ELETRIPTAN HYDROBROMIDE
(e-le-trip'tan)
Relpax
Classifications: autonomic nervous system agent; 5-ht₁ serotonin agonist
Prototype: Sumatriptan
Pregnancy Category: C

Availability

20 mg, 40 mg tablets

Actions

Eletriptan is a potent agonist at central serotonin 5-HT_1B, 5-HT_1D, and 5-HT_1F receptors, and has modest affinity for 5-HT_1A, 5-HT_1E, 5-HT_2B, and 5-HT₇ receptors. Eletriptan stimulates presynaptic 5-HT_1D receptors inhibiting dural vasodilation and agonizes vascular 5-HT_1B receptors causing vasoconstriction of intracranial extracerebral vessels.

Therapeutic Effects

Inhibits dural vasodilation and inflammation, and causes vasoconstriction of painfully dilated intracranial extracerebral vessels, thus relieving the migraine headache. Also relieves photophobia, phonophobia, and nausea and vomiting associated with migraine attacks.

Uses

Treatment of acute migraine attacks with or without aura.

Contraindications

Hypersensitivity to eletriptan; CVA or TIA; within 24 h of administering of another ergotamine; pregnancy (category C), lactation within 24 h after dose; children <18 y; severe hepatic insufficiency; hemiplegic or basilar migraine; ischemic heart disease; peripheral vascular disease; uncontrolled hypertension.

Cautious Use

Hypotension in the elderly; lactation; mild to moderate hepatic impairment; ischemic or vasospastic coronary artery disease; diabetes, obesity, smoking, high cholesterol; history of coronary artery disease; men over 40 y of age; postmenopausal women. Use within 72 h of potent CYP3A4 metabolizing drugs.

Route & Dosage

Acute Migraine
Adult: PO 20 mg or 40 mg at onset of migraine (max: 40 mg/dose and 80 mg/d), may repeat dose in 2 h if partial response
Geriatric: Use not recommended

Hepatic Impairment
Use not recommended in severe hepatic impairment

Administration

Oral

Give one tablet as soon as the migraine begins.
May give 2nd tablet if headache improves but returns after 2 h.
If 1st tablet is ineffective, do not give a 2nd without consulting physician.
Do not give within 72 h of potent CYP3A4 inhibitors (see INTERACTIONS).
Store at 15°–30° C (59°–86° F). Protect from light and moisture

Adverse Effects (1%)

Body as a Whole: Asthenia, paresthesia, flushing, back pain, chills. CNS: Dizziness, drowsiness, headache, somnolence, hypertonia, hypesthesia. CV: Chest tightness/pressure, palpitation, hypertension. The following are rare, usually seen in patients with cardiovascular disease risk factors: Coronary vasospasm, transient myocardial ischemia, MI, ventricular tachycardia, atrial fibrillation, ventricular fibrillation. GI: Abdominal pain, dyspepsia, dysphagia, nausea, vomiting, dry mouth. Respiratory: Pharyngitis. Skin: Sweating.

Interactions

Drug: Drugs that inhibit CYP3A4 may increase eletriptan levels and toxicity, do not administer eletriptan within 72 h of azole antifungals (especially itraconazole, ketoconazole, voriconazole), amiodarone, cimetidine, dalfopristin, quinupristin, diltiazem, metronidazole, nicardipine, norfloxacin, quinine, verapamil, zafirlukast, zileuton, macrolide antibiotics, nonnucleotide reverse transcriptase inhibitors, protease inhibitors, selective serotonin reuptake inhibitors, sibutramine; ergot alkaloids may prolong vasospastic adverse reactions (do not use within 24 h of ergot-containing drugs); do not administer within 24 h of other 5-ht₁ agonists (may cause increased adverse effects). Food: Grapefruit juice may increase eletriptan levels and toxicity. Herbal: Gingko, ginseng, echinacea, St. John's wort may increase triptan toxicity.

Pharmacokinetics

Absorption: Rapidly absorbed, 50% reaches systemic circulation. Onset: 1–2 h. Peak: 1.5 h. Distribution: 85% protein bound. Metabolism: Metabolized in liver by CYP3A4. Elimination: 90% cleared by nonrenal routes, 9% eliminated in urine. Half-Life: 4–5 h.

Nursing Implications

Assessment & Drug Effects

Monitor CV status carefully following first dose in patients at risk for coronary artery disease (e.g., history of hypertension, postmenopausal women, men >40 y, persons with known CAD risk factors) or who have coronary artery vasospasms.
Report immediately chest pain, tightness in chest or throat that is severe or does not quickly resolve following a dose of eletriptan.
Monitor therapeutic effectiveness. Pain relief is usually achieved within 1 h.

Patient & Family Education

Note: If first dose is ineffective, do not take a second dose as it will not work for the same attack.
Inform physician of all prescription, nonprescription, and herbal drugs you are taking. Do not add additional drugs without informing physician as many drugs interact with eletriptan.
Report promptly any of the following: headache more severe than usual, migraine; dizziness, faintness, blurred vision; chest, neck, or throat pain; irregular heart beat, palpitations; shortness of breath, wheezing, difficulty breathing; tingling, pain, or numbness in the face, hands, or feet; seizures; severe stomach pain, cramping, or bloody diarrhea.
Do not drive or engage in any potentially hazardous task until reaction to drug is known.
Do not breast feed without consulting physician.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug