Drug/Small Molecule:
salmeterol

PharmGKB contains no dosing guidelines for this drug/small molecule. To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.

PharmGKB has no annotated drug labels with pharmacogenomic information for this drug/small molecule. If you know of a drug label with PGx, send us a message.

Links to Unannotated Labels

These links are to labels associated with salmeterol that have not been annotated by PharmGKB.

  1. DailyMed - DrugLabel PA166105243

PharmGKB contains no Clinical Variants that meet the highest level of criteria.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?

The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

Gene ? Variant?
(138)
Alternate Names / Tag SNPs ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available CA VA
rs1042713 148206440G>A, 148206440G>G, 46A>A, 46A>G, 46G>A, 5285A>A, 5285A>G, 9369367G>A, 9369367G>G, ADRB2:16Arg>Gly, ADRB2:Arg16Gly, ADRB2:Gly16Arg, Arg16, Arg16=
G > A
Missense
Arg16Gly
VIP No Clinical Annotations available No Variant Annotations available
rs776746 12083G>A, 219-237G>A, 321-1G>A, 37303382C>T, 581-237G>A, 689-1G>A, 99270539C>T, CYP3A5*1, CYP3A5*3, CYP3A5*3C, CYP3A5:6986A>G, g.6986A>G, intron 3 splicing defect, rs776746 A>G
C > T
Acceptor
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 138
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • Salmeterolum [Latin]
Trade Names
  • Aeromax
  • Arial
  • Astmerole
  • Fujimycin
  • Salmetedur
  • Serevent
Brand Mixture Names
  • Advair 100 Diskus (Fluticasone Propionate + Salmeterol Xinafoate)
  • Advair 125 (Fluticasone Propionate + Salmeterol Xinafoate)
  • Advair 250 (Fluticasone Propionate + Salmeterol Xinafoate)
  • Advair 250 Diskus (Fluticasone Propionate + Salmeterol Xinafoate)
  • Advair 500 Diskus (Fluticasone Propionate + Salmeterol Xinafoate)

PharmGKB Accession Id:
PA451300

Description

Salmeterol is a long-acting beta2-adrenergic receptor agonist drug that is currently prescribed for the treatment of asthma and chronic obstructive pulmonary disease COPD.

Source: Drug Bank

Indication

For the treatment of asthma and chronic obstructive pulmonary disease (COPD).

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Salmeterol's long, lipophilic side chain binds to exosites near beta(2)-receptors in the lungs and on bronchiolar smooth muscle, allowing the active portion of the molecule to remain at the receptor site, continually binding and releasing. Beta(2)-receptor stimulation in the lung causes relaxation of bronchial smooth muscle, bronchodilation, and increased bronchial airflow.

Source: Drug Bank

Pharmacology

Salmeterol is a long acting beta2-adrenoceptor agonist (LABA), usually only prescribed for severe persistent asthma following previous treatment with a short-acting beta agonist such as salbutamol and is prescribed concurrently with a corticosteroid, such as beclometasone. The primary noticable difference of salmeterol to salbutamol is that the duration of action lasts approximately 12 hours in comparison with 4-6 hours of salbutamol. When used regularly every day as presecribed, inhaled salmeterol decreases the number and severity of asthma attacks. However, it is not for use for relieving an asthma attack that has already started. Inhaled salmeterol works like other beta 2-agonists, causing bronchodilatation by relaxing the smooth muscle in the airway so as to treat the exacerbation of asthma. Salmeterol is similar in action to formoterol, however formoterol has been demonstrated to have a faster onset of action than salmeterol as a result of a lower lipophilicity, and has also been demonstrated to be more potent - a 12 microg dose of formoterol has been demonstrated to be equivalent to a 50 microg dose of salmeterol.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic, metabolized by hydroxylation via CYP3A4

Source: Drug Bank

Protein Binding

96%

Source: Drug Bank

Absorption

Because of the small therapeutic dose, systemic levels of salmeterol are low or undetectable after inhalation of recommended doses.

Source: Drug Bank

Half-Life

5.5 hours

Source: Drug Bank

Toxicity

Symptoms of overdose include angina (chest pain), dizziness, dry mouth, fatigue, flu-like symptoms, headache, heart irregularities, high or low blood pressure, high blood sugar, insomnia, muscle cramps, nausea, nervousness, rapid heartbeat, seizures, and tremor. By the oral route, no deaths occurred in rats at 1,000 mg/kg (approximately 81,000 times the maximum recommended daily inhalation dose in adults and approximately 38,000 times the maximum recommended daily inhalation dose in children on a mg/m 2 basis).

Source: Drug Bank

Chemical Properties

Chemical Formula

C25H37NO4

Source: Drug Bank

Isomeric SMILES

c1ccc(cc1)CCCCOCCCCCCNCC(c2ccc(c(c2)CO)O)O

Source: OpenEye

Canonical SMILES

OCC1=C(O)C=CC(=C1)C(O)CNCCCCCCOCCCCC1=CC=CC=C1

Source: Drug Bank

Average Molecular Weight

415.5656

Source: Drug Bank

Monoisotopic Molecular Weight

415.272258677

Source: Drug Bank

PharmGKB Curated Pathways

Pathways created internally by PharmGKB based primarily on literature evidence.

  1. Beta-agonist/Beta-blocker Pathway, Pharmacodynamics
    Simplified pharmacodynamic pathway of drug action on beta 2 adrenergic receptor in a stylized airway cell.
  1. Sympathetic Nerve Pathway (Neuroeffector Junction)
    Simplified diagram of a sympathetic neuroeffector junction displaying genes which may be involved.

External Pathways

Links to non-PharmGKB pathways.

PharmGKB contains no links to external pathways for this drug. To report a pathway, click here.

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

EvidenceGene
No Dosing Guideline available No Drug Label available CA VA No VIP available PW
ADRB2
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
CYP3A4
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
CYP3A5

Drug Targets

Gene Description
ADRB2 (source: Drug Bank)

Drug Interactions

Drug Description
salmeterol Antagonism (source: Drug Bank)
salmeterol Antagonism (source: Drug Bank)
salmeterol Antagonism (source: Drug Bank)
salmeterol Antagonism (source: Drug Bank)
salmeterol Antagonism (source: Drug Bank)
salmeterol Antagonism (source: Drug Bank)
salmeterol Antagonism (source: Drug Bank)
salmeterol Antagonism (source: Drug Bank)
salmeterol Antagonism (source: Drug Bank)
salmeterol Antagonism (source: Drug Bank)
salmeterol Antagonism (source: Drug Bank)
salmeterol Antagonism (source: Drug Bank)
salmeterol Antagonism (source: Drug Bank)
salmeterol Antagonism (source: Drug Bank)
salmeterol Antagonism (source: Drug Bank)
salmeterol Antagonism (source: Drug Bank)
salmeterol Antagonism (source: Drug Bank)
salmeterol Antagonism (source: Drug Bank)
salmeterol Antagonism (source: Drug Bank)
salmeterol Antagonism (source: Drug Bank)
salmeterol Antagonism (source: Drug Bank)
salmeterol This combination presents an increased risk of toxicity (source: Drug Bank)
salmeterol Telithromycin may reduce clearance of Salmeterol. Concomitant therapy is contraindicated. (source: Drug Bank)
salmeterol Antagonism (source: Drug Bank)
salmeterol Antagonism (source: Drug Bank)
salmeterol Voriconazole, a strong CYP3A4 inhibitor may increase the serum concentration of salmeterol by decreasing its metabolism. Consider alternate therapy. (source: Drug Bank)

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
May Prevent
Contraindicated With

Publications related to salmeterol: 24

No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
The effects of a Gly16Arg ADRB2 polymorphism on responses to salmeterol or montelukast in Japanese patients with mild persistent asthma. Pharmacogenetics and genomics. 2014. Konno Satoshi, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Arg16 ADRB2 genotype increases the risk of asthma exacerbation in children with a reported use of long-acting beta2-agonists: results of the pacman cohort. Pharmacogenomics. 2013. Zuurhout Miranda Jl, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Tailored second line therapy in asthmatic children with the arginine-16 genotype. Clinical science (London, England : 1979). 2012. Lipworth Brian J, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Integrative systems biology approaches in asthma pharmacogenomics. Pharmacogenomics. 2012. Dahlin Amber, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
beta2-adrenergic receptor haplotype may be associated with susceptibility to desensitization to long-acting beta2-agonists in COPD patients. Lung. 2012. Mochizuki Hideaki, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB summary: very important pharmacogene information for CYP3A5. Pharmacogenetics and genomics. 2012. Lamba Jatinder, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Beta2-receptor polymorphisms in patients receiving salmeterol with or without fluticasone propionate. American journal of respiratory and critical care medicine. 2010. Bleecker Eugene R, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Adrenergic beta(2)-receptor genotype predisposes to exacerbations in steroid-treated asthmatic patients taking frequent albuterol or salmeterol. The Journal of allergy and clinical immunology. 2009. Basu Kaninika, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Effect of beta2-adrenergic receptor polymorphism on response to longacting beta2 agonist in asthma (LARGE trial): a genotype-stratified, randomised, placebo-controlled, crossover trial. Lancet. 2009. Wechsler Michael E, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Acute and chronic lung function responses to salmeterol and salmeterol plus fluticasone propionate in relation to Arg16Gly beta(2)-adrenergic polymorphisms. Current medical research and opinion. 2009. Yancey Steven W, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Association between CRHR1 polymorphism and improved lung function in response to inhaled corticosteroid in patients with COPD. Respirology (Carlton, Vic.). 2009. Kim Woo J, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation. Analytical and bioanalytical chemistry. 2008. Zanger Ulrich M, et al. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Effect of ADRB2 polymorphisms on response to longacting beta2-agonist therapy: a pharmacogenetic analysis of two randomised studies. Lancet. 2007. Bleecker Eugene R, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Salmeterol and fluticasone propionate and survival in chronic obstructive pulmonary disease. The New England journal of medicine. 2007. Calverley Peter M A, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Arginine-16 beta2 adrenoceptor genotype predisposes to exacerbations in young asthmatics taking regular salmeterol. Thorax. 2006. Palmer C N A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Salmeterol response is not affected by beta2-adrenergic receptor genotype in subjects with persistent asthma. The Journal of allergy and clinical immunology. 2006. Bleecker Eugene R, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
beta-Adrenergic receptor polymorphisms and response to salmeterol. American journal of respiratory and critical care medicine. 2006. Wechsler Michael E, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Molecular mechanisms of beta(2)-adrenergic receptor function, response, and regulation. The Journal of allergy and clinical immunology. 2006. Johnson Malcolm. PubMed
No Dosing Guideline available No Drug Label available CA No Variant Annotation available No VIP available No VIP available
Use of regularly scheduled albuterol treatment in asthma: genotype-stratified, randomised, placebo-controlled cross-over trial. Lancet. 2004. Israel Elliot, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Salmeterol (Serevent) asthma trial halted early. CMAJ : Canadian Medical Association journal = journal de l'Association medicale canadienne. 2003. Wooltorton Eric. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenetics of asthma. American journal of respiratory and critical care medicine. 2002. Palmer Lyle J, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The Ile164 beta(2)-adrenoceptor polymorphism alters salmeterol exosite binding and conventional agonist coupling to G(s). European journal of pharmacology. 2001. Green S A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Asthma exacerbations during long term beta agonist use: influence of beta(2) adrenoceptor polymorphism. Thorax. 2000. Taylor D R, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The aliphatic oxidation of salmeterol to alpha-hydroxysalmeterol in human liver microsomes is catalyzed by CYP3A. Drug metabolism and disposition: the biological fate of chemicals. 1996. Manchee G R, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00938
KEGG Compound:
C07241
KEGG Drug:
D05792
PubChem Compound:
5152
PubChem Substance:
205141
46508024
IUPHAR Ligand:
559
Drugs Product Database (DPD):
2231129
BindingDB:
25771
ChemSpider:
4968
Therapeutic Targets Database:
DAP000947

Clinical Trials

These are trials that mention salmeterol and are related to either pharmacogenetics or pharmacogenomics.

Common Searches

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.