NARATRIPTAN (nar-a-trip'tan) Amerge Classifications: autonomic nervous system agent; adrenergic antagonist (sympatholytic); 5-ht1 serotonin agonist Prototype: Sumatriptan Pregnancy Category: C
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1 mg, 2.5 mg tablets
Binds to the serotonin receptors (5HT1D and 5HT1B) on intracranial blood vessels, resulting in selective vasoconstriction of dilated vessels in the carotid circulation.
Inhibits vasoconstriction of dilated vessels selectively and also the release of proinflammatory neuropeptides. This results
in the relief of acute migraine headache attacks.
Acute migraine headaches with or without aura.
Severe renal impairment (creatinine clearance <15 mL/min); severe hepatic impairment; history of ischemic heart disease (i.e.,
angina pectoris, MI); cerebrovascular syndromes (i.e., strokes or TIA); uncontrolled hypertension; patients with hemiplegic
or basilar migraine; hypersensitivity to naratriptan; older adults.
Cardiovascular disease; renal or hepatic insufficiency; pregnancy (category C), lactation. Safety and efficacy in children
<18 y are not established.
Acute Migraine Adult: PO 12.5 mg; may repeat in 4 h if necessary (max: 5 mg/24 h); patients with mild or moderate renal or hepatic impairment
should not exceed 2.5 mg/24 h
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Oral
- Give any time after symptoms of migraine appear. If the first tablet was effective but symptoms return, a second tablet may
be given, but no sooner than 4 h after the first. Do not exceed 5 mg in 24 h.
- If there is no response to the first tablet, contact physician before administering a second tablet.
- Do not give within 24 h of an ergot-containing drug or other 5-HT1 agonist.
- Store at 2°25° C (36°77° F); protect from light.
Body as a Whole: Asthenia, fatigue, malaise, pain, pressure sensation, paresthesias, throat pressure, warm/cold sensations, hot flushes. CNS: Somnolence, dizziness, drowsiness, headache, hypesthesia, decreased mental acuity, euphoria, tremor. CV: Coronary artery vasospasm, transient myocardial ischemia, MI, ventricular tachycardia, ventricular fibrillation, chest pain/tightness/heaviness, palpitations. GI: Dry mouth, nausea, vomiting, diarrhea. Respiratory: Dyspnea. Skin: Flushing.
Drug: Dihydroergotamine, methysergide, and other 5-ht 1 agonists may cause prolonged vasospastic reactions; ssris have rarely caused weakness, hyperreflexia, and incoordination; maois should not be used with 5-ht 1 agonists. Herbal: Gingko, ginseng, echinacea, St. John's wort may increase triptan toxicity.
Absorption: Rapidly absorbed, 70% bioavailability. Peak: 24 h. Distribution: 2831% protein bound. Metabolism: Metabolized in liver. Elimination: Excreted primarily in urine. Half-Life: 6 h.
Assessment & Drug Effects
- Monitor carefully cardiovascular status following first dose in patients at risk for CAD (e.g., postmenopausal women, men
over 40 y, persons with known CAD risk factors) or coronary artery vasospasms.
- Be aware that ECG is recommended following first administration of naratriptan to someone with known CAD risk factors and
periodically with long-term use.
- Report immediately to the physician: chest pain, nausea, or tightness in chest or throat that is severe or does not quickly
resolve.
- Obtain periodic cardiovascular evaluation with continued use.
Patient & Family Education
- Carefully review patient information leaflet and guidelines for administration.
- Contact physician immediately for any of the following: symptoms of angina (e.g., severe and/or persistent pain or tightness
in chest or throat, severe nausea); hypersensitivity (e.g., wheezing, facial swelling, skin rash, or hives); or abdominal
pain.
- Report any other adverse effects (e.g., tingling, flushing, dizziness) at next physician visit.
- Do not breast feed while taking this drug without consulting physician.