Embedded Files
Pharmacologic Category
Antimigraine Agent; Serotonin 5-HT1B, 1D Receptor Agonist
Dosing: Adult
Note: If the first dose is ineffective, diagnosis needs to be re-evaluated. Safety of treating >3 headaches/month has not been established.
Acute migraine: Oral: Initial: 20 to 40 mg as a single dose (maximum: 40 mg/dose); if the headache improves but returns, dose may be repeated after 2 hours have elapsed since first dose (maximum: 80 mg/day). Note: 80 mg single doses have been evaluated in clinical trials, however this dose has been associated with a slightly greater incidence of adverse reactions (McCormack 2006).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
* See Dosage and Administration in AHFS Essentials for additional information.
Dosing: Geriatric
Refer to adult dosing.
Dosing: Renal Impairment: Adult
There are no dosage adjustments provided in the manufacturer's labeling; however, adjustment likely not needed based on pharmacokinetic analysis.
Dosing: Hepatic Impairment: Adult
Mild to moderate impairment: No dosage adjustment necessary.
Severe impairment: Use is not recommended.
Use: Labeled Indications
Migraines: Acute treatment of migraine, with or without aura in adults
* See Uses in AHFS Essentials for additional information.
Class and Related Monographs
Serotonin 5-HT1 Receptor Agonists (Triptans)
Comparative Efficacy
Administration: Oral
Administer as soon as symptoms appear. May take with or without food.
Storage/Stability
Store at 20°C to 25°C (68°F to 77°F); excursions are permitted between 15°C and 30°C (59°F and 86°F).
Medication Patient Education with HCAHPS Considerations
What is this drug used for?
• It is used to treat migraine headaches.
All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:
• Loss of strength and energy
• Fatigue
WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:
• Severe nausea
• Vomiting
• Severe or persistent headache
• Severe dizziness
• Passing out
• Vision changes
• Constipation
• Diarrhea
• Severe abdominal pain
• Bloody stools
• Burning or numbness feeling
• Weight loss
• Leg cramps
• Sensation of heaviness or tightness in legs
• Sensation of cold
• Burning or pain in feet or toes
• Blue/gray skin discoloration
• Serotonin syndrome like dizziness, severe headache, agitation, sensing things that seem real but are not, fast heartbeat, abnormal heartbeat, flushing, tremors, sweating a lot, change in balance, severe nausea, or severe diarrhea
• Severe cardiac abnormalities like chest, throat, neck, or jaw tightness, pain, pressure, or heaviness; break out in a cold sweat; shortness of breath; fast heartbeat; abnormal heartbeat; or severe dizziness or passing out
• Change in strength on one side is greater than the other, trouble speaking or thinking, change in balance, or vision changes
• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.
Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.
Contraindications
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 or basilar migraine; 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.
Warnings/Precautions
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 or basilar migraine. 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:
• Elderly: Blood pressure was increased to a greater extent in elderly subjects than in younger subjects.
* See Cautions in AHFS Essentials for additional information.
Geriatric Considerations
Since elderly often have cardiovascular disease, careful evaluation of the use of 5-HT agonists is needed to avoid complications with the use of these agents. Safety and efficacy in elderly >65 years of age have not been established, however, pharmacokinetic disposition is similar to that in younger adults. Use lowest recommended doses initially.
Pregnancy Considerations
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).
Breast-Feeding Considerations
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 breastmilk can be minimized by pumping and discarding breast milk for 24 hours after the last maternal dose.
Briggs' Drugs in Pregnancy & Lactation
Adverse Reactions
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
* See Cautions in AHFS Essentials for additional information.
Allergy and Idiosyncratic Reactions
Toxicology
Metabolism/Transport Effects
Substrate of CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Drug Interactions Open Interactions
Abametapir: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
Conivaptan: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
CYP3A4 Inhibitors (Moderate): May increase the serum concentration of Eletriptan. Management: The use of eletriptan within 72 hours of a moderate CYP3A4 inhibitor should be avoided. Risk D: Consider therapy modification
CYP3A4 Inhibitors (Strong): May increase the serum concentration of Eletriptan. Exceptions: Nefazodone. Risk X: Avoid combination
Droxidopa: Serotonin 5-HT1D Receptor Agonists (Triptans) may enhance the hypertensive effect of Droxidopa. Risk C: Monitor therapy
Erdafitinib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
Ergot Derivatives: Serotonin 5-HT1D Receptor Agonists (Triptans) may enhance the vasoconstricting effect of Ergot Derivatives. Ergot Derivatives may enhance the vasoconstricting effect of Serotonin 5-HT1D Receptor Agonists (Triptans). Exceptions: Lisuride; Nicergoline. Risk X: Avoid combination
Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Idelalisib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Larotrectinib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
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). Exceptions: Rasagiline; Safinamide; Selegiline. 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
Palbociclib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
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. Exceptions: Isocarboxazid; Linezolid; Methylene Blue; Moclobemide; Nefazodone; Phenelzine; Tranylcypromine. Risk C: Monitor therapy
Simeprevir: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
Stiripentol: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. Risk D: Consider therapy modification
SUMAtriptan: Serotonin 5-HT1D Receptor Agonists (Triptans) may enhance the adverse/toxic effect of SUMAtriptan. Risk X: Avoid combination
Food Interactions
A high-fat meal increases bioavailability. Management: Administer without regard to meals.
Genes of Interest
Monitoring Parameters
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
Advanced Practitioners Physical Assessment/Monitoring
For use with clear diagnosis of migraine. Cardiovascular status should be evaluated prior to initiating medication and periodically thereafter. Monitor for hypertension and cardiac events.
Nursing Physical Assessment/Monitoring
Monitor for hypertension and cardiac events. Teach patient proper use (treatment of acute migraine).
Dosage Forms: US
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 aluminum lake]
Generic: 20 mg, 40 mg
Dosage Forms: Canada
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 aluminum lake]
Generic: 20 mg, 40 mg
Anatomic Therapeutic Chemical (ATC) Classification
- N02CC06
Generic Available (US)
Yes
Pricing: US
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): $78.40
40 mg (per each): $78.40
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.
Mechanism of Action
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
Pharmacodynamics/Kinetics
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
Pharmacodynamics/Kinetics: Additional Considerations
Renal function impairment: 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%.
Geriatric: Increased half-life from approximately 4.4 to 5.7 hours in elderly patients (65 to 93 years of age).
Race: Japanese men had a 35% reduction in eletriptan exposure.
Local Anesthetic/Vasoconstrictor Precautions
No information available to require special precautions
Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation)
Effects on Bleeding
No information available to require special precautions
Related Information
Index Terms
Eletriptan Hydrobromide
FDA Approval Date
December 26, 2002
References
Amundsen S, Nordeng H, Fuskevåg OM, et al. Transfer of triptans into human breast milk and estimation of infant drug exposure through breastfeeding. Reprod Toxicol. 2019;88:141. doi:10.1016/j.reprotox.2019.05.032
Anderson PO, Sauberan JB. Modeling drug passage into human milk. Clin Pharmacol Ther. 2016;100(1):42-52. doi:10.1002/cpt.377[PubMed 27060684]
Boyer EW, Shannon M. The Serotonin Syndrome. N Engl J Med. 2005;352:1112-1120.[PubMed 15784664]
Ito S. Drug therapy for breast-feeding women. N Engl J Med. 2000;343(2):118-126. doi:10.1056/NEJM200007133430208[PubMed 10891521]
Källén B, Nilsson E, Otterblad Olausson P. Delivery outcome after maternal use of drugs for migraine: a register study in sweden. Drug Saf. 2011;34(8):691-703.[PubMed 21751829]
MacGregor EA. Migraine in pregnancy and lactation. Neurol Sci. 2014;35(suppl 1):61-64. doi:10.1007/s10072-014-1744-2[PubMed 24867839]
McCormack PL, Keating GM. Eletriptan: a review of its use in the acute treatment of migraine. Drugs. 2006;66(8):1129-1149.[PubMed 16789799]
Negro A, Delaruelle Z, Ivanova TA, et al; European Headache Federation School of Advanced Studies (EHF-SAS). Headache and pregnancy: a systematic review. J Headache Pain. 2017;18(1):106. doi:10.1186/s10194-017-0816-0[PubMed 29052046]
Nezvalová-Henriksen K, Spigset O, and Nordeng HM, "Errata in 'Triptan Exposure During Pregnancy and the Risk of Major Congenital Malformations and Adverse Pregnancy Outcomes: Results From the Norwegian Mother and Child Cohort Study,'" Headache, 2012, 52(8):1319-20.[PubMed 22946832]
Nezvalová-Henriksen K, Spigset O, and Nordeng H, "Triptan Exposure During Pregnancy and the Risk of Major Congenital Malformations and Adverse Pregnancy Outcomes: Results From the Norwegian Mother and Child Cohort Study," Headache, 2010, 50(4):563-75.[PubMed 20132339]
Relpax (eletriptan) [prescribing information]. New York, NY: Pfizer; March 2020.
Relpax (eletriptan) [product monograph]. Kirkland, Quebec, Canada: Upjohn Canada ULC; May 2020.
Spielmann K, Kayser A, Beck E, Meister R, Schaefer C. Pregnancy outcome after anti-migraine triptan use: A prospective observational cohort study. Cephalalgia. 2018;38(6):1081-1092. doi:10.1177/0333102417724152[PubMed 28758416]
Worthington I, Pringsheim T, Gawel MJ, et al; Canadian Headache Society Acute Migraine Treatment Guideline Development Group. Canadian Headache Society guideline: acute drug therapy for migraine headache. Can J Neurol Sci. 2013;40(5)(suppl 3):S1-S80.[PubMed 23968886]
Brand Names: International
Demigra (EG); Elle (PK); Migrablock (EG); Relert (BE, FI, IL, LU, PT); Relpax (AE, AT, AU, BB, BG, BH, BR, CH, CL, CO, CR, CY, CZ, DE, DK, DO, EE, EG, ES, FR, GB, GR, GT, HN, IE, IS, IT, JO, KW, LV, MX, NI, NL, NO, NZ, PA, PL, QA, RO, RU, SA, SE, SG, SI, SK, SV, TH, TR, ZA); Tromzalor (EG)
Last Updated 9/9/20
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