Version May 2024
Migraine, moderate to severe, acute treatment:
Note: Do not use within 24 hours of an ergotamine preparation or a different triptan. Limit use to <10 days per month to avoid medication-overuse headache. Administration early in the course of a migraine attack, at the first sign of pain, may improve response to treatment. When attack is complicated by severe nausea or vomiting, a non-oral medication may be more effective (AHS [Ailani 2021]).
Oral: 20 to 40 mg as a single dose; some experts prefer 40 mg as a single dose due to greater efficacy (CHS [Worthington 2013]). If symptoms persist or return, may repeat dose after ≥2 hours. Maximum: 40 mg/dose; 80 mg per 24 hours (Garcia-Ramos 2003; manufacturer's labeling). Dosages of 80 mg/dose and 160 mg per 24 hours have been evaluated; however, use was associated with increased adverse effects and similar efficacy compared to lower doses (McCormack 2006; Sheftell 2003; Stark 2002).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in the manufacturer's labeling; however, adjustment likely not needed based on pharmacokinetic analysis.
Mild to moderate impairment: No dosage adjustment necessary.
Severe impairment: Use is not recommended.
Arrhythmia, life threatening (eg, ventricular tachycardia, ventricular fibrillation): Discontinue therapy.
Serotonin syndrome: Discontinue therapy if serotonin syndrome occurs or is suspected.
Refer to adult dosing.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
1% to 10%:
Cardiovascular: Chest pain (2% to 4%; chest tightness, pain, and pressure), palpitations
Central nervous system: Dizziness (6% to 7%), drowsiness (6% to 7%), headache (4%), paresthesia (3% to 4%), chills, hypertonia, hypoesthesia, pain, vertigo
Dermatologic: Diaphoresis
Gastrointestinal: Nausea (8%), xerostomia (3% to 4%), abdominal pain (2%; pain, discomfort, stomach pain, cramps, and pressure), dyspepsia (2%), dysphagia (1% to 2%)
Neuromuscular & skeletal: Weakness (4% to 10%), back pain
Respiratory: Pharyngitis
<1%, postmarketing, and/or case reports (limited to important or life-threatening): Abnormal dreams, abnormal hepatic function tests, agitation, alopecia, amnesia, anaphylactoid reaction, anaphylaxis, anemia, angina pectoris, angioedema, aphasia, ataxia, cardiac arrhythmia, confusion, constipation, depersonalization, depression, diarrhea, diplopia, dysgeusia, dyspnea, dystonia, edema, emotional lability, esophagitis, euphoria, gingivitis, hallucination, hyperesthesia, hyperglycemia, hyperkinesia, hypersensitivity reaction, hypertension, impotence, increased creatine phosphokinase, insomnia, ischemic colitis, lacrimation, manic behavior, myalgia, myasthenia, myocardial infarction, nervousness, paralysis, peripheral edema, peripheral vascular disorder, photophobia, polyuria, Prinzmetal angina, pruritus, purpura, seizure, sensation of pressure (chest/neck/throat/jaw), shock, sialorrhea, skin discoloration, skin rash, speech disturbance, stupor, syncope, tachycardia, thrombophlebitis, tinnitus, tongue edema, tremor, twitching, urinary frequency, urticaria, vasospasm, ventricular fibrillation, visual disturbance, vomiting
Ischemic coronary artery disease (eg, angina pectoris, history of myocardial infarction, documented silent ischemia); coronary artery vasospasm, including Prinzmetal angina; Wolff-Parkinson-White syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders; history of stroke, transient ischemic attack, or history or current evidence of hemiplegic migraine or migraine with brainstem aura (basilar migraine) (IHS 2018); peripheral vascular disease; ischemic bowel disease; uncontrolled hypertension; recent use (within 24 hours) of treatment with another 5-HT1 agonist, or an ergotamine-containing or ergot-type medication (eg, dihydroergotamine or methysergide); recent use (within at least 72 hours) of the following potent CYP3A4 inhibitors: ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir, or nelfinavir; known hypersensitivity to eletriptan or any component of the formulation (including anaphylaxis and angioedema).
Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Canadian labeling: Additional contraindications (not in US labeling): Cardiac arrhythmias (especially tachycardias), valvular heart disease, congenital heart disease, atherosclerotic disease; ophthalmoplegic migraine; Raynaud syndrome; severe hepatic impairment.
Concerns related to adverse effects:
• Anaphylactic/Anaphylactoid reactions: Anaphylaxis, anaphylactoid, and hypersensitivity reactions (including angioedema) have occurred; may be life-threatening or fatal.
• Cardiac events: Coronary artery vasospasm, transient ischemia, myocardial infarction, ventricular tachycardia/fibrillation, cardiac arrest, and death have been reported with 5-HT1 agonist administration; some events have occurred within a few hours of administration. Patients who experience sensations of chest pain/pressure/tightness or symptoms suggestive of angina following dosing should be evaluated for coronary artery disease or Prinzmetal angina before receiving additional doses; if dosing is resumed and similar symptoms recur, monitor with ECG.
• Cerebrovascular events: Cerebral/subarachnoid hemorrhage and stroke (some fatal) have been reported with 5-HT1 agonist administration.
• Elevated BP: Significant elevation in BP, including hypertensive crisis with acute impairment of organ systems, has also been reported on rare occasions in patients with and without a history of hypertension.
• Serotonin syndrome: Symptoms of agitation, confusion, hallucinations, hyper-reflexia, myoclonus, shivering, and tachycardia may rarely occur with concomitant proserotonergic drugs (ie, SSRIs/SNRIs or triptans) or agents which reduce eletriptan's metabolism. Concurrent use of serotonin precursors (eg, tryptophan) is not recommended. If concomitant administration with SSRIs is warranted, monitor closely, especially at initiation and with dose increases.
• Vasospasm-related events: Peripheral vascular ischemia, gastrointestinal vascular ischemia/infarction, and Raynaud syndrome have been reported with 5-HT1 agonists.
Disease-related concerns:
• Coronary artery disease: Should not be given to patients who have risk factors for CAD (eg, hypertension, hypercholesterolemia, smoker, obesity, diabetes, strong family history of CAD, menopause, male >40 years of age) without adequate cardiac evaluation. Patients with suspected CAD should have cardiovascular evaluation to rule out CAD before considering use; if cardiovascular evaluation is “satisfactory,” first dose should be given in the healthcare provider's office (consider ECG monitoring). Periodic evaluation of cardiovascular status should be done in all patients.
• Hepatic impairment: Not recommended for use in patients with severe hepatic impairment.
Other warnings/precautions:
• Appropriate use: Only indicated for treatment of acute migraine; not indicated for migraine prophylaxis, or for the treatment of cluster headache, hemiplegic migraine, or migraine with brainstem aura (basilar migraine) (IHS 2018). If a patient does not respond to the first dose, the diagnosis of migraine should be reconsidered; rule out underlying neurologic disease in patients with atypical headache and in patients with no prior history of migraine. Acute migraine agents (eg, triptans, opioids, ergotamine, or a combination of the agents) used for 10 or more days per month may lead to worsening of headaches (medication overuse headache); withdrawal treatment may be necessary in the setting of overuse.
Special populations:
• Older adult: BP was increased to a greater extent in older adults than in younger subjects.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Relpax: 20 mg
Relpax: 40 mg [contains fd&c yellow #6(sunset yellow)alumin lake]
Generic: 20 mg, 40 mg
Yes
Tablets (Eletriptan Hydrobromide Oral)
20 mg (per each): $61.12 - $61.46
40 mg (per each): $61.12 - $61.46
Tablets (Relpax Oral)
20 mg (per each): $92.30
40 mg (per each): $92.31
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Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Relpax: 20 mg, 40 mg [contains fd&c yellow #6(sunset yellow)alumin lake]
Generic: 20 mg, 40 mg
Administer orally as soon as symptoms appear. May take with or without food.
Migraine, moderate to severe, acute treatment: Acute treatment of migraine, with or without aura in adults (AHS [Ailani 2021]; AHS [Pringsheim 2016]).
Substrate of CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Bromocriptine: May enhance the adverse/toxic effect of Serotonin 5-HT1D Receptor Agonists (Triptans). Management: Consider alternatives to this combination when possible. If combined, monitor for increased bromocriptine and triptan toxicities. Risk D: Consider therapy modification
Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
CYP3A4 Inhibitors (Moderate): May increase the serum concentration of Eletriptan. Risk X: Avoid combination
CYP3A4 Inhibitors (Strong): May increase the serum concentration of Eletriptan. Risk X: Avoid combination
Droxidopa: Serotonin 5-HT1D Receptor Agonists (Triptans) may enhance the hypertensive effect of Droxidopa. Risk C: Monitor therapy
Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates): Serotonin 5-HT1D Receptor Agonists (Triptans) may enhance the vasoconstricting effect of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid combination
Fexinidazole: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Monoamine Oxidase Inhibitors: Serotonin 5-HT1D Receptor Agonists (Triptans) may enhance the serotonergic effect of Monoamine Oxidase Inhibitors. This could result in serotonin syndrome. Monoamine Oxidase Inhibitors may increase the serum concentration of Serotonin 5-HT1D Receptor Agonists (Triptans). Risk X: Avoid combination
Nefazodone: Eletriptan may enhance the serotonergic effect of Nefazodone. This could result in serotonin syndrome. Nefazodone may increase the serum concentration of Eletriptan. Risk X: Avoid combination
Serotonergic Agents (High Risk): Eletriptan may enhance the serotonergic effect of Serotonergic Agents (High Risk). This could result in serotonin syndrome. Management: Monitor for signs and symptoms of serotonin syndrome/serotonin toxicity (eg, hyperreflexia, clonus, hyperthermia, diaphoresis, tremor, autonomic instability, mental status changes) when these agents are combined. Risk C: Monitor therapy
Serotonin 5-HT1D Receptor Agonists (Triptans): May enhance the vasoconstricting effect of other Serotonin 5-HT1D Receptor Agonists (Triptans). Risk X: Avoid combination
A high-fat meal increases bioavailability. Management: Administer without regard to meals.
Outcome data following maternal use of eletriptan during pregnancy are limited in comparison to other 5-HT1B/1D agonists (triptans) (Källén 2011; Nezvalová-Henriksen, 2010; Nezvalová-Henriksen 2012; Nezvalová-Henriksen 2013; Spielmann 2018).
Triptans relieve migraine pain by selectively binding to serotonin receptors, resulting in vasoconstriction of cranial arteries. Although the effects on uterine blood flow have not been evaluated, one case report suggests excessive use of a triptan may cause placental hypoperfusion (ACOG 2022; Viard 2021).
Treatment for migraine headaches in pregnant patients should be individualized (AHS [Ailani 2021]). Triptans are not the preferred initial treatment for acute migraine headache in pregnant patients (ACOG 2022). Until additional data are available, eletriptan is not the preferred triptan when first-line therapy is ineffective. Triptans should be avoided in pregnant patients with cardiac disease or hypertension (ACOG 2022; CHS [Worthington 2013]).
Eletriptan is present in breast milk.
Data related to the presence of 5-HT1B/1D agonists (triptans) in breast milk are available from a study of 19 lactating women (6 weeks to 30 months postpartum) treated for migraine headaches. During the study, infants were fed previously expressed breast milk. Breast milk was sampled prior to and at intervals up to 24 hours after the dose in patients taking eletriptan 40 mg/day (n = 2) or eletriptan 20 mg/day (n = 1). Using the average breast milk concentrations observed, authors of the study calculated the estimated exposure of eletriptan to the breastfed infant to be 3.5 to 3.6 mcg/kg/day, providing a relative infant dose (RID) of 0.6% to 0.8% based on the weight adjusted maternal dose of 40 mg/day. The estimated exposure to the breastfed infant was 0.9 mcg/kg/day (RID 0.3%) based on a maternal dose of 20 mg/day. Using the maximum breast milk concentrations, the RID of eletriptan was 2% (range: 0.8% to 3.3%). The active metabolite of eletriptan was not included in the calculations (concentrations were near or below the limit of quantification). A large interindividual variability among breast milk concentrations was found with all the triptans in the study, even when considering dose and dosage form (Amundsen 2021). In general, breastfeeding is considered acceptable when the RID of a medication is <10% (Anderson 2016; Ito 2000).
Treatment for migraine headaches in lactating patients should be individualized (AHS [Ailani 2021]). According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother. Withholding breastfeeding for 24 hours after the maternal dose will minimize infant exposure via breast milk. The decision to withhold breastfeeding following a dose of eletriptan should be part of a shared decision-making process (ACOG 2022).
Headache severity; signs/symptoms suggestive of angina; blood pressure, heart rate, and/or ECG with first dose in patients with likelihood of unrecognized coronary disease, such as patients with significant hypertension, hypercholesterolemia, obese patients, patients with diabetes, smokers with other risk factors or strong family history of coronary artery disease; signs/symptoms of serotonin syndrome and hypersensitivity reactions
Selective agonist for serotonin (5-HT1B, 5-HT1D, and 5-HT1F receptors) in cranial arteries; causes vasoconstriction and reduces sterile inflammation associated with antidromic neuronal transmission correlating with relief of migraine
Absorption: Well absorbed.
Distribution: Vd: 138 L.
Protein binding: ~85%.
Metabolism: Hepatic via CYP3A4; forms one metabolite (active).
Bioavailability: ~50%, increased with high-fat meal.
Half-life elimination: ~4 hours (Older adults: 4.4 to 5.7 hours); Metabolite: ~13 hours.
Time to peak, plasma: 1.5 to 2 hours.
Altered kidney function: BP elevations were observed.
Hepatic function impairment: Mild to moderate impairment results in an increase in both AUC (34%) and half-life, and Cmax increased 18%.
Older adult: Increased half-life from approximately 4.4 to 5.7 hours in older adults (65 to 93 years of age).
Race/ethnicity: Japanese men had a 35% reduction in eletriptan exposure.
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