Trade Names:Amerge- Tablets 1 mg (as hydrochloride)- Tablets 2.5 mg (as hydrochloride)
Binds to serotonin (5-HT) 1 B and 1 D receptors in intracranial arteries leading to vasoconstriction and subsequent relief of migraine headache.
Bioavailability of naratriptan is 70%, AUC is 98 mcg/L•h, T max is 2 to 3 h, T max during migraine attack is 3 to 4 h, and C max is 12.6 mcg/L.
Naratriptan Vd is 170 L and protein binding is 28% to 31%.
Naratriptan is metabolized in the liver by CYP-450 enzymes to inactive metabolites.
Naratriptan is eliminated in urine, 50% unchanged and 30% as metabolites (inactive). The t ½ is 6 h, systemic Cl is 6.6 mL/min/kg, and renal Cl is 220 mL/min.
Naratriptan Cl is reduced 50% with moderate impairment (CrCl 18 to 39 mL/min). This resulted in an increase of t ½ from 6 to 11 h, and mean C max was increased about 40%.Hepatic Function Impairment
Naratriptan Cl is decreased 30%, which resulted in about a 40% increase in the t ½ from 8 to 16 h.Gender
C max is 50% higher in women.
Treatment of acute migraine attacks with or without aura.
Patients with history, signs, or symptoms of ischemic heart disease (eg, angina, including Prinzmetal variant, MI, silent myocardial ischemia), cerebrovascular or peripheral vascular syndromes, uncontrolled hypertension, severe renal or hepatic insufficiency, patients with hemiplegic or basilar migraine, or hypersensitivity to any component of the product. Naratriptan is contraindicated within 24 h of use with other serotonin agonists, ergotamine compounds, or methysergide.
PO 1 or 2.5 mg with onset of migraine headache. Dose is individualized based on response and adverse reactions. The dose may be repeated once after 4 h if partial response or if the headache returns. The max daily dose is 5 mg in 24 h.
Store tablets at controlled room temperature (68° to 77°F).
Increased risk of vasospastic reactions; therefore, coadministration of two 5-HT 1 agonists within 24 h of each other is contraindicated.Ergot-containing drugs
May cause additive, prolonged vasospasm.Selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, fluvoxamine, paroxetine, sertraline)
Weakness, hyperreflexia, and incoordination have been rarely reported.Sibutramine
Serotonin syndrome, including CNS irritability, motor weakness, shivering, myoclonus, and altered consciousness may occur.
None well documented.
Angina, MI (postmarketing).
Dizziness, drowsiness, malaise/fatigue, paresthesia (2%); vertigo (at least 1%); cerebral vascular accident, including transient ischemic attack, subarachnoid hemorrhage, and cerebral infarction (postmarketing).
Ear, nose, and throat infections, photophobia (at least 1%).
Nausea (5%); hyposalivation, vomiting (at least 1%); colonic ischemia (postmarketing).
Hypersensitivity, including anaphylaxis/anaphylactoid reactions (postmarketing).
Atypical sensation (4%); pain and pressure in neck and throat (2%); warm/cold temperature sensation, sensations of pressure, tightness, and heaviness (at least 1%).
Category C .
Safety and efficacy not established.
Hypersensitivity reactions (including anaphylaxis and anaphylactoid reactions) may occur.
May cause coronary vasospasm in patients with coronary artery disease (CAD).
Cerebral hemorrhage, subarachnoid hemorrhage, stroke, and other cerebrovascular events have been reported with 5-HT 1 agonists.
Elevation in BP, including hypertensive crisis, have been reported with administration of 5-HT 1 agonists.
Hypertension, cardiac ischemia, lightheadedness, neck tension, loss of coordination.
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