Eletriptan
RELPAX
Pronunciation: el-i-TRIP-tan (REL-pax)
What it is5-HT1B/1D agonist; acute migraine.
Why this oneIt is the high-efficacy oral triptan whose selection is most often limited by CYP3A4 interactions.
What limits itStrong CYP3A4 inhibitors are contraindicated. Coronary vasospasm precludes use in ischemic or vasospastic disease.
FDA-approved for
- migraine (2002)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Acute migraine (with or without aura) | Adults | 20 or 40 mg PRN | 40 mg PRN | 40 mg single dose; 80 mg/24h |
Renal Undefined
Hepatic Severe: not recommended (not evaluated); mild-moderate not specifically addressed
Second dose no sooner than 2 h after first; max 80 mg per 24 h
Instructions
- May repeat once ≥2 h after first dose if no response or recurrence; do not exceed 80 mg in 24 h.
- Do not treat an average of more than 3 migraine attacks per 30 days (not established).
Available strengths
- tab 20, 40 mg
Contraindications
- Ischemic coronary artery disease or coronary vasospasm (incl. Prinzmetal's angina)
- Wolff-Parkinson-White syndrome or arrhythmias with other accessory conduction pathway disorders
- History of stroke or TIA, or hemiplegic or basilar migraine
- Peripheral vascular disease
- Ischemic bowel disease
- Uncontrolled hypertension
- Use within 24 h of another 5-HT1 agonist or ergotamine/ergot-type medication
- Use within 72 h of potent CYP3A4 inhibitors (ketoconazole, itraconazole, nefazodone, clarithromycin, ritonavir, nelfinavir)
Cautions
- Myocardial ischemia/infarction and Prinzmetal's angina — cardiac evaluation in high-risk patients
- Arrhythmias — discontinue if they occur
- Chest/throat/neck/jaw pain or pressure
- Cerebrovascular events
- GI and peripheral vasospastic reactions
- Medication overuse headache
- MAOIs due to risk of serotonin syndrome
- Blood pressure increase
Adverse reactions
- Asthenia
- Nausea
- Dizziness
- Somnolence
Pregnancy Insufficient human data; animal developmental toxicity at clinically relevant doses.
Lactation Excreted in human milk; minimize infant exposure by avoiding breastfeeding for 24 h after treatment.
Cost
Generic entry2017
NO BOXED WARNINGS
Principal riskCoronary vasospasm; CYP3A4-dependent
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.
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.