Version May 2024
Note: Do not use within 24 hours of an ergotamine preparation or a different triptan. Limit use to <10 days per month to avoid medication-overuse headache (AHS [Ailani 2021]).
Menstrual migraine prevention (off-label use): Oral: 1 mg twice daily beginning 2 to 3 days prior to expected onset of symptoms; continue for a total of 5 to 6 days (Mannix 2007; Newman 2001).
Migraine, moderate to severe, acute treatment:
Note: Administration early in the course of a migraine attack, at the first sign of pain, may improve response to treatment. When attack is complicated by severe nausea or vomiting, a nonoral medication may be more effective (AHS [Ailani 2021]).
Oral: 2.5 mg as a single dose; if symptoms persist or return, may repeat dose after ≥4 hours. Maximum: 2.5 mg/dose; 5 mg per 24 hours (Mathew 1997; manufacturer’s labeling).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Mild to moderate renal impairment: Initial: 1 mg; maximum dose: 2.5 mg per 24 hours.
Severe renal impairment (CrCl <15 mL/minute): Use is contraindicated.
Mild to moderate hepatic impairment (Child-Pugh grade A or B): Initial: 1 mg; maximum dose: 2.5 mg per 24 hours.
Severe hepatic impairment (Child-Pugh grade C): Use is contraindicated.
Refer to adult dosing. Dosing should generally start at the lower end of the dosing range due to possible increased incidence of hepatic, renal, and cardiac impairment.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
1% to 10%:
Central nervous system: Pain (4%), fatigue (2%), dizziness (1% to 2%), drowsiness (1% to 2%), paresthesia (1% to 2%), hot and cold flashes (1%), sensation of pressure (1%; chest/neck/throat/jaw), vertigo (1%)
Gastrointestinal: Nausea (4% to 5%), vomiting (1%), xerostomia (1%)
Neuromuscular & skeletal: Neck pain (2%)
Ophthalmic: Photophobia (1%)
Respiratory: Constriction of the pharynx (2%), ENT infection (1%)
<1%, postmarketing, and/or case reports (limited to important or life-threatening): Abnormal bilirubin levels, abnormal hepatic function tests, anaphylactoid reaction, anaphylaxis, anemia, angina pectoris, angioedema, bradycardia, cerebral infarction, colonic ischemia, coronary artery vasospasm, depression, dyspnea, ECG changes (atrial fibrillation, atrial flutter, premature ventricular contractions, PR prolongation, or QTc prolongation), glycosuria, hallucination, heart murmur, hypercholesterolemia, hyperglycemia, hyperlipidemia, hypersensitivity reaction (some cases severe, including circulatory collapse), hypertension, hypotension, hypothyroidism, ischemic heart disease, ketonuria, myocardial infarction, palpitations, panic, seizure, serotonin syndrome, skin rash, subarachnoid hemorrhage, subconjunctival hemorrhage, syncope, thrombocytopenia, transient ischemic attacks, ventricular fibrillation, ventricular tachycardia
Ischemic coronary artery disease (CAD) (angina pectoris, history of myocardial infarction [MI], or documented silent ischemia); coronary artery vasospasm, including Prinzmetal's angina; Wolff-Parkinson-White syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders; history of stroke, transient ischemic attack (TIA), or history of hemiplegic migraine or migraine with brainstem aura; peripheral vascular disease; ischemic bowel disease; uncontrolled hypertension; recent use (within 24 hours) of another 5-HT1 agonist, ergotamine-containing medication, or ergot-type medication (eg, dihydroergotamine or methysergide); severe renal impairment (CrCl <15 mL/minute) or severe hepatic impairment; hypersensitivity to naratriptan or any component of the formulation
Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Canadian labeling: Additional contraindications (not in US labeling): Severe hypertension, cardiac arrhythmias (especially tachycardias); valvular heart disease, significant underlying cardiovascular disease (eg, congenital heart disease, atherosclerotic disease); management of ophthalmoplegic migraine
Concerns related to adverse effects:
• Anaphylactic reactions: Anaphylaxis and hypersensitivity reactions (including angioedema) have occurred; may be life-threatening or fatal. Use is contraindicated in patients with known hypersensitivity to naratriptan.
• Cardiac events: Coronary artery vasospasm, transient ischemia, myocardial infarction, ventricular tachycardia/fibrillation, cardiac arrest, and death have been reported with 5-HT1 agonist administration; some events have occurred within a few hours of administration. Discontinue if these events occur. Patients who experience sensations of chest pain/pressure/tightness or symptoms suggestive of angina following dosing should be evaluated for coronary artery disease (CAD) or Prinzmetal's angina before receiving additional doses; if dosing is resumed and similar symptoms recur, monitor with ECG. Use is contraindicated in patients with ischemic or vasospastic CAD and Wolff-Parkinson-White syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders.
• Cerebrovascular events: Cerebral/subarachnoid hemorrhage and stroke (some fatal) have been reported with 5-HT1 agonist administration. Use is contraindicated in patients with a history of stroke or transient ischemic attack.
• CNS depression: May cause CNS depression, such as dizziness, weakness, or drowsiness, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
• Elevated blood pressure: Significant elevation in blood pressure, including hypertensive crisis with acute impairment of organ systems, has been reported on rare occasions in patients with and without a history of hypertension. Monitor blood pressure; use is contraindicated in patients with uncontrolled hypertension.
• Headaches: Acute migraine agents (eg, triptans, opioids, ergotamine, or a combination of the agents) used for 10 or more days per month may lead to worsening of headaches (medication overuse headache); withdrawal treatment may be necessary in the setting of overuse.
• Vasospasm-related events: Peripheral vascular ischemia and colonic ischemia, gastrointestinal vascular ischemia and infarction, splenic infarction, and Raynaud syndrome have been reported with 5-HT1 agonist administration.
• Visual effects: Partial vision loss and blindness (transient and permanent) have been reported with use of 5-HT1 agonists; a causal relationship between these events and 5-HT1 agonist administration has not been clearly determined.
Disease-related concerns:
• Coronary artery disease: Should not be given to patients who have risk factors for CAD (eg, hypertension, hypercholesterolemia, smoker, obesity, diabetes, strong family history of CAD, menopause, male >40 years of age) without adequate cardiac evaluation. Use is contraindicated if there is evidence of CAD or coronary artery vasospasm. Patients with suspected CAD should have cardiovascular evaluation to rule out CAD before considering use; if cardiovascular evaluation is “satisfactory,” first dose should be given in the health care provider's office (consider ECG monitoring). Periodic evaluation of cardiovascular status should be done in all patients.
• Hepatic impairment: Use is contraindicated in patients with severe hepatic impairment (Child-Pugh grade C).
• Renal impairment: Use is contraindicated in patients with severe renal impairment (CrCl <15 mL/minute).
Concurrent drug therapy issues:
• Serotonin syndrome: Symptoms of agitation, confusion, hallucinations, hyper-reflexia, myoclonus, shivering, and tachycardia may occur with concomitant proserotonergic drugs (ie, SSRIs/SNRIs or triptans) or agents which reduce naratriptan's metabolism. Concurrent use of serotonin precursors (eg, tryptophan) is not recommended. If concomitant administration with SSRIs is warranted, monitor closely, especially at initiation and with dose increases. Discontinue naratriptan if serotonin syndrome is suspected.
Special populations:
• Older adult: Blood pressure increases may be more pronounced in the elderly.
Other warnings/precautions:
• Appropriate use: Only indicated for the acute treatment of migraine; not indicated for migraine prophylaxis, or for the treatment of cluster headache, hemiplegic, or basilar migraine. If a patient does not respond to the first dose, the diagnosis of migraine should be reconsidered; rule out underlying neurologic disease in patients with atypical headache and in patients with no prior history of migraine.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Tablet, Oral:
Amerge: 1 mg [DSC], 2.5 mg [DSC]
Generic: 1 mg, 2.5 mg
Yes
Tablets (Naratriptan HCl Oral)
1 mg (per each): $25.00 - $29.49
2.5 mg (per each): $25.00 - $29.49
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Tablet, Oral:
Amerge: 1 mg [DSC]
Amerge: 2.5 mg [DSC] [contains fd&c blue #2 (indigo carm) aluminum lake]
Generic: 1 mg, 2.5 mg
Oral: Administer orally as soon as symptoms appear; may take with or without food. Do not crush or chew tablet; swallow whole with water.
Migraine, moderate to severe, acute treatment: Acute treatment of migraine attacks with or without aura in adults.
Menstrual migraine prevention
Amerge may be confused with Altace, Amaryl
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Bromocriptine: May enhance the adverse/toxic effect of Serotonin 5-HT1D Receptor Agonists (Triptans). Management: Consider alternatives to this combination when possible. If combined, monitor for increased bromocriptine and triptan toxicities. Risk D: Consider therapy modification
Droxidopa: Serotonin 5-HT1D Receptor Agonists (Triptans) may enhance the hypertensive effect of Droxidopa. Risk C: Monitor therapy
Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates): Serotonin 5-HT1D Receptor Agonists (Triptans) may enhance the vasoconstricting effect of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk X: Avoid combination
Monoamine Oxidase Inhibitors: Serotonin 5-HT1D Receptor Agonists (Triptans) may enhance the serotonergic effect of Monoamine Oxidase Inhibitors. This could result in serotonin syndrome. Monoamine Oxidase Inhibitors may increase the serum concentration of Serotonin 5-HT1D Receptor Agonists (Triptans). Risk X: Avoid combination
Serotonergic Agents (High Risk): Serotonin 5-HT1D Receptor Agonists (Triptans) may enhance the serotonergic effect of Serotonergic Agents (High Risk). This could result in serotonin syndrome. Management: Monitor for signs and symptoms of serotonin syndrome/serotonin toxicity (eg, hyperreflexia, clonus, hyperthermia, diaphoresis, tremor, autonomic instability, mental status changes) when these agents are combined. Risk C: Monitor therapy
Serotonin 5-HT1D Receptor Agonists (Triptans): May enhance the vasoconstricting effect of other Serotonin 5-HT1D Receptor Agonists (Triptans). Risk X: Avoid combination
Pregnancy outcome data for naratriptan is available from a pregnancy registry sponsored by GlaxoSmithKline. As of September 2012, data were available for 57 infants/fetuses exposed to naratriptan (52 during the first trimester), and seven exposed to both naratriptan and sumatriptan. Following naratriptan exposure, there was one infant born with a birth defect; this infant was also exposed to sumatriptan during the first trimester of pregnancy. The pregnancy registry was closed to enrollment in January 2012 (Ephross 2014). Additional data related to the use of naratriptan in pregnancy is limited in comparison to other 5-HT1B/1D agonists (triptans) (Källén 2011; Nezvalová-Henriksen 2010; Nezvalová-Henriksen 2012; Nezvalová-Henriksen 2013; Spielmann 2018; Yusuf 2018).
Triptans relieve migraine pain by selectively binding to serotonin receptors, resulting in vasoconstriction of cranial arteries. Although the effects on uterine blood flow have not been evaluated, one case report suggests excessive use of a triptan may cause placental hypoperfusion (ACOG 2022; Viard 2021).
Treatment for migraine headaches in pregnant patients should be individualized (AHS [Ailani 2021]). Triptans are not the preferred initial treatment for acute migraine headache in pregnant patients (ACOG 2022). Until additional data are available, naratriptan is not the preferred triptan when first-line therapy is ineffective. Triptans should be avoided in pregnant patients with cardiac disease or hypertension (ACOG 2022; CHS [Worthington 2013]).
Naratriptan is present in breast milk.
Data related to the presence of 5-HT1B/1D agonists (triptans) in breast milk is available from a study of 19 lactating women (6 weeks to 30 months postpartum) treated for migraine headaches. During the study, infants were fed previously expressed breast milk. Breast milk was sampled prior to and at intervals up to 24 hours after the dose in one patient taking naratriptan 2.5 mg. Using the average breast milk concentration observed, authors of the study calculated the estimated exposure of naratriptan to the breastfed infant to be 1.9 mcg/kg/day, providing a relative infant dose (RID) of 5% based on the weight adjusted maternal dose. Using the maximum breast milk concentration, the RID of naratriptan was calculated to be 9%. A large interindividual variability among breast milk concentrations was found with all the triptans in the study, even when considering dose and dosage form (Amundsen 2021). In general, breastfeeding is considered acceptable when the RID is <10% (Anderson 2016; Ito 2000).
According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother. Treatment for migraine headaches in lactating patients should be individualized (AHS [Ailani 2021]). Withholding breastfeeding for 24 hours after the maternal dose will minimize infant exposure via breast milk. The decision to withhold breastfeeding following a dose of naratriptan should be part of a shared decision-making process (ACOG 2022).
Headache severity, blood pressure, signs/symptoms suggestive of angina; perform a cardiovascular evaluation in triptan-naïve patients who have multiple cardiovascular risk factors (eg, increased age, diabetes, hypertension, smoking, obesity, strong family history of CAD), monitor ECG with first dose in patients with multiple cardiovascular risk factors who have a negative cardiovascular evaluation and consider periodic cardiovascular evaluation in such patients if they are intermittent long-term users; signs/symptoms of serotonin syndrome and hypersensitivity reactions.
Selective agonist for serotonin (5-HT1B and 5-HT1D receptors) in cranial arteries; causes vasoconstriction and reduces sterile inflammation associated with antidromic neuronal transmission correlating with relief of migraine
Onset of action: ~1 to 2 hours (Bomhof 1999; Tfelt-Hansen 2000)
Absorption: Well absorbed
Distribution: Vdss: 170 L
Protein binding, plasma: 28% to 31%
Metabolism: Hepatic via CYP
Bioavailability: ~70%
Half-life elimination: 6 hours; Increased in renal impairment (moderate impairment; mean: 11 hours; range: 7 to 20 hours); Increased in hepatic impairment (moderate impairment: 8 to 16 hours)
Time to peak: 2 to 3 hours
Excretion: Urine (50% of total dose as unchanged drug; 30% of total dose as metabolites)
Altered kidney function: Naratriptan clearance is reduced 50% with moderate impairment (CrCl 18 to 39 mL/minute); mean Cmax increased ~40%.
Hepatic function impairment: Naratriptan clearance is decreased 30% in patients with moderate impairment (Child-Pugh class A or B).
Older adult: Clearance is decreased ~26% in healthy elderly subjects (65 to 77 years) compared with younger patients.
Sex: Cmax is 50% higher in women.
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