ELETRIPTAN HYDROBROMIDE
| ELETRIPTAN HYDROBROMIDE (e-le-trip'tan) Relpax Classifications: serotonin 5-ht1 receptor agonist; Therapeutic: antimigraine Prototype: Sumatriptan Pregnancy Category: C |
Availability
20 mg, 40 mg tablets
Action
Eletriptan is a potent agonist at central serotonin 5-HT1B, 5-HT1D, and 5-HT1F receptors. Eletriptan stimulates presynaptic 5-HT1D receptors inhibiting dural vasodilation and agonizes vascular 5-HT1B receptors causing vasoconstriction of intracranial extracerebral vessels.
Therapeutic Effect
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; history of coronary artery disease; ischemic or vasospastic coronary artery disease, arteriosclerosis, history of MI; ischemic colititis, Raynaud's disease uncontrolled hypertension; 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; peripheral vascular disease; concurrent MAOI therapy.
Cautious Use
Hypotension in the elderly; older adults >65 y; mild to moderate hepatic impairment; diabetes, obesity, smoking, high cholesterol; men >40 y; postmenopausal women. Use within 72 h of potent CYP3A4 metabolizing drugs; lactation.
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: 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.
Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; 
Canadian drug name; 
Prototype drug