Eletriptan for migraine

What eletriptan is

Eletriptan is a serotonin (5-HT1B/1D) receptor agonist, or triptan. The Relpax label indicates it for acute treatment of migraine with or without aura in adults, once migraine has been clearly diagnosed. It is not intended for preventing attacks. Safety and effectiveness in pediatric patients have not been established.

The label covers one form, a film-coated tablet. Peak blood levels occur about 1.5 hours after a dose in healthy people; in moderate to severe migraine the median is 2 hours. The dose comes from the label or the prescriber. Approval and brands differ by country.

CYP3A4 inhibitors

Potent CYP3A4 inhibitors significantly increase eletriptan exposure. The label says eletriptan should not be used within at least 72 hours of treatment with:

• ketoconazole;
• itraconazole;
• nefazodone;
• troleandomycin;
• clarithromycin;
• ritonavir;
• nelfinavir.

The label applies the same 72-hour limit to other medicines shown to be potent CYP3A4 inhibitors, so this list is not complete. A doctor or pharmacist can check other medicines.

Results at 2 hours

The label reports headache response in seven placebo-controlled trials: moderate or severe pain reduced to mild or none. For the one dose tested in all seven trials, response was 53.9% to 65.0%, against 19.0% to 39.5% with placebo. Results varied with dose. The label does not report pain freedom at 2 hours in these trials.

Other contraindications and warnings

The label also says eletriptan must not be used with:

• ischemic coronary artery disease or coronary vasospasm, including Prinzmetal’s angina;
• Wolff-Parkinson-White syndrome or related arrhythmias;
• a history of stroke, transient ischemic attack, or hemiplegic or basilar migraine;
• peripheral vascular disease, ischemic bowel disease, or uncontrolled hypertension;
• another 5-HT1 agonist, ergotamine or ergot-type medicine within 24 hours;
• hypersensitivity to eletriptan.

The label states eletriptan is not recommended in severe liver impairment. Its warnings cover heart attack, arrhythmia, chest or jaw tightness, stroke, reduced blood flow to the bowel or limbs, serotonin syndrome, raised blood pressure and anaphylactic reactions. The label names SSRIs, SNRIs, tricyclic antidepressants and MAO inhibitors as the medicines with which serotonin syndrome particularly occurs. It adds that blood pressure rose more in elderly than in young subjects.

Monthly limit

ICHD-3 places eletriptan with all other triptans: 10 or more days a month for more than 3 months. The Relpax label warns about medication-overuse headache at 10 or more days a month. Use the medication days counter for your own total.

In a headache diary

Along with the dose time and the pain at 2 hours, keep a dated list of other medicines. Short courses are easy to forget, and the 72-hour rule depends on their dates. Show this list to whoever prescribes or dispenses the eletriptan.