Eletriptan
Triptans (5-HT1B/1D agonists)
Triptans (5-HT1B/1D agonists)
An oral triptan for migraine attacks, metabolized by CYP3A4: strong CYP3A4 inhibitors such as clarithromycin or ketoconazole are excluded.
Also called: Eletriptan hydrobromide
Quick facts
- Group
- Triptans (5-HT1B/1D agonists)
- Target
- Serotonin 5-HT1B and 5-HT1D receptors
- Used for
- Acute treatment of migraine
- Key effects
- Weakness · Nausea · Chest
- Monitor
- Cardiovascular evaluation · Blood pressure
- ATC
- N02CC06
No doses: the clinician sets them by the current guideline.
Mechanism of action
The figure shows donitriptan, an experimental triptan, in the serotonin-binding pocket of the human 5-HT1B receptor; eletriptan binds 5-HT1B, 5-HT1D and 5-HT1F receptors with high affinity.
Eletriptan binds 5-HT1B, 5-HT1D and 5-HT1F receptors with high affinity. Like other triptans, it constricts intracranial vessels and reduces neuropeptide release from trigeminal endings, stopping the attack.
- Eletriptan activates 5-HT1B/1D (and 5-HT1F) receptors
- Vessels constrict and trigeminal endings release less neuropeptide
- The migraine attack eases
Indications
- Acute treatment of migraine with or without aura in adults Migraine →
Adverse effects
Common
- Weakness, drowsiness and dizziness (dose-related)
- Nausea
- Chest, throat, neck or jaw tightness
Contraindications
- Ischaemic coronary artery disease or coronary vasospasm (including Prinzmetal angina)
- History of stroke or TIA; hemiplegic or basilar migraine
- Peripheral vascular disease and ischaemic bowel disease
- Uncontrolled hypertension
- Another triptan or an ergot alkaloid in the previous 24 hours
- Wolff-Parkinson-White syndrome or other accessory pathway arrhythmias
- Potent CYP3A4 inhibitors (ketoconazole, itraconazole, clarithromycin, ritonavir, nelfinavir, nefazodone) within at least 72 hours
Key interactions
- Ketoconazole, itraconazole, clarithromycin, ritonavir, nelfinavir
- Much higher eletriptan exposure; contraindicated
- Ergot alkaloids or other triptans within 24 hours
- Additive vasospasm; contraindicated
- SSRIs, SNRIs, tricyclics, MAO inhibitors
- Serotonin syndrome
What is monitored
- Cardiovascular evaluation in triptan-naive patients with several risk factors
- Blood pressure
- Review of new antibiotics, antifungals and HIV medicines (CYP3A4)
Administration and safety
- Used only when the migraine diagnosis is clear
- For attacks only; not a preventive
Pregnancy and breastfeeding
Human data are not sufficient to define the risk; animal studies showed developmental toxicity.
Nursing care
- Before the first dose, ask about chest pain, heart disease, stroke, high blood pressure and cardiovascular risk factors
- Check the medication list for ergots, other triptans, MAO inhibitors and serotonergic antidepressants
- Explain that chest or throat tightness is common, but crushing chest pain needs urgent care
- Encourage a headache diary to spot medication overuse
- Teach signs of serotonin syndrome: agitation, fever, sweating, tremor, muscle jerks
Pharmacokinetics
- Absorption
- Well absorbed; bioavailability about 50%; peak about 1.5 to 2 hours
- Metabolism
- Mainly CYP3A4; one active N-demethylated metabolite
- Half-life
- About 4 hours
Test yourself
Think of the answer, then tap the question to see it.
Which enzyme metabolizes eletriptan?
CYP3A4.
Which antibiotic is contraindicated with eletriptan?
Clarithromycin (a potent CYP3A4 inhibitor).
Does eletriptan prevent migraine?
No; it treats acute attacks only.
Connections
← Back to the class: Triptans (5-HT1B/1D agonists)
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: DailyMed - ELETRIPTAN HYDROBROMIDE tablet, film coated (DailyMed (U.S. National Library of Medicine), 2026); Eletriptan: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.