy-rare-kidney-disease | access-date=18 December 2021 | archive-date=19 December 2021 | archive-url=https://web.archive.org/web/20211219081148/https://www.fda.gov/drugs/fda-approves-first-drug-decrease-urine-protein-iga-nephropathy-rare-kidney-disease | url-status=live }} {{PD-notice}}</ref><ref name="Kinpeygo EPAR" />

==Side effects==
Nasal budesonide inhalers have been associated with a number of side effects.<ref name="emedicinehealth">{{Cite web|url=https://www.emedicinehealth.com/script/main/notfoundstatic.asp?refurl=/budesonide-nasal_aerosol_inhaler/article.htm|archive-url=https://web.archive.org/web/20081106080137/http://www.emedicinehealth.com/budesonide-nasal_aerosol_inhaler/article.htm|url-status=dead|title=GENERIC NAME: BUDESONIDE - NASAL AEROSOL INHALER (byou-DESS-oh-nide)|archive-date=6 November 2008|website=eMedicineHealth}}</ref><ref>{{cite web |title=What are the possible side effects of budesonide nasal (Childrens Rhinocort Allergy, Rhinocort Allergy, Rhinocort Aqua)? |url=https://www.emedicinehealth.com/drug-budesonide_nasal/article_em.htm#sideeffects |website=eMedicineHealth |access-date=25 August 2020 |archive-date=6 August 2020 |archive-url=https://web.archive.org/web/20200806011138/https://www.emedicinehealth.com/drug-budesonide_nasal/article_em.htm#sideeffects |url-status=live }}</ref> These include 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 [[Biology:Mucus|mucus]], and blurred vision.<ref>{{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=[[Organization:European Medicines Agency|European Medicines Agency]] (EMA)|access-date=19 May 2017|date=10 March 2017|url-status=live|archive-url=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|archive-date=8 September 2017}}</ref> Other symptoms which should be reported immediately include difficulty in breathing, swelling of the face, white patches in the throat, mouth, or nose, irregular menstrual periods, severe acne, and on rare occasions, behavioral changes (mostly affecting children).<ref name="emedicinehealth" />

==Contraindications==
Budesonide is contraindicated as a primary treatment of status asthmaticus or other acute episode of asthma where intensive measures are required.<ref>{{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 | journal = Eur Respir J | volume = 19 | issue = 6| pages = 1207–9 | pmid = 12108877 | doi=10.1183/09031936.02.00274402| doi-access = free }}</ref> It is also contraindicated for patients who have hypersensitivity to budesonide.<ref>{{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 | journal = Arch Dis Child | volume = 87 | issue = 6| pages = 457–61 | pmid = 12456538 | pmc=1755820 | doi=10.1136/adc.87.6.457}}</ref>

==Interactions==
Those taking tablets or capsules orally should avoid [[Biology:Grapefruit|grapefruit]] and grapefruit juice<ref name="BaylessHanauer2014">{{cite book| veditors = Bayless TM, Hanauer SB |title=Advanced Therapy of Inflammatory Bowel Disease, volume 2: IBD and Crohn's Disease | vauthors = Marshall JK | chapter = Topically Active Steroid Preparations | chapter-url=https://books.google.com/books?id=-AJri58Yj5EC&q=Budesonide&pg=651 | page = 651 |date=May 2014|publisher=PMPH-USA|isbn=978-1-60795-217-6 }}</ref><ref>{{cite book | veditors = Boullata JI, Armenti VT|title=Handbook of drug-nutrient interactions |date=2010 |publisher=Humana Press |location=New York, NY |isbn=978-1-60327-362-6 |edition=2nd | vauthors = Baily DG | chapter = Grapefruit and Other Fruit Juices Interactions with Medicines | chapter-url = https://books.google.com/books?id=6MSRviXlDtAC&pg=PA282 | page = 282 }}</ref> and [[Biology:Echinacea|echinacea]].<ref name="KiziorHodgson2014">{{cite book| vauthors = Kizior RJ, Hodgson BB |title=Saunders Nursing Drug Handbook 2015 - E-Book|url=https://books.google.com/books?id=qVRTBAAAQBAJ&q=Budesonide+echinacea&pg=160|date=22 August 2014|publisher=Elsevier Health Sciences|isbn=978-0-323-28018-1|page=160}}</ref>{{rp|160}}

Also, high-fat meals delay absorption but do not impede absorption.<ref>{{cite book | vauthors = Taketomo CK, Hodding JH, Kraus DM | date = 2009 | url = https://books.google.com/books?id=ElYtAQAAMAAJ&q=Budesonide+high+fat+meals+absorption | title = Pediatric Dosage Handbook; Including Neonatal Dosing, Drug Administration & Extemporaneous Preparations | publisher = Lexi-Comp | isbn = 978-1-59195-267-1 }}</ref>

==Pharmacology==
Budesonide is an [[Biology:Agonist|agonist]] of [[Biology:Glucocorticoid receptor|glucocorticoid receptor]]s. Among its effects are:

* Controls the rate of protein synthesis.<ref name="KiziorHodgson2018b">{{cite book| vauthors = Kizior RJ, Hodgson BB |title=Saunders Nursing Drug Handbook 2019 E-Book|url=https://books.google.com/books?id=eJNNDwAAQBAJ&q=Budesonide+protein+synthesis&pg=160|date=21 February 2018|publisher=Elsevier Health Sciences|isbn=978-0-323-61257-9|page=160}}</ref>
* Depresses the migration of polymorphonuclear leukocytes and fibroblasts.<ref name="NPRN2020">{{cite book| vauthors = Skidmore-Roth L, Richardson F |title=Mosby's Canadian Nursing Drug Reference - E-Book|url=https://books.google.com/books?id=iS_wDwAAQBAJ&q=Budesonide+fibroblasts+migration&pg=187|date=9 July 2020|publisher=Elsevier Health Sciences|isbn=978-1-77172-084-7|page=187}}</ref>
* Reverses capillary permeability and lysosomal stabilization at the cellular level to prevent or control inflammation.
* Has a potent glucocorticoid activity and weak [[Chemistry:Mineralocorticoid|mineralocorticoid]] activity.{{medical citation needed|date=April 2019}}

==Pharmacokinetics==
* Onset of action: [[Medicine:Nebulizer|Nebulization]]: 2–8 days; Inhalation: 24 hours; Nasal: 10 hours
* Peak effect: Nebulization: 4–6 weeks; Inhalation: 1–2 weeks
* Distribution: 2.2-3.9 L/kg
* Protein binding: 85% to 90%
* [[Biology:Metabolism|Metabolism]]: Hepatic via [[Biology:CYP3A4|CYP3A4]] to two [[Biology:Metabolite|metabolite]]s: 16 alpha-hydroxyprednisolone and 6 beta-hydroxybudesonide; minor activity
**Budesonide is extensively metabolized in [[Chemistry:First pass effect|first pass]], resulting in a low bioavailability and systemic effects<ref>{{cite journal | vauthors = Abdalla MI, Herfarth H | title = Budesonide for the treatment of ulcerative colitis | journal = Expert Opinion on Pharmacotherapy | volume = 17 | issue = 11 | pages = 1549–1559 | date = August 2016 | pmid = 27157244 | pmc = 4989907 | doi = 10.1080/14656566.2016.1183648 }}</ref>
** Bioavailability: 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

==Chemistry==

Budesonide, also known as 11β,21-dihydroxy-16α,17α-(butylidenebis(oxy))pregna-1,4-diene-3,20-dione, is a synthetic [[Chemistry:Pregnane|pregnane]] [[Biology:Steroid|steroid]] and non-[[Chemistry:Halogen|halogen]]ated cyclic ketal [[Biology:Corticosteroid|corticosteroid]].<ref name="Elks2014">{{cite book| vauthors = Elks J |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|url-status=live|archive-url=https://web.archive.org/web/20170908174614/https://books.google.com/books?id=0vXTBwAAQBAJ&pg=PA186|archive-date=8 September 2017}}</ref><ref name="LemkeWilliams2008">{{cite book| vauthors = Lemke TL, Williams DA |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–|url-status=live|archive-url=https://web.archive.org/web/20170908174614/https://books.google.com/books?id=R0W1ErpsQpkC&pg=PA1253|archive-date=8 September 2017}}</ref> It is the C16α [[Chemistry:Hydroxyl group|hydroxyl]], C16α,17α cyclic ketal with [[Chemistry:Butyraldehyde|butyraldehyde]] [[Chemistry:Chemical derivative|derivative]] of [[Chemistry:Prednisolone|prednisolone]] (11β,17α,21-trihydroxypregna-1,4-diene-3,20-dione).<ref name="Elks2014" /><ref name="LemkeWilliams2008" />

===Stereoisomerism===
{| class="wikitable" style="text-align:center"
|- class="hintergrundfarbe6"
! colspan="2"| Budesonide<br /><small>(2 stereoisomers)</small>
|-
| [[File:22R-Budesonid V4.svg|220px|''(R)''-Budesonid]]<br /><small>(22''R'')-configuration</small>
| [[File:22S-Budesonid V4.svg|220px|''(S)''-Budesonid]]<br /><small>(22''S'')-configuration</small>
|}

==Society and culture==
=== Legal status ===
On 19 May 2022, the Committee for Medicinal Products for Human Use (CHMP) of the [[Organization:European Medicines Agency|European Medicines Agency]] (EMA) adopted a positive opinion, recommending the granting of a conditional marketing authorization for the medicinal product Kinpeygo, intended for the treatment of primary immunoglobulin A nephropathy.<ref name="Kinpeygo: Pending EC decision" /> The applicant for this medicinal product is Calliditas Therapeutics AB.<ref name="Kinpeygo: Pending EC decision" /> Kinpeygo is a hybrid medicine of Entocort which has been authorised in the EU since 2 April 1992.<ref name="Kinpeygo: Pending EC decision" /> Kinpeygo contains the same active substance as Entocort but has a different formulation and a different indication.<ref name="Kinpeygo: Pending EC decision">{{cite web | title=Kinpeygo: Pending EC decision | website=[[Organization:European Medicines Agency|European Medicines Agency]] (EMA) | date=20 May 2022 | url=https://www.ema.europa.eu/en/medicines/human/summaries-opinion/kinpeygo | access-date=20 May 2022 | archive-date=20 May 2022 | archive-url=https://web.archive.org/web/20220520151855/https://www.ema.europa.eu/en/medicines/human/summaries-opinion/kinpeygo | url-status=live }} Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.</ref> Kinpeygo was approved for medical use in the European Union in July 2022.<ref name="Kinpeygo EPAR">{{cite web | title=Kinpeygo EPAR | website=[[Organization:European Medicines Agency|European Medicines Agency]] (EMA) | date=17 May 2022 | url=https://www.ema.europa.eu/en/medicines/human/EPAR/kinpeygo | access-date=3 March 2023 | archive-date=4 March 2023 | archive-url=https://web.archive.org/web/20230304065605/https://www.ema.europa.eu/en/medicines/human/EPAR/kinpeygo | url-status=live }}</ref><ref>{{cite web | title=Kinpeygo Product information | website=Union Register of medicinal products | url=https://ec.europa.eu/health/documents/community-register/html/h1657.htm | access-date=3 March 2023 | archive-date=4 March 2023 | archive-url=https://web.archive.org/web/20230304065613/https://ec.europa.eu/health/documents/community-register/html/h1657.htm | url-status=live }}</ref>

===Brand names===
[[File:Budesonide and formoterol inhaler.jpg|thumb|200px|Inhaler for a powder based on budesonide and [[Chemistry:Formoterol|formoterol]]]]

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); Busonid (BR); Clebudan (CN); Cortiment (CA, GB, AU); 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);<ref name="KiziorHodgson2014" />{{rp|13}} 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, HR, ID, IN, NI, NL, NO, PA, PK, PL, PT, RU, SE, SV, TR, TW, UY, VE, ZA);<ref name="KiziorHodgson2014" />{{rp|13}} Pulmicort Nasal Turbohaler (CL, KE, MU, NG); Pulmicort Turbuhaler (KE, MU, NG); Rafton (FR); Rhinocort (AU); Rhinocort Aqua (HK);<ref>{{cite book | vauthors = Griffith HW | date =2014 | url = https://books.google.com/books?id=DHWBAwAAQBAJ&pg=PA12 | title = Complete Guide to Prescription and Nonprescription Drugs 2015; Features an A-Z List of Conditions and the Drugs Most Commonly Used | publisher =Penguin | isbn =9780698165519 | edition = 2015 }}</ref> Rhinoside (GR); Symbicort (DE, FR, UK, US, ZA) Uceris (US).

== Research ==
===COVID-19===
Budesonide was recommended in April 2021 by the UK's NHS to treat COVID-19 on a case-by-case basis for those aged 50 years of age and older.<ref>{{cite web |title=COVID-19 Therapeutic Alert - Inhaled Budesonide for Adults (50 Years and Over) with COVID-19 |url=https://www.cas.mhra.gov.uk/ViewandAcknowledgment/ViewAlert.aspx?AlertID=103154 |website=Central Alerting System |date=12 April 2021 |access-date=16 April 2021 |archive-date=12 April 2021 |archive-url=https://web.archive.org/web/20210412150959/https://www.cas.mhra.gov.uk/ViewandAcknowledgment/ViewAlert.aspx?AlertID=103154 |url-status=live }}</ref> After a [[Organization:University of Oxford|University of Oxford]] research team found in a trial with 1,700 patients that budesonide could benefit many people over 50 with [[Medicine:COVID-19|COVID-19]] symptoms, it was recommended from 12 April 2021, by the National Health Service in the UK for general practitioners (GPs) to treat COVID-19 on a case-by-case basis.<ref>{{Cite news |title=Covid: Asthma drug 'speeds up recovery at home' |vauthors=Roxby P |website=BBC News |date=12 April 2021 |url=https://www.bbc.co.uk/news/health-56717486 |access-date=12 April 2021 |archive-date=12 April 2021 |archive-url=https://web.archive.org/web/20210412184831/https://www.bbc.co.uk/news/health-56717486 |url-status=live }}</ref><ref>{{Cite news|vauthors=Blakely R|title=Asthma drug Budesonide speeds up Covid recovery times|url=https://www.thetimes.co.uk/article/asthma-drug-speeds-up-covid-recovery-times-t0630b7lp|newspaper=The Times|date=12 April 2021|url-access=subscription|issn=0140-0460|access-date=13 April 2021|archive-date=6 November 2021|archive-url=https://web.archive.org/web/20211106022706/https://www.thetimes.co.uk/article/asthma-drug-speeds-up-covid-recovery-times-t0630b7lp|url-status=live}}</ref> Results of a large-scale trial published in August 2021 suggest that inhaled budesonide improves the time of recovery and people's well-being during the recovery process.<ref>{{Cite journal |title=Platform trial rules out treatments for COVID-19 |url=https://evidence.nihr.ac.uk/alert/platform-trial-rules-out-covid-treatments/ |journal=NIHR Evidence |date=31 May 2022 |doi=10.3310/nihrevidence_50873 |type=Plain English summary |access-date=1 June 2022 |archive-date=1 June 2022 |archive-url=https://web.archive.org/web/20220601095141/https://evidence.nihr.ac.uk/alert/platform-trial-rules-out-covid-treatments/ |url-status=live }}</ref><ref>{{cite journal | vauthors = Yu LM, Bafadhel M, Dorward J, Hayward G, Saville BR, Gbinigie O, Van Hecke O, Ogburn E, Evans PH, Thomas NP, Patel MG, Richards D, Berry N, Detry MA, Saunders C, Fitzgerald M, Harris V, Shanyinde M, de Lusignan S, Andersson MI, Barnes PJ, Russell RE, Nicolau DV, Ramakrishnan S, Hobbs FD, Butler CC | display-authors = 6 | title = Inhaled budesonide for COVID-19 in people at high risk of complications in the community in the UK (PRINCIPLE): a randomised, controlled, open-label, adaptive platform trial | journal = Lancet | volume = 398 | issue = 10303 | pages = 843–855 | date = September 2021 | pmid = 34388395 | pmc = 8354567 | doi = 10.1016/S0140-6736(21)01744-X }}</ref> Inhalational budesonide was added to the recommended treatment for cases of COVID-19 in India in April 2021.<ref>{{cite news|date=29 April 2021|title=New guidelines prescribe inhaled steroid 'Budesonide', antiparasitic drug 'Ivermectin' for mild Covid cases|url=https://www.newindianexpress.com/nation/2021/apr/29/new-guidelines-prescribe-inhaled-steroid-budesonide-antiparasitic-drug-ivermectin-for-mild-covid-cases-2296446.html|website=The New Indian Express|access-date=11 July 2021|archive-date=6 November 2021|archive-url=https://web.archive.org/web/20211106022707/https://www.newindianexpress.com/nation/2021/apr/29/new-guidelines-prescribe-inhaled-steroid-budesonide-antiparasitic-drug-ivermectin-for-mild-covid-cases-2296446.html|url-status=live}}</ref><ref>{{Cite web|date=24 May 2021|title=Clinical Management Protocol for Covid-19 (in Adults)|url=https://www.mohfw.gov.in/pdf/UpdatedDetailedClinicalManagementProtocolforCOVID19adultsdated24052021.pdf|website=Ministry of Health and Family Welfare (India)|access-date=10 July 2021|archive-date=5 December 2021|archive-url=https://web.archive.org/web/20211205052720/https://www.mohfw.gov.in/pdf/UpdatedDetailedClinicalManagementProtocolforCOVID19adultsdated24052021.pdf|url-status=live}}</ref> The NIH recommendation was withdrawn in December 2021 citing the need for more research.<ref>{{Cite web |vauthors=Burns C |title=NICE removes budesonide from recommended COVID-19 treatments |url=https://pharmaceutical-journal.com/article/news/nice-removes-budesonide-from-recommended-covid-treatments |access-date=1 June 2022 |website=The Pharmaceutical Journal |date=15 December 2021 |archive-date=26 June 2022 |archive-url=https://web.archive.org/web/20220626033349/https://pharmaceutical-journal.com/article/news/nice-removes-budesonide-from-recommended-covid-treatments |url-status=live }}</ref><ref>{{cite web | title=Withdrawal of the Recommendation for Consideration of Inhaled Budesonide as a Treatment Option for COVID-19 | website=Central Alerting System | url=https://www.cas.mhra.gov.uk/ViewandAcknowledgment/ViewAlert.aspx?AlertID=103185 | access-date=20 May 2022 | archive-date=30 June 2022 | archive-url=https://web.archive.org/web/20220630023652/https://www.cas.mhra.gov.uk/ViewandAcknowledgment/ViewAlert.aspx?AlertID=103185 | url-status=live }}</ref>

==References==
{{Reflist}}

==External links==
* {{cite web | title=Budesonide Nasal Spray | website=MedlinePlus | url=https://medlineplus.gov/druginfo/meds/a601030.html }}
* {{cite web | title=Budesonide Oral Inhalation | website=MedlinePlus | url=https://medlineplus.gov/druginfo/meds/a699056.html }}

{{Glucocorticoids}}
{{Antidiarrheals, intestinal anti-inflammatory/anti-infective agents}}
{{Nasal preparations}}
{{Asthma_and_copd_rx}}
{{Glucocorticoidics}}
{{AstraZeneca}}

[[Category:Aldols]]
[[Category:Corticosteroid cyclic ketals]]
[[Category:Corticosteroids]]
[[Category:Cyclic acetals with aldehydes]]
[[Category:Diketones]]
[[Category:Diols]]
[[Category:Enones]]
[[Category:Glucocorticoids]]
[[Category:Orphan drugs]]
[[Category:Pregnanes]]
[[Category:World Health Organization essential medicines]]
[[Category:Wikipedia medicine articles ready to translate]]

{{Sourceattribution|Budesonide}}