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Eletriptan

Pronunciation

(el e TRIP tan)

Index Terms

  • Eletriptan Hydrobromide

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Relpax: 20 mg, 40 mg

Brand Names: U.S.

  • Relpax

Pharmacologic Category

  • Antimigraine Agent
  • Serotonin 5-HT1B, 1D Receptor Agonist

Pharmacology

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

Metabolism

Hepatic via CYP3A4; forms one metabolite (active)

Time to Peak

Plasma: 1.5-2 hours

Half-Life Elimination

~4 hours (Elderly: 4.4-5.7 hours); Metabolite: ~13 hours

Protein Binding

~85%

Special Populations: Renal Function Impairment

BP elevations were observed.

Special Populations: Hepatic Function Impairment

Mild to moderate impairment results in an increase in both AUC(34%) and half-life, and Cmax increased 18%.

Special Populations: Elderly

Increased half-life from approximately 4.4 to 5.7 hours in elderly patients (65 to 93 years of age).

Special Populations: Race

Japanese men had a 35% reduction in eletriptan exposure.

Use: Labeled Indications

Migraines: Acute treatment of migraine, with or without aura in adults

Contraindications

Ischemic coronary artery disease (eg, angina pectoris, history of myocardial infarction, documented silent ischemia); coronary artery vasospasm, including Prinzmetal’s 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 U.S. labeling): Cardiac arrhythmias (especially tachycardias), valvular heart disease, congenital heart disease, atherosclerotic disease; ophthalmoplegic migraine; Raynaud’s 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.

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:

U.S. labeling: Initial: 20-40 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 daily)

Canadian labeling: Initial: 20-40 mg as a single dose (maximum: 40 mg/dose). If after an initial dose of 20 mg, the headache improves but returns a repeat 20 mg dose may be administered after 2 hours have elapsed since first dose. If an initial dose of 40 mg was administered, a repeat dose is not recommended (maximum: 40 mg daily).

Dosing: Geriatric

Refer to adult dosing.

Dosing: Renal Impairment

No dosage adjustment provided in manufacturer’s labeling; however, adjustment likely not needed based on pharmacokinetic analysis; monitor for increased blood pressure.

Dosing: Hepatic Impairment

Mild-to-moderate impairment: No dosage adjustment necessary.

Severe impairment:

U.S. labeling: Use is not recommended.

Canadian labeling: Use is contraindicated.

Administration

Administer orally as soon as symptoms appear. May take with or without food.

Storage

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).

Drug Interactions

Analgesics (Opioid): May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy

Antiemetics (5HT3 Antagonists): May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy

Anti-Parkinson Agents (Monoamine Oxidase Inhibitor): May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Management: Monitor for signs and symptoms of serotonin syndrome/serotonin toxicity if selegiline or rasagiline is combined with a serotonin modulator. Use of transdermal selegiline with serotonin modulators is contraindicated. Consider therapy modification

Antipsychotic Agents: Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy

Conivaptan: May increase the serum concentration of CYP3A4 Substrates. 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. Consider therapy modification

CYP3A4 Inhibitors (Strong): May increase the serum concentration of Eletriptan. Avoid combination

Dapoxetine: May enhance the adverse/toxic effect of Serotonin Modulators. Avoid combination

Dasatinib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Droxidopa: Serotonin 5-HT1D Receptor Agonists may enhance the hypertensive effect of Droxidopa. Monitor therapy

Ergot Derivatives: Serotonin 5-HT1D Receptor Agonists may enhance the vasoconstricting effect of Ergot Derivatives. Ergot Derivatives may enhance the vasoconstricting effect of Serotonin 5-HT1D Receptor Agonists. Exceptions: Nicergoline. Avoid combination

Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates. Avoid combination

Idelalisib: May increase the serum concentration of CYP3A4 Substrates. Avoid combination

Ivacaftor: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Linezolid: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Management: Due to a risk of serotonin syndrome/serotonin toxicity, discontinue serotonin modulators 2 weeks prior to the administration of linezolid. If urgent initiation of linezolid is needed, discontinue serotonin modulators immediately and monitor closely. Consider therapy modification

Luliconazole: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Metaxalone: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy

Methylene Blue: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Avoid combination

Metoclopramide: Serotonin Modulators may enhance the adverse/toxic effect of Metoclopramide. This may be manifest as symptoms consistent with serotonin syndrome or neuroleptic malignant syndrome. Monitor therapy

Palbociclib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Serotonin Modulators: May enhance the adverse/toxic effect of other Serotonin Modulators. The development of serotonin syndrome may occur. Exceptions: Nicergoline; Tedizolid. Monitor therapy

Simeprevir: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Stiripentol: May increase the serum concentration of CYP3A4 Substrates. 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. Consider therapy modification

SUMAtriptan: Serotonin 5-HT1D Receptor Agonists may enhance the adverse/toxic effect of SUMAtriptan. Avoid combination

Tedizolid: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy

TraMADol: Serotonin Modulators may enhance the adverse/toxic effect of TraMADol. The risk of seizures may be increased. TraMADol may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy

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% (Limited to important or life-threatening): Abnormal hepatic function tests, anaphylactoid reaction, anaphylaxis, angina pectoris, angioedema, cardiac arrhythmia, confusion, depersonalization, depression, edema, emotional lability, hyperesthesia, hyperkinesia, hypersensitivity reaction, hypertension, impotence, increased creatine phosphokinase, insomnia, ischemic colitis, lacrimation, myalgia, myasthenia, myocardial infarction, peripheral vascular disorder, photophobia, polyuria, Prinzmetal angina, seizure, skin rash, speech disturbance, stupor, tachycardia, thrombophlebitis, vasospasm, ventricular fibrillation, visual disturbance

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's 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.

• Headaches: 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.

• Vasospasm-related events: Peripheral vascular ischemia, gastrointestinal vascular ischemia/infarction, and Raynaud’s 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. The Canadian labeling contraindicates use in severe impairment.

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information. Use is contraindicated within 72 hours of patients taking strong CYP3A4 inhibitors; use caution in patients taking moderate or strong CYP3A4 inducers and major CYP3A4 substrates. Consider alternative agents that avoid or lessen the potential for CYP-mediated interactions.

• Serotonin syndrome: Symptoms of agitation, confusion, hallucinations, hyper-reflexia, myoclonus, shivering, and tachycardia may 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.

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.

Special populations:

• Elderly: Blood pressure was increased to a greater extent in elderly subjects than in younger subjects.

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

Pregnancy Risk Factor

C

Pregnancy Considerations

Adverse events were observed in animal reproduction studies. Information related to eletriptan use in pregnancy is limited (Källén, 2011; Nezvalová-Henriksen, 2010; Nezvalová-Henriksen, 2012). Until additional information is available, other agents are preferred for the initial treatment of migraine in pregnancy (Da Silva, 2012; MacGregor, 2012; Williams, 2012).

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience dizziness, loss of strength and energy, or fatigue. Have patient report immediately to prescriber severe nausea, severe vomiting, severe headache, constipation, diarrhea, severe abdominal pain, bloody stools, burning or numbness feeling, weight loss, leg cramps, leg pain, sensation of cold, burning or pain in feet or toes, shortness of breath, signs of serotonin syndrome (dizziness, severe headache, agitation, hallucinations, tachycardia, abnormal heartbeat, flushing, tremors, sweating a lot, change in balance, severe nausea, or severe diarrhea), signs of severe cardiac abnormalities (chest, throat, neck, or jaw tightness, pain, pressure, or heaviness; break out in a cold sweat; shortness of breath; tachycardia; abnormal heartbeat; or severe dizziness or passing out), or signs of severe cerebrovascular disease (change in strength on one side is greater than the other, difficulty speaking or thinking, change in balance, or vision changes) (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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