Class: Antimigraine Serotonin Receptor Agonist
Dosage Forms. Tablet: 20 mg, 40 mg
Common FDA Label Indication, Dosing, and Titration.
1. Migraine: 20-40 mg po at onset of migraine, may repeat after 2 h prn; max single dose 40 mg, max 80 mg/d
Off-Label Uses. None
MOA. Eletriptan binds with high affinity to serotonin (5-HT) subtypes 1B, 1D, and 1F receptors. It has no significant affinity or pharmacological activity at adrenergic α1, α,2, or β,; dopaminergic D1 or D2; muscarinic; or opioid receptors. Serotonin receptor agonists are believed to be effective in migraine, either through vasoconstriction (via activation of 5-HT1 receptors located on intracranial blood vessels) or through activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system, resulting in the inhibition of proinflammatory neuropeptide release.
Drug Characteristics: Eletriptan
Medication Safety Issues: Eletriptan
Drug Interactions: Eletriptan
Adverse Reactions: Eletriptan
Efficacy Monitoring Parameters. Resolution of signs of migraine headache.
Toxicity Monitoring Parameters. Seek medical attention for signs of ischemic bowel disease (eg, sudden severe abdominal pain, bloody diarrhea) or peripheral vascular disease (eg, Raynaud syndrome), serotonin syndrome (eg, agitation, hallucinations, tachycardia, hyperreflexia, incoordination, diarrhea, nausea), ischemic cardiac syndrome, or hypertensive crisis.
Key Patient Counseling Points. Should avoid activities requiring mental alertness or coordination until drug effects are realized, as this drug may cause dizziness or somnolence.
Clinical Pearls. These agents are not for prophylaxis—these are used for the treatment of acute migraine headache. Several serotonin agonists (“trip-tans”) exist for migraine, administered via a variety of routes (oral, inhaled, and injected). Each differs in onset and duration of action. If one agent is ineffective at max dose, recommend changing agents or route. Instruct patient to take a second dose 2 or more hours after the first, if needed, and no more than 80 mg a day.