Eletriptan is a selective serotonin (5-HT1B/1D) receptor agonist (triptan) used for the acute treatment of migraine with or without aura in adults. It is not indicated for migraine prophylaxis, hemiplegic or basilar migraine, or cluster headache. It is a second-generation triptan with high oral bioavailability and rapid absorption, making it effective for rapid relief of migraine pain and associated symptoms like nausea, photophobia, and phonophobia.
Adult: 40mg taken orally as a single dose at the onset of migraine headache. If headache recurs, a second dose may be taken after at least 2 hours. Maximum dose: 80mg in a 24-hour period.
Note: Swallow tablet whole with a glass of water. Can be taken with or without food, but a high-fat meal delays absorption. Do not crush or chew. If no response to the first dose, do not take a second dose for the same attack. Do not use for more than 10 headache days per month to avoid medication-overuse headache.
Eletriptan binds with high affinity to 5-hydroxytryptamine 1B/1D (5-HT1B/1D) receptors located on intracranial blood vessels and sensory nerve terminals of the trigeminal system. This binding causes vasoconstriction of dilated cerebral blood vessels, inhibits the release of pro-inflammatory neuropeptides (like CGRP and substance P) from perivascular trigeminal nerves, and reduces pain signal transmission in the trigeminal nucleus caudalis.
Pregnancy: Category C: Animal studies have shown adverse effects. There are no adequate and well-controlled studies in pregnant women. Use only if potential benefit justifies potential risk to the fetus.
Driving: May cause dizziness, somnolence, or visual disturbances. Patients should be cautioned about driving or operating machinery until they are certain they are not affected.
| Strong CYP3A4 Inhibitors (e.g., Ketoconazole, Itraconazole, Clarithromycin, Ritonavir, Nelfinavir) | Markedly increases eletriptan plasma levels (AUC increased up to 6-fold). Risk of serious adverse events. | Contraindicated |
| Moderate CYP3A4 Inhibitors (e.g., Erythromycin, Verapamil, Diltiazem, Fluconazole) | Increases eletriptan exposure. Maximum dose should not exceed 40mg in 24 hours. | Major |
| Other 5-HT1 Agonists (Triptans) or Ergot Derivatives | Increased risk of vasospastic reactions. Additive vasoconstriction. | Contraindicated (within 24 hours) |
| Selective Serotonin Reuptake Inhibitors (SSRIs) / Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs) | Potential increased risk of serotonin syndrome (hyperthermia, rigidity, myoclonus, autonomic instability). | Moderate |
| Monoamine Oxidase Inhibitors (MAOIs) | Theoretical risk of reduced eletriptan metabolism and increased serotonergic effects. | Moderate |