Section 02 · Monograph

Eletriptan

Reviewed Nov 2026FDA label

RelpaxTriptan

Indications

Selective agonist at 5-HT1B/1D receptors causing cranial vasoconstriction and inhibition of trigeminal neuropeptide release
Highly lipophilic relative to other triptans, contributing to good oral bioavailability

Adults: 20mg or 40mg single dose; may repeat once after ≥2 hours if headache recurs
Maximum single dose: 40mg; maximum 80mg in 24 hours
No more than an average of 3 treatment days per 30-day period is recommended given limited long-term safety data at high use frequency

No dose adjustment needed for mild-moderate hepatic or renal impairment; not studied in severe impairment

Ischemic or vasospastic coronary artery disease
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
Use within 72 hours of a strong CYP3A4 inhibitor (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, nelfinavir, nefazodone, troleandomycin)
Known hypersensitivity to eletriptan

Strong CYP3A4 inhibitors markedly increase eletriptan exposure (up to ~3-fold Cmax, ~6-fold AUC with ketoconazole) — contraindicated within 72 hours of use
Eletriptan is a CYP3A4 substrate — greater interaction potential with this class than other triptans, which is its defining PK feature
MAO-A inhibitors: increase exposure — contraindicated
SSRIs/SNRIs: increased risk of serotonin syndrome
Other triptans or ergot-containing drugs within 24 hours: additive vasospastic risk — contraindicated

Common (dose-related): asthenia, nausea, dizziness, somnolence
Serious (rare, class-wide): myocardial infarction, arrhythmia, coronary vasospasm, cerebrovascular events, serotonin syndrome, medication-overuse headache

Cardiovascular risk assessment before first dose in at-risk patients
Review concomitant medication list for strong CYP3A4 inhibitors before prescribing or refilling
Frequency of use — limit to avoid medication-overuse headache

Animal studies showed developmental toxicity at clinically relevant exposures; human data insufficient to establish safety
Use during pregnancy only if potential benefit justifies potential fetal risk
Limited data on presence in human milk; caution advised with breastfeeding