Sumatriptan
IMITREX
Pronunciation: soo-ma-TRIP-tan (IM-i-trex)
“Sumo tripped In my tracks”
What it is5-HT1B/1D agonist causing cranial vasoconstriction; acute migraine and cluster headache.
Why this oneIts subcutaneous form has the fastest onset among triptans, useful when vomiting precludes oral treatment.
What limits itCoronary vasospasm makes it unsuitable in ischemic heart disease or uncontrolled hypertension; overuse causes rebound headache.
FDA-approved for
- migraine (1992)
Off-label
- cluster headache
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Acute migraine (with or without aura) | Adults | 25-100 mg PRN single dose | 50-100 mg PRN single dose | 200 mg/24h |
| Acute migraine, mild-moderate hepatic impairment | Adults | ≤50 mg PRN single dose | ≤50 mg PRN single dose | 50 mg single dose |
Renal Undefined
Hepatic Mild-moderate: max single dose 50 mg; severe: contraindicated
Max 200 mg per 24 hours; safety of treating >4 headaches/30 days not established
Instructions
- Second dose only if partial response to first; separate doses by ≥2 hours
- After Imitrex injection: additional tablets up to 100 mg/day, ≥2 h between doses
Available strengths
- tab 25, 50, 100 mg
- powder 11 mg
- nasal spray 5, 10, 20 mg/spray
- inj 3, 4, 6 mg/0.5 mL
Contraindications
- MAOIs (concurrently or within 14 days)
- Ischemic coronary artery disease or coronary vasospasm (incl. Prinzmetal's angina)
- Wolff-Parkinson-White syndrome / arrhythmias with accessory conduction pathways
- History of stroke/TIA, or hemiplegic or basilar migraine
- Peripheral vascular disease; ischemic bowel disease
- Uncontrolled hypertension
- Recent (within 24 h) ergotamine/ergot-type drug or another 5-HT1 agonist
- Current or recent (within 2 weeks) MAO-A inhibitor use
- Severe hepatic impairment
Cautions
- Myocardial ischemia/infarction and Prinzmetal's angina
- Arrhythmias; chest/throat/neck/jaw tightness
- Cerebral/subarachnoid hemorrhage and stroke
- GI and peripheral vasospastic ischemia
- Medication overuse headache; serotonin syndrome; BP increase; seizures
Adverse reactions
- Paresthesia
- Warm/cold sensation
- Chest pain/tightness/pressure
- Neck/throat/jaw pain/tightness
- Malaise/fatigue
Pregnancy Registry/epidemiologic data have not detected increased birth defects; animal data show embryolethality/fetal abnormalities
Lactation Present in human milk; minimize infant exposure; transient breast pain reported
Cost
| Strength | #/mo | generic $/unit | CostPlus | |
|---|---|---|---|---|
| 25 mg | tab | per unit | $0.24/ea | offered |
| 50 mg | tab | per unit | $0.30/ea | offered |
| 100 mg | tab | per unit | $0.44/ea | offered |
Other forms: Sumatriptan SC injection (IMITREX)
Generic entry2016
NO BOXED WARNINGS
Principal riskCoronary vasospasm; contraindicated in ischemic heart disease
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilityAgent-specific vascular, serotonergic or hepatic risks; acute overdose is usually limited outside ergot or cardiovascular agents.
Serotonicity
This drug is routinely called serotonergic. By Gillman’s human-effect criteria it does not raise serotonin in the synapse.
Triptan receptor agonism is not a mechanistic serotonin-toxicity interaction with SRIs.
Label contraindicationMAOIs (concurrently or within 14 days). The label governs prescribing; Gillman’s point concerns serotonin toxicity only.
Gillman’s four human testsA measurable SERT affinity that fails all four is not clinical serotonicity.
- Retarded orgasm
- Efficacy in OCD and cataplexy
- Clonus and hyperreflexia in single-drug overdose
- Serotonin toxicity when combined with an MAOI
Non-elevating action5-HT1B/1D agonist
Evidence confidenceHigh
Background: what serotonicity is · what is and is not an SRI · what counts as a relevant MAOI.
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