pharmacopeia
GET
/api/v1/drug/sumatriptan
2D structure
1-[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]-N-methylmethanesulfonamide
SMILES CNS(=O)(=O)CC1=CC2=C(C=C1)NC=C2CCN(C)C
InChIKey KQKPFRSPSRPDEB-UHFFFAOYSA-N

Mechanism of action

Sourced from openFDA

Sumatriptan binds with high affinity to human cloned 5-HT 1B/1D receptors. Sumatriptan presumably exerts its therapeutic effects in the treatment of migraine and cluster headaches through agonist effects at the 5-HT 1B/1D receptors on intracranial blood vessels and sensory nerves of the trigeminal system, which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release.

Monoamine OxidaseSerotoninSerotonin 1b ReceptorSerotonin 1d Receptor

Indications

Sourced from openFDA
  • Sumatriptan Injection, USP is indicated in adults for (1) the acute treatment of migraine, with or without aura, and (2) the acute treatment of cluster headache. Limitations of Use: • Use only if a clear diagnosis of migraine or cluster headache has been established.ICD-10: G43.909, R51.9

Contraindications

Sourced from openFDA
  • Sumatriptan Injection is contraindicated in patients with: • Ischemic coronary artery disease (CAD) (angina pectoris, history of myocardial infarction, or documented silent ischemia) or coronary artery vasospasm, including Prinzmetal’s angina [see Warnings and Precautions (5.1)]. • Wolff-Parkinson-White syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders [see Warnings and Precautions (5.2)].contraindicated

Dosage & administration

Sourced from openFDA

• For subcutaneous use only (2.1) • Acute treatment of migraine: single dose of 1 to 6 mg (2.1) • Acute treatment of cluster headache: single dose of 6 mg (2.1) • Maximum dose in a 24-hour period: 12 mg, separate doses by at least 1 hour (2.1) • Patients receiving doses other than 4 or 6 mg: Use the 6-mg single-dose vial (2.3) 2.1 Dosing Information The maximum single recommended adult dose of Sumatriptan injection, USP for the acute treatment of migraine or cluster headache is 6 mg injected subcutaneously. For the treatment of migraine, if side effects are dose limiting, lower doses (1 mg to 5 mg) may be used [see Clinical Studies (14.1)]. For the treatment of cluster headache, the efficacy of lower doses has not been established. The maximum cumulative dose that may be given in 24 hours is 12 mg, two 6 mg injections separated by at least 1 hour. A second 6-mg dose should only be considered if some response to a first injection was observed. 2.3 Administration of Doses of Sumatriptan Other than 4 or 6 mg In patients receiving doses other than 4mg or 6 mg, use the 6-mg single-dose vial; Visually inspect the vial for particulate matter and discoloration before administration. Do not use if particulates and discolorations are noted.

Warnings & precautions

Sourced from openFDA

• Myocardial ischemia/infarction and Prinzmetal’s angina: Perform cardiac evaluation in patients with multiple cardiovascular risk factors (5.1) • Arrhythmias: Discontinue Sumatriptan Injection if occurs (5.2) • Chest/throat/neck/jaw pain, tightness, pressure, or heaviness: Generally not associated with myocardial ischemia; evaluate for coronary artery disease in patients at high risk (5.3) • Cerebral hemorrhage, subarachnoid hemorrhage, and stroke: Discontinue Sumatriptan Injection if occurs (5.4) • Gastrointestinal ischemic reactions and peripheral vasospastic reactions: Discontinue Sumatriptan Injection if occurs (5.5) • Medication overuse headache: Detoxification may be necessary (5.6) • Serotonin syndrome: Discontinue Sumatriptan Injection if occurs (5.7) • Seizures: Use with caution in patients with epilepsy or a lowered seizure threshold (5.10) 5.1 Myocardial Ischemia, Myocardial Infarction, and Prinzmetal's Angina The use of sumatriptan injection is contraindicated in patients with ischemic or vasospastic CAD. There have been rare reports of serious cardiac adverse reactions, including acute myocardial infarction, occurring within a few hours following administration of sumatriptan injection. Some of these reactions occurred in patients without known CAD. Sumatriptan injection may cause coronary artery vasospasm (Prinzmetal’s angina), even in patients without a history of CAD.

Adverse reactions

Sourced from openFDA

The following serious adverse reactions are described below and elsewhere in the labeling: · Myocardial ischemia, myocardial infarction, and Prinzmetal’s angina [see Warnings and Precautions (5.1)] · Arrhythmias [see Warnings and Precautions (5.2)] · Chest, throat, neck, and/or jaw pain/tightness/pressure [see Warnings and Precautions (5.3)] · Cerebrovascular events [see Warnings and Precautions (5.4)] · Other vasospasm reactions [see Warnings and Precautions (5.5)] · Medication overuse headache [see Warnings and Precautions (5.6)] · Serotonin syndrome [see Warnings and Precautions (5.7)] · Increase in blood pressure [see Warnings and Precautions (5.8)] · Hypersensitivity reactions [see Contraindications (4), Warnings and Precautions (5.9)] · Seizures [see Warnings and Precautions (5.10)] Most common adverse reactions (≥5% and >placebo) were injection site reactions, tingling, dizziness/vertigo, warm/hot sensation, burning sensation, feeling of heaviness, pressure sensation, flushing, feeling of tightness, and numbness (6.1) To report SUSPECTED ADVERSE REACTIONS, contact Caplin Steriles Limited at 1-866-978-6111 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared with rates in the clinical trials of another drug and may not reflect the rates observed in practice. Migraine Headache Table 1 lists adverse reactions that occurred in 2 U.S.

Use in specific populations

Sourced from openFDA

Pregnancy: Based on animal data, may cause fetal harm (8.1) 8.1 Pregnancy Risk Summary Data from a prospective pregnancy exposure registry and epidemiological studies of pregnant women have not detected an increased frequency of birth defects or a consistent pattern of birth defects among women exposed to sumatriptan compared with the general population (see Data). In developmental toxicity studies in rats and rabbits, oral administration of sumatriptan to pregnant animals was associated with embryolethality, fetal abnormalities, and pup mortality. When administered by the intravenous route to pregnant rabbits, sumatriptan was embryolethal (see Data). In the U.S. general population, the estimated background risk of major birth defects and of miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. The reported rate of major birth defects among deliveries to women with migraine ranged from 2.2% to 2.9% and the reported rate of miscarriage was 17%, which were similar to rates reported in women without migraine. Clinical Considerations Disease-Associated Maternal and/or Embryo/Fetal Risk: Several studies have suggested that women with migraine may be at increased risk of preeclampsia during pregnancy.

Pharmacokinetics

Sourced from openFDA
Metabolism
Absorption The bioavailability of sumatriptan via subcutaneous site injection to 18 healthy male subjects was 97% ± 16% of that obtained following intravenous injection. After a single 6-mg subcutaneous manual injection into the deltoid area of the arm in 18 healthy males (age: 24 ± 6 years, weight: 70 kg), the maximum serum concentration (C max ) of sumatriptan was (mean ± standard deviation) 74 ± 15 ng/mL and the time to peak concentration (T max ) was 12 minutes after injection (range: 5 to 20 minutes).

Overdosage

Sourced from openFDA

Coronary vasospasm was observed after intravenous administration of sumatriptan injection [see Contraindications (4)]. Overdoses would be expected from animal data (dogs at 0.1 g/kg, rats at 2 g/kg) to possibly cause convulsions, tremor, inactivity, erythema of the extremities, reduced respiratory rate, cyanosis, ataxia, mydriasis, injection site reactions (desquamation, hair loss, and scab formation), and paralysis. The elimination half-life of sumatriptan is about 2 hours [see Clinical Pharmacology (12.3)] ; therefore, monitoring of patients after overdose with sumatriptan injection should continue for at least 10 hours or while symptoms or signs persist. It is unknown what effect hemodialysis or peritoneal dialysis has on the serum concentrations of sumatriptan.

Approval history

Sourced from openFDA
  • Dec 28, 1992NDANDA020080Glaxosmithkline
  • Jun 1, 1995NDANDA020132Glaxosmithkline
  • Aug 26, 1997NDANDA020626Glaxosmithkline
  • Apr 15, 2008NDANDA021926Currax
  • Feb 9, 2009ANDAANDA076572Sun Pharm Inds Ltd
  • Jan 27, 2016NDANDA206099Currax
  • Jan 28, 2016NDANDA208223Tonix Meds
  • Jan 25, 2019NDANDA210884Tonix Meds

FDA shortages

View JSON

Reference statistics from the openFDA drug-shortage dataset. For a live view, consult the FDA database directly. Not clinical guidance.

  • Imitrex, Nasal Spray, 20 mg/100 uL (NDC 66993-082-69)To be discontinued
    Sponsor: Prasco Laboratories
    Updated
  • Imitrex, Nasal Spray, 5 mg/100 uL (NDC 66993-081-69)To be discontinued
    Sponsor: Prasco Laboratories
    Updated

FAERS reports

View JSON
Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
45,391 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Drug Ineffective6,49614%
  2. 2Headache3,8288.4%
  3. 3Nausea3,4557.6%
  4. 4Migraine3,3887.5%
  5. 5Fatigue2,5735.7%
  6. 6Pain2,3595.2%
  7. 7Dizziness2,0794.6%
  8. 8Vomiting1,9264.2%
  9. 9Dyspnoea1,6553.6%
  10. 10Off Label Use1,6023.5%
  11. 11Anxiety1,5413.4%
  12. 12Diarrhoea1,4423.2%
  13. 13Arthralgia1,2912.8%
  14. 14Malaise1,2912.8%
  15. 15Depression1,2492.8%

Literature

View JSON

Recent PubMed references pinned to Sumatriptan as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

View JSON

The 10 most recently updated of 133 ClinicalTrials.gov registrations naming Sumatriptan as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Structural analogs

View JSON

Ranked by 2D fingerprint (Tanimoto) similarity over PubChem structures. Structural proximity only — not a claim of therapeutic equivalence.

Frequently asked questions

How does Sumatriptan work?
Sumatriptan binds with high affinity to human cloned 5-HT 1B/1D receptors. Sumatriptan presumably exerts its therapeutic effects in the treatment of migraine and cluster headaches through agonist effects at the 5-HT 1B/1D receptors on intracranial blood vessels and sensory nerves of the trigeminal system, which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release.
What is Sumatriptan used for?
According to FDA labeling, Sumatriptan carries indications including: Sumatriptan Injection, USP is indicated in adults for (1) the acute treatment of migraine, with or without aura, and (2) the acute treatment of cluster headache. Limitations of Use: • Use only if a clear diagnosis of migraine or cluster headache has been established.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Sumatriptan?
Sumatriptan is classified as Selective serotonin (5HT1) agonists, Serotonin-1b and Serotonin-1d Receptor Agonist, Monoamine Oxidase Inhibitors, Serotonin 1b Receptor Agonists, Serotonin 1d Receptor Agonists, Serotonin Agonists, Cerebral Arterial Vasoconstriction, Increased Central Nervous System Serotonin Activity.
What are the brand names for Sumatriptan?
Sumatriptan is marketed under brand names including Imitrex, Onzetra, Tosymra, Treximet, Zembrace.
What are the contraindications for Sumatriptan?
Sumatriptan labeling lists contraindications including: Sumatriptan Injection is contraindicated in patients with: • Ischemic coronary artery disease (CAD) (angina pectoris, history of myocardial infarction, or documented silent ischemia) or coronary artery vasospasm, including Prinzmetal’s angina [see Warnings and Precautions (5.1)]. • Wolff-Parkinson-White syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders [see Warnings and Precautions (5.2)].. Always consult the full prescribing information and a clinician.
Note. Data for sumatriptan is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

Search pharmacopeia

Search drugs, classes, and ingredients