Eletriptan

Pronunciation

(el e TRIP tan)

U.S. Brand Names

Relpax®

Synonyms

Eletriptan Hydrobromide

Generic Available

No

Use

Acute treatment of migraine, with or without aura

Pregnancy Risk Factor

C

Pregnancy Implications

There are no adequate and well-controlled studies in pregnant women; use during pregnancy only if the potential benefit to the mother outweighs the possible risk to the fetus. Teratogenic effects were observed in animal studies.

Lactation

Enters breast milk/use caution

Contraindications

Hypersensitivity to eletriptan or any component of the formulation; ischemic heart disease or signs or symptoms of ischemic heart disease (including Prinzmetal's angina, angina pectoris, MI, silent myocardial ischemia); cerebrovascular syndromes (including strokes, transient ischemic attacks); peripheral vascular syndromes (including ischemic bowel disease); uncontrolled hypertension; use within 24 hours of ergotamine derivatives; use within 24 hours of another 5-HT1 agonist; use within 72 hours of potent CYP3A4 inhibitors; management of hemiplegic or basilar migraine; prophylactic treatment of migraine; severe hepatic impairment

Warnings/Precautions

Eletriptan is indicated only in patients 18 years of age with a clear diagnosis of migraine headache. If a patient does not respond to the first dose, the diagnosis of migraine should be reconsidered. Do not give to patients with risk factors for CAD until a cardiovascular evaluation has been performed; if evaluation is satisfactory, the healthcare provider should administer the first dose and cardiovascular status should be periodically evaluated. Cardiac events (coronary artery vasospasm, transient ischemia, MI, ventricular tachycardia/fibrillation, cardiac arrest, and death), cerebral/subarachnoid hemorrhage, stroke, peripheral vascular ischemia, and colonic ischemia have been reported with 5-HT1 agonist administration. Significant elevation in blood pressure, including hypertensive crisis, has also been reported on rare occasions in patients with and without a history of hypertension. Use with caution with renal or mild to moderate hepatic impairment. Safety and efficacy in pediatric patients have not been established.

Adverse Reactions

1% to 10%:

Cardiovascular: Chest pain/tightness (1% to 4%; placebo 1%), palpitation

Central nervous system: Dizziness (3% to 7%; placebo 3%), somnolence (3% to 7%; placebo 4%), headache (3% to 4%; placebo 3%), chills, pain, vertigo

Gastrointestinal: Nausea (4% to 8%; placebo 5%), xerostomia (2% to 4%, placebo 2%), dysphagia (1% to 2%), abdominal pain/discomfort (1% to 2%; placebo 1%), dyspepsia (1% to 2%; placebo 1%)

Neuromuscular & skeletal: Weakness (4% to 10%), paresthesia (3% to 4%), back pain, hypertonia, hypesthesia

Respiratory: Pharyngitis

Miscellaneous: Diaphoresis

<1% (Limited to important or life-threatening): Agitation, allergic reaction, angina, arrhythmia, ataxia, confusion, constipation, CPK increased, depersonalization, depression, diarrhea, dreams (abnormal), dyspnea, edema, emotional lability, esophagitis, euphoria, hyperesthesia, hyperkinesia, hypertension, impotence, incoordination, insomnia, lacrimation disorder, liver function tests abnormal, myalgia, myasthenia, nervousness, peripheral vascular disorder, photophobia, polyuria, pruritus, rash, salivation increased, shock, speech disorder, stupor, tachycardia, taste perversion, thrombophlebitis, tinnitus, tongue edema, tremor, urinary frequency, vasospasm, vision abnormal

Overdosage/Toxicology

Hypertension or more serious cardiovascular symptoms may occur. Clinical and electrocardiographic monitoring needed for at least 20 hours even if patient is asymptomatic. Treatment is symptom-directed and supportive.

Drug Interactions

Substrate of CYP3A4 (major)

CYP3A4 inhibitors: May increase the levels/effects of eletriptan. Example inhibitors include azole antifungals, ciprofloxacin, clarithromycin, diclofenac, doxycycline, erythromycin, imatinib, isoniazid, nefazodone, nicardipine, propofol, protease inhibitors, quinidine, and verapamil.

Ergot-containing drugs: Prolong vasospastic reactions; do not use eletriptan or ergot-containing drugs within 24 hours of each other.

Ethanol/Nutrition/Herb Interactions

Food: High-fat meal increases bioavailability.

Stability

Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F)

Mechanism of Action

Selective agonist for serotonin (5-HT1B, 5-HT1D, 5-HT1F receptors) in cranial arteries; causes vasoconstriction and reduce 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: 4.4-5.7 hours); Metabolite: ~13 hours

Time to peak, plasma: 1.5-2 hours

Dosage

Oral: Adults: Acute migraine: 20-40 mg; if the headache improves but returns, dose may be repeated after 2 hours have elapsed since first dose; maximum 80 mg/day.

Note: If the first dose is ineffective, diagnosis needs to be re-evaluated. Safety of treating >3 headaches/month has not been established.

Dosage adjustment in renal impairment: No dosing adjustment needed; monitor for increased blood pressure

Dosage adjustment in hepatic impairment:

Mild to moderate impairment: No adjustment necessary

Severe impairment: Use is contraindicated

Patient Education

Inform prescriber of all prescriptions (including oral contraceptives), OTC medications, or herbal products you are taking, and any allergies you have. This drug is to be used to reduce your migraine, not to prevent the number of attacks. Follow exact instructions for use. Do not crush, break, or chew tablet. Do not take within 24 hours of any other medication without first consulting prescriber. If headache improves but returns, dose may be repeated after 2 hours. Do not exceed two doses in 24 hours (may take either 20 mg or 40 mg twice daily). If you have no relief with the first dose, do not take a second dose without consulting prescriber. May cause dizziness or drowsiness (use caution when driving or engaging in tasks requiring alertness until response to drug is known); nausea, vomiting, or abdominal pain. Report immediately any chest pain, tightness, or palpitations; muscle weakness or tremors; back pain; respiratory difficulty; changes in CNS (abnormal thought processes, depression, insomnia, confusion, agitation); swelling of eyelids, face, lips, throat; rash, hives, or any other adverse reactions. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Consult prescriber if breast-feeding.

Dental Health: Effects on Dental Treatment

Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation).

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Dosage Forms

Tablet, as hydrobromide [film coated]: 20 mg, 40 mg [as base]

International Brand Names

Relert® (BE, ES, FI, IL); Relpax® (AT, AU, BR, CH, CR, CZ, DE, DK, ES, FR, GB, GT, IT, MX, NO, NZ, PA, PL, SE, VE, YU, ZA)