NAV

Budesonide

Identification

Summary

Budesonideis a corticosteroid used to treat Crohn's disease, asthma, COPD, hay fever and allergies, and ulcerative colitis.

Brand Names
Breyna, Breztri, Cortiment, Entocort, Ortikos, Pulmicort, Pulmicort Turbuhaler, Rhinocort, Symbicort, Tarpeyo, Uceris
总的来说ic Name
Budesonide
DrugBank Accession Number
DB01222
Background

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 1994.8It is also available in a combination product withformoterol.14

Type
Small Molecule
Groups
Approved
Structure
 3D
Similar Structures
Weight
Average: 430.5339
Monoisotopic: 430.23553882
Chemical Formula
C25H34O6
Synonyms
  • (-16年11β,16α),17 - (Butylidenebis(氧))-11年,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.9,10Various inhaled budesonide products are indicated for prophylactic therapy in asthma11,12,14and to reduce exacerbations of COPD.14A budesonide nasal spray is available over the counter for symptoms of hay fever and upper respiratory allergies.13Extended-release capsules are indicated to induce remission of mild to moderate ulcerative colitis15and a rectal foam is used for mild to moderate distal ulcerative colitis.16In addition, a delayed-release capsule formulation of budesonide is indicated to reduce proteinuria in adults with IgA nephropathy at risk of rapid disease progression.17,19In Europe, budesonide is indicated to treat eosinophilic esophagitis (EoE) in adults.20

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Associated Conditions
Associated Therapies
Contraindications & Blackbox Warnings
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Pharmacodynamics

Budesonide is a glucocorticoid used to treat respiratory and digestive conditions by reducing inflammation.9,10,11,12,14,15,16It has a wide therapeutic index, as dosing varies highly from patient to patient.9,10,11,12,14,15,16Patients should be counselled regarding the risk of hypercorticism and adrenal axis suppression.9,10,11,12,14,15,16

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.1Corticosteroids binding to the glucocorticoid receptor mediates changes in gene expression that lead to multiple downstream effects over hours to days.1

糖皮质激素抑制中性粒细胞凋亡和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.1High 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
agonist
 Humans
UAnnexin A1
substrate
 Humans
Absorption

Extended release oral capsules are 9-21% bioavailable.9,10A 9mg dose reaches a Cmaxof 1.50±0.79ng/mL with a Tmaxof 2-8h and an AUC of 7.33ng*hr/mL.9,10A high fat meal increases the Tmaxby 2.3h but otherwise does not affect the pharmacokinetics of budesonide.9,10

180-360µg metered inhaled doses of budesonide are 34% deposited in the lungs, 39% bioavailable, and reach a Cmaxof 0.6-1.6nmol/L with a Tmaxof 10 minutes.11

A 1mg nebulized dose is 6% bioavailable, reaching a Cmaxof 2.6nmol/L with a Tmaxof 20 minutes.12

A 9mg oral extended release tablet reaches a Cmaxof 1.35±0.96ng/mL with a Tmaxof 13.3±5.9h and an AUC of 16.43±10.52ng*hr/mL.15

Budesonide rectal foam 2mg twice daily has an AUC of 4.31ng*hr/mL.16

Volume of distribution

The volume of distribution of budesonide is 2.2-3.9L/kg.9,10,11,12,15,16

Protein binding

Corticosteroids are generally bound to corticosteroid binding globulin2and serum albumin3in plasma. Budesonide is 85-90% protein bound in plasma.9,10,11,12,15,16

Metabolism

Budesonide is 80-90% metabolized at first pass.4Budesonide is metabolized by CYP3A to its 2 major metabolites, 6beta-hydroxybudesonide and 16alpha-hydroxyprednisolone.4,7The glucocorticoid activity of these metabolites is negligible (<1/100) in relation to that of the parent compound.4CYP3A4 is the strongest metabolizer of budesonide, followed by CYP3A5, and CYP3A7.7

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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.9,10,11,12,14,15,16No unchanged budesonide is recovered in urine.9,10,11,12,14,15,16

Half-life

Budesonide has a plasma elimination half life of 2-3.6h.9,10,11,15The terminal elimination half life in asthmatic children 4-6 years old is 2.3h.12

Clearance

Budesonide has a plasma clearance of 0.9-1.8L/min.9,10,15,16The 22R form has a clearance of 1.4L/min while the 22S form has a clearance of 1.0L/min.11The clearance in asthmatic children 4-6 years old is 0.5L/min.12,14

Adverse Effects
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Toxicity

Acute overdose of corticosteroids is rare, however prolonged high dosing of corticosteroids can lead to hypercorticism and adrenal axis suppression.9,10,11,12,14,15,16In the case of overdose, reduce the dosage of corticosteroids temporarily.9,10,11,12,14,15,16

A 200mg oral dose is lethal to female mice while a 400mg oral dose is lethal to male mice.9,10,15

Pathways
Not Available
Pharmacogenomic Effects/ADRsBrowse all" title="" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
Interacting Gene/Enzyme Allele name Genotype(s) Defining Change(s) Type(s) Description Details
T-box transcription factor TBX21 --- (C;G) CG allele (heterozygotes) EffectDirectly Studied The presence of this polymorphism in TBX21 may be associated with improved responsiveness to budenoside for the treatment of asthma. Details

Interactions

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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
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Abacavir 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.
Abemaciclib The metabolism of Abemaciclib 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 Budesonide is combined with Acarbose.
Aceclofenac The risk or severity of gastrointestinal irritation can be increased when Budesonide is combined with Aceclofenac.
Acemetacin The risk or severity of gastrointestinal irritation can be increased when Budesonide is combined with Acemetacin.
Acenocoumarol Budesonide may increase the anticoagulant activities of Acenocoumarol.
对乙酰氨基酚 对乙酰氨基酚may decrease the excretion rate of Budesonide which could result in a higher serum level.
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Food Interactions
  • Take with or without food. Food delays drug absorption, but not to a clinically significant extent.

Products

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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
Budesonide Capsule, extended release 3 mg Oral Tillotts Pharma Gmbh 2020-01-17 Not applicable Canada flag
Budesonide Aerosol, foam 28 mg/1 Rectal Oceanside Pharmaceuticals 2022-07-15 Not applicable US flag
Budesonide Capsule 3 mg/1 Oral Padagis US LLC 2018-06-29 Not applicable US flag
Budesonide Spray, metered 32 ug/1 Nasal Astra Zeneca Lp 2014-05-13 2018-02-28 US flag
Cortiment Tablet, extended release 9 mg Oral Ferring Pharmaceuticals 2016-07-25 Not applicable Canada flag
Entocort Capsule, extended release 3 mg Oral Tillotts Pharma Gmbh 1997-01-30 Not applicable Canada flag
Entocort EC Capsule 3 mg/1 Oral Padagis US LLC 2001-10-29 Not applicable US flag
Entocort EC Capsule 3 mg/1 Oral AstraZeneca Pharmaceuticals LP 2001-10-02 2019-01-31 US flag
Entocort EC Capsule 3 mg/1 Oral Prometheus Laboratories 2001-10-29 Not applicable US flag
Entocort EC Capsule 3 mg/1 Oral Physicians Total Care, Inc. 2006-05-22 Not applicable US flag
总的来说ic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image
Budesonide Suspension 0.25 mg/2mL Respiratory (inhalation) Apotex Corp. 2009-03-30 2021-06-20 US flag
Budesonide Capsule, delayed release 3 mg/1 Oral Amneal Pharmaceuticals LLC 2017-09-15 Not applicable US flag
Budesonide 胶囊,涂pellets 3 mg/1 Oral American Health Packaging 2021-03-09 Not applicable US flag
Budesonide Capsule, delayed release 3 mg/1 Oral Major Pharmaceuticals 2017-09-15 Not applicable US flag
Budesonide Spray, metered 32 ug/1 Nasal Par Pharmaceutical 2014-10-21 2016-11-03 US flag
Budesonide 胶囊,涂pellets 3 mg/1 Oral Zydus Lifesciences Limited 2017-06-08 Not applicable US flag
Budesonide Suspension 0.25 mg/2mL Respiratory (inhalation) Teva Pharmaceuticals USA, Inc. 2008-11-19 Not applicable US flag
Budesonide Suspension 0.25 mg/2mL Respiratory (inhalation) Sandoz Inc 2015-07-24 Not applicable US flag
Budesonide Suspension 0.5 mg/2mL Respiratory (inhalation) Preferred Pharmaceuticals Inc. 2016-11-03 2020-04-07 US flag
Budesonide Capsule 3 mg/1 Oral Carilion Materials Management 2013-08-23 Not applicable US flag
Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image
Budesonide Spray, metered 32 ug/1 Nasal Apotex Corp. 2018-04-26 Not applicable US flag
Budesonide Spray, metered 32 ug/1 Nasal Safeway 2016-09-15 2023-10-24 US flag
Budesonide Spray, metered 32 ug/1 Nasal Apotex Corp. 2016-04-19 Not applicable US flag
Budesonide Spray, metered 32 ug/1 Nasal Rite Aid 2019-10-10 Not applicable US flag
Budesonide Spray, metered 32 ug/1 Nasal Amerisource Bergen 2016-09-15 Not applicable US flag
Budesonide Spray, metered 32 ug/1 Nasal Topco Associates LLC 2016-08-31 2020-07-31 US flag
Budesonide Spray, metered 32 ug/1 Nasal CVS PHARMACY 2016-04-09 Not applicable US flag
Budesonide Spray, metered 32 ug/1 Nasal Walmart 2016-08-22 Not applicable US flag
Budesonide Spray, metered 32 ug/1 Nasal Walgreens 2016-04-11 Not applicable US flag
Budesonide Spray, metered 32 ug/1 Nasal RUGBY LABORATORIES 2016-07-13 Not applicable US flag
Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image
AIRBIR 3/100 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL, 120 KPS Budesonide(100 mcg)+Arformoterol(3 mcg) Powder Respiratory (inhalation) NEUTEC İNHALER İLAÇ SAN. VE TİC. A.Ş. 2020-08-14 Not applicable Turkey flag
AIRBIR 3/100 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL, 60 KPS Budesonide(100 mcg)+Arformoterol(3 mcg) Powder Respiratory (inhalation) NEUTEC İNHALER İLAÇ SAN. VE TİC. A.Ş. 2020-08-14 Not applicable Turkey flag
AIRBIR 3/200 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL ,120 KAPSÜL Budesonide（200 mcg)+Arformoterol(3 mcg) Powder Respiratory (inhalation) NEUTEC İNHALER İLAÇ SAN. VE TİC. A.Ş. 2020-08-14 Not applicable Turkey flag
AIRBIR 3/200 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL ,60 KAPSÜL Budesonide（200 mcg)+Arformoterol(3 mcg) Powder Respiratory (inhalation) NEUTEC İNHALER İLAÇ SAN. VE TİC. A.Ş. 2020-08-14 Not applicable Turkey flag
AIRBIR 6/200 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL, 120 ADET Budesonide（200 mcg)+Arformoterol(6 mcg) Powder Respiratory (inhalation) NEUTEC İNHALER İLAÇ SAN. VE TİC. A.Ş. 2020-08-14 Not applicable Turkey flag
AIRBIR 6/200 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL, 60 ADET Budesonide（200 mcg)+Arformoterol(6 mcg) Powder Respiratory (inhalation) NEUTEC İNHALER İLAÇ SAN. VE TİC. A.Ş. 2020-08-14 Not applicable Turkey flag
AIRBIR 6/400 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL, 120 KPS Budesonide(400 mcg)+Arformoterol(6 mcg) Powder Respiratory (inhalation) NEUTEC İNHALER İLAÇ SAN. VE TİC. A.Ş. 2020-08-14 Not applicable Turkey flag
AIRBIR 6/400 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL, 60 KPS Budesonide(400 mcg)+Arformoterol(6 mcg) Powder Respiratory (inhalation) NEUTEC İNHALER İLAÇ SAN. VE TİC. A.Ş. 2020-08-14 Not applicable Turkey flag
AIRBUFO FORSPIRO 160/4.5UG Budesonide(160 µg)+Formoterol fumarate(4.5 µg) Powder Respiratory (inhalation) 2016-07-01 Not applicable Germany flag
AIRBUFO FORSPIRO 160/4.5UG Budesonide(160 µg)+Formoterol fumarate(4.5 µg) Powder Respiratory (inhalation) 2016-07-01 Not applicable Germany flag

Categories

ATC Codes
R03AL11 — Formoterol, glycopyrronium bromide and budesonide D07AC09 — Budesonide R01AD05 — Budesonide R03AK07 — Formoterol and budesonide A07EA06 — Budesonide R03BA02 — Budesonide R03AK12 — Salmeterol and budesonide
Drug Categories
Chemical TaxonomyProvided byClassyfire
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)
Affected organisms
  • Humans and other mammals

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[10.8.0.0^{2,9}.0^{4,8}.0^{13,18}]icosa-14,17-dien-16-one
SMILES
[H][C@@]12C[C@H]3OC(CCC)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@H](O)[C@@]1([H])[C@@]2([H])CCC2=CC(=O)C=C[C@]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
总的来说al References
  1. Yasir M, Sonthalia S: Corticosteroid Adverse Effects . [Article]
  2. 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. [Article]
  3. 凯勒Czock D, F, Rasche调频,Haussler U:药学kinetics and pharmacodynamics of systemically administered glucocorticoids. Clin Pharmacokinet. 2005;44(1):61-98. doi: 10.2165/00003088-200544010-00003. [Article]
  4. 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. [Article]
  5. Ellul-Micallef R, Hansson E, Johansson SA: Budesonide: a new corticosteroid in bronchial asthma. Eur J Respir Dis. 1980 Jun;61(3):167-73. [Article]
  6. 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. [Article]
  7. 摩尔CD,罗伯茨JK,奥尔顿CR、井T,费德勒TP, Reilly CA, Ward RM, Yost GS: Metabolic pathways of inhaled glucocorticoids by the CYP3A enzymes. Drug Metab Dispos. 2013 Feb;41(2):379-89. doi: 10.1124/dmd.112.046318. Epub 2012 Nov 9. [Article]
  8. FDA批准的药物产品:Rhinocort布地奈德Nasal Metered Aerosol (Discontinued) [Link]
  9. FDA Approved Drug Products: Entocort Budesonide Oral Extended Release Capsules [Link]
  10. FDA Approved Drug Products: Ortikos Budesonide Oral Extended Release Capsules [Link]
  11. FDA批准的药物产品:Pulmicort布地奈德nhalation Powder [Link]
  12. FDA批准的药物产品:Pulmicort布地奈德nhalation Suspension [Link]
  13. FDA批准的药物产品:Rhinocort布地奈德Nasal Metered Spray [Link]
  14. FDA Approved Drug Products: Symbicort (budesonide/formoterol fumarate) inhalation aerosol [Link]
  15. FDA Approved Drug Products: Uceris Budesonide Oral Extended Release Tablets [Link]
  16. FDA Approved Drug Products: Uceris Budesonide Rectal Aerosol Foam [Link]
  17. FDA Approved Drug Products: Tarpeyo (budesonide) delayed-release capsules for oral use [Link]
  18. BioSpace News: Viatris Inc. Announces Receipt of the First FDA Approval for Generic Version of Symbicort® Inhalation Aerosol, Breyna™ (Budesonide and Formoterol Fumarate Dihydrate Inhalation Aerosol), in Partnership with Kindeva [Link]
  19. EMA Approved Drug Products: Kinpeygo (budesonide) Oral Capsules [Link]
  20. EMA Approved Drug Products: Jorveza (budesonide) Oral Tablets [Link]
  21. FDA Approved Drug Products: AIRSUPRA (albuterol and budesonide) inhalation aerosol, for oral inhalation use [Link]
Human Metabolome Database
HMDB0015353
KEGG Drug
D00246
PubChem Compound
5281004
PubChem Substance
46504869
ChemSpider
4444479
BindingDB
50354850
RxNav
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
FDA label
Download (52.3 KB)
MSDS
Download (73.7 KB)

Clinical Trials

Clinical TrialsLearn More" title="" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count
4 Active Not Recruiting Basic Science Environmental Exposures/Epigenetic Effects of Intranasal Steroids 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 Cancer 1
4 Completed Treatment Acute Lymphocytic Leukemia, Pediatric/Asthma 1
4 Completed Treatment Airway Inflammation/Asthma 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, metered Respiratory (inhalation)
Aerosol; suspension Respiratory (inhalation) 200 mcg
Aerosol; suspension Respiratory (inhalation) 400 mcg
Spray Nasal 100 MICROGRAMMI
Spray Nasal 50 MICROGRAMMI
Spray Nasal 50微克
Aerosol Buccal 50 mcg
Solution Nasal; Respiratory (inhalation) 0.1 g
Aerosol Oral; Respiratory (inhalation) 0.3256 %
Ointment Topical 25 mg
Aerosol Respiratory (inhalation) 200 cg
Spray, suspension Nasal 50 mcg/1dose
Spray Nasal 1.28 mg
Spray, metered Nasal
Lotion Topical 0.025 g
Cream Topical 0025 %
Ointment Cutaneous 0025 %
Solution Topical 0025 %
Spray, suspension Respiratory (inhalation) 0.25 MG/ML
Spray, suspension Respiratory (inhalation) 0.5 MG/ML
Aerosol, metered Respiratory (inhalation)
Solution Nasal; Respiratory (inhalation) 80 mg
Suspension Buccal; Respiratory (inhalation) 400 cg
Suspension Respiratory (inhalation) 0.05 mg
Spray Nasal 0.05 mg/0.051g
Aerosol, metered Respiratory (inhalation) 100 mcg
Aerosol Respiratory (inhalation) 0.2 % w/v
Aerosol Respiratory (inhalation) 0.132 g
Aerosol Respiratory (inhalation) 0.263 g
Suspension Respiratory (inhalation) 0.025 % w/v
Capsule
胶囊,涂 Oral 3 mg
Capsule 3 mg
Suppository 4 mg
Aerosol, foam Rectal 2 mg/1dose
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 Respiratory (inhalation) 0.25 g
Aerosol, powder Respiratory (inhalation) 0.1 MG
Suspension Respiratory (inhalation) 0.022 g
Suspension Respiratory (inhalation) 1 mg
Suspension Respiratory (inhalation) 200 cg
Aerosol Respiratory (inhalation) 200 mcg
Suspension Respiratory (inhalation) 0.4 g
Suspension Respiratory (inhalation) 0.01 g
Suspension Oral 0.1 mg
Aerosol, foam Rectal 2 mg/1
胶囊,涂pellets Oral 3 mg/1
Capsule, delayed release 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) 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
Spray, suspension Nasal 64 mcg/dose
Suspension Respiratory (inhalation) 25 MG/ML
Suspension Respiratory (inhalation) 5 MG/ML
Suspension Respiratory (inhalation) 0.25 MG/ML
Aerosol, powder Respiratory (inhalation) 200 mcg
Powder, metered Respiratory (inhalation) 200 MCG
Powder, metered Respiratory (inhalation) 400 MCG
Suspension Respiratory (inhalation) 100 mcg/1dose
Suspension Respiratory (inhalation) 200 mcg/1dose
Aerosol Respiratory (inhalation) 100 mcg
Suspension Buccal; Respiratory (inhalation) 40 mg
Suspension Respiratory (inhalation) 200 mcg
Solution Respiratory (inhalation) 200 mcg
Gas Respiratory (inhalation) 0.2 mg/1
Aerosol, metered Respiratory (inhalation) 200 Mikrogramm
Gas Respiratory (inhalation) 200 UG
Aerosol, metered Respiratory (inhalation) 0.2 mg/actuation
Aerosol, foam Rectal 2 mg/spray
Capsule Oral 3 mg
Granule, delayed release Oral 9 mg
Spray, suspension Nasal 32 mcg
Spray, suspension Nasal 64 mcg
Spray Nasal 64 mcg
Suspension Nasal; Respiratory (inhalation) 100 cg
Suspension Oral 200 cg
Aerosol Respiratory (inhalation) 0.3125 g
Aerosol Respiratory (inhalation) 0.4 mg
Tablet, extended release Oral
Tablet, extended release Oral 9 mg
Tablet, film coated, extended release Oral 9 mg
Capsule Respiratory (inhalation) 0.2 mg/1
Capsule Respiratory (inhalation) 0.4 mg/1
Aerosol, metered Respiratory (inhalation) 200 MICROGRAMMI
Capsule Respiratory (inhalation)
胶囊,涂 Oral 0.4 mg
胶囊,涂 Oral 0.1 mg
Powder, metered Respiratory (inhalation) 160 mcg/inhalation
Powder, metered Respiratory (inhalation) 320 mcg/inhalation
Spray, suspension Nasal
Tablet Rectal 0.02 mg/ml
Enema; tablet Rectal 2.3 mg
Capsule, extended release Oral 3 mg
Capsule Oral 3 mg/1
Enema; kit; tablet Rectal
Tablet, soluble Oral 2.3 mg
Spray Nasal 2.0 mg/ml
Solution Respiratory (inhalation)
Capsule Respiratory (inhalation)
Powder Respiratory (inhalation) 400 mcg/1dose
Powder, metered Respiratory (inhalation) 200 mcg/dose
Powder Respiratory (inhalation) 100 mcg/1dose
Powder Respiratory (inhalation)
Powder, metered Respiratory (inhalation) 100 mcg
Suspension Respiratory (inhalation) 0.5 mg
Aerosol Respiratory (inhalation) 4 mg
Solution Respiratory (inhalation) 4 mg
Aerosol, metered Respiratory (inhalation) 50 mcg
Suspension Nasal; Respiratory (inhalation) 100 mcg
Suspension Respiratory (inhalation) 0.2 mg
Aerosol, foam Rectal 2 MG
Granule
Tablet, orally disintegrating Oral 0.5 mg
Tablet, orally disintegrating Oral 1 mg
Capsule, extended release Oral 4 mg
Cream Topical 0.25 g
Aerosol, metered Respiratory (inhalation) 200 MCG
Capsule Respiratory (inhalation) 200 Mikrogramm
Capsule Respiratory (inhalation) 200 UG
Capsule Respiratory (inhalation) 400 Mikrogramm
Capsule Respiratory (inhalation) 400 UG
Capsule, liquid filled Oral 200 cg
胶囊,涂 Respiratory (inhalation) 400 mcg
Powder Respiratory (inhalation) 200 mcg
Spray, metered Nasal 100 mcg / act
Spray, metered Nasal 64 mcg / act
Suspension Intrasinal; Respiratory (inhalation) 1 mg
Suspension Intrasinal; Respiratory (inhalation) 2 mg
Powder Respiratory (inhalation) 200 Mikrogramm
Powder Respiratory (inhalation) 400 Mikrogramm
Powder, metered Respiratory (inhalation) 200 mcg/1dose
Capsule Oral 6 mg/1
Capsule Oral 9 mg/1
Cream Topical
Ointment
Powder Respiratory (inhalation) 100 MCG
Powder Respiratory (inhalation) 400 MCG
Spray, suspension Respiratory (inhalation) 0125 MG/ML
Aerosol, powder Respiratory (inhalation) 180 ug/1
Aerosol, powder Respiratory (inhalation) 90 ug/1
Spray Nasal 64 μg
Suspension Respiratory (inhalation) 0.125 mg / mL
Suspension Respiratory (inhalation) 0.25 mg / mL
Suspension Respiratory (inhalation) 0.5 mg / mL
Suspension Respiratory (inhalation) 0.25 mg/2mL
Suspension Respiratory (inhalation) 0.5 mg/2mL
Aerosol Respiratory (inhalation) 0.5 mg/2ml
Aerosol Respiratory (inhalation) 1 mg/2ml
Suspension Respiratory (inhalation)
Suspension Respiratory (inhalation) 0.5 mg/ml
Solution Respiratory (inhalation) 500 mcg/2ml
Solution Respiratory (inhalation) 1 mg/2ml
Aerosol, powder Respiratory (inhalation) 200 UG
Aerosol, powder Respiratory (inhalation) 400 UG
Powder Respiratory (inhalation) 0.1 mg
Aerosol, powder Respiratory (inhalation) 0.2 mg
Aerosol, powder Respiratory (inhalation) 0.4 mg
Powder Respiratory (inhalation) 200 mcg/1dose
Powder, metered Respiratory (inhalation) 100 mcg / act
Powder, metered Respiratory (inhalation) 200 mcg / act
Powder, metered Respiratory (inhalation) 200 ug/1
Powder, metered Respiratory (inhalation) 400 mcg / act
Powder Respiratory (inhalation) 100 cg
Powder Respiratory (inhalation) 200 cg
Aerosol, metered Respiratory (inhalation)
Powder Respiratory (inhalation) 400 cg
Powder Nasal
Spray Nasal
Spray, metered Nasal 32 ug/1
Suspension Respiratory (inhalation) 1.28 mg
Spray, suspension Nasal 1.28 mg/mL
Aerosol, metered Nasal 100 mcg / act
Powder Nasal; Respiratory (inhalation) 100 mcg / act
Powder, metered Nasal 100 mcg
Solution Respiratory (inhalation) 40 mg
Solution Respiratory (inhalation) 48 % w/w
胶囊,涂 Respiratory (inhalation) 0.1 mg
Aerosol, metered Respiratory (inhalation) 200 mcg/1dose
Suspension Respiratory (inhalation) 0.25 mg
Powder, metered Respiratory (inhalation)
Spray, suspension Respiratory (inhalation)
Aerosol Respiratory (inhalation)
Aerosol, powder Respiratory (inhalation)
Powder Respiratory (inhalation)
Suspension Respiratory (inhalation)
Aerosol, metered; suspension Respiratory (inhalation)
Aerosol, metered Respiratory (inhalation) 160 mcg
Aerosol, metered Respiratory (inhalation) 40 mcg
Aerosol, metered Respiratory (inhalation) 80 mcg
Suspension Buccal; Respiratory (inhalation)
Powder, metered Respiratory (inhalation) 160 mcg
Powder, metered Respiratory (inhalation) 80 mcg
Kit Cutaneous
Capsule, delayed release Oral 4 mg/1
Solution Respiratory (inhalation) 0.4 g
Aerosol Respiratory (inhalation) 0.01 g
Suspension Respiratory (inhalation) 0.1 g
Suspension Nasal; Respiratory (inhalation) 0.2 % w/v
Suspension Nasal; Respiratory (inhalation) 0.2 g
Aerosol, foam Rectal 28 mg/1
Kit Rectal 2 mg / act
Aerosol Buccal 100 mcg
Aerosol Respiratory (inhalation) 100 mcg/1dose
Aerosol Respiratory (inhalation) 50 mcg/1dose
Spray Nasal 100 mcg/1dose
Capsule Respiratory (inhalation) 100 mcg
Capsule Respiratory (inhalation) 400 mcg
Spray Nasal 1.28 mg/mL
Capsule Respiratory (inhalation) 200 mcg
Spray Nasal 32 mcg/1dose
Spray, suspension Nasal 64 mcg/1dose
Aerosol Respiratory (inhalation) 200 mcg/1dose
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毫克/ 2毫升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
US6423340 No 2002-07-23 2010-11-15 US flag
CA2071518 No 2002-11-12 2010-11-15 Canada flag
US6598603 Yes 2003-07-29 2019-06-23 US flag
US6899099 Yes 2005-05-31 2019-06-23 US flag
US7524834 Yes 2009-04-28 2019-05-11 US flag
US7759328 Yes 2010-07-20 2023-07-29 US flag
US7897646 Yes 2011-03-01 2019-03-09 US flag
US8143239 Yes 2012-03-27 2023-07-29 US flag
US8461211 Yes 2013-06-11 2019-03-09 US flag
US8575137 Yes 2013-11-05 2023-07-29 US flag
US6123924 No 2000-09-26 2017-09-26 US flag
US7967011 Yes 2011-06-28 2022-02-11 US flag
US8616196 Yes 2013-12-31 2029-10-07 US flag
US8387615 Yes 2013-03-05 2025-05-10 US flag
US7587988 Yes 2009-09-15 2026-10-10 US flag
US7367333 Yes 2008-05-06 2019-05-11 US flag
US8528545 Yes 2013-09-10 2029-04-16 US flag
US8875699 Yes 2014-11-04 2025-05-10 US flag
US6027714 No 2000-02-22 2018-01-09 US flag
US7143764 No 2006-12-05 2018-03-13 US flag
US6142145 No 2000-11-07 2018-05-08 US flag
US6287540 No 2001-09-11 2018-01-09 US flag
US9320716 No 2016-04-26 2020-06-09 US flag
US9192581 No 2015-11-24 2031-09-07 US flag
US7410651 No 2008-08-12 2020-06-09 US flag
USRE43799 No 2012-11-13 2020-06-09 US flag
US8895064 No 2014-11-25 2031-09-07 US flag
US7431943 No 2008-10-07 2020-06-09 US flag
US9132093 No 2015-09-15 2031-09-07 US flag
US8784888 No 2014-07-22 2020-06-09 US flag
US8293273 No 2012-10-23 2020-06-09 US flag
US5914122 No 1999-06-22 2015-12-19 US flag
US9532954 No 2017-01-03 2020-06-09 US flag
US9463161 No 2016-10-11 2030-05-28 US flag
US9415009 No 2016-08-16 2030-05-28 US flag
US8808713 No 2014-08-19 2030-05-28 US flag
US8324266 No 2012-12-04 2030-05-28 US flag
US8703806 No 2014-04-22 2030-05-28 US flag
US8815258 No 2014-08-26 2031-03-17 US flag
US10064878 No 2018-09-04 2020-06-09 US flag
US10105374 No 2018-10-23 2020-06-09 US flag
US10166247 Yes 2019-01-01 2023-07-29 US flag
US10143698 No 2018-12-04 2020-06-09 US flag
US9707182 No 2017-07-18 2036-09-09 US flag
US10172802 No 2019-01-08 2036-09-09 US flag
US10307375 No 2019-06-04 2031-09-07 US flag
US10660858 No 2020-05-26 2031-09-07 US flag
US10716753 No 2020-07-21 2030-05-28 US flag
US8491932 No 2013-07-23 2029-05-07 US flag
US11311558 Yes 2003-07-29 2023-07-29 US flag
US11331442 No 2018-05-10 2038-05-10 US flag

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) 13.75 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 46.88 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
ADMET data is predicted usingadmetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

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

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Details 1.Glucocorticoid receptor
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
总的来说al 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
分子量
85658.57 Da
References
  1. 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. [Article]
  2. 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. [Article]
  3. 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. [Article]
  4. 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. [Article]
  5. 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. [Article]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Details 2.Annexin A1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
总的来说al 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
分子量
38713.855 Da
References
  1. 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. [Article]

Enzymes

Details 1.Cytochrome P450 3A5
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inducer
总的来说al 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
分子量
57108.065 Da
References
  1. Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [Article]
Details 2.Cytochrome P450 3A Subfamily (Protein Group)
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inducer
总的来说al 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
  1. 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. [Article]
  2. 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. [Article]
Details 3.Cytochrome P450 2A6
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
总的来说al 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
分子量
56501.005 Da
References
  1. 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. [Article]
Details 4.Cytochrome P450 1B1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
总的来说al 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
分子量
60845.33 Da
References
  1. 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. [Article]
Details 5.Cytochrome P450 2B6
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
总的来说al 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
分子量
56277.81 Da
References
  1. 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. [Article]
Details 6.Cytochrome P450 2C8
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
总的来说al 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
分子量
55824.275 Da
References
  1. 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. [Article]
Details 7.Cytochrome P450 2C9
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
总的来说al 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
分子量
55627.365 Da
References
  1. 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. [Article]
Details 8.Cytochrome P450 2C19
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
总的来说al 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
分子量
55930.545 Da
References
  1. 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. [Article]
Details 9.Cytochrome P450 3A4
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Inducer
总的来说al 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
分子量
57342.67 Da
References
  1. 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. [Article]
  2. Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [Article]
  3. 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. [Article]
  4. 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. [Article]
  5. 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. [Article]
  6. 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. [Article]
  7. 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. [Article]
  8. FDA Approved Drug Products: Entocort Budesonide Oral Extended Release Capsules [Link]
  9. FDA Approved Drug Products: Ortikos Budesonide Oral Extended Release Capsules [Link]
  10. FDA批准的药物产品:Pulmicort布地奈德nhalation Powder [Link]
  11. FDA批准的药物产品:Pulmicort布地奈德nhalation Suspension [Link]
  12. FDA批准的药物产品:Rhinocort布地奈德Nasal Metered Spray [Link]
  13. FDA Approved Drug Products: Symbicort (budesonide/formoterol fumarate) inhalation aerosol [Link]
  14. FDA Approved Drug Products: Uceris Budesonide Oral Extended Release Tablets [Link]
  15. FDA Approved Drug Products: Uceris Budesonide Rectal Aerosol Foam [Link]

Carriers

Details 1.Corticosteroid-binding globulin
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
总的来说al 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
分子量
45140.49 Da
References
  1. 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. [Article]
Details 2.Serum albumin
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
总的来说al 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
分子量
69365.94 Da
References
  1. 凯勒Czock D, F, Rasche调频,Haussler U:药学kinetics and pharmacodynamics of systemically administered glucocorticoids. Clin Pharmacokinet. 2005;44(1):61-98. doi: 10.2165/00003088-200544010-00003. [Article]

Transporters

Details 1.Bile salt export pump
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
总的来说al 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
分子量
146405.83 Da
References
  1. 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. [Article]
Details 2.P-glycoprotein 1
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
总的来说al 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
分子量
141477.255 Da
References
  1. 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. [Article]
Details 3.Solute carrier organic anion transporter family member 1A2
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
总的来说al 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
分子量
74144.105 Da
References
  1. 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. [Article]
Details 4.Solute carrier family 22 member 8
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
总的来说al 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
分子量
59855.585 Da
References
  1. 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. [Article]

Drug created at June 13, 2005 13:24 / Updated at April 28, 2023 03:25