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Identification
NameBudesonide
Accession NumberDB01222  (APRD00442)
TypeSmall Molecule
GroupsApproved
DescriptionBudesonide is a glucocorticoid used in the management of asthma, the treatment of various skin disorders, and allergic rhinitis. [PubChem] The extended release oral tablet, marketed as Uceris, was FDA approved on January 14, 2013 for the management of ulcerative colitis. Budesonide is provided as a mixture of two epimers (22R and 22S). Interestingly, the 22R form is two times more active than the 22S epimer. The two forms do not interconvert.
Structure
Thumb
Synonyms
(11beta,16alpha)-16,17-(Butylidenebis(oxy))-11,21-dihydroxypregna-1,4-diene-3,20-dione
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Budesonidespray, metered32 ug/1nasalPar Pharmaceutical Inc.2014-10-21Not applicableUs
Budesonidecapsule3 mg/1oralPar Pharmaceutical Inc.2011-08-18Not applicableUs
Budesonidespray, metered32 ug/1nasalAstra Zeneca Lp2014-05-13Not applicableUs
Cortimenttablet (delayed and extended release)9 mgoralFerring Inc2016-07-25Not applicableCanada
Entocortcapsule (sustained-release)3 mgoralTillotts Pharma Gmbh1997-01-30Not applicableCanada
Entocort ECcapsule3 mg/1oralAstra Zeneca Lp2001-10-29Not applicableUs
Entocort ECcapsule3 mg/1oralPhysicians Total Care, Inc.2006-05-22Not applicableUs
Entocort ECcapsule3 mg/1oralPrometheus Laboratories Inc2001-10-29Not applicableUs
Mylan-budesonide AQspray, metered dose100 mcgnasalMylan Pharmaceuticals Ulc1997-02-12Not applicableCanada
Mylan-budesonide AQspray, metered dose64 mcgnasalMylan Pharmaceuticals Ulc1999-11-23Not applicableCanada
Pulmicort Flexhaleraerosol, powder90 ug/1respiratory (inhalation)Rebel Distributors Corp2010-07-30Not applicableUs
Pulmicort Flexhaleraerosol, powder180 ug/1respiratory (inhalation)Astra Zeneca Lp2007-03-19Not applicableUs
Pulmicort Flexhaleraerosol, powder90 ug/1respiratory (inhalation)Astra Zeneca Lp2007-03-19Not applicableUs
Pulmicort Flexhaleraerosol, powder180 ug/1respiratory (inhalation)Physicians Total Care, Inc.2007-12-28Not applicableUs
Pulmicort Nebuamp 0.125 mg/mlsuspension0.125 mginhalationAstrazeneca Canada Inc1997-06-16Not applicableCanada
Pulmicort Nebuamp 0.25 mg/mlsuspension0.25 mginhalationAstrazeneca Canada Inc1992-12-31Not applicableCanada
Pulmicort Nebuamp 0.5 mg/mlsuspension0.5 mginhalationAstrazeneca Canada Inc1992-12-31Not applicableCanada
Pulmicort Respulessuspension.5 mg/2mLrespiratory (inhalation)Cardinal Health2009-11-20Not applicableUs
Pulmicort Respulessuspension.25 mg/2mLrespiratory (inhalation)Astra Zeneca Lp2000-09-08Not applicableUs
Pulmicort Respulessuspension.5 mg/2mLrespiratory (inhalation)Physicians Total Care, Inc.2006-06-29Not applicableUs
Pulmicort Respulessuspension.5 mg/2mLrespiratory (inhalation)Astra Zeneca Lp2000-09-08Not applicableUs
Pulmicort Respulessuspension.25 mg/2mLrespiratory (inhalation)Physicians Total Care, Inc.2007-06-01Not applicableUs
Pulmicort Respulessuspension1 mg/2mLrespiratory (inhalation)Astra Zeneca Lp2007-09-17Not applicableUs
Pulmicort Turbuhaler 100 Mcg/dosemetered-dose aerosol; powder100 mcginhalationAstrazeneca Canada Inc1990-12-31Not applicableCanada
Pulmicort Turbuhaler 200 Mcg/dosemetered-dose aerosol; powder200 mcginhalationAstrazeneca Canada Inc1990-12-31Not applicableCanada
Pulmicort Turbuhaler 400 Mcg/dosemetered-dose aerosol; powder400 mcginhalationAstrazeneca Canada Inc1992-12-31Not applicableCanada
Rhinocort Aquaspray, metered dose64 mcgnasalAstrazeneca Canada Inc1997-09-17Not applicableCanada
Rhinocort Aquaspray, metered32 ug/1nasalAstra Zeneca Lp2001-04-02Not applicableUs
Rhinocort Aquaspray, metered32 ug/1nasalPhysicians Total Care, Inc.2001-08-20Not applicableUs
Rhinocort Aqua 100mcgmetered-dose aerosol100 mcgnasalAstra Pharma Inc.1993-12-311999-07-29Canada
Rhinocort Turbuhaler 100 Mcg/dosepowder100 mcginhalation; nasalAstrazeneca Canada Inc1993-12-31Not applicableCanada
Ucerisaerosol, foam28 mg/1rectalSalix Pharmaceuticals, Inc.2014-12-01Not applicableUs
Uceristablet, extended release9 mg/1oralSantarus, Inc.2013-01-14Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Budesonidesuspension.25 mg/2mLrespiratory (inhalation)Sandoz Inc2015-07-24Not applicableUs
Budesonidesuspension.25 mg/2mLrespiratory (inhalation)Teva Pharmaceuticals USA Inc2008-11-19Not applicableUs
Budesonidesuspension.25 mg/2mLrespiratory (inhalation)Apotex Corp.2009-03-30Not applicableUs
Budesonidesuspension.25 mg/2mLrespiratory (inhalation)Physicians Total Care, Inc.2010-01-19Not applicableUs
Budesonideinhalant.5 mg/2mLrespiratory (inhalation)Nephron Pharmaceuticals Corporation2013-10-01Not applicableUs
Budesonidesuspension.5 mg/2mLrespiratory (inhalation)Dispensing Solutions, Inc.2008-11-19Not applicableUs
Budesonidesuspension.5 mg/2mLrespiratory (inhalation)Sandoz Inc2015-07-24Not applicableUs
Budesonidesuspension1 mg/2mLrespiratory (inhalation)Teva Pharmaceuticals USA Inc2016-03-11Not applicableUs
Budesonidesuspension.5 mg/2mLrespiratory (inhalation)Teva Pharmaceuticals USA Inc2008-11-19Not applicableUs
Budesonidesuspension.5 mg/2mLrespiratory (inhalation)Apotex Corp.2009-03-30Not applicableUs
Budesonidesuspension.5 mg/2mLrespiratory (inhalation)Physicians Total Care, Inc.2009-02-04Not applicableUs
Budesonidesuspension.25 mg/2mLrespiratory (inhalation)Preferred Pharmaceuticals, Inc.2009-02-04Not applicableUs
Budesonidesuspension1 mg/2mLrespiratory (inhalation)Sandoz Inc2015-07-24Not applicableUs
Budesonidecapsule3 mg/1oralMylan Pharmaceuticals Inc.2013-08-23Not applicableUs
Budesonidesuspension.5 mg/2mLrespiratory (inhalation)Cardinal Health2009-12-15Not applicableUs
Budesonidesuspension.5 mg/2mLrespiratory (inhalation)Preferred Pharmaceuticals, Inc.2009-02-04Not applicableUs
Budesonidecapsule3 mg/1oralMylan Institutional Inc.2011-09-02Not applicableUs
Budesonidecapsule3 mg/1oralCarilion Materials Management2013-08-23Not applicableUs
Budesonideinhalant.25 mg/2mLrespiratory (inhalation)Nephron Pharmaceuticals Corporation2013-10-01Not applicableUs
Budesonidecapsule3 mg/1oralGolden State Medical Supply, Inc.2015-07-10Not applicableUs
Budesonide Inhalationsuspension.5 mg/2mLrespiratory (inhalation)Preferred Pharmaceuticals Inc.2015-08-17Not applicableUs
Budesonide Inhalationsuspension.25 mg/2mLrespiratory (inhalation)Watson Laboratories, Inc.2013-04-02Not applicableUs
Budesonide Inhalationsuspension.5 mg/2mLrespiratory (inhalation)Watson Laboratories, Inc.2013-04-02Not applicableUs
Budesonide Nasalspray, metered32 ug/1nasalApotex Corp.2014-05-12Not applicableUs
Approved Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Budesonidespray, metered32 ug/1nasalApotex Corp.2016-04-19Not applicableUs
Rhinocort Allergyspray, metered32 ug/1nasalJohnson & Johnson Consumer Inc., Mc Neil Consumer Healthcare Division2016-01-14Not applicableUs
Unapproved/Other Products Not Available
International Brands
NameCompany
BidienNot Available
BudesonNot Available
BudicortNot Available
ENTOCORTNot Available
NoexEurofarma
PulmicortAstraZeneca
RhinocortAstraZeneca
RhinosolNot Available
SpirocortNot Available
Brand mixtures
NameLabellerIngredients
Entocort EnemaTillotts Pharma Gmbh
SymbicortAstra Zeneca Lp
Symbicort 100 TurbuhalerAstrazeneca Canada Inc
Symbicort 200 TurbuhalerAstrazeneca Canada Inc
Symbicort Forte TurbuhalerAstrazeneca Canada Inc
SaltsNot Available
Categories
UNIIQ3OKS62Q6X
CAS number51333-22-3
WeightAverage: 430.5339
Monoisotopic: 430.23553882
Chemical FormulaC25H34O6
InChI KeyInChIKey=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[[email protected]]3OC(CCC)O[C@@]3(C(=O)CO)[C@@]1(C)C[[email protected]](O)[C@@]1([H])[C@@]2([H])CCC2=CC(=O)C=C[C@]12C
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassLipids and lipid-like molecules
ClassSteroids and steroid derivatives
Sub ClassHydroxysteroids
Direct Parent21-hydroxysteroids
Alternative Parents
Substituents
  • 21-hydroxysteroid
  • Progestogin-skeleton
  • Pregnane-skeleton
  • 20-oxosteroid
  • 11-hydroxysteroid
  • 11-beta-hydroxysteroid
  • Oxosteroid
  • 3-oxosteroid
  • 3-oxo-delta-1,4-steroid
  • Delta-1,4-steroid
  • Cyclic alcohol
  • Alpha-hydroxy ketone
  • Meta-dioxolane
  • Cyclic ketone
  • Secondary alcohol
  • Ketone
  • Oxacycle
  • Organoheterocyclic compound
  • Acetal
  • Hydrocarbon derivative
  • Primary alcohol
  • Organooxygen compound
  • Carbonyl group
  • Alcohol
  • Aliphatic heteropolycyclic compound
Molecular FrameworkAliphatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationThe oral capsule is used for the treatment of mild to moderate active Crohn's disease. The oral tablet is used for induction of remission in patients with active, mild to moderate ulcerative colitis. The oral inhalation formulation is used for the treatment of asthma, non-infectious rhinitis (including hay fever and other allergies), and for treatment and prevention of nasal polyposis.
PharmacodynamicsBudesonide has a high glucocorticoid effect and a weak mineralocorticoid effect. It binds to the glucocorticoid receptor with a higher binding affinity than cortisol and prednisolone. When budesonide is systemically administered, suppression of endogenous cortisol concentrations and an impairment of the hypothalamus-pituitary-adrenal (HPA) axis function has been observed. Furthermore, a decrease in airway reactivity to histamine and other entities has been observed with the inhaled formulation. Generally, the inhaled formulation has a rapid onset action and improvement in asthma control can occur within 24 hours of initiation of treatment.
Mechanism of actionBudesonide is an anti-inflammatory corticosteroid that exhibits potent glucocorticoid activity and weak mineralocorticoid activity. The precise mechanism of corticosteroid actions on inflammation in asthma, Crohn's disease, or ulcerative colitis is not known. Inflammation is an important component in the pathogenesis of asthma. Corticosteroids have been shown to have a wide range of inhibitory activities against multiple cell types (eg, mast cells, eosinophils, neutrophils, macrophages, and lymphocytes) and mediators (eg, histamine, eicosanoids, leukotrienes, and cytokines) involved in allergic and non-allergic-mediated inflammation. These anti-inflammatory actions of corticosteroids may contribute to their efficacy in the aforementioned diseases. Because budesonide undergoes significant first-pass elimination, the both oral preparations are formulated as an extended release tablet. As a result, budesonide release is delyaed until exposure to a pH ≥ 7 in the small intestine.
Related Articles
AbsorptionAbsorption is complete following oral administration. The pharmacokinetic parameters of the inhaled powder formulation are as follows: Tmax = 30 minutes; Absolute systemic availability = 39%. When a single oral administration of 9 mg of Uceris are given, the pharmacokinetic parameters are as follows: Tmax = 13.3 ± 5.9 hours; Cmax = 1.35 ± 0.96 ng/mL; AUC = 16.43 ± 10.52 ng·hr/mL. It is important to note that the parameters have a high degree of variability. When a single oral administration of Entocort EC are given, the pharmacokinetic parameters are as follows: Tmax = 3- 600 minutes; Cmax = 5 nmol/L; AUC = 30 nmol•hr/L.
Volume of distribution

Tablet and capsule, healthy subjects and patients = 2.2 – 3.9 L/kg;
Powder, metered = 3 L/kg

Protein binding85-90% protein bound.
Metabolism

Following absorption, budesonide is subject to high first pass metabolism (80-90%). Budesonide is rapidly and extensively biotransformed, mainly by CYP3A4, to its 2 major metabolites, 6b-hydroxybudesonide and 16a- hydroxyprednisolone. The glucocorticoid activity of these metabolites is negligible (<1/100) in relation to that of the parent compound.

SubstrateEnzymesProduct
Budesonide
16-alpha-hydroxyprednisoloneDetails
Budesonide
6-beta-hydroxybudesonideDetails
Route of eliminationBudesonide is excreted in urine and feces in the form of metabolites. Approximately 60% of an intravenous radiolabelled dose was recovered in the urine. No unchanged budesonide was detected in the urine.
Half lifeFollowing IV administration of budesonide, the elimination half-life is 2.0 to 3.6 hours. This value does not differ between healthy adults and patients with Crohn’s disease.
Clearance

Plasma clearance, tablet = 0.9 – 1.8 L/min;
Systemic clearance, powder, 22R = 1.4 L/min;
Systemic clearance, powder, 22S = 1.0 L/min;
0.5 L/min [Athmatic children 4 to 6 years of age]

ToxicitySingle oral doses of 200 and 400 mg/kg were lethal in female and male mice, respectively. The signs of acute toxicity were decreased motor activity, piloerection and generalized edema.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated Effects
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeEffectReference(s)
T-box transcription factor TBX21
Gene symbol: TBX21
UniProt: Q9UL17
rs2240017 Not AvailableC AlleleImproved response for long-term asthma treatment15604153
T-box transcription factor TBX21
Gene symbol: TBX21
UniProt: Q9UL17
rs2240017 Not AvailableCG allele (heterozygotes)Better response to drug treatment (for asthma) than rs2240017(G;G) homozygotes.15604153
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
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 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Capsuleoral3 mg/1
Inhalantrespiratory (inhalation).25 mg/2mL
Inhalantrespiratory (inhalation).5 mg/2mL
Suspensionrespiratory (inhalation).25 mg/2mL
Suspensionrespiratory (inhalation).5 mg/2mL
Tablet (delayed and extended release)oral9 mg
Capsule (sustained-release)oral3 mg
Enema; kit; tabletrectal
Spray, metered dosenasal100 mcg
Aerosol, powderrespiratory (inhalation)180 ug/1
Aerosol, powderrespiratory (inhalation)90 ug/1
Suspensioninhalation0.125 mg
Suspensioninhalation0.25 mg
Suspensioninhalation0.5 mg
Suspensionrespiratory (inhalation)1 mg/2mL
Metered-dose aerosol; powderinhalation100 mcg
Metered-dose aerosol; powderinhalation200 mcg
Metered-dose aerosol; powderinhalation400 mcg
Spray, meterednasal32 ug/1
Spray, metered dosenasal64 mcg
Metered-dose aerosolnasal100 mcg
Powderinhalation; nasal100 mcg
Aerosolrespiratory (inhalation)
Powderinhalation
Aerosol, foamrectal28 mg/1
Tablet, extended releaseoral9 mg/1
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)
CA2071518 No2002-11-122010-11-15Canada
US5914122 No1995-12-192015-12-19Us
US6027714 No1998-01-092018-01-09Us
US6123924 No1997-09-262017-09-26Us
US6142145 No1998-05-082018-05-08Us
US6287540 No1998-01-092018-01-09Us
US6423340 No1993-11-152010-11-15Us
US6598603 Yes1999-06-232019-06-23Us
US6899099 Yes1999-06-232019-06-23Us
US7143764 No1998-03-132018-03-13Us
US7367333 No1998-11-112018-11-11Us
US7410651 No2000-06-092020-06-09Us
US7431943 No2000-06-092020-06-09Us
US7524834 Yes1999-05-112019-05-11Us
US7587988 No2006-04-102026-04-10Us
US7759328 No2003-01-292023-01-29Us
US7897646 No1998-09-092018-09-09Us
US7967011 No2001-08-112021-08-11Us
US8143239 No2003-01-292023-01-29Us
US8293273 No2000-06-092020-06-09Us
US8387615 No2004-11-102024-11-10Us
US8461211 No1998-09-092018-09-09Us
US8528545 No2008-10-162028-10-16Us
US8575137 No2003-01-292023-01-29Us
US8616196 No2009-04-072029-04-07Us
US8784888 No2000-06-092020-06-09Us
US8875699 No2004-11-102024-11-10Us
US8895064 No2011-09-072031-09-07Us
US9132093 No2011-09-072031-09-07Us
US9192581 No2011-09-072031-09-07Us
US9320716 No2000-06-092020-06-09Us
USRE43799 No2000-06-092020-06-09Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point226°CPhysProp
water solubilityinsolubleNot Available
logP1.9Not Available
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 RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
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 ReferencesNot Available
External Links
ATC CodesR03AK07A07EA06R03BA02D07AC09R03AK12R01AD05
AHFS Codes
  • 52:08.08
  • 68:04.00
PDB EntriesNot Available
FDA labelDownload (52.3 KB)
MSDSDownload (73.7 KB)
Interactions
Drug Interactions
Drug
1,10-PhenanthrolineThe risk or severity of adverse effects can be increased when Budesonide is combined with 1,10-Phenanthroline.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Budesonide.
AldesleukinBudesonide may decrease the antineoplastic activities of Aldesleukin.
Aluminum hydroxideThe bioavailability of Budesonide can be decreased when combined with Aluminum hydroxide.
Aluminum phosphateThe bioavailability of Budesonide can be decreased when combined with Aluminum phosphate.
AmbenoniumThe risk or severity of adverse effects can be increased when Budesonide is combined with Ambenonium.
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Budesonide.
AmiodaroneThe serum concentration of Budesonide can be increased when it is combined with Amiodarone.
Amphotericin BBudesonide may increase the hypokalemic activities of Amphotericin B.
AprepitantThe metabolism of Budesonide can be decreased when combined with Aprepitant.
AtazanavirThe serum concentration of Budesonide can be increased when it is combined with Atazanavir.
AtomoxetineThe metabolism of Budesonide can be decreased when combined with Atomoxetine.
Atracurium besylateAtracurium besylate may increase the adverse neuromuscular activities of Budesonide.
BazedoxifeneThe serum concentration of Budesonide can be increased when it is combined with Bazedoxifene.
BendroflumethiazideBudesonide may increase the hypokalemic activities of Bendroflumethiazide.
Benzoic AcidThe therapeutic efficacy of Benzoic Acid can be decreased when used in combination with Budesonide.
BexaroteneThe serum concentration of Budesonide can be decreased when it is combined with Bexarotene.
Bismuth SubcitrateThe bioavailability of Budesonide can be decreased when combined with Bismuth Subcitrate.
BoceprevirThe serum concentration of Budesonide can be increased when it is combined with Boceprevir.
BortezomibThe metabolism of Budesonide can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Budesonide can be decreased when it is combined with Bosentan.
BumetanideBudesonide may increase the hypokalemic activities of Bumetanide.
CalcitriolThe therapeutic efficacy of Calcitriol can be decreased when used in combination with Budesonide.
Calcium carbonateThe bioavailability of Budesonide can be decreased when combined with Calcium carbonate.
CarbamazepineThe serum concentration of Budesonide can be decreased when it is combined with Carbamazepine.
CeritinibBudesonide may increase the hyperglycemic activities of Ceritinib.
CeritinibThe serum concentration of Budesonide can be increased when it is combined with Ceritinib.
ChlorothiazideBudesonide may increase the hypokalemic activities of Chlorothiazide.
ChlorotrianiseneThe serum concentration of Budesonide can be increased when it is combined with Chlorotrianisene.
ChlorthalidoneBudesonide may increase the hypokalemic activities of Chlorthalidone.
CholestyramineCholestyramine can cause a decrease in the absorption of Budesonide resulting in a reduced serum concentration and potentially a decrease in efficacy.
ClarithromycinThe serum concentration of Budesonide can be increased when it is combined with Clarithromycin.
ClemastineThe metabolism of Budesonide can be decreased when combined with Clemastine.
ClotrimazoleThe metabolism of Budesonide can be decreased when combined with Clotrimazole.
CobicistatThe serum concentration of Budesonide can be increased when it is combined with Cobicistat.
ColesevelamColesevelam can cause a decrease in the absorption of Budesonide resulting in a reduced serum concentration and potentially a decrease in efficacy.
ColestipolColestipol can cause a decrease in the absorption of Budesonide resulting in a reduced serum concentration and potentially a decrease in efficacy.
ConivaptanThe metabolism of Budesonide can be decreased when combined with Conivaptan.
Conjugated Equine EstrogensThe serum concentration of Budesonide can be increased when it is combined with Conjugated Equine Estrogens.
Corticorelin ovine triflutateThe therapeutic efficacy of Corticorelin ovine triflutate can be decreased when used in combination with Budesonide.
CoumaphosThe risk or severity of adverse effects can be increased when Budesonide is combined with Coumaphos.
CrizotinibThe metabolism of Budesonide can be decreased when combined with Crizotinib.
CyclosporineThe metabolism of Budesonide can be decreased when combined with Cyclosporine.
DabrafenibThe serum concentration of Budesonide can be decreased when it is combined with Dabrafenib.
DarunavirThe serum concentration of Budesonide can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Budesonide can be increased when it is combined with Dasatinib.
DecamethoniumThe risk or severity of adverse effects can be increased when Budesonide is combined with Decamethonium.
DeferasiroxThe serum concentration of Budesonide can be decreased when it is combined with Deferasirox.
DeferasiroxThe risk or severity of adverse effects can be increased when Budesonide is combined with Deferasirox.
DelavirdineThe metabolism of Budesonide can be decreased when combined with Delavirdine.
DemecariumThe risk or severity of adverse effects can be increased when Budesonide is combined with Demecarium.
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Budesonide.
DexamethasoneThe serum concentration of Budesonide can be decreased when it is combined with Dexamethasone.
DichlorvosThe risk or severity of adverse effects can be increased when Budesonide is combined with Dichlorvos.
DienestrolThe serum concentration of Budesonide can be increased when it is combined with Dienestrol.
DiethylstilbestrolThe serum concentration of Budesonide can be increased when it is combined with Diethylstilbestrol.
DiflunisalThe risk or severity of adverse effects can be increased when Diflunisal is combined with Budesonide.
DihydroergotamineThe metabolism of Budesonide can be decreased when combined with Dihydroergotamine.
DihydrotestosteroneBudesonide may increase the fluid retaining activities of Dihydrotestosterone.
DiltiazemThe metabolism of Budesonide can be decreased when combined with Diltiazem.
DonepezilThe risk or severity of adverse effects can be increased when Budesonide is combined with Donepezil.
DoxycyclineThe metabolism of Budesonide can be decreased when combined with Doxycycline.
DronedaroneThe metabolism of Budesonide can be decreased when combined with Dronedarone.
EchothiophateThe risk or severity of adverse effects can be increased when Budesonide is combined with Echothiophate.
EdrophoniumThe risk or severity of adverse effects can be increased when Budesonide is combined with Edrophonium.
EfavirenzThe serum concentration of Budesonide can be decreased when it is combined with Efavirenz.
EnzalutamideThe serum concentration of Budesonide can be decreased when it is combined with Enzalutamide.
ErythromycinThe metabolism of Budesonide can be decreased when combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Budesonide can be decreased when it is combined with Eslicarbazepine acetate.
EstradiolThe serum concentration of Budesonide can be increased when it is combined with Estradiol.
EstriolThe serum concentration of Budesonide can be increased when it is combined with Estriol.
EstroneThe serum concentration of Budesonide can be increased when it is combined with Estrone.
Etacrynic acidBudesonide may increase the hypokalemic activities of Etacrynic acid.
Ethinyl EstradiolThe serum concentration of Budesonide can be increased when it is combined with Ethinyl Estradiol.
EtravirineThe serum concentration of Budesonide can be decreased when it is combined with Etravirine.
FenthionThe risk or severity of adverse effects can be increased when Budesonide is combined with Fenthion.
FingolimodBudesonide may increase the immunosuppressive activities of Fingolimod.
FluconazoleThe metabolism of Budesonide can be decreased when combined with Fluconazole.
FluoxymesteroneBudesonide may increase the fluid retaining activities of Fluoxymesterone.
FluvoxamineThe metabolism of Budesonide can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Budesonide can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Budesonide can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Budesonide can be decreased when it is combined with Fosphenytoin.
FurosemideBudesonide may increase the hypokalemic activities of Furosemide.
Fusidic AcidThe serum concentration of Budesonide can be increased when it is combined with Fusidic Acid.
GalantamineThe risk or severity of adverse effects can be increased when Budesonide is combined with Galantamine.
Gallamine TriethiodideThe risk or severity of adverse effects can be increased when Budesonide is combined with Gallamine Triethiodide.
GenisteinThe serum concentration of Budesonide can be increased when it is combined with Genistein.
Ginkgo bilobaThe risk or severity of adverse effects can be increased when Budesonide is combined with Ginkgo biloba.
Glycerol PhenylbutyrateThe therapeutic efficacy of Glycerol Phenylbutyrate can be decreased when used in combination with Budesonide.
HexestrolThe serum concentration of Budesonide can be increased when it is combined with Hexestrol.
Huperzine AThe risk or severity of adverse effects can be increased when Budesonide is combined with Huperzine A.
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Budesonide.
HydrochlorothiazideBudesonide may increase the hypokalemic activities of Hydrochlorothiazide.
HydroflumethiazideBudesonide may increase the hypokalemic activities of Hydroflumethiazide.
IdelalisibThe serum concentration of Budesonide can be increased when it is combined with Idelalisib.
ImatinibThe metabolism of Budesonide can be decreased when combined with Imatinib.
IndacaterolIndacaterol may increase the hypokalemic activities of Budesonide.
IndapamideBudesonide may increase the hypokalemic activities of Indapamide.
IndinavirThe serum concentration of Budesonide can be increased when it is combined with Indinavir.
IsavuconazoniumThe metabolism of Budesonide can be decreased when combined with Isavuconazonium.
IsoflurophateThe risk or severity of adverse effects can be increased when Budesonide is combined with Isoflurophate.
IsoniazidThe serum concentration of Isoniazid can be decreased when it is combined with Budesonide.
IsradipineThe metabolism of Budesonide can be decreased when combined with Isradipine.
ItraconazoleThe serum concentration of Budesonide can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Budesonide can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of Budesonide can be increased when it is combined with Ketoconazole.
LeflunomideThe risk or severity of adverse effects can be increased when Budesonide is combined with Leflunomide.
LopinavirThe serum concentration of Budesonide can be increased when it is combined with Lopinavir.
LovastatinThe metabolism of Budesonide can be decreased when combined with Lovastatin.
LuliconazoleThe metabolism of Budesonide can be decreased when combined with Luliconazole.
MagaldrateThe bioavailability of Budesonide can be decreased when combined with Magaldrate.
Magnesium carbonateThe bioavailability of Budesonide can be decreased when combined with Magnesium carbonate.
Magnesium hydroxideThe bioavailability of Budesonide can be decreased when combined with Magnesium hydroxide.
Magnesium oxideThe bioavailability of Budesonide can be decreased when combined with Magnesium oxide.
Magnesium TrisilicateThe bioavailability of Budesonide can be decreased when combined with Magnesium Trisilicate.
MalathionThe risk or severity of adverse effects can be increased when Budesonide is combined with Malathion.
MefloquineThe risk or severity of adverse effects can be increased when Budesonide is combined with Mefloquine.
MemantineThe risk or severity of adverse effects can be increased when Budesonide is combined with Memantine.
MesalazineThe risk or severity of adverse effects can be increased when Mesalazine is combined with Budesonide.
MestranolThe serum concentration of Budesonide can be increased when it is combined with Mestranol.
MethyclothiazideBudesonide may increase the hypokalemic activities of Methyclothiazide.
MethyltestosteroneBudesonide may increase the fluid retaining activities of Methyltestosterone.
MetolazoneBudesonide may increase the hypokalemic activities of Metolazone.
MifepristoneThe metabolism of Budesonide can be decreased when combined with Mifepristone.
MinaprineThe risk or severity of adverse effects can be increased when Budesonide is combined with Minaprine.
MitotaneThe serum concentration of Budesonide can be decreased when it is combined with Mitotane.
MivacuriumMivacurium may increase the adverse neuromuscular activities of Budesonide.
ModafinilThe serum concentration of Budesonide can be decreased when it is combined with Modafinil.
NafcillinThe serum concentration of Budesonide can be decreased when it is combined with Nafcillin.
NatalizumabThe risk or severity of adverse effects can be increased when Budesonide is combined with Natalizumab.
NefazodoneThe serum concentration of Budesonide can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Budesonide can be increased when it is combined with Nelfinavir.
NeostigmineThe risk or severity of adverse effects can be increased when Budesonide is combined with Neostigmine.
NetupitantThe metabolism of Budesonide can be decreased when combined with Netupitant.
NevirapineThe metabolism of Budesonide can be decreased when combined with Nevirapine.
NicorandilThe risk or severity of adverse effects can be increased when Budesonide is combined with Nicorandil.
NilotinibThe metabolism of Budesonide can be decreased when combined with Nilotinib.
OlaparibThe metabolism of Budesonide can be decreased when combined with Olaparib.
OsimertinibThe serum concentration of Budesonide can be increased when it is combined with Osimertinib.
OxandroloneBudesonide may increase the fluid retaining activities of Oxandrolone.
OxymetholoneBudesonide may increase the fluid retaining activities of Oxymetholone.
PalbociclibThe serum concentration of Budesonide can be increased when it is combined with Palbociclib.
PentobarbitalThe serum concentration of Budesonide can be decreased when it is combined with Pentobarbital.
PhenobarbitalThe serum concentration of Budesonide can be decreased when it is combined with Phenobarbital.
Phenylacetic acidThe therapeutic efficacy of Phenylacetic acid can be decreased when used in combination with Budesonide.
PhenytoinThe serum concentration of Budesonide can be decreased when it is combined with Phenytoin.
PhysostigmineThe risk or severity of adverse effects can be increased when Budesonide is combined with Physostigmine.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Budesonide.
PiretanideBudesonide may increase the hypokalemic activities of Piretanide.
Polyestradiol phosphateThe serum concentration of Budesonide can be increased when it is combined with Polyestradiol phosphate.
PolythiazideBudesonide may increase the hypokalemic activities of Polythiazide.
PosaconazoleThe serum concentration of Budesonide can be increased when it is combined with Posaconazole.
PrimidoneThe serum concentration of Budesonide can be decreased when it is combined with Primidone.
PyridostigmineThe risk or severity of adverse effects can be increased when Budesonide is combined with Pyridostigmine.
QuinestrolThe serum concentration of Budesonide can be increased when it is combined with Quinestrol.
QuinethazoneBudesonide may increase the hypokalemic activities of Quinethazone.
Rabies vaccineThe risk or severity of adverse effects can be increased when Budesonide is combined with Rabies vaccine.
RanolazineThe metabolism of Budesonide can be decreased when combined with Ranolazine.
RapacuroniumRapacuronium may increase the adverse neuromuscular activities of Budesonide.
RifabutinThe serum concentration of Budesonide can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Budesonide can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Budesonide can be decreased when it is combined with Rifapentine.
RitonavirThe serum concentration of Budesonide can be increased when it is combined with Ritonavir.
RivastigmineThe risk or severity of adverse effects can be increased when Budesonide is combined with Rivastigmine.
RoflumilastRoflumilast may increase the immunosuppressive activities of Budesonide.
Salicylic acidThe risk or severity of adverse effects can be increased when Salicylic acid is combined with Budesonide.
SaquinavirThe serum concentration of Budesonide can be increased when it is combined with Saquinavir.
SildenafilThe metabolism of Budesonide can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Budesonide can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Budesonide can be increased when it is combined with Simeprevir.
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Budesonide.
Sodium phenylbutyrateThe therapeutic efficacy of Sodium phenylbutyrate can be decreased when used in combination with Budesonide.
St. John's WortThe serum concentration of Budesonide can be decreased when it is combined with St. John&#39;s Wort.
StanozololBudesonide may increase the fluid retaining activities of Stanozolol.
StiripentolThe serum concentration of Budesonide can be increased when it is combined with Stiripentol.
SulfisoxazoleThe metabolism of Budesonide can be decreased when combined with Sulfisoxazole.
Synthetic Conjugated Estrogens, AThe serum concentration of Budesonide can be increased when it is combined with Synthetic Conjugated Estrogens, A.
Synthetic Conjugated Estrogens, BThe serum concentration of Budesonide can be increased when it is combined with Synthetic Conjugated Estrogens, B.
TacrineThe risk or severity of adverse effects can be increased when Budesonide is combined with Tacrine.
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Budesonide.
TelaprevirThe serum concentration of Telaprevir can be decreased when it is combined with Budesonide.
TelaprevirThe serum concentration of Budesonide can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Budesonide can be increased when it is combined with Telithromycin.
TestosteroneBudesonide may increase the fluid retaining activities of Testosterone.
TiboloneThe serum concentration of Budesonide can be increased when it is combined with Tibolone.
TiclopidineThe metabolism of Budesonide can be decreased when combined with Ticlopidine.
TocilizumabThe serum concentration of Budesonide can be decreased when it is combined with Tocilizumab.
TofacitinibBudesonide may increase the immunosuppressive activities of Tofacitinib.
TorasemideBudesonide may increase the hypokalemic activities of Torasemide.
TrastuzumabTrastuzumab may increase the neutropenic activities of Budesonide.
TrichlorfonThe risk or severity of adverse effects can be increased when Budesonide is combined with Trichlorfon.
TrichlormethiazideBudesonide may increase the hypokalemic activities of Trichlormethiazide.
TubocurarineThe risk or severity of adverse effects can be increased when Budesonide is combined with Tubocurarine.
VenlafaxineThe metabolism of Budesonide can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Budesonide can be decreased when combined with Verapamil.
VoriconazoleThe serum concentration of Budesonide can be increased when it is combined with Voriconazole.
WarfarinBudesonide may increase the anticoagulant activities of Warfarin.
ZeranolThe serum concentration of Budesonide can be increased when it is combined with Zeranol.
ZiprasidoneThe metabolism of Budesonide can be decreased when combined with Ziprasidone.
Food Interactions
  • A mean delay in time to peak concentration of 2.5 hours is observed with the intake of a high-fat meal, with no significant differences in AUC.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Zinc ion binding
Specific Function:
Receptor for glucocorticoids (GC). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modulator of other transcription factors. Affects inflammatory responses, cellular proliferation and differentiation in target tissues. Could act as a coactivator for STAT5-dependent transcription upon grow...
Gene Name:
NR3C1
Uniprot ID:
P04150
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. [PubMed:11040338 ]
  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. [PubMed:11258648 ]
  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. [PubMed:11730731 ]
  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. [PubMed:12601049 ]
  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. [PubMed:12920235 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Jonsson G, Astrom A, Andersson P: Budesonide is metabolized by cytochrome P450 3A (CYP3A) enzymes in human liver. Drug Metab Dispos. 1995 Jan;23(1):137-42. [PubMed:7720517 ]
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Drug created on June 13, 2005 07:24 / Updated on September 26, 2016 03:28