NARATRIPTAN
(nar-a-trip'tan)
Amerge
Classifications: autonomic nervous system agent; adrenergic antagonist (sympatholytic); 5-ht1 serotonin agonist
Prototype: Sumatriptan
Pregnancy Category: C

Availability

1 mg, 2.5 mg tablets

Actions

Binds to the serotonin receptors (5HT1D and 5HT1B) on intracranial blood vessels, resulting in selective vasoconstriction of dilated vessels in the carotid circulation.

Therapeutic Effects

Inhibits vasoconstriction of dilated vessels selectively and also the release of proinflammatory neuropeptides. This results in the relief of acute migraine headache attacks.

Uses

Acute migraine headaches with or without aura.

Contraindications

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.

Cautious Use

Cardiovascular disease; renal or hepatic insufficiency; pregnancy (category C), lactation. Safety and efficacy in children <18 y are not established.

Route & Dosage

Acute Migraine
Adult: PO 1–2.5 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

Administration

Oral

Adverse Effects (1%)

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.

Interactions

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.

Pharmacokinetics

Absorption: Rapidly absorbed, 70% bioavailability. Peak: 2–4 h. Distribution: 28–31% protein bound. Metabolism: Metabolized in liver. Elimination: Excreted primarily in urine. Half-Life: 6 h.

Nursing Implications

Assessment & Drug Effects

Patient & Family Education


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