PharmGKB: The Pharmacogenomics Knowledge Base

Drug/Small Molecule:
budesonide

2D structure

Overview

Generic Names: budesonide
Trade Names: Bidien; Budeson; Cortivent; Desowen; Entocort; Entocort EC; Micronyl; Preferid; Pulmicort; Pulmicort Nebuamp; Pulmicort Respules; Pulmicort Turbuhaler; Rhinocort; Rhinocort Aqua; Rhinocort Turbuhaler; Spirocort; Tridesilon
Brand Mixtures: Entocort Enema 0.02 Mg/Ml (Budesonide + Sodium Chloride); Symbicort 100 Turbuhaler (Budesonide + Formoterol Fumarate Dihydrate); Symbicort 200 Turbuhaler (Budesonide + Formoterol Fumarate Dihydrate)
PharmGKB Accession Id: PA448681

Description

A glucocorticoid used in the management of asthma, the treatment of various skin disorders, and allergic rhinitis. PubChem (source: Drug Bank)

Indication

For the treatment of mild to moderate active Crohn's disease. Also for the treatment of asthma, non-infectious rhinitis (including hay fever and other allergies), and for treatment and prevention of nasal polyposis. (source: Drug Bank)

ATC Therapeutic Categories

  • A07EA:Corticosteroids acting locally
  • D07AC:Corticosteroids, potent (group III)
  • R01AD:Corticosteroids
  • R03BA:Glucocorticoids

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

The exact mechanism of action of budesonide in the treatment of Crohn's disease is not fully understood. However, being a glucocorticosteroid, budesonide has a high local anti-inflammatory effect. (source: Drug Bank)

Pharmacology

Budesonide is a synthetic corticosteroid used in Crohn's disease to decrease the symptoms and inflammation associated with the disease, especially at times of flare up. Budesonide has a high topical glucocorticosteroid (GCS) activity and a substantial first pass elimination. The formulation contains granules which are coated to protect dissolution in gastric juice, but which dissolve at pH >5.5, ie, normally when the granules reach the duodenum. Thereafter, a matrix of ethylcellulose with budesonide controls the release of the drug into the intestinal lumen in a time-dependent manner. (source: Drug Bank)

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. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Following absorption, budesonide is subject to high first pass metabolism (80-90%). In vitro experiments in human liver microsomes demonstrate that budesonide is rapidly and extensively biotransformed, mainly by CYP3A4, to its 2 major metabolites, 6b-hydroxy budesonide and 16a- hydroxy prednisolone. The glucocorticoid activity of these metabolites is negligible (<1/100) in relation to that of the parent compound. (source: Drug Bank)

Protein Binding

85-90% (source: Drug Bank)

Absorption

Absorption is complete following oral administration. (source: Drug Bank)

Toxicity

Single 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. (source: Drug Bank)

Isomeric SMILES Code:

CCCC1O[C@@H]2C[C@H]3[C@@H]4CCC5=CC(=O)C=C[C@@]5([C@H]4[C@H](C[C@@]3([C@@]2(O1)C(=O)CO)C)O)C (source: Drug Bank)

Curated Annotations (Curated Annotation)

  1. rs1042713 at chr5:148186633 in ADRB2
    The ADRB2:Arg16Gly variant was not associated with asthma exacerbation in patients treated with inhaled corticosteroids plus longacting beta agonists.
    Variant Name:
    ADRB2:Arg16Gly
    Related Drugs:
    budesonide, fluticasone propionate, formoterol, salmeterol
    Related Diseases:
    Asthma
    Evidence:
    PMID:18156033
  2. rs2781659 at chr6:131933513 in ARG1
    This variant is associated with acute response to inhaled ß agonists in both childhood and adult asthmatic patients.
    Related Drugs:
    budesonide, fluticasone propionate, nedocromil, salbutamol
    Related Diseases:
    Asthma
    Evidence:
    PMID:18617639
  3. rs2240017 at chr17:43165918 in TBX21
    This variant is associated with improved response to inhaled corticosteroids for asthma patients
    Variant Name:
    TBX21:H33Q
    Related Drugs:
    budesonide, nedocromil
    Related Diseases:
    Asthma
    Evidence:
    PMID:15604153
  4. rs28364072 at chr19:7661285 in FCER2
    This variant is associated with severe exacerbations with asthma in both white and african american childen. This variant also leads to decreased FEER2 expression and may be used to predict treatment outcome in asthma.
    Variant Name:
    FCER2:T2206C
    Related Drugs:
    budesonide, nedocromil
    Related Diseases:
    Asthma
    Evidence:
    PMID:17980418
Variant names are different names that have been used in the literature and other resources to refer to the same variant.

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Has annotations
ABCB1
  •   
  •   
  • PK
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
ADRB2
  • CO
  •   
  •   
  •   
  • GN
Publications, Variants
No phenotype data No genotype data Literature annotations available Not annotated
ARG1
  •   
  •   
  •   
  •   
  •   
Variants
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A4
  •   
  •   
  • PK
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A5
  •   
  •   
  • PK
  •   
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
FCER2
  •   
  •   
  •   
  •   
  •   
Variants
Phenotype data available Genotype Data Available Literature annotations available Has annotations
NR1I2
  •   
  •   
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
NR3C1
  •   
  • PD
  •   
  • FA
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
RNASE3
  •   
  • PD
  •   
  •   
  •   
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
TBX21
  •   
  •   
  •   
  •   
  •   
Variants
No phenotype data Genotype Data Available Literature annotations available Not annotated
VCAM1
  •   
  • PD
  •   
  • FA
  •   
Publications

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
NR3C1 Uncurated Annotation (source: Drug Bank)

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
itraconazole Uncurated Annotation The imidazole increases levels/effect of budesonide (source: Drug Bank)
ketoconazole Uncurated Annotation The imidazole increases levels/effect of budesonide (source: Drug Bank)

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Asthma
  • CO
  • PD
  •   
  •   
  • GN
Publications, Variants
No phenotype data No genotype data Literature annotations available Not annotated
Inflammatory Bowel Diseases
  •   
  •   
  • PK
  •   
  • GN
Publications

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB01222
KEGG Drug ID:
D00246
PubChem Compound ID:
63006
PubChem Substance ID:
7847312

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

PharmGKB integrates drug information from different sources: DrugBank, Open Eye Scientific Software.
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