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5-HT1B/1D Agonist (Triptan) Pregnancy: Safety in human pregnancy not established. Animal studies do not indicate direct teratogenic effects, but some embryotoxicity findings suggested impaired embryo viability. Use only if the expected benefit to the mother is greater than any possible risk to the foetus. Breast-feeding: zolmitriptan passes into the milk of lactating animals; no human milk data — exercise caution (SPC §4.6).

Zolmitriptan

Brand names: Zomig

Zolmitriptan is a selective serotonin 5-HT1B/1D receptor agonist (a triptan) used for the acute treatment of migraine, with or without aura, and for cluster headache.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: 2.5 mg to treat a migraine attack; if symptoms return within 24 hours a second dose may be taken, but not within 2 hours of the initial dose. If satisfactory relief is not achieved with 2.5 mg doses, subsequent attacks can be treated with 5 mg doses (caution — increased incidence of undesirable effects).
Route: Oral — film-coated tablet swallowed with a drink of water
Frequency: As required for an acute migraine attack; second dose no sooner than 2 hours after the first; not more than 2 doses in any 24-hour period
Max: Total intake should not exceed 10 mg in any 24-hour period (and not more than 2 doses in 24 hours). Maximum 5 mg in 24 hours in moderate or severe hepatic impairment, and in patients taking MAO-A inhibitors, specific CYP1A2 inhibitors (e.g. fluvoxamine), quinolones (e.g. ciprofloxacin) or cimetidine.
UK SPC (Zolmitriptan 2.5 mg Film-coated Tablets, eMC §4.2). Zolmitriptan is equally effective whenever taken during an attack, but it is advisable to take it as early as possible after the onset of migraine headache. If a patient does not respond to the first dose, a second dose is unlikely to be of benefit in the same attack; a controlled study failed to show superiority of 5 mg over 2.5 mg, though 5 mg may benefit some patients. HEPATIC IMPAIRMENT: no dose adjustment in mild impairment; maximum 5 mg in 24 hours in moderate or severe impairment. RENAL IMPAIRMENT: no dosage adjustment required if creatinine clearance is more than 15 ml/min. PAEDIATRIC (SPC §4.2): in children under 12 years efficacy has not been established and no posology recommendation can be made; in adolescents aged 12–17 years efficacy was not demonstrated in a placebo-controlled trial and use is NOT recommended — verify against a children's formulary. ELDERLY: safety and efficacy in individuals over 65 years have not been evaluated and use is not recommended. NOTE ON SOURCES: the cross-check US label in the bundle (Amneal, 2019) is for a zolmitriptan NASAL SPRAY (2.5 mg starting dose, max single dose 5 mg, max 10 mg/24 h; limit to 2.5 mg single / 5 mg per 24 h with cimetidine) — do not apply nasal-spray wording to the oral tablet page.

Dose adjustments

Renal

No dosage adjustment required in patients with a creatinine clearance of more than 15 ml/min (SPC §4.2). No guidance stated for creatinine clearance of 15 ml/min or below.

Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC; US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

  • Hypersensitivity to zolmitriptan or to any of the excipients
  • Moderate to severe hypertension, and mild uncontrolled hypertension
  • Ischaemic heart disease
  • Coronary vasospasm / Prinzmetal's angina
  • History of cerebrovascular accident (CVA) or transient ischaemic attack (TIA)
  • Concomitant administration with ergotamine or ergotamine derivatives or other 5-HT1 receptor agonists

Side effects

  • Nervous system: dizziness, headache, paraesthesia, hyperaesthesia, somnolence, warm sensation, and other abnormalities or disturbances of sensation
  • General: asthenia, and heaviness, tightness, pain or pressure in the throat, neck, limbs or chest
  • Gastrointestinal: nausea, vomiting, dry mouth, abdominal pain, dysphagia
  • Cardiac: palpitations, tachycardia; more rarely angina pectoris, coronary vasospasm and myocardial infarction
  • Musculoskeletal: muscle weakness, myalgia
  • Immune/skin: anaphylaxis/anaphylactoid and hypersensitivity reactions, angioedema, urticaria; also transient increases in systemic blood pressure
  • Note: frequency categories (common / uncommon / rare / very rare) are tabulated in SPC §4.8 but the column alignment was not preserved in the fetched text — clinician to confirm frequencies against the source SPC. Certain symptoms may be part of the migraine attack itself.

Interactions

  • Ergotamine, ergotamine derivatives and other 5-HT1 receptor agonists — concomitant administration is contraindicated (SPC §4.3)
  • MAO-A inhibitors — maximum 5 mg zolmitriptan in 24 hours (SPC §4.2, dose-adjustment interactions)
  • Specific CYP1A2 inhibitors such as fluvoxamine — maximum 5 mg zolmitriptan in 24 hours
  • Quinolones (e.g. ciprofloxacin) — maximum 5 mg zolmitriptan in 24 hours
  • Cimetidine — maximum 5 mg zolmitriptan in 24 hours
  • SSRIs and SNRIs — serotonin syndrome has been reported with combined use of triptans and SSRIs/SNRIs; potentially life-threatening (SPC §4.4)

Clinical monograph

How it works

It activates 5-HT1B/1D receptors, causing constriction of dilated cranial blood vessels and inhibiting the release of vasoactive neuropeptides from trigeminal nerve terminals.

Prescribing in practice

  • Contraindicated in patients with ischaemic heart disease, coronary vasospasm, uncontrolled hypertension, and previous stroke or transient ischaemic attack because of its vasoconstrictor action.
  • It is for acute attack relief only and should not be used for migraine prophylaxis; avoid concurrent use with ergot-type preparations and other triptans within the same day.
  • Use with caution alongside serotonergic agents such as SSRIs and SNRIs because of the risk of serotonin syndrome.

Monitoring

No routine laboratory monitoring is required, but cardiovascular risk should be assessed before first use and frequency of use reviewed to detect medication-overuse headache.

Counselling the patient

  • Take as early as possible once the migraine headache has started; it does not prevent attacks.
  • Do not exceed the recommended frequency of dosing, and avoid using on too many days each month to prevent rebound headache.
  • Seek urgent advice if you develop chest tightness, pain, or pressure after taking it.

Evidence & guidelines

Triptans are recommended by NICE as a first-line option for acute migraine attacks when simple analgesia is insufficient.

Reference: NICE NG150 Headaches; British Association for the Study of Headache (BASH) Guidelines; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Related

Curated clinical cross-links plus same-class fallbacks.