- Overview
- Properties
- Genetics
- Related Genes
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Overview
| Generic Names: | NP101; Sumatriptan Succinate; Sumatriptanum [INN-Latin]; estradiol; sumatriptan; triptan |
|---|---|
| Trade Names: | Imigran; Imitrex; Sumatran; Sumax |
| 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 in adults (source: Drug Bank)
ATC Therapeutic Category
- N02CC:Selective serotonin (5HT1) agonists
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Sumatriptan stimulates 5-HT receptors of the 1D subtype, most likely presynaptic receptors, resulting in selective vasoconstriction of inflamed and dilated cranial blood vessels in the carotid circulation. Sumatriptan also blocks the release of vasoactive neuropeptides from perivascular trigeminal axons in the dura mater during migraine and may inhibit the release of inflammatory mediators from the trigeminal nerve. (source: Drug Bank)
Pharmacology
Sumatriptan, an antimigraine drug, is structurally similar to serotonin. It is thought that the cerebral blood vessel constriction induced by activation of 5-HT1 receptors on those vessels may contribute to the antimigrainous effect of sumatriptan in humans. (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)
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)
Isomeric SMILES Code:
CNS(=O)(=O)Cc1ccc2c(c1)c(c[nH]2)CCN(C)C (source: Drug Bank)
Curated Annotations (
)
-
rs5443
at chr12:6825136
in
GNB3,
USP5
A study on a total of 180 migraine and cluster headache patients found that pain relief by triptans is significantly modulated by this common genetic GNB3 variant.- Variant Name:
- GNB3:825C>T; GNB3:Ser275Ser
- Related Drugs:
- almotriptan, eletriptan, naratriptan, rizatriptan, sumatriptan, zolmitriptan
- Related Diseases:
- Migraine without Aura
- Evidence:
-
PMID:17361120
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
|
GNB3 |
|
Variants |
|
|
USP5 |
|
Variants |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| HTR1B |
|
(source: Drug Bank) |
| HTR1D |
|
(source: Drug Bank) |
| HTR1F |
|
(source: Drug Bank) |
| HTR2B |
|
(source: Drug Bank) |
PharmGKB Curated Pathways
A list of non-curated publications that mention this drug along with other drugs is available.
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.