Zolmitriptan
ZOMIG
Pronunciation: zoel-mi-TRIP-tan
What it is5-HT1B/1D agonist; acute migraine and cluster headache.
Why this oneThe nasal spray works within fifteen minutes and is useful when vomiting prevents oral dosing.
What limits itCoronary vasospasm. Medication-overuse headache above ten days a month.
FDA-approved for
- migraine (1997)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Acute migraine (with or without aura) | Adults | 1.25-2.5 mg | 2.5 mg | 5 mg single dose; 10 mg/24h |
Renal Undefined
Hepatic Moderate-severe impairment: 1.25 mg; limit severe impairment to ≤5 mg/day
May repeat ≥2 h after the first dose; do not exceed 10 mg in any 24 h
Instructions
- 1.25 mg is achieved by breaking the functionally-scored 2.5 mg tablet in half
- With cimetidine: limit single dose to 2.5 mg, not to exceed 5 mg/24h
Available strengths
- tab 2.5, 5 mg
- nasal spray 2.5, 5 mg/spray
- ODT 2.5, 5 mg
Contraindications
- MAOIs (concurrently or within 14 days)
- Ischemic or vasospastic coronary artery disease (angina, prior MI, silent ischemia, Prinzmetal's)
- Wolff-Parkinson-White syndrome or arrhythmias with other cardiac accessory conduction pathway disorders
- History of stroke, TIA, or hemiplegic/basilar migraine
- Peripheral vascular disease
- Ischemic bowel disease
- Uncontrolled hypertension
- Recent (within 24 h) use of another 5-HT1 agonist or an ergotamine/ergot-type medication
- Current or recent (within 2 weeks) use of an MAO-A inhibitor
Cautions
- Myocardial ischemia/infarction and Prinzmetal angina
- Life-threatening arrhythmias
- Chest/throat/neck/jaw pain, tightness, pressure (usually non-cardiac)
- Cerebrovascular events (hemorrhage, stroke)
- Other vasospasm reactions (peripheral, GI ischemia, Raynaud's)
- Medication overuse headache
- Serotonin syndrome
- Blood pressure elevation
Adverse reactions
- Neck/throat/jaw pain/tightness/pressure
- Dizziness
- Paresthesia
- Asthenia
- Somnolence
- Warm/cold sensation
- Nausea
- Sensation of heaviness
- Dry mouth
Pregnancy No adequate human data; animal studies show embryolethality and fetal malformations at clinically relevant exposures.
Lactation No human data; present in rat milk at up to 4× maternal plasma levels.
Cost
Generic entry2013
NO BOXED WARNINGS
Principal riskCoronary vasospasm
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.