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: 40 mg as a single dose; 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).
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.
Refer to adult dosing.
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
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.
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; 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.
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.
Documentation of allergenic cross-reactivity for serotonin 5-HT1 receptor agonists (triptans) in this class is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty.
Concerns related to adverse effects:
• Anaphylactic/Anaphylactoid reactions: Anaphylaxis, anaphylactoid, and hypersensitivity reactions (including angioedema) have occurred; may be life-threatening or fatal. Use is contraindicated in patients with known hypersensitivity to eletriptan.
• 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. Use is contraindicated in patients with ischemic or vasospastic CAD and Wolff-Parkinson-White syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders.
• Cerebrovascular events: Cerebral/subarachnoid hemorrhage and stroke (some fatal) have been reported with 5-HT1 agonist administration. Use is contraindicated in patients with a history of stroke or transient ischemic attack.
• Elevated blood pressure: Significant elevation in blood pressure, 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. Monitor blood pressure; use is contraindicated in patients with uncontrolled 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. Discontinue eletriptan if serotonin syndrome is suspected.
• 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. 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: Blood pressure was increased to a greater extent in elderly subjects than in younger subjects.
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
SUMAtriptan: Serotonin 5-HT1D Receptor Agonists (Triptans) may enhance the adverse/toxic effect of SUMAtriptan. Risk X: Avoid combination
A high-fat meal increases bioavailability. Management: Administer without regard to meals.
In comparison to other medications in this class, information related to eletriptan use in pregnancy is limited (Källén 2011; Nezvalová-Henriksen, 2010; Nezvalová-Henriksen 2012; Spielmann 2018).
Until additional information is available, other agents are preferred for the acute management of migraine in pregnancy (CHS [Worthington 2013]; MacGregor 2014).
Eletriptan is present in breast milk.
In a premarketing study, eight women were given a single dose of eletriptan 80 mg. The amount of drug detected in breast milk over 24 hours was ~0.02% of the maternal dose. The presence of the active metabolite was not measured. In a second report, eletriptan was given to three women at least 1 month postpartum. Breast milk was sampled for 24 hours after the dose. The estimated relative infant dose (RID) was calculated to be 0.6% (range 0.3% to 0.8%) by the authors of the study (additional details not provided). Concentrations of the N-desmtheyl eletriptan metabolite were low or barely detectable in breast milk (Amundsen 2019).
In general, breastfeeding is considered acceptable when the RID of a medication is <10% (Anderson 2016; Ito 2000).
Due to the low concentrations in breast milk, eletriptan is considered compatible with breastfeeding (Negro 2017). 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. Exposure to eletriptan via breast milk can be minimized by pumping and discarding breast milk for 24 hours after the last maternal dose.
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 (Elderly: 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 elderly patients (65 to 93 years of age).
Race/ethnicity: Japanese men had a 35% reduction in eletriptan exposure.
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): $86.27
40 mg (per each): $86.27
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
