Identification
- Name
- Budesonide
- Accession Number
- DB01222
- Description
Budesonide is a glucocorticoid that is a mix of the 22R and 22S epimer used to treat inflammatory conditions of the lungs and intestines such as asthma, COPD, Crohn's disease, and ulcerative colitis.5,6
Budesonide was granted FDA approval on 14 February 1994.7
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Budesonide (DB01222)
- Weight
- Average: 430.5339
Monoisotopic: 430.23553882 - Chemical Formula
- C25H34O6
- Synonyms
- (11β,16α)-16,17-(Butylidenebis(oxy))-11,21-dihydroxypregna-1,4-diene-3,20-dione
- Budesónida
- Budesonide
- External IDs
- MAP-0010
- MAP0010
- S-1320
Pharmacology
- Indication
Budesonide extended release capsules are indicated for the treatment and maintenance of mild to moderate Crohn’s disease.8,9 Various inhaled budesonide products are indicated for prophylactic therapy in asthma10,11,13 and reducing exacerbations of COPD.13 A budesonide nasal spray is available over the counter for symptoms of hay fever and upper respiratory allergies.12 Extended release capsules are indicated to induce remission of mild to moderate ulcerative colitis14 and a rectal foam is used for mild to moderate distal ulcerative colitis.15
- Associated Conditions
- Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More- Pharmacodynamics
Budesonide is a glucocorticoid used to treat respiratory and digestive conditions by reducing inflammation.8,9,10,11,13,14,15 It has a wide therapeutic index, as dosing varies highly from patient to patient.8,9,10,11,13,14,15 Patients should be counselled regarding the risk of hypercorticism and adrenal axis suppression.8,9,10,11,13,14,15
- Mechanism of action
The short term effects of corticosteroids are decreased vasodilation and permeability of capillaries, as well as decreased leukocyte migration to sites of inflammation.1 Corticosteroids binding to the glucocorticoid receptor mediates changes in gene expression that lead to multiple downstream effects over hours to days.1
Glucocorticoids inhibit neutrophil apoptosis and demargination; they inhibit phospholipase A2, which decreases the formation of arachidonic acid derivatives; they inhibit NF-Kappa B and other inflammatory transcription factors; they promote anti-inflammatory genes like interleukin-10.1
Lower doses of corticosteroids provide an anti-inflammatory effect, while higher doses are immunosuppressive.1 High doses of glucocorticoids for an extended period bind to the mineralocorticoid receptor, raising sodium levels and decreasing potassium levels.1
Target Actions Organism AGlucocorticoid receptor antagonistHumans UAnnexin A1 substrateHumans - Absorption
Extended release oral capsules are 9-21% bioavailable.8,9 A 9mg dose reaches a Cmax of 1.50±0.79ng/mL with a Tmax of 2-8h and an AUC of 7.33ng*hr/mL.8,9 A high fat meal increases the Tmax by 2.3h but otherwise does not affect the pharmacokinetics of budesonide.8,9
180-360µg metered inhaled doses of budesonide are 34% deposited in the lungs, 39% bioavailable, and reach a Cmax of 0.6-1.6nmol/L with a Tmax of 10 minutes.10
A 1mg nebulized dose is 6% bioavailable, reaching a Cmax of 2.6nmol/L with a Tmax of 20 minutes.11
A 9mg oral extended release tablet reaches a Cmax of 1.35±0.96ng/mL with a Tmax of 13.3±5.9h and an AUC of 16.43±10.52ng*hr/mL.14
Budesonide rectal foam 2mg twice daily has an AUC of 4.31ng*hr/mL.15
- Volume of distribution
The volume of distribution of budesonide is 2.2-3.9L/kg.8,9,10,11,14,15
- Protein binding
Corticosteroids are generally bound to corticosteroid binding globulin2 and serum albumin3 in plasma. Budesonide is 85-90% protein bound in plasma.8,9,10,11,14,15
- Metabolism
Budesonide is 80-90% metabolized at first pass.4 Budesonide is metabolized by CYP3A4 to its 2 major metabolites, 6beta-hydroxybudesonide and 16alpha-hydroxyprednisolone.4 The glucocorticoid activity of these metabolites is negligible (<1/100) in relation to that of the parent compound.4
Hover over products below to view reaction partners
- Route of elimination
Approximately 60% of a budesonide dose is recovered in the urine as the major metabolites 6beta-hydroxybudesonide, 16alpha-hydroxyprednisolone, and their conjugates.8,9,10,11,13,14,15 No unchanged budesonide is recovered in urine.8,9,10,11,13,14,15
- Half-life
Budesonide has a plasma elimination half life of 2-3.6h.8,9,10,14 The terminal elimination half life in asthmatic children 4-6 years old is 2.3h.11
- Clearance
Budesonide has a plasma clearance of 0.9-1.8L/min.8,9,14,15 The 22R form has a clearance of 1.4L/min while the 22S form has a clearance of 1.0L/min.10 The clearance in asthmatic children 4-6 years old is 0.5L/min.11,13
- Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More- Toxicity
Acute overdose of corticosteroids is rare, however prolonged high dosing of corticosteroids can lead to hypercorticism and adrenal axis suppression.8,9,10,11,13,14,15 In the case of overdose, reduce the dosage of corticosteroids temporarily.8,9,10,11,13,14,15
A 200mg oral dose is lethal to female mice while a 400mg oral dose is lethal to male mice.8,9,14
- Affected organisms
- Humans and other mammals
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
Interacting Gene/Enzyme Allele name Genotype(s) Defining Change(s) Type(s) Description Details T-box transcription factor TBX21 --- (C;G) CG allele (heterozygotes) Effect Directly Studied The presence of this polymorphism in TBX21 may be associated with improved responsiveness to budenoside for the treatment of asthma. Details
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Unlock Additional DataAbacavir Abacavir may decrease the excretion rate of Budesonide which could result in a higher serum level. Abametapir The serum concentration of Budesonide can be increased when it is combined with Abametapir. Abatacept The risk or severity of adverse effects can be increased when Budesonide is combined with Abatacept. Abiraterone The metabolism of Abiraterone can be increased when combined with Budesonide. Acalabrutinib The metabolism of Acalabrutinib can be increased when combined with Budesonide. Acarbose The risk or severity of hyperglycemia can be increased when Acarbose is combined with Budesonide. Aceclofenac The risk or severity of gastrointestinal irritation can be increased when Aceclofenac is combined with Budesonide. Acemetacin The risk or severity of gastrointestinal irritation can be increased when Acemetacin is combined with Budesonide. Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Budesonide. Acetaminophen Acetaminophen may decrease the excretion rate of Budesonide which could result in a higher serum level. Additional Data Available- Extended DescriptionExtended DescriptionAvailable for Purchase
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - SeveritySeverityAvailable for Purchase
A severity rating for each drug interaction, from minor to major.
Learn more - Evidence LevelEvidence LevelAvailable for Purchase
A rating for the strength of the evidence supporting each drug interaction.
Learn more - ActionActionAvailable for Purchase
An effect category for each drug interaction. Know how this interaction affects the subject drug.
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- Food Interactions
- Take with or without food. Food delays drug absorption, but not to a clinically significant extent.
Products
Purchasing individual compounds or compound libraries for your research?
Learn More- Product Images
- International/Other Brands
- Bidien / Budeson / Budicort / Noex (Eurofarma) / Pulmicort (AstraZeneca) / Rhinosol / Spirocort
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataBudesonide Capsule 3 mg/1 Oral Paddock Laboratories, LLC 2018-06-29 Not applicable US 
Budesonide Capsule, extended release 3 mg Oral Tillotts Pharma Gmbh 2020-01-17 Not applicable Canada 
Budesonide Spray, metered 32 ug/1 Nasal Astra Zeneca Lp 2014-05-13 2018-02-28 US Budesonide/formoterol Teva Respiratory (inhalation) Teva Pharma B.V. 2014-11-19 2017-01-31 EU 
Budesonide/formoterol Teva Respiratory (inhalation) Teva Pharma B.V. 2014-11-19 2017-01-31 EU Cortiment Tablet, extended release Oral Ferring Pharmaceuticals 2016-07-25 Not applicable Canada Entocort Capsule, extended release Oral Tillotts Pharma Gmbh 1997-01-30 Not applicable Canada Entocort EC Capsule 3 mg/1 Oral Paddock Laboratories, LLC 2001-10-29 Not applicable US Entocort EC Capsule 3 mg/1 Oral AstraZeneca Pharmaceuticals LP 2001-10-02 2019-01-31 US Entocort EC Capsule 3 mg/1 Oral Prometheus Laboratories 2001-10-29 Not applicable US Additional Data Available- Application NumberApplication NumberAvailable for Purchase
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct CodeAvailable for Purchase
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
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- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataBudesonide Suspension 1 mg/2mL Respiratory (inhalation) Sandoz Inc 2015-07-24 Not applicable US Budesonide Capsule 3 mg/1 Oral Appco Pharma Llc 2017-06-01 Not applicable US Budesonide Suspension 0.5 mg/2mL Respiratory (inhalation) Physicians Total Care, Inc. 2009-02-04 Not applicable US Budesonide Inhalant 0.25 mg/2mL Respiratory (inhalation) Nephron Sc Inc. 2013-10-01 Not applicable US Budesonide Capsule 3 mg/1 Oral Mylan Institutional Inc. 2011-09-02 Not applicable US Budesonide Capsule 3 mg/1 Oral Golden State Medical Supply, Inc. 2011-05-16 Not applicable US Budesonide Suspension 0.5 mg/2mL Respiratory (inhalation) Apotex Corp. 2009-03-30 2021-06-20 US Budesonide Suspension 0.5 mg/2mL Respiratory (inhalation) Preferred Pharmaceuticals Inc. 2016-11-03 2020-04-07 US Budesonide Spray, metered 32 ug/1 Nasal Par Pharmaceutical 2014-10-21 2016-11-03 US Budesonide Capsule, coated pellets 3 mg/1 Oral Zydus Pharmaceuticals (USA) Inc. 2017-06-08 Not applicable US Additional Data Available- Application NumberApplication NumberAvailable for Purchase
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct CodeAvailable for Purchase
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
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- Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataBudesonide Spray, metered 32 ug/1 Nasal RUGBY LABORATORIES 2016-07-13 Not applicable US Budesonide Spray, metered 32 ug/1 Nasal Rite Aid 2016-07-13 Not applicable US Budesonide Spray, metered 32 ug/1 Nasal Apotex Corp. 2018-04-26 Not applicable US Budesonide Spray, metered 32 ug/1 Nasal Safeway 2016-09-15 Not applicable US Budesonide Spray, metered 32 ug/1 Nasal Apotex Corp. 2016-04-19 Not applicable US Budesonide Spray, metered 32 ug/1 Nasal Rite Aid 2019-10-10 Not applicable US Budesonide Spray, metered 32 ug/1 Nasal Amerisource Bergen 2016-09-15 Not applicable US Budesonide Spray, metered 32 ug/1 Nasal Topco Associates LLC 2016-08-31 2020-07-31 US Budesonide Spray, metered 32 ug/1 Nasal CVS Health 2016-04-09 Not applicable US Budesonide Spray, metered 32 ug/1 Nasal Walmart 2016-08-22 Not applicable US Additional Data Available- Application NumberApplication NumberAvailable for Purchase
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct CodeAvailable for Purchase
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
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- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Breztri Budesonide (160 ug/1) + Formoterol (4.8 ug/1) + Glycopyrronium bromide (9 ug/1) Aerosol, metered Respiratory (inhalation) AstraZeneca Pharmaceuticals LP 2020-07-23 Not applicable US Budesonide and Formoterol Fumarate Dihydrate Budesonide (160 ug/1) + Formoterol fumarate (4.5 ug/1) Aerosol Respiratory (inhalation) AstraZeneca Pharmaceuticals LP 2020-01-03 Not applicable US Budesonide and Formoterol Fumarate Dihydrate Budesonide (80 ug/1) + Formoterol fumarate (4.5 ug/1) Aerosol Respiratory (inhalation) AstraZeneca Pharmaceuticals LP 2020-01-03 Not applicable US Entocort Enema Budesonide (2.3 mg) + Sodium chloride (115 ml) Enema; Kit; Tablet Rectal Tillotts Pharma Gmbh 1994-12-31 Not applicable Canada Symbicort Budesonide (160 ug/1) + Formoterol fumarate (4.5 ug/1) Aerosol Respiratory (inhalation) Remedy Repack 2016-04-04 2016-04-05 US Symbicort Budesonide (80 ug/1) + Formoterol fumarate (4.5 ug/1) Aerosol Respiratory (inhalation) AstraZeneca Pharmaceuticals LP 2007-05-29 Not applicable US Symbicort Budesonide (160 ug/1) + Formoterol fumarate (4.5 ug/1) Aerosol Respiratory (inhalation) A-S Medication Solutions 2007-05-29 Not applicable US Symbicort Budesonide (160 ug/1) + Formoterol fumarate (4.5 ug/1) Aerosol Respiratory (inhalation) AstraZeneca Pharmaceuticals LP 2007-05-29 Not applicable US Symbicort 100 Turbuhaler Budesonide (100 mcg) + Formoterol fumarate (6 mcg) Powder Respiratory (inhalation) Astra Zeneca 2002-02-08 Not applicable Canada Symbicort 200 Turbuhaler Budesonide (200 mcg) + Formoterol fumarate (6 mcg) Powder Respiratory (inhalation) Astra Zeneca 2002-02-08 Not applicable Canada
Categories
- ATC Codes
- R03AL11 — Formoterol, glycopyrronium bromide and budesonide
- R03AL — Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
- R03A — ADRENERGICS, INHALANTS
- R03 — DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
- R — RESPIRATORY SYSTEM
- D07AC — Corticosteroids, potent (group III)
- D07A — CORTICOSTEROIDS, PLAIN
- D07 — CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
- D — DERMATOLOGICALS
- R01AD — Corticosteroids
- R01A — DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
- R01 — NASAL PREPARATIONS
- R — RESPIRATORY SYSTEM
- R03AK — Adrenergics in combination with corticosteroids or other drugs, excl. anticholinergics
- R03A — ADRENERGICS, INHALANTS
- R03 — DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
- R — RESPIRATORY SYSTEM
- A07EA — Corticosteroids acting locally
- A07E — INTESTINAL ANTIINFLAMMATORY AGENTS
- A07 — ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS
- A — ALIMENTARY TRACT AND METABOLISM
- R03BA — Glucocorticoids
- R03B — OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS
- R03 — DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
- R — RESPIRATORY SYSTEM
- Drug Categories
- Adrenal Cortex Hormones
- Adrenals
- Agents to Treat Airway Disease
- Alimentary Tract and Metabolism
- Anti-Asthmatic Agents
- Anti-Inflammatory Agents
- Antidiarrheals, Intestinal Antiinflammatory/antiinfective Agents
- Autonomic Agents
- Bronchodilator Agents
- BSEP/ABCB11 Substrates
- Corticosteroid Hormone Receptor Agonists
- Corticosteroids
- Corticosteroids Acting Locally
- Corticosteroids for Systemic Use
- Corticosteroids, Dermatological Preparations
- Corticosteroids, Potent (Group III)
- Cytochrome P-450 CYP2A6 Inducers
- Cytochrome P-450 CYP2B6 Inducers
- Cytochrome P-450 CYP2B6 Inducers (strength unknown)
- Cytochrome P-450 CYP2C19 Inducers
- Cytochrome P-450 CYP2C19 Inducers (strength unknown)
- Cytochrome P-450 CYP2C8 Inducers
- Cytochrome P-450 CYP2C8 Inducers (strength unknown)
- Cytochrome P-450 CYP2C9 Inducers
- Cytochrome P-450 CYP2C9 Inducers (strength unknown)
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inducers
- Cytochrome P-450 CYP3A4 Inducers (strength unknown)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Inducers
- Cytochrome P-450 CYP3A5 Inducers (moderate)
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Substrates
- Dermatologicals
- Drugs for Obstructive Airway Diseases
- Drugs that are Mainly Renally Excreted
- Fused-Ring Compounds
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Immunosuppressive Agents
- Intestinal Antiinflammatory Agents
- Nasal Preparations
- OAT3/SLC22A8 Substrates
- P-glycoprotein substrates
- Peripheral Nervous System Agents
- Pregnanes
- Pregnenediones
- Pregnenes
- Respiratory System Agents
- Steroids
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as 21-hydroxysteroids. These are steroids carrying a hydroxyl group at the 21-position of the steroid backbone.
- Kingdom
- Organic compounds
- Super Class
- Lipids and lipid-like molecules
- Class
- Steroids and steroid derivatives
- Sub Class
- Hydroxysteroids
- Direct Parent
- 21-hydroxysteroids
- Alternative Parents
- Gluco/mineralocorticoids, progestogins and derivatives / 20-oxosteroids / 3-oxo delta-1,4-steroids / 11-beta-hydroxysteroids / Delta-1,4-steroids / Alpha-hydroxy ketones / 1,3-dioxolanes / Secondary alcohols / Cyclic ketones / Cyclic alcohols and derivatives show 5 more
- Substituents
- 11-beta-hydroxysteroid / 11-hydroxysteroid / 20-oxosteroid / 21-hydroxysteroid / 3-oxo-delta-1,4-steroid / 3-oxosteroid / Acetal / Alcohol / Aliphatic heteropolycyclic compound / Alpha-hydroxy ketone show 17 more
- Molecular Framework
- Aliphatic heteropolycyclic compounds
- External Descriptors
- 11beta-hydroxy steroid, glucocorticoid, cyclic acetal, 20-oxo steroid, 3-oxo-Delta(1),Delta(4)-steroid, 21-hydroxy steroid (CHEBI:3207)
Chemical Identifiers
- UNII
- Q3OKS62Q6X
- CAS number
- 51333-22-3
- InChI Key
- VOVIALXJUBGFJZ-KWVAZRHASA-N
- 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
- IUPAC Name
- (1S,2S,4R,8S,9S,11S,12S,13R)-11-hydroxy-8-(2-hydroxyacetyl)-9,13-dimethyl-6-propyl-5,7-dioxapentacyclo[10.8.0.0²,⁹.0⁴,⁸.0¹³,¹⁸]icosa-14,17-dien-16-one
- SMILES
- [H][[email protected]@]12C[[email protected]]3OC(CCC)O[[email protected]@]3(C(=O)CO)[[email protected]@]1(C)C[[email protected]](O)[[email protected]@]1([H])[[email protected]@]2([H])CCC2=CC(=O)C=C[[email protected]]12C
References
- Synthesis Reference
Peter Gruber, Hans Joachim Lach, Norbert Otterbeck, "Budesonide pellets with a controlled released pattern and process for producing the same." U.S. Patent US5932249, issued May, 1991.
US5932249- General References
- Yasir M, Sonthalia S: Corticosteroid Adverse Effects . [PubMed:30285357]
- Gardill BR, Vogl MR, Lin HY, Hammond GL, Muller YA: Corticosteroid-binding globulin: structure-function implications from species differences. PLoS One. 2012;7(12):e52759. doi: 10.1371/journal.pone.0052759. Epub 2012 Dec 26. [PubMed:23300763]
- Czock D, Keller F, Rasche FM, Haussler U: Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids. Clin Pharmacokinet. 2005;44(1):61-98. doi: 10.2165/00003088-200544010-00003. [PubMed:15634032]
- O'Donnell S, O'Morain CA: Therapeutic benefits of budesonide in gastroenterology. Ther Adv Chronic Dis. 2010 Jul;1(4):177-86. doi: 10.1177/2040622310379293. [PubMed:23251737]
- Ellul-Micallef R, Hansson E, Johansson SA: Budesonide: a new corticosteroid in bronchial asthma. Eur J Respir Dis. 1980 Jun;61(3):167-73. [PubMed:7002575]
- Roth G, Wikby A, Nilsson L, Thalen A: High-performance liquid chromatographic determination of epimers, impurities, and content of the glucocorticoid budesonide and preparation of primary standard. J Pharm Sci. 1980 Jul;69(7):766-70. doi: 10.1002/jps.2600690705. [PubMed:7391935]
- FDA Approved Drug Products: Rhinocort Budesonide Nasal Metered Aerosol (Discontinued) [Link]
- FDA Approved Drug Products: Entocort Budesonide Oral Extended Release Capsules [Link]
- FDA Approved Drug Products: Ortikos Budesonide Oral Extended Release Capsules [Link]
- FDA Approved Drug Products: Pulmicort Budesonide Inhalation Powder [Link]
- FDA Approved Drug Products: Pulmicort Budesonide Inhalation Suspension [Link]
- FDA Approved Drug Products: Rhinocort Budesonide Nasal Metered Spray [Link]
- FDA Approved Drug Products: Symbicort (budesonide/formoterol fumarate) inhalation aerosol [Link]
- FDA Approved Drug Products: Uceris Budesonide Oral Extended Release Tablets [Link]
- FDA Approved Drug Products: Uceris Budesonide Rectal Aerosol Foam [Link]
- External Links
- Human Metabolome Database
- HMDB0015353
- KEGG Drug
- D00246
- PubChem Compound
- 5281004
- PubChem Substance
- 46504869
- ChemSpider
- 4444479
- BindingDB
- 50354850
- 19831
- ChEBI
- 3207
- ChEMBL
- CHEMBL1370
- Therapeutic Targets Database
- DAP000320
- PharmGKB
- PA448681
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Budesonide
- AHFS Codes
- 68:04.00 — Adrenals
- 52:08.00 — Anti-inflammatory Agents
- 56:36.00 — Anti-inflammatory Agents
- 52:08.08 — Corticosteroids
- FDA label
- Download (52.3 KB)
- MSDS
- Download (73.7 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Airway Inflammation / Asthma 1 4 Completed Not Available Asthma 1 4 Completed Basic Science Chronic Obstructive Pulmonary Disease (COPD) 2 4 Completed Basic Science Mild Intermittent Asthma 1 4 Completed Other Asthma 1 4 Completed Prevention Asthma 1 4 Completed Supportive Care Asthma 1 4 Completed Supportive Care Lung Cancers 1 4 Completed Treatment Allergic Rhinitis (AR) 1 4 Completed Treatment Allergic Rhinosinusitis / Bacterial Sinusitis / Chronic Eosinophilic Rhinosinusitis 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- 3M Health Care
- A-S Medication Solutions LLC
- Astra Pharma Inc.
- AstraZeneca Inc.
- Dispensing Solutions
- Galderma Laboratories
- Ivax Pharmaceuticals
- Kaiser Foundation Hospital
- Lake Erie Medical and Surgical Supply
- Physicians Total Care Inc.
- Prometheus Laboratories Inc.
- Redpharm Drug
- Spectrum Pharmaceuticals
- Teva Pharmaceutical Industries Ltd.
- Dosage Forms
Form Route Strength Powder Respiratory (inhalation) 3 mcg Powder Respiratory (inhalation) 6 mcg Powder Respiratory (inhalation) 160 µg Aerosol; suspension Respiratory (inhalation) 200 mcg Aerosol; suspension Respiratory (inhalation) 400 mcg Spray Nasal 100 MICROGRAMMI Spray Nasal 50 MICROGRAMMI Spray Nasal 50 UG Aerosol Buccal 50 mcg Aerosol Oral; Respiratory (inhalation) 0.3256 % Spray, suspension Nasal 50 mcg/1dose Spray Nasal Cream Cutaneous 0.025 % Ointment 0.025 % Solution Respiratory (inhalation) 0.025 % Spray, suspension Respiratory (inhalation) 0.25 MG/ML Spray, suspension Respiratory (inhalation) 0.5 MG/ML Powder Respiratory (inhalation) 12 mcg Aerosol, metered Respiratory (inhalation) Spray Nasal 0.05 mg/0.051g Aerosol, metered Respiratory (inhalation) 100 mcg/1dose Powder Respiratory (inhalation) 0.2 mg Aerosol Respiratory (inhalation) 100 mcg Aerosol Respiratory (inhalation) 0.132 g Aerosol Respiratory (inhalation) 0.263 g Suspension Respiratory (inhalation) 0.025 % w/v Aerosol, foam Rectal 2 mg/1dose Capsule Capsule, delayed release Oral 3 mg Capsule, coated Oral 3 mg Aerosol Rectal 2 mg Gas Respiratory (inhalation) 0.2 MG Spray Nasal 32 UG Spray Nasal 64 UG Spray Nasal 0.05 mg/0.051mL Solution Respiratory (inhalation) Aerosol, powder Respiratory (inhalation) 0.2 MG Aerosol, powder Respiratory (inhalation) 0.4 MG Aerosol, powder Respiratory (inhalation) 0.1 MG Suspension Respiratory (inhalation) 0.5 mg Suspension Respiratory (inhalation) 1 mg Aerosol, metered Respiratory (inhalation) 200 mcg/1dose Capsule, coated pellets Oral 3 mg/1 Capsule, extended release Oral 3 mg Capsule, gelatin coated Oral 3 mg/1 Inhalant Respiratory (inhalation) 0.25 mg/2mL Inhalant Respiratory (inhalation) 0.5 mg/2mL Powder Not applicable 1 g/1g Suspension Respiratory (inhalation) Suspension Respiratory (inhalation) 1 mg/2mL Tablet, extended release Oral 9 mg/1 Tablet, film coated, extended release Oral 9 mg/1 Capsule, delayed release pellets Oral 3 mg/1 Aerosol Respiratory (inhalation) Inhalant Oral 0.25 mg/2mL Inhalant Oral 0.5 mg/2mL Inhalant Oral 1 mg/2mL Suspension Respiratory (inhalation) 25 MG/ML Suspension Respiratory (inhalation) 5 MG/ML Suspension Respiratory (inhalation) 0.25 MG/ML Suspension Respiratory (inhalation) 0.5 MG/ML Aerosol, powder Respiratory (inhalation) 200 mcg Powder Respiratory (inhalation) 200 MCG Powder Respiratory (inhalation) 400 MCG Powder Respiratory (inhalation) 160 MICROGRAMMI Powder Respiratory (inhalation) 320 MICROGRAMMI Suspension Buccal; Respiratory (inhalation) 40 mg Suspension Respiratory (inhalation) 200 mcg Aerosol, metered Respiratory (inhalation) 200 MCG Aerosol, metered Respiratory (inhalation) 0.2 mg Solution Respiratory (inhalation) 200 mcg Gas Respiratory (inhalation) 0.2 mg/1 Gas Respiratory (inhalation) 200 UG Gas Respiratory (inhalation) Granule, delayed release Oral 9 mg Aerosol, powder Respiratory (inhalation) 160 mcg/1 Aerosol, powder Respiratory (inhalation) 320 mcg/1 Aerosol, powder Respiratory (inhalation) 80 mcg/1 Spray, suspension Nasal 100 mcg/1dose Suspension Respiratory (inhalation) 500 mcg/2mL Aerosol Respiratory (inhalation) 0.1 mg Aerosol Respiratory (inhalation) 0.2 mg Tablet, extended release Oral Tablet, extended release Oral 9 mg Tablet Capsule Respiratory (inhalation) 0.2 mg/1 Capsule Respiratory (inhalation) 0.4 mg/1 Aerosol, powder Respiratory (inhalation) 160 mcg Aerosol, powder Respiratory (inhalation) 320 mcg Capsule Oral 3 MG Capsule, extended release Oral Tablet Rectal 0.02 mg/ml Capsule Oral 3 mg/1 Enema; kit; tablet Rectal Powder Respiratory (inhalation) 12 μg Solution Respiratory (inhalation) 80 mcg Powder Respiratory (inhalation) 4.5 µg Powder Respiratory (inhalation) 9 µg Aerosol, powder Respiratory (inhalation) 9 mcg Suspension Respiratory (inhalation) 100 mcg Capsule Respiratory (inhalation) 12 mcg Powder Respiratory (inhalation) 320 mcg Powder Respiratory (inhalation) 4.5 mcg Powder Respiratory (inhalation) 9 mcg Powder Respiratory (inhalation) 160 mcg Powder Respiratory (inhalation) 200 mcg/1dose Powder Respiratory (inhalation) Powder Respiratory (inhalation) 200 Mikrogramm Powder Respiratory (inhalation) 400 Mikrogramm Capsule Respiratory (inhalation) 100 mcg Aerosol, metered Respiratory (inhalation) 50 mcg Suspension Nasal; Respiratory (inhalation) 100 mcg Aerosol, foam Rectal 2 MG Tablet, orally disintegrating Oral Tablet, orally disintegrating Oral 1 MG Capsule Respiratory (inhalation) 200 MCG Capsule Respiratory (inhalation) 400 MCG Capsule Respiratory (inhalation) Capsule Respiratory (inhalation) 200 Mikrogramm Capsule Respiratory (inhalation) 200 UG Capsule Respiratory (inhalation) 400 Mikrogramm Capsule Respiratory (inhalation) 400 UG Spray, metered Nasal Capsule Oral 6 mg/1 Capsule Oral 9 mg/1 Powder Respiratory (inhalation) 2 mcg Powder Respiratory (inhalation) 4 mcg Powder Respiratory (inhalation) 100 MCG Spray, suspension Respiratory (inhalation) 0.125 MG/ML Powder, metered Respiratory (inhalation) 100 MICROGRAMMI Powder, metered Respiratory (inhalation) 200 MICROGRAMMI Powder, metered Respiratory (inhalation) 400 MICROGRAMMI Aerosol, powder Respiratory (inhalation) 194 μg Aerosol, powder Respiratory (inhalation) 380 μg Aerosol, powder Respiratory (inhalation) 97 μg Powder, metered Respiratory (inhalation) 100 mcg Powder, metered Respiratory (inhalation) 200 mcg Powder, metered Respiratory (inhalation) 400 mcg Aerosol, powder Respiratory (inhalation) 180 ug/1 Aerosol, powder Respiratory (inhalation) 90 ug/1 Spray Nasal 64 μg Suspension Respiratory (inhalation) 0.25 mg/2mL Suspension Respiratory (inhalation) 0.5 mg/2mL Aerosol, powder Respiratory (inhalation) 200 UG Aerosol, powder Respiratory (inhalation) Aerosol, powder Respiratory (inhalation) 400 UG Powder Respiratory (inhalation) 100 mcg/1dose Powder, metered Respiratory (inhalation) 200 ug/1 Spray, metered Nasal 32 ug/1 Spray, metered Nasal 64 mcg Spray, suspension Nasal 64 mcg/1dose Aerosol, metered Nasal Powder Nasal; Respiratory (inhalation) Suspension Respiratory (inhalation) 160 mcg Suspension Respiratory (inhalation) 320 mcg Suspension Respiratory (inhalation) 80 mcg Aerosol Respiratory (inhalation) Aerosol, powder Respiratory (inhalation) 4.5 mcg Powder, metered Respiratory (inhalation) 160 MICROGRAMMI Powder, metered Respiratory (inhalation) 320 MICROGRAMMI Powder, metered Respiratory (inhalation) 4.5 mcg Powder, metered Respiratory (inhalation) 9 mcg Powder Respiratory (inhalation) Powder Respiratory (inhalation) 320 mcg/1dose Aerosol, powder Respiratory (inhalation) 80 μg Aerosol, metered Respiratory (inhalation) 160 mcg/1dose Aerosol, metered Respiratory (inhalation) 40 mcg/1dose Aerosol, metered Respiratory (inhalation) 80 mcg/1dose Aerosol, metered; suspension Respiratory (inhalation) 160 mcg Suspension Buccal; Respiratory (inhalation) 160 mcg Suspension Buccal; Respiratory (inhalation) 80 mcg Aerosol, powder Respiratory (inhalation) 320 μg Aerosol, powder Respiratory (inhalation) 160 µg Powder Respiratory (inhalation) 160 mcg/1dose Powder Respiratory (inhalation) 80 mcg/1dose Powder, metered Respiratory (inhalation) 80 MICROGRAMMI Patch Cutaneous Suspension Solution Respiratory (inhalation) 0.4 g Suspension Respiratory (inhalation) 0.1 g Suspension Nasal; Respiratory (inhalation) 0.2 g Capsule Respiratory (inhalation) 9 mcg Aerosol, foam Rectal 28 mg/1 Kit Rectal 2 mg Capsule Respiratory (inhalation) 320 mcg - Prices
Unit description Cost Unit Budesonide micronized powder 346.5USD g DesOwen Lot w/Cetaphil Cream 0.05% Kit Box 255.84USD box Desowen 0.05% ointment kit 217.2USD kit Desowen 0.05% cream kit 212.4USD kit DesOwen 0.05% Lotion 118ml Bottle 183.17USD bottle Pulmicort Flexhaler 180 mcg/act Aerosol Inhaler 163.34USD inhaler Pulmicort 180 mcg flexhaler 157.06USD inhaler DesOwen 0.05% Lotion 59ml Bottle 123.38USD bottle Pulmicort Flexhaler 90 mcg/act Aerosol Inhaler 121.98USD inhaler Pulmicort 90 mcg flexhaler 117.29USD inhaler Rhinocort Aqua 32 mcg/act 8.6 gm Bottle 111.96USD bottle Rhinocort aqua nasal spray 13.93USD g Entocort EC 3 mg 24 Hour Capsule 13.86USD capsule Entocort ec 3 mg capsule 12.22USD capsule Budesonide 0.5 mg/2ml Suspension 2ml Plastic Container 9.73USD plastic Pulmicort 0.5 mg/2ml Suspension 2ml Plastic Container 9.24USD plastic Budesonide 0.25 mg/2ml Suspension 2ml Plastic Container 9.07USD plastic Entocort (115 Ml) 2.3 mg/enm Enema 8.93USD enema Pulmicort 1 mg/2 ml respule 8.89USD ml Pulmicort 0.25 mg/2ml Suspension 2ml Plastic Container 7.85USD plastic Pulmicort 0.5 mg/2 ml respule 4.45USD ml Pulmicort 0.25 mg/2 ml respul 3.78USD ml Desowen 0.05% cream 2.43USD g Pulmicort Nebuamp 0.5 mg/ml Suspension 0.93USD ml Pulmicort Turbuhaler 400 mcg/dose Metered Inhalation Powder 0.62USD dose Pulmicort Nebuamp 0.25 mg/ml Suspension 0.46USD ml Pulmicort Turbuhaler 200 mcg/dose Metered Inhalation Powder 0.34USD dose Pulmicort Nebuamp 0.125 mg/ml Suspension 0.23USD ml Pulmicort Turbuhaler 100 mcg/dose Metered Inhalation Powder 0.17USD dose Rhinocort Turbuhaler 100 mcg/dose Metered Dose Aerosol 0.13USD dose Mylan-Budesonide Aq 100 mcg/dose Metered Dose Spray 0.1USD dose DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region Unlock Additional DataUS6423340 No 2002-07-23 2010-11-15 US CA2071518 No 2002-11-12 2010-11-15 Canada US6598603 Yes 2003-07-29 2019-06-23 US US6899099 Yes 2005-05-31 2019-06-23 US US7524834 Yes 2009-04-28 2019-05-11 US US7759328 Yes 2010-07-20 2023-07-29 US US7897646 Yes 2011-03-01 2019-03-09 US US8143239 Yes 2012-03-27 2023-07-29 US US8461211 Yes 2013-06-11 2019-03-09 US US8575137 Yes 2013-11-05 2023-07-29 US US6123924 No 2000-09-26 2017-09-26 US US7967011 Yes 2011-06-28 2022-02-11 US US8616196 Yes 2013-12-31 2029-10-07 US US8387615 Yes 2013-03-05 2025-05-10 US US7587988 Yes 2009-09-15 2026-10-10 US US7367333 Yes 2008-05-06 2019-05-11 US US8528545 Yes 2013-09-10 2029-04-16 US US8875699 Yes 2014-11-04 2025-05-10 US US6027714 No 2000-02-22 2018-01-09 US US7143764 No 2006-12-05 2018-03-13 US US6142145 No 2000-11-07 2018-05-08 US US6287540 No 2001-09-11 2018-01-09 US US9320716 No 2016-04-26 2020-06-09 US US9192581 No 2015-11-24 2031-09-07 US US7410651 No 2008-08-12 2020-06-09 US USRE43799 No 2012-11-13 2020-06-09 US US8895064 No 2014-11-25 2031-09-07 US US7431943 No 2008-10-07 2020-06-09 US US9132093 No 2015-09-15 2031-09-07 US US8784888 No 2014-07-22 2020-06-09 US US8293273 No 2012-10-23 2020-06-09 US US5914122 No 1999-06-22 2015-12-19 US US9532954 No 2017-01-03 2020-06-09 US US9463161 No 2016-10-11 2030-05-28 US US9415009 No 2016-08-16 2030-05-28 US US8808713 No 2014-08-19 2030-05-28 US US8324266 No 2012-12-04 2030-05-28 US US8703806 No 2014-04-22 2030-05-28 US US8815258 No 2014-08-26 2031-03-17 US US10064878 No 2018-09-04 2020-06-09 US US10105374 No 2018-10-23 2020-06-09 US US10166247 Yes 2019-01-01 2023-07-29 US US10143698 No 2018-12-04 2020-06-09 US US9707182 No 2017-07-18 2036-09-09 US US10172802 No 2019-01-08 2036-09-09 US US10307375 No 2019-06-04 2031-09-07 US US10660858 No 2011-09-07 2031-09-07 US US10716753 No 2010-05-28 2030-05-28 US Additional Data Available- Filed OnFiled OnAvailable for Purchase
The date on which a patent was filed with the relevant government.
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Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 226°C PhysProp boiling point (°C) 599.7 ChemSpider logP 1.914 ChemSpider - Predicted Properties
Property Value Source Water Solubility 0.0457 mg/mL ALOGPS logP 2.42 ALOGPS logP 2.73 ChemAxon logS -4 ALOGPS pKa (Strongest Acidic) 13.74 ChemAxon pKa (Strongest Basic) -2.9 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 6 ChemAxon Hydrogen Donor Count 2 ChemAxon Polar Surface Area 93.06 Å2 ChemAxon Rotatable Bond Count 4 ChemAxon Refractivity 116.11 m3·mol-1 ChemAxon Polarizability 47.11 Å3 ChemAxon Number of Rings 5 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter Yes ChemAxon Veber's Rule No ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9872 Blood Brain Barrier + 0.9533 Caco-2 permeable - 0.6097 P-glycoprotein substrate Substrate 0.804 P-glycoprotein inhibitor I Non-inhibitor 0.5881 P-glycoprotein inhibitor II Non-inhibitor 0.5911 Renal organic cation transporter Non-inhibitor 0.7867 CYP450 2C9 substrate Non-substrate 0.8488 CYP450 2D6 substrate Non-substrate 0.9116 CYP450 3A4 substrate Substrate 0.7337 CYP450 1A2 substrate Non-inhibitor 0.9046 CYP450 2C9 inhibitor Non-inhibitor 0.9075 CYP450 2D6 inhibitor Non-inhibitor 0.9441 CYP450 2C19 inhibitor Non-inhibitor 0.939 CYP450 3A4 inhibitor Inhibitor 0.796 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8886 Ames test Non AMES toxic 0.9117 Carcinogenicity Non-carcinogens 0.9466 Biodegradation Not ready biodegradable 0.9759 Rat acute toxicity 2.1601 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9483 hERG inhibition (predictor II) Non-inhibitor 0.5627
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available LC-MS/MS Spectrum - LC-ESI-qTof , Positive LC-MS/MS Not Available LC-MS/MS Spectrum - LC-ESI-qTof , Positive LC-MS/MS Not Available MS/MS Spectrum - , positive LC-MS/MS splash10-03k9-1794300000-d4cdef973973a6b24ba4 MS/MS Spectrum - , positive LC-MS/MS splash10-00dj-3950000000-8e98d604876730f53851
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Zinc ion binding
- Specific Function
- Receptor for glucocorticoids (GC). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modula...
- Gene Name
- NR3C1
- Uniprot ID
- P04150
- Uniprot Name
- Glucocorticoid receptor
- Molecular Weight
- 85658.57 Da
References
- Zhang X, Moilanen E, Kankaanranta H: Enhancement of human eosinophil apoptosis by fluticasone propionate, budesonide, and beclomethasone. Eur J Pharmacol. 2000 Oct 20;406(3):325-32. [PubMed:11040338]
- Henriksson G, Norlander T, Forsgren J, Stierna P: Effects of topical budesonide treatment on glucocorticoid receptor mRNA down-regulation and cytokine patterns in nasal polyps. Am J Rhinol. 2001 Jan-Feb;15(1):1-8. [PubMed:11258648]
- Zhang X, Moilanen E, Kankaanranta H: Beclomethasone, budesonide and fluticasone propionate inhibit human neutrophil apoptosis. Eur J Pharmacol. 2001 Nov 23;431(3):365-71. [PubMed:11730731]
- Kompella UB, Bandi N, Ayalasomayajula SP: Subconjunctival nano- and microparticles sustain retinal delivery of budesonide, a corticosteroid capable of inhibiting VEGF expression. Invest Ophthalmol Vis Sci. 2003 Mar;44(3):1192-201. [PubMed:12601049]
- Kunz S, Sandoval R, Carlsson P, Carlstedt-Duke J, Bloom JW, Miesfeld RL: Identification of a novel glucocorticoid receptor mutation in budesonide-resistant human bronchial epithelial cells. Mol Endocrinol. 2003 Dec;17(12):2566-82. Epub 2003 Aug 14. [PubMed:12920235]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Structural molecule activity
- Specific Function
- Plays important roles in the innate immune response as effector of glucocorticoid-mediated responses and regulator of the inflammatory process. Has anti-inflammatory activity (PubMed:8425544). Play...
- Gene Name
- ANXA1
- Uniprot ID
- P04083
- Uniprot Name
- Annexin A1
- Molecular Weight
- 38713.855 Da
References
- Serres M, Viac J, Comera C, Schmitt D: Expression of annexin I in freshly isolated human epidermal cells and in cultured keratinocytes. Arch Dermatol Res. 1994;286(5):268-72. [PubMed:8060156]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInducer
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Jonsson G, Astrom A, Andersson P: Budesonide is metabolized by cytochrome P450 3A (CYP3A) enzymes in human liver. Drug Metab Dispos. 1995 Jan;23(1):137-42. [PubMed:7720517]
- Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [PubMed:11996015]
- Chen N, Cui D, Wang Q, Wen Z, Finkelman RD, Welty D: In vitro drug-drug interactions of budesonide: inhibition and induction of transporters and cytochrome P450 enzymes. Xenobiotica. 2018 Jun;48(6):637-646. doi: 10.1080/00498254.2017.1344911. Epub 2017 Jul 21. [PubMed:28730856]
- Zimmermann C, van Waterschoot RA, Harmsen S, Maier A, Gutmann H, Schinkel AH: PXR-mediated induction of human CYP3A4 and mouse Cyp3a11 by the glucocorticoid budesonide. Eur J Pharm Sci. 2009 Mar 2;36(4-5):565-71. doi: 10.1016/j.ejps.2008.12.007. Epub 2008 Dec 24. [PubMed:19138736]
- Usui T, Saitoh Y, Komada F: Induction of CYP3As in HepG2 cells by several drugs. Association between induction of CYP3A4 and expression of glucocorticoid receptor. Biol Pharm Bull. 2003 Apr;26(4):510-7. doi: 10.1248/bpb.26.510. [PubMed:12673034]
- Pichard L, Fabre I, Daujat M, Domergue J, Joyeux H, Maurel P: Effect of corticosteroids on the expression of cytochromes P450 and on cyclosporin A oxidase activity in primary cultures of human hepatocytes. Mol Pharmacol. 1992 Jun;41(6):1047-55. [PubMed:1614409]
- Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [PubMed:24451000]
- FDA Approved Drug Products: Entocort Budesonide Oral Extended Release Capsules [Link]
- FDA Approved Drug Products: Ortikos Budesonide Oral Extended Release Capsules [Link]
- FDA Approved Drug Products: Pulmicort Budesonide Inhalation Powder [Link]
- FDA Approved Drug Products: Pulmicort Budesonide Inhalation Suspension [Link]
- FDA Approved Drug Products: Rhinocort Budesonide Nasal Metered Spray [Link]
- FDA Approved Drug Products: Symbicort (budesonide/formoterol fumarate) inhalation aerosol [Link]
- FDA Approved Drug Products: Uceris Budesonide Oral Extended Release Tablets [Link]
- FDA Approved Drug Products: Uceris Budesonide Rectal Aerosol Foam [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inducer
- General Function
- Oxygen binding
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [PubMed:11996015]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInducer
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Components:
| Name | UniProt ID |
|---|---|
| Cytochrome P450 3A4 | P08684 |
| Cytochrome P450 3A43 | Q9HB55 |
| Cytochrome P450 3A5 | P20815 |
| Cytochrome P450 3A7 | P24462 |
References
- Roberts JK, Moore CD, Romero EG, Ward RM, Yost GS, Reilly CA: Regulation of CYP3A genes by glucocorticoids in human lung cells. F1000Res. 2013 Aug 13;2:173. doi: 10.12688/f1000research.2-173.v2. eCollection 2013. [PubMed:24555085]
- Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [PubMed:24451000]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Steroid hydroxylase activity
- Specific Function
- Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Const...
- Gene Name
- CYP2A6
- Uniprot ID
- P11509
- Uniprot Name
- Cytochrome P450 2A6
- Molecular Weight
- 56501.005 Da
References
- Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [PubMed:24451000]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Oxygen binding
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1B1
- Uniprot ID
- Q16678
- Uniprot Name
- Cytochrome P450 1B1
- Molecular Weight
- 60845.33 Da
References
- Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [PubMed:24451000]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2B6
- Uniprot ID
- P20813
- Uniprot Name
- Cytochrome P450 2B6
- Molecular Weight
- 56277.81 Da
References
- Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [PubMed:24451000]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C8
- Uniprot ID
- P10632
- Uniprot Name
- Cytochrome P450 2C8
- Molecular Weight
- 55824.275 Da
References
- Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [PubMed:24451000]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [PubMed:24451000]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55930.545 Da
References
- Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [PubMed:24451000]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Steroid binding
- Specific Function
- Major transport protein for glucocorticoids and progestins in the blood of almost all vertebrate species.
- Gene Name
- SERPINA6
- Uniprot ID
- P08185
- Uniprot Name
- Corticosteroid-binding globulin
- Molecular Weight
- 45140.49 Da
References
- Gardill BR, Vogl MR, Lin HY, Hammond GL, Muller YA: Corticosteroid-binding globulin: structure-function implications from species differences. PLoS One. 2012;7(12):e52759. doi: 10.1371/journal.pone.0052759. Epub 2012 Dec 26. [PubMed:23300763]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
- Czock D, Keller F, Rasche FM, Haussler U: Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids. Clin Pharmacokinet. 2005;44(1):61-98. doi: 10.2165/00003088-200544010-00003. [PubMed:15634032]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Transporter activity
- Specific Function
- Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
- Gene Name
- ABCB11
- Uniprot ID
- O95342
- Uniprot Name
- Bile salt export pump
- Molecular Weight
- 146405.83 Da
References
- Pedersen JM, Matsson P, Bergstrom CA, Hoogstraate J, Noren A, LeCluyse EL, Artursson P: Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43. doi: 10.1093/toxsci/kft197. Epub 2013 Sep 6. [PubMed:24014644]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Chen N, Cui D, Wang Q, Wen Z, Finkelman RD, Welty D: In vitro drug-drug interactions of budesonide: inhibition and induction of transporters and cytochrome P450 enzymes. Xenobiotica. 2018 Jun;48(6):637-646. doi: 10.1080/00498254.2017.1344911. Epub 2017 Jul 21. [PubMed:28730856]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibit...
- Gene Name
- SLCO1A2
- Uniprot ID
- P46721
- Uniprot Name
- Solute carrier organic anion transporter family member 1A2
- Molecular Weight
- 74144.105 Da
References
- Bossuyt X, Muller M, Hagenbuch B, Meier PJ: Polyspecific drug and steroid clearance by an organic anion transporter of mammalian liver. J Pharmacol Exp Ther. 1996 Mar;276(3):891-6. [PubMed:8786566]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
- Gene Name
- SLC22A8
- Uniprot ID
- Q8TCC7
- Uniprot Name
- Solute carrier family 22 member 8
- Molecular Weight
- 59855.585 Da
References
- VanWert AL, Gionfriddo MR, Sweet DH: Organic anion transporters: discovery, pharmacology, regulation and roles in pathophysiology. Biopharm Drug Dispos. 2010 Jan;31(1):1-71. doi: 10.1002/bdd.693. [PubMed:19953504]
Drug created on June 13, 2005 07:24 / Updated on October 31, 2020 10:29
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