Section 02 · Monograph

Zolmitriptan

Reviewed Nov 2026FDA label

ZomigTriptan

Indications

Acute treatment of migraine with or without aura in adults; nasal spray also approved for pediatric patients 12 years and olderFDA-labeled

Selective agonist at 5-HT1B/1D receptors causing cranial vessel vasoconstriction and inhibition of trigeminal neuropeptide (e.g., CGRP) release
Metabolized to an active N-desmethyl metabolite that is 2-6 times more potent at 5-HT1B/1D receptors than the parent drug and contributes substantially to clinical effect
Some CNS penetration relative to other triptans, consistent with a modest central component to its action

Tablet/ODT: initiate 1.25mg or 2.5mg; may repeat after ≥2 hours; maximum 10mg in 24 hours
Nasal spray: initiate 2.5mg per nostril (single spray); may repeat after ≥2 hours; maximum single dose 5mg, maximum 10mg in 24 hours
ODT formulation dissolves on the tongue without water; useful for patients with nausea/vomiting who cannot swallow tablets or take liquids
Nasal spray offers faster absorption than oral tablet, useful when rapid onset or GI absorption is a concern
Concomitant cimetidine: reduces zolmitriptan clearance — reduce maximum single dose to 2.5mg and maximum daily dose to 5mg

Hepatic impairment (moderate-severe): reduce dose; not recommended in severe hepatic impairment

Ischemic or vasospastic coronary artery disease
Wolff-Parkinson-White syndrome or other cardiac accessory conduction pathway disorders
History of stroke, TIA, or peripheral vascular disease
Ischemic bowel disease
Uncontrolled hypertension
Hemiplegic or basilar migraine
Use of another 5-HT1 agonist or ergot-type medication within 24 hours
Use of an MAO-A inhibitor within the preceding 2 weeks
Known hypersensitivity to zolmitriptan

Cimetidine approximately doubles zolmitriptan half-life and AUC — requires dose reduction
MAO-A inhibitors increase zolmitriptan exposure and active metabolite levels substantially — contraindicated
SSRIs/SNRIs: increased risk of serotonin syndrome
Other triptans or ergot-containing drugs within 24 hours: additive vasospastic risk — contraindicated
Propranolol increases zolmitriptan plasma concentration modestly; generally does not require dose adjustment

Common: unusual taste (nasal spray, up to ~20%), paresthesia, dizziness, somnolence, hyperesthesia, nasal discomfort (with spray)
Serious (rare, class-wide): myocardial infarction, coronary vasospasm, arrhythmia, cerebrovascular events, serotonin syndrome, gastrointestinal ischemia, medication-overuse headache

Animal studies showed embryolethality and fetal structural abnormalities at clinically relevant exposures; adequate human data lacking
Use during pregnancy only if potential benefit justifies potential fetal risk
Limited data on presence in human milk; caution advised with breastfeeding