Drug/Small Molecule:
sumatriptan

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 contains no drug labels with pharmacogenomic information for this drug/small molecule. To report a drug label with PGx, click here.

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
rs5443 10501C>T, 47295C>T, 6894875C>T, 6954875C>T, 825C>T, GNB3:825C>T, GNB3:Ser275Ser, Ser275=
C > T
Synonymous
Ser275Ser
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 138
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • NP101
  • Sumatriptan Succinate
  • Sumatriptanum [INN-Latin]
  • estradiol
  • sumatriptan
  • triptan
Trade Names
  • Imigran
  • Imitrex
  • Imitrex Oral
  • Sumatran
  • Sumax
Brand Mixture Names

PharmGKB Accession Id:
PA451566

Description

A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of migraine disorders. A transdermal patch version of sumatriptan is currently in phase I trials in the U.S. under the code name NP101 (NuPathe).

Source: Drug Bank

Indication

For the treatment of migraine attacks with or without aura.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

The 5-HT 1B and 5-HT 1D receptors function as autoreceptors, which inhibit the firing of serotonin neurons and a reduction in the synthesis and release of serotonin upon activation. After sumatriptan binds to these receptors, adenylate cyclase activity is inhibited via regulatory G proteins, incrases intracellular calcium, and affects other intracellular events. This results in vasoconstriction and inhibtion of sensory nociceptive (trigeminal) nerve firing and vasoactive neuropeptide release.

Source: Drug Bank

Pharmacology

Sumatriptan, an antimigraine drug, is a selective agonist of vascular serotonin ((5-hydroxytryptamine; 5-HT) type 1-like receptors, likely the 5-HT 1D and 5-HT 1B subtypes. It has no significant affinity (as measured using standard radioligand binding assays) or pharmacological activity at 5-HT2, 5-HT3 receptor subtypes or at alpha1-, alpha2-, or beta-adrenergic; dopamine1; dopamine2; muscarinic; or benzodiazepine receptors.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic. In vitro studies with human microsomes suggest that sumatriptan is metabolized by monoamine oxidase (MAO), predominantly the A isoenzyme.

Source: Drug Bank

Protein Binding

14%-21%

Source: Drug Bank

Absorption

Approximately 15%

Source: Drug Bank

Half-Life

2.5 hours

Source: Drug Bank

Toxicity

Symptoms of overdose include convulsions, tremor, paralysis, inactivity, ptosis, erythema of the extremities, abnormal respiration, cyanosis, ataxia, mydriasis, salivation, and lacrimation.

Source: Drug Bank

Clearance

Source: Drug Bank

Route of Elimination

Only 3% of the dose is excreted in the urine as unchanged sumatriptan; 42% of the dose is excreted as the major metabolite, the indole acetic acid analogue of sumatriptan.

Source: Drug Bank

Volume of Distribution

Source: Drug Bank

Chemical Properties

Chemical Formula

C14H21N3O2S

Source: Drug Bank

Isomeric SMILES

CNS(=O)(=O)Cc1ccc2c(c1)c(c[nH]2)CCN(C)C

Source: OpenEye

Canonical SMILES

CNS(=O)(=O)CC1=CC2=C(NC=C2CCN(C)C)C=C1

Source: Drug Bank

Average Molecular Weight

295.4

Source: Drug Bank

Monoisotopic Molecular Weight

295.135447621

Source: Drug Bank

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 No VIP available
GNB3

Drug Targets

Gene Description
HTR1A (source: Drug Bank)
HTR1B (source: Drug Bank)
HTR1D (source: Drug Bank)
HTR1F (source: Drug Bank)
HTR2B (source: Drug Bank)

Drug Interactions

Drug Description
sumatriptan Increased risk of CNS adverse effects (source: Drug Bank)
sumatriptan Increased risk of CNS adverse effects (source: Drug Bank)
sumatriptan Possible severe and prolonged vasoconstriction (source: Drug Bank)
sumatriptan Possible severe and prolonged vasoconstriction (source: Drug Bank)
sumatriptan Possible severe and prolonged vasoconstriction (source: Drug Bank)
sumatriptan Possible severe and prolonged vasoconstriction (source: Drug Bank)
sumatriptan Increased risk of CNS adverse effects (source: Drug Bank)
sumatriptan Increased risk of CNS adverse effects (source: Drug Bank)
sumatriptan Increased risk of CNS adverse effects (source: Drug Bank)
sumatriptan Increased risk of CNS adverse effects (source: Drug Bank)
sumatriptan Increased risk of CNS adverse effects (source: Drug Bank)
sumatriptan Increased risk of CNS adverse effects (source: Drug Bank)
sumatriptan MAO inhibitor increases the effects and toxicity of 5-HT agonist (source: Drug Bank)
sumatriptan MAO inhibitor increases the effects and toxicity of 5-HT agonist (source: Drug Bank)
sumatriptan Possible serotoninergic syndrome with this combination (source: Drug Bank)
sumatriptan Possible serotoninergic syndrome with this combination (source: Drug Bank)
sumatriptan Possible severe and prolonged vasoconstriction (source: Drug Bank)
sumatriptan Possible severe and prolonged vasoconstriction (source: Drug Bank)
sumatriptan Increased risk of CNS adverse effects (source: Drug Bank)
sumatriptan Increased risk of CNS adverse effects (source: Drug Bank)
sumatriptan Increased risk of CNS adverse effects (source: Drug Bank)
sumatriptan Increased risk of CNS adverse effects (source: Drug Bank)
sumatriptan The MAO inhibitor increases the effect and toxicity of 5-HT agonist (source: Drug Bank)
sumatriptan The MAO inhibitor increases the effect and toxicity of 5-HT agonist (source: Drug Bank)
sumatriptan Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome. (source: Drug Bank)
sumatriptan The MAO inhibitor, Tranylcypromine, may reduce the metabolism and clearance of the serotonin 5-HT1D receptor agonist, Sumatriptan. Risk of serotonin syndrome and Sumatriptan toxicity. Concomitant therapy should be avoided. (source: Drug Bank)
sumatriptan Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome. (source: Drug Bank)
sumatriptan Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome. (source: Drug Bank)
sumatriptan Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome. (source: Drug Bank)
sumatriptan Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome. (source: Drug Bank)
sumatriptan Concomitant use of two serotonin 5-HT1D receptor agonists, such as zolmitriptan and sumatriptan, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated. (source: Drug Bank)

Curated Information ?

EvidenceDisease
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Cluster Headache

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

May Treat
Contraindicated With

Publications related to sumatriptan: 1

No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
G protein beta3 polymorphism and triptan response in cluster headache. Clinical pharmacology and therapeutics. 2007. Sch├╝rks M, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0173-0524-00
DrugBank:
DB00669
ChEBI:
10650
KEGG Compound:
C07319
KEGG Drug:
D00451
PubChem Compound:
5358
PubChem Substance:
46506520
7847517
IUPHAR Ligand:
119
54
Drugs Product Database (DPD):
2239738
ChemSpider:
5165
Therapeutic Targets Database:
DNC001649
FDA Drug Label at DailyMed:
cc11b09d-e6cc-4cf8-1495-5ac64d5aae5f

Clinical Trials

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

Common Searches

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