PharmGKB: The Pharmacogenomics Knowledge Base

Drug/Small Molecule:
salbutamol

2D structure

Overview

Generic Names: Albuterol; Albuterol Sulfate; Albuterol Sulphate; Levalbuterol; Salbutamol Sulfate; Salbutamol Sulphate
Trade Names: Accuneb; Aerolin; Airomir; Asmaven; Asmol; Asthalin; Asthavent; Broncovaleas; Buventol; Cetsim; Cobutolin; Ecovent; Loftan; ProAir; Proventil; Rotahaler; Salamol; Salbulin; Salbutard; Salbutine; Salbuvent; Solbutamol; Sultanol; Venetlin; Ventalin Inhaler; Ventolin; Ventolin Inhaler; Ventolin Rotacaps; Volma; Volmax; Xopenex
Brand Mixtures: Combivent (Ipratropium Bromide + Salbutamol Sulfate); Gen-Combo Sterinebs (Ipratropium Bromide + Salbutamol Sulfate)
PharmGKB Accession Id: PA448068

Description

A racemic mixture with a 1:1 ratio of the r-isomer, levalbuterol, and s-albuterol. It is a short-acting beta2-adrenergic agonist with its main clinical use in asthma. PubChem (source: Drug Bank)

Indication

For relief and prevention of bronchospasm due to asthma, emphysema, and chronic bronchitis. (source: Drug Bank)

ATC Therapeutic Categories

  • R03AC:Selective beta-2-adrenoreceptor agonists
  • R03CC:Selective beta-2-adrenoreceptor agonists

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Salbutamol is a beta(2)-adrenergic agonist and thus it stimulates beta(2)-adrenergic receptors. Binding of albuterol to beta(2)-receptors in the lungs results in relaxation of bronchial smooth muscles. It is believed that salbutamol increases cAMP production by activating adenylate cyclase, and the actions of salbutamol are mediated by cAMP. Increased intracellular cyclic AMP increases the activity of cAMP-dependent protein kinase A, which inhibits the phosphorylation of myosin and lowers intracellular calcium concentrations. A lowered intracellular calcium concentration leads to a smooth muscle relaxation. Increased intracellular cyclic AMP concentrations also cause an inhibition of the release of mediators from mast cells in the airways. (source: Drug Bank)

Pharmacology

Salbutamol (INN) or albuterol (USAN), a moderately selective beta(2)-receptor agonist similar in structure to terbutaline, is widely used as a bronchodilator to manage asthma and other chronic obstructive airway diseases. The R-isomer, levalbuterol, is responsible for bronchodilation while the S-isomer increases bronchial reactivity. The R-enantiomer is sold in its pure form as Levalbuterol. The manufacturer of levalbuterol, Sepracor, has implied (although not directly claimed) that the presence of only the R-enantiomer produces fewer side-effects. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hydrolyzed by esterases in tissue and blood to the active compound colterol. The drug is also conjugatively metabolized to salbutamol 4'-O-sulfate. (source: Drug Bank)

Absorption

Systemic absorption is rapid following aerosol administration. (source: Drug Bank)

Toxicity

LD<sub>50</sub>=1100 mg/kg (orally in mice) (source: Drug Bank)

Isomeric SMILES Code:

CC(C)(C)NC[C@@H](C1=CC(=C(C=C1)O)CO)O (source: Drug Bank)

Curated Annotations (Curated Annotation)

  1. rs1042713 at chr5:148186633 in ADRB2
    Subjects who are homozygous for Arg16 and who were on regular albuterol treatment were reported to have lower morning peak flows compared with those who were not on regular albuterol treatment, suggesting that regular albuterol therapy may not be appropriate for Arg16 homozygous subjects.
    Variant Name:
    ADRB2: Gly16Arg; 46G>A; Arg16
    Related Drugs:
    salbutamol
    Related Diseases:
    Asthma
    Evidence:
    PMID:15500895
  2. rs881152 at chr5:172131161 in DUSP1
    Risk or phenotype-associated allele: GG. Phenotype: The GG genotype was associated with greater change in FEV in response to salbutamol in asthma patients with concurrent use of inhaled corticosteroids. This association was found in the GALA cohort and replicated in the SAPPHIRE cohort but not the SAGE cohort. Study size: n = 646 (GALA); n = 264 (SAGE); n = 430 (SAPPHIRE). Study population/ethnicity: Asthma; Genetics of Asthma in Latino Americans (GALA) study; Study of African Americans, Asthma, Genes & Environments (SAGE); Study of Asthma Phenotypes and Pharmacogenomic Interactions by Race-ethnicity (SAPPHIRE); Mexican American; Puerto Rican American; Hispanic; African American. Significance metric(s): p = 0.02 (GALA). Type of association: PD.
    Variant Name:
    DUSP1 rs881152 G>A
    Related Drugs:
    beclomethasone, corticosteroids, glucocorticoids, salbutamol
    Related Diseases:
    Asthma
    Evidence:
    PMID:20673984
  3. 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
  4. rs2267715 at chr7:30682612 in CRHR2
    This variant in the corticotropin-releasing hormone receptor-2 gene was associated with acute bronchodilator response in the 608-participant Childhood Asthma Management Program (CAMP), but was not found to be associated in the 427-participant Sepracor study or the 152-participant LODO trial. The mean ages of the participants in the CAMP, Sepracor, and Lodo cohorts were 8.9, 32.6, and 42.9 years of age, respectively. Only Caucasians were analyzed in each of these studies.
    Related Drugs:
    salbutamol, selective beta-2-adrenoreceptor agonists
    Related Diseases:
    Asthma
    Evidence:
    PMID:18408560
  5. rs2284220 at chr7:30684628 in CRHR2
    This variant in the corticotropin-releasing hormone receptor-2 gene was associated with acute bronchodilator response in the 427-participant Sepracor study, but not in the 608-participant Childhood Asthma Management Program (CAMP) or the 152-participant LODO trial. The mean ages of the participants in the CAMP, Sepracor, and Lodo cohorts were 8.9, 32.6, and 42.9 years of age, respectively. Only Caucasians were analyzed in each of these studies.
    Related Drugs:
    salbutamol, selective beta-2-adrenoreceptor agonists
    Related Diseases:
    Asthma
    Evidence:
    PMID:18408560
  6. rs7793837 at chr7:30693302 in CRHR2
    Risk or phenotype-associated allele: T Phenotype: The T variant of CRHR2 rs7793837 was associated with reduced acute bronchodilation response to short-acting beta2-agonist treatment in the CAMP and LODO studies but not the Sepracor study. Study size: 607 (CAMP); 152 (LODO); 427 (Sepracor) Study population/ethnicity: Caucasian children with asthma with a mean age of 8.83 years enrolled in the Childhood Asthma Management Program (CAMP); Adult Caucasian participants with asthma enrolled in the Clinical Trial of Low-Dose Theophylline and Montelukast conducted by the American Lung Association Asthma Clinical Research Centers (LODO); Adult Caucasian participants with asthma enrolled in a completed clinical trial conducted by Sepracor Inc. Significance metric(s): p = 0.003 (CAMP); p = 0.05 (LODO); p = 0.24 (Sepracor) Type of association: PD
    Variant Name:
    CRHR2: Intronic, downstream of exon beta 1b
    Related Drugs:
    salbutamol, selective beta-2-adrenoreceptor agonists
    Related Diseases:
    Asthma
    Evidence:
    PMID:18408560
  7. rs255100 at chr7:30695433 in CRHR2
    This variant in the corticotropin-releasing hormone receptor-2 gene was associated with acute bronchodilator response in the 608-participant Childhood Asthma Management Program (CAMP), but was not found to be associated in the 427-participant Sepracor study or the 152-participant LODO trial. The mean ages of the participants in the CAMP, Sepracor, and Lodo cohorts were 8.9, 32.6, and 42.9 years of age, respectively. Only Caucasians were analyzed in each of these studies.
    Related Drugs:
    salbutamol, selective beta-2-adrenoreceptor agonists
    Related Diseases:
    Asthma
    Evidence:
    PMID:18408560
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
No phenotype data Genotype Data Available Literature annotations available Not annotated
ADH5
  •   
  •   
  •   
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
ADRB2
  • CO
  • PD
  • PK
  • FA
  • GN
Publications, Variants
No phenotype data No genotype data Literature annotations available Not annotated
ARG1
  • CO
  •   
  •   
  •   
  • GN
Publications, Variants
No phenotype data No genotype data Literature annotations available Not annotated
BEST3
  • CO
  •   
  •   
  •   
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
CRHR2
  • CO
  •   
  •   
  •   
  • GN
Publications, Variants
No phenotype data No genotype data Literature annotations available Not annotated
DDC
  • CO
  •   
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
DUSP1
  •   
  • PD
  •   
  •   
  • GN
Publications, Variants
No phenotype data Genotype Data Available Literature annotations available Not annotated
GPR162
  • CO
  •   
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
IL12B
  • CO
  •   
  •   
  •   
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
IL6
  •   
  •   
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
IL6R
  •   
  •   
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
IL8RA
  • CO
  •   
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
LRIG3
  • CO
  •   
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
MAPT
  • CO
  •   
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
NCOR2
  • CO
  •   
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
PPM1H
  • CO
  •   
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
PRKCA
  • CO
  •   
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
SRGAP1
  • CO
  •   
  •   
  •   
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
TBX21
  • CO
  •   
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
TMEM19
  • CO
  •   
  •   
  •   
  • GN
Publications

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

Drug Targets

Gene Description
ADRB2 Uncurated Annotation (source: Drug Bank)
IL8 Uncurated Annotation (source: Drug Bank)

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

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
  • PK
  • FA
  • GN
Publications, Variants
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Essential hypertension
  •   
  • PD
  •   
  •   
  • GN
Publications

Non-Curated Information

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

Curated Phenotype Datasets

These datasets are sorted alphabetically by title.

  1. Bronchodilator response to beta agonist in asthmatics
    • Genotype data available
    • Phenotype data available
    • No literature annotations
    • Not annotated
    • PD
    Submitted by Richard Judson, PhD involving ADRB2, salbutamol, and Asthma

Additional Datasets

These datasets are minimally curated and are sorted alphabetically by title.

  1. National Heart, Lung, and Blood Institute SNP Health Association Asthma Resource Project (SHARP). dbGaP ID: phs000166.v1.p1
  2. Physicochemical determinants of human renal clearance
  3. The Connectivity Map: using gene-expression signatures to connect small molecules, genes, and disease

Downloads

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LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB01001
ChEBI ID:
2549
KEGG Drug ID:
D02147
PubChem Compound ID:
2083
PubChem Substance ID:
171517
IUPHAR Ligand ID:
558

Common Searches

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Non-Curated Publications

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

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