Identification

Summary

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

Brand Names
Breztri, Cortiment, Entocort, Ortikos, Pulmicort, Pulmicort Turbuhaler, Rhinocort, Symbicort, Uceris
Generic 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 1994.8

Type
Small Molecule
Groups
Approved
Structure
Thumb
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.9,10 Various inhaled budesonide products are indicated for prophylactic therapy in asthma11,12,14 and reducing exacerbations of COPD.14 A budesonide nasal spray is available over the counter for symptoms of hay fever and upper respiratory allergies.13 Extended release capsules are indicated to induce remission of mild to moderate ulcerative colitis15 and a rectal foam is used for mild to moderate distal ulcerative colitis.16

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Budesonide is a glucocorticoid used to treat respiratory and digestive conditions by reducing inflammation.9,10,11,12,14,15,16 It has a wide therapeutic index, as dosing varies highly from patient to patient.9,10,11,12,14,15,16 Patients 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.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

TargetActionsOrganism
AGlucocorticoid receptor
agonist
Humans
UAnnexin A1
substrate
Humans
Absorption

Extended release oral capsules are 9-21% bioavailable.9,10 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.9,10 A high fat meal increases the Tmax by 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 Cmax of 0.6-1.6nmol/L with a Tmax of 10 minutes.11

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

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.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 globulin2 and serum albumin3 in plasma. Budesonide is 85-90% protein bound in plasma.9,10,11,12,15,16

Metabolism

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

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.9,10,11,12,14,15,16 No 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.9,10,11,15 The 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.9,10,15,16 The 22R form has a clearance of 1.4L/min while the 22S form has a clearance of 1.0L/min.11 The clearance in asthmatic children 4-6 years old is 0.5L/min.12,14

Adverse Effects
Adverseeffects
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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.9,10,11,12,14,15,16 In 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/ADRs
Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
T-box transcription factor TBX21---(C;G)CG allele (heterozygotes)Effect Directly StudiedThe 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.
DrugInteraction
AbacavirAbacavir may decrease the excretion rate of Budesonide which could result in a higher serum level.
AbametapirThe serum concentration of Budesonide can be increased when it is combined with Abametapir.
AbataceptThe risk or severity of adverse effects can be increased when Budesonide is combined with Abatacept.
AbemaciclibThe metabolism of Abemaciclib can be increased when combined with Budesonide.
AbirateroneThe metabolism of Budesonide can be decreased when combined with Abiraterone.
AcalabrutinibThe metabolism of Acalabrutinib can be increased when combined with Budesonide.
AcarboseThe risk or severity of hyperglycemia can be increased when Budesonide is combined with Acarbose.
AceclofenacThe risk or severity of gastrointestinal irritation can be increased when Budesonide is combined with Aceclofenac.
AcemetacinThe risk or severity of gastrointestinal irritation can be increased when Budesonide is combined with Acemetacin.
AcenocoumarolBudesonide may increase the anticoagulant activities of Acenocoumarol.
Interactions
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Food Interactions
  • Take with or without food. Food delays drug absorption, but not to a clinically significant extent.

Products

Products2
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Product Images
International/Other Brands
Bidien / Budeson / Budicort / Noex (Eurofarma) / Pulmicort (AstraZeneca) / Rhinosol / Spirocort
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
BudesonideSpray, metered32 ug/1NasalAstra Zeneca Lp2014-05-132018-02-28US flag
BudesonideCapsule, extended release3 mgOralTillotts Pharma Gmbh2020-01-17Not applicableCanada flag
BudesonideCapsule3 mg/1OralPaddock Laboratories, LLC.2018-06-29Not applicableUS flag
CortimentTablet, extended release9 mgOralFerring Pharmaceuticals2016-07-25Not applicableCanada flag
EntocortCapsule, extended release3 mgOralTillotts Pharma Gmbh1997-01-30Not applicableCanada flag
Entocort ECCapsule3 mg/1OralPrometheus Laboratories2001-10-29Not applicableUS flag65483 070220210417 24165 rox16
Entocort ECCapsule3 mg/1OralPhysicians Total Care, Inc.2006-05-22Not applicableUS flag65483 0702 10 nlmimage10 f6387b33
Entocort ECCapsule3 mg/1OralPaddock Laboratories, LLC2001-10-29Not applicableUS flag
Entocort ECCapsule3 mg/1OralAstraZeneca Pharmaceuticals LP2001-10-022019-01-31US flag
JorvezaTablet, orally disintegrating1 mgOralDr. Falk Pharma Gmb H2020-12-16Not applicableEU flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
BudesonideSuspension0.5 mg/2mLRespiratory (inhalation)Sun Pharmaceutical Industries, Inc.2021-05-01Not applicableUS flag
BudesonideSuspension0.5 mg/2mLRespiratory (inhalation)Cardinal Health2019-01-11Not applicableUS flag
BudesonideCapsule3 mg/1OralMylan Institutional Inc.2011-09-02Not applicableUS flag
BudesonideSuspension0.5 mg/2mLRespiratory (inhalation)Preferred Pharmaceuticals Inc.2016-11-032020-04-07US flag
BudesonideSuspension0.5 mg/2mLRespiratory (inhalation)Sandoz Inc2015-07-24Not applicableUS flag
BudesonideCapsule, coated pellets3 mg/1OralCadila Healthcare Limited2017-06-08Not applicableUS flag
BudesonideSuspension1 mg/2mLRespiratory (inhalation)Apotex Corp.2009-03-302009-03-31US flag
BudesonideCapsule3 mg/1OralGolden State Medical Supply, Inc.2011-05-16Not applicableUS flag
BudesonideSuspension0.5 mg/2mLRespiratory (inhalation)Preferred Pharmaceuticals, Inc.2009-02-042018-07-31US flag
BudesonideInhalant0.5 mg/2mLRespiratory (inhalation)Nephron Pharmaceuticals Corporation2013-10-01Not applicableUS flag
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
BudesonideSpray, metered32 ug/1NasalTopco Associates LLC2016-08-312020-07-31US flag
BudesonideSpray, metered32 ug/1NasalWalmart2016-08-22Not applicableUS flag
BudesonideSpray, metered32 ug/1NasalWalgreens2016-04-11Not applicableUS flag
BudesonideSpray, metered32 ug/1NasalRite Aid2016-07-13Not applicableUS flag
BudesonideSpray, metered32 ug/1NasalRUGBY LABORATORIES2016-07-13Not applicableUS flag
BudesonideSpray, metered32 ug/1NasalApotex Corp.2018-04-26Not applicableUS flag
BudesonideSpray, metered32 ug/1NasalApotex Corp.2016-04-19Not applicableUS flag
BudesonideSpray, metered32 ug/1NasalSafeway2016-09-15Not applicableUS flag
BudesonideSpray, metered32 ug/1NasalRite Aid2019-10-10Not applicableUS flag
BudesonideSpray, metered32 ug/1NasalAmerisource Bergen2016-09-15Not applicableUS flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
AIRBIR 3/100 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL, 120 KPSBudesonide (100 mcg) + Arformoterol (3 mcg)PowderRespiratory (inhalation)NEUTEC İLAÇ SAN. TİC. A.Ş.2020-08-14Not applicableTurkey flag
AIRBIR 3/100 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL, 60 KPSBudesonide (100 mcg) + Arformoterol (3 mcg)PowderRespiratory (inhalation)NEUTEC İLAÇ SAN. TİC. A.Ş.2020-08-14Not applicableTurkey flag
AIRBIR 3/200 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL ,120 KAPSÜLBudesonide (200 mcg) + Arformoterol (3 mcg)PowderRespiratory (inhalation)NEUTEC İLAÇ SAN. TİC. A.Ş.2020-08-14Not applicableTurkey flag
AIRBIR 3/200 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL ,60 KAPSÜLBudesonide (200 mcg) + Arformoterol (3 mcg)PowderRespiratory (inhalation)NEUTEC İLAÇ SAN. TİC. A.Ş.2020-08-14Not applicableTurkey flag
AIRBIR 6/200 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL, 120 ADETBudesonide (200 mcg) + Arformoterol (6 mcg)PowderRespiratory (inhalation)NEUTEC İLAÇ SAN. TİC. A.Ş.2020-08-14Not applicableTurkey flag
AIRBIR 6/200 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL, 60 ADETBudesonide (200 mcg) + Arformoterol (6 mcg)PowderRespiratory (inhalation)NEUTEC İLAÇ SAN. TİC. A.Ş.2020-08-14Not applicableTurkey flag
AIRBIR 6/400 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL, 120 KPSBudesonide (400 mcg) + Arformoterol (6 mcg)PowderRespiratory (inhalation)NEUTEC İLAÇ SAN. TİC. A.Ş.2020-08-14Not applicableTurkey flag
AIRBIR 6/400 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL, 60 KPSBudesonide (400 mcg) + Arformoterol (6 mcg)PowderRespiratory (inhalation)NEUTEC İLAÇ SAN. TİC. A.Ş.2020-08-14Not applicableTurkey flag
Biresp SpiromaxBudesonide (320 mcg) + Formoterol fumarate (9 mcg)Respiratory (inhalation)Teva Pharma B.V.2021-02-11Not applicableEU flag
Biresp SpiromaxBudesonide (160 mcg) + Formoterol fumarate (4.5 mcg)Respiratory (inhalation)Teva Pharma B.V.2021-02-11Not applicableEU flag

Categories

ATC Codes
R03AL11 — Formoterol, glycopyrronium bromide and budesonideD07AC09 — BudesonideR01AD05 — BudesonideR03AK07 — Formoterol and budesonideA07EA06 — BudesonideR03BA02 — BudesonideR03AK12 — Salmeterol and budesonide
Drug Categories
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)
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[10.8.0.0²,⁹.0⁴,⁸.0¹³,¹⁸]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
General 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. 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. [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. Moore CD, Roberts JK, Orton CR, Murai T, Fidler 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 Approved Drug Products: Rhinocort Budesonide 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 Approved Drug Products: Pulmicort Budesonide Inhalation Powder [Link]
  12. FDA Approved Drug Products: Pulmicort Budesonide Inhalation Suspension [Link]
  13. FDA Approved Drug Products: Rhinocort Budesonide 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]
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 Trials
PhaseStatusPurposeConditionsCount
4CompletedNot AvailableAsthma1
4CompletedBasic ScienceChronic Obstructive Pulmonary Disease (COPD)2
4CompletedBasic ScienceMild Intermittent Asthma1
4CompletedOtherAsthma1
4CompletedPreventionAsthma1
4CompletedSupportive CareAsthma1
4CompletedSupportive CareLung Cancers1
4CompletedTreatmentALL, Pediatric / Asthma1
4CompletedTreatmentAllergic Rhinitis (Disorder)1
4CompletedTreatmentAllergic Rhinosinusitis / Eosinophilic Chronic Rhinosinusitis / Rhino Sinusitis1

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
FormRouteStrength
Powder, meteredRespiratory (inhalation)
PowderRespiratory (inhalation)
Aerosol; suspensionRespiratory (inhalation)200 mcg
Aerosol; suspensionRespiratory (inhalation)400 mcg
SprayNasal100 MICROGRAMMI
SprayNasal50 MICROGRAMMI
SprayNasal50 UG
AerosolBuccal50 mcg
SolutionNasal; Respiratory (inhalation)0.1 g
AerosolOral; Respiratory (inhalation)0.3256 %
OintmentTopical25 mg
AerosolRespiratory (inhalation)200 cg
Spray, suspensionNasal50 mcg/1dose
SprayNasal1.28 mg
Spray, meteredNasal
LotionTopical0.025 g
CreamTopical0025 %
OintmentCutaneous0025 %
SolutionTopical0025 %
Spray, suspensionRespiratory (inhalation)0.25 MG/ML
Spray, suspensionRespiratory (inhalation)0.5 MG/ML
Aerosol, meteredRespiratory (inhalation)
SolutionNasal; Respiratory (inhalation)80 mg
SuspensionBuccal; Respiratory (inhalation)400 cg
SuspensionRespiratory (inhalation)0.05 mg
SprayNasal0.05 mg/0.051g
PowderRespiratory (inhalation)0.2 mg
AerosolRespiratory (inhalation)0.2 % w/v
AerosolRespiratory (inhalation)0.132 g
AerosolRespiratory (inhalation)0.263 g
SuspensionRespiratory (inhalation)0.025 % w/v
Capsule
Capsule, coatedOral3 mg
Capsule3 mg
Aerosol, foamRectal2 mg/1dose
AerosolRectal2 mg
GasRespiratory (inhalation)0.2 MG
SprayNasal32 UG
SprayNasal64 UG
SprayNasal0.05 mg/0.051mL
SolutionRespiratory (inhalation)
AerosolRespiratory (inhalation)0.25 g
Aerosol, powderRespiratory (inhalation)0.2 MG
Aerosol, powderRespiratory (inhalation)0.4 MG
Aerosol, powderRespiratory (inhalation)0.1 MG
SuspensionRespiratory (inhalation)0.022 g
SuspensionRespiratory (inhalation)1 mg
SuspensionRespiratory (inhalation)200 cg
AerosolRespiratory (inhalation)200 mcg
SuspensionRespiratory (inhalation)0.4 g
SuspensionRespiratory (inhalation)0.01 g
SuspensionOral0.1 mg
Capsule, coated pelletsOral3 mg/1
Capsule, delayed releaseOral3 mg/1
Capsule, gelatin coatedOral3 mg/1
InhalantRespiratory (inhalation)0.25 mg/2mL
InhalantRespiratory (inhalation)0.5 mg/2mL
PowderNot applicable1 g/1g
SuspensionRespiratory (inhalation)1 mg/2mL
Tablet, extended releaseOral9 mg/1
Tablet, film coated, extended releaseOral9 mg/1
Capsule, delayed release pelletsOral3 mg/1
AerosolRespiratory (inhalation)
InhalantOral0.25 mg/2mL
InhalantOral0.5 mg/2mL
InhalantOral1 mg/2mL
Spray, suspensionNasal64 mcg/dose
SuspensionRespiratory (inhalation)25 MG/ML
SuspensionRespiratory (inhalation)5 MG/ML
SuspensionRespiratory (inhalation)0.25 MG/ML
SuspensionRespiratory (inhalation)0.5 MG/ML
Aerosol, powderRespiratory (inhalation)200 mcg
Powder, meteredRespiratory (inhalation)200 MCG
Powder, meteredRespiratory (inhalation)400 MCG
SuspensionRespiratory (inhalation)100 mcg/1dose
SuspensionRespiratory (inhalation)200 mcg/1dose
SuspensionBuccal; Respiratory (inhalation)40 mg
AerosolRespiratory (inhalation)100 mcg
SuspensionRespiratory (inhalation)200 mcg
Aerosol, meteredRespiratory (inhalation)
GasRespiratory (inhalation)0.2 mg/1
GasRespiratory (inhalation)200 UG
Aerosol, meteredRespiratory (inhalation)0.2 mg/actuation
Aerosol, foamRectal
CapsuleOral
Granule, delayed releaseOral
SprayNasal64 mcg
SuspensionNasal; Respiratory (inhalation)100 cg
SuspensionOral200 cg
AerosolRespiratory (inhalation)0.3125 g
AerosolRespiratory (inhalation)0.4 mg
Tablet, extended releaseOral9 MG
Tablet, film coated, extended releaseOral9 mg
Tablet, extended releaseOral
CapsuleRespiratory (inhalation)0.2 mg/1
CapsuleRespiratory (inhalation)0.4 mg/1
Aerosol, meteredRespiratory (inhalation)200 MICROGRAMMI
Capsule, coatedOral0.4 mg
Capsule, coatedOral0.1 mg
Powder, meteredRespiratory (inhalation)160 mcg/inhalation
Powder, meteredRespiratory (inhalation)320 mcg/inhalation
Spray, suspensionNasal
CapsuleOral3 MG
TabletRectal
Enema; tabletRectal
Capsule, extended releaseOral3 mg
CapsuleOral3 mg/1
Enema; kit; tabletRectal
Tablet, solubleOral2.3 mg
SprayNasal2.0 mg/ml
SolutionRespiratory (inhalation)
CapsuleRespiratory (inhalation)
PowderRespiratory (inhalation)400 mcg/1dose
Powder, meteredRespiratory (inhalation)200 mcg/dose
PowderRespiratory (inhalation)100 mcg/1dose
PowderRespiratory (inhalation)
Powder, meteredRespiratory (inhalation)100 mcg
SuspensionRespiratory (inhalation)0.5 mg
AerosolRespiratory (inhalation)4 mg
SolutionRespiratory (inhalation)4 mg
SuspensionNasal; Respiratory (inhalation)
SuspensionRespiratory (inhalation)0.2 mg
Aerosol, foamRectal2 MG
Granule
Tablet, orally disintegratingOral0.5 MG
Tablet, orally disintegratingOral1 MG
CreamTopical0.25 g
Aerosol, meteredRespiratory (inhalation)200 MCG
CapsuleRespiratory (inhalation)
CapsuleRespiratory (inhalation)200 UG
CapsuleRespiratory (inhalation)400 UG
Capsule, liquid filledOral200 cg
Capsule, coatedRespiratory (inhalation)400 mcg
PowderRespiratory (inhalation)200 mcg
Spray, meteredNasal100 mcg / act
Spray, meteredNasal64 mcg / act
SuspensionIntrasinal; Respiratory (inhalation)1 mg
SuspensionIntrasinal; Respiratory (inhalation)2 mg
Powder, meteredRespiratory (inhalation)200 mcg/1dose
CapsuleOral6 mg/1
CapsuleOral9 mg/1
CreamTopical
Ointment
PowderRespiratory (inhalation)100 MCG
PowderRespiratory (inhalation)400 MCG
Spray, suspensionRespiratory (inhalation)0125 MG/ML
SuspensionRespiratory (inhalation)
Aerosol, powderRespiratory (inhalation)180 ug/1
Aerosol, powderRespiratory (inhalation)90 ug/1
SprayNasal64 μg
SuspensionRespiratory (inhalation)0.125 mg / mL
SuspensionRespiratory (inhalation)0.25 mg / mL
SuspensionRespiratory (inhalation)0.5 mg / mL
SuspensionRespiratory (inhalation)0.25 mg/2mL
SuspensionRespiratory (inhalation)0.5 mg/2mL
AerosolRespiratory (inhalation)0.5 mg/2ml
AerosolRespiratory (inhalation)1 mg/2ml
SolutionRespiratory (inhalation)500 mcg/2ml
SolutionRespiratory (inhalation)1 mg/2ml
Aerosol, powderRespiratory (inhalation)200 UG
Aerosol, powderRespiratory (inhalation)400 UG
Aerosol, powderRespiratory (inhalation)
PowderRespiratory (inhalation)200 mcg/1dose
Powder, meteredRespiratory (inhalation)100 mcg / act
Powder, meteredRespiratory (inhalation)200 ug/1
Powder, meteredRespiratory (inhalation)200 mcg / act
Powder, meteredRespiratory (inhalation)400 mcg / act
PowderRespiratory (inhalation)100 cg
PowderRespiratory (inhalation)200 cg
PowderRespiratory (inhalation)400 cg
PowderNasal
SprayNasal
Spray, meteredNasal32 ug/1
SuspensionRespiratory (inhalation)1.28 mg
Spray, suspensionNasal1.28 mg/mL
Aerosol, meteredNasal100 mcg / act
PowderNasal; Respiratory (inhalation)100 mcg / act
Powder, meteredNasal100 mcg
SolutionRespiratory (inhalation)40 mg
SolutionRespiratory (inhalation)48 % w/w
Capsule, coatedRespiratory (inhalation)0.1 mg
Aerosol, meteredRespiratory (inhalation)200 mcg/1dose
Powder, meteredRespiratory (inhalation)
Spray, suspensionRespiratory (inhalation)
AerosolRespiratory (inhalation)
Aerosol, powderRespiratory (inhalation)
SuspensionRespiratory (inhalation)
Aerosol, metered; suspensionRespiratory (inhalation)
Aerosol, meteredRespiratory (inhalation)160 mcg
Aerosol, meteredRespiratory (inhalation)40 mcg
Aerosol, meteredRespiratory (inhalation)80 mcg
SuspensionBuccal; Respiratory (inhalation)
Powder, meteredRespiratory (inhalation)160 mcg
Powder, meteredRespiratory (inhalation)80 mcg
Powder, meteredRespiratory (inhalation)320 mcg
PatchCutaneous
SolutionRespiratory (inhalation)0.4 g
AerosolRespiratory (inhalation)0.01 g
SuspensionRespiratory (inhalation)0.1 g
SuspensionNasal; Respiratory (inhalation)0.2 % w/v
SuspensionNasal; Respiratory (inhalation)0.2 g
Aerosol, foamRectal28 mg/1
KitRectal2 mg / act
AerosolBuccal100 mcg
AerosolRespiratory (inhalation)100 mcg/1dose
AerosolRespiratory (inhalation)50 mcg/1dose
SprayNasal100 mcg/1dose
CapsuleRespiratory (inhalation)100 mcg
CapsuleRespiratory (inhalation)400 mcg
SprayNasal1.28 mg/mL
CapsuleRespiratory (inhalation)200 mcg
SprayNasal32 mcg/1dose
Spray, suspensionNasal64 mcg/1dose
AerosolRespiratory (inhalation)200 mcg/1dose
Prices
Unit descriptionCostUnit
Budesonide micronized powder346.5USD g
DesOwen Lot w/Cetaphil Cream 0.05% Kit Box255.84USD box
Desowen 0.05% ointment kit217.2USD kit
Desowen 0.05% cream kit212.4USD kit
DesOwen 0.05% Lotion 118ml Bottle183.17USD bottle
Pulmicort Flexhaler 180 mcg/act Aerosol Inhaler163.34USD inhaler
Pulmicort 180 mcg flexhaler157.06USD inhaler
DesOwen 0.05% Lotion 59ml Bottle123.38USD bottle
Pulmicort Flexhaler 90 mcg/act Aerosol Inhaler121.98USD inhaler
Pulmicort 90 mcg flexhaler117.29USD inhaler
Rhinocort Aqua 32 mcg/act 8.6 gm Bottle111.96USD bottle
Rhinocort aqua nasal spray13.93USD g
Entocort EC 3 mg 24 Hour Capsule13.86USD capsule
Entocort ec 3 mg capsule12.22USD capsule
Budesonide 0.5 mg/2ml Suspension 2ml Plastic Container9.73USD plastic
Pulmicort 0.5 mg/2ml Suspension 2ml Plastic Container9.24USD plastic
Budesonide 0.25 mg/2ml Suspension 2ml Plastic Container9.07USD plastic
Entocort (115 Ml) 2.3 mg/enm Enema8.93USD enema
Pulmicort 1 mg/2 ml respule8.89USD ml
Pulmicort 0.25 mg/2ml Suspension 2ml Plastic Container7.85USD plastic
Pulmicort 0.5 mg/2 ml respule4.45USD ml
Pulmicort 0.25 mg/2 ml respul3.78USD ml
Desowen 0.05% cream2.43USD g
Pulmicort Nebuamp 0.5 mg/ml Suspension0.93USD ml
Pulmicort Turbuhaler 400 mcg/dose Metered Inhalation Powder0.62USD dose
Pulmicort Nebuamp 0.25 mg/ml Suspension0.46USD ml
Pulmicort Turbuhaler 200 mcg/dose Metered Inhalation Powder0.34USD dose
Pulmicort Nebuamp 0.125 mg/ml Suspension0.23USD ml
Pulmicort Turbuhaler 100 mcg/dose Metered Inhalation Powder0.17USD dose
Rhinocort Turbuhaler 100 mcg/dose Metered Dose Aerosol0.13USD dose
Mylan-Budesonide Aq 100 mcg/dose Metered Dose Spray0.1USD dose
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US6423340No2002-07-232010-11-15US flag
CA2071518No2002-11-122010-11-15Canada flag
US6598603Yes2003-07-292019-06-23US flag
US6899099Yes2005-05-312019-06-23US flag
US7524834Yes2009-04-282019-05-11US flag
US7759328Yes2010-07-202023-07-29US flag
US7897646Yes2011-03-012019-03-09US flag
US8143239Yes2012-03-272023-07-29US flag
US8461211Yes2013-06-112019-03-09US flag
US8575137Yes2013-11-052023-07-29US flag
US6123924No2000-09-262017-09-26US flag
US7967011Yes2011-06-282022-02-11US flag
US8616196Yes2013-12-312029-10-07US flag
US8387615Yes2013-03-052025-05-10US flag
US7587988Yes2009-09-152026-10-10US flag
US7367333Yes2008-05-062019-05-11US flag
US8528545Yes2013-09-102029-04-16US flag
US8875699Yes2014-11-042025-05-10US flag
US6027714No2000-02-222018-01-09US flag
US7143764No2006-12-052018-03-13US flag
US6142145No2000-11-072018-05-08US flag
US6287540No2001-09-112018-01-09US flag
US9320716No2016-04-262020-06-09US flag
US9192581No2015-11-242031-09-07US flag
US7410651No2008-08-122020-06-09US flag
USRE43799No2012-11-132020-06-09US flag
US8895064No2014-11-252031-09-07US flag
US7431943No2008-10-072020-06-09US flag
US9132093No2015-09-152031-09-07US flag
US8784888No2014-07-222020-06-09US flag
US8293273No2012-10-232020-06-09US flag
US5914122No1999-06-222015-12-19US flag
US9532954No2017-01-032020-06-09US flag
US9463161No2016-10-112030-05-28US flag
US9415009No2016-08-162030-05-28US flag
US8808713No2014-08-192030-05-28US flag
US8324266No2012-12-042030-05-28US flag
US8703806No2014-04-222030-05-28US flag
US8815258No2014-08-262031-03-17US flag
US10064878No2018-09-042020-06-09US flag
US10105374No2018-10-232020-06-09US flag
US10166247Yes2019-01-012023-07-29US flag
US10143698No2018-12-042020-06-09US flag
US9707182No2017-07-182036-09-09US flag
US10172802No2019-01-082036-09-09US flag
US10307375No2019-06-042031-09-07US flag
US10660858No2020-05-262031-09-07US flag
US10716753No2020-07-212030-05-28US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)226°CPhysProp
boiling point (°C)599.7ChemSpider
logP1.914ChemSpider
Predicted Properties
PropertyValueSource
Water Solubility0.0457 mg/mLALOGPS
logP2.42ALOGPS
logP2.73ChemAxon
logS-4ALOGPS
pKa (Strongest Acidic)13.74ChemAxon
pKa (Strongest Basic)-2.9ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area93.06 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity116.11 m3·mol-1ChemAxon
Polarizability47.11 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9872
Blood Brain Barrier+0.9533
Caco-2 permeable-0.6097
P-glycoprotein substrateSubstrate0.804
P-glycoprotein inhibitor INon-inhibitor0.5881
P-glycoprotein inhibitor IINon-inhibitor0.5911
Renal organic cation transporterNon-inhibitor0.7867
CYP450 2C9 substrateNon-substrate0.8488
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.7337
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.9075
CYP450 2D6 inhibitorNon-inhibitor0.9441
CYP450 2C19 inhibitorNon-inhibitor0.939
CYP450 3A4 inhibitorInhibitor0.796
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8886
Ames testNon AMES toxic0.9117
CarcinogenicityNon-carcinogens0.9466
BiodegradationNot ready biodegradable0.9759
Rat acute toxicity2.1601 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9483
hERG inhibition (predictor II)Non-inhibitor0.5627
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-03k9-1794300000-d4cdef973973a6b24ba4
MS/MS Spectrum - , positiveLC-MS/MSsplash10-00dj-3950000000-8e98d604876730f53851

Targets

Drugtargets2
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Details
1. Glucocorticoid receptor
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
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
  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]
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
  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

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Inducer
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
  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 Approved Drug Products: Pulmicort Budesonide Inhalation Powder [Link]
  11. FDA Approved Drug Products: Pulmicort Budesonide Inhalation Suspension [Link]
  12. FDA Approved Drug Products: Rhinocort Budesonide 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]
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
  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]
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inducer
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:
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]
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
  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]
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
  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]
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
  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]
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
  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]
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
  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]
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
  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]

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
  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]
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
  1. 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. [Article]

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
  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]
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
  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]
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
  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]
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
  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 October 26, 2021 21:40