Naratriptan

Uses

Naratriptan is a 5-HT1B/1D receptor agonist used to treat migraines.

For the acute treatment of migraine attacks with or without aura in adults.

Naratriptan is also used to associated treatment for these conditions: Migraine with acute onset aura, Acute Migraine without aura

How Naratriptan works

Three distinct pharmacological actions have been implicated in the antimigraine effect of the triptans: (1) stimulation of presynaptic 5-HT1D receptors, which serves to inhibit both dural vasodilation and inflammation; (2) direct inhibition of trigeminal nuclei cell excitability via 5-HT1B/1D receptor agonism in the brainstem and (3) vasoconstriction of meningeal, dural, cerebral or pial vessels as a result of vascular 5-HT1B receptor agonism.

Toxicity

Symptoms of overdose include light-headedness, loss of coordination, tension in the neck, and tiredness.

Food Interaction

• Take with or without food. The absorption is unaffected by food.

Naratriptan Cholesterol interaction

[Major] The group of drugs known as 5-hydroxytryptamine1 receptor (5-HT1) agonists can cause vasospastic reactions, including coronary vasospasm, peripheral vascular ischemia, and colonic ischemia.

Rarely, serious adverse cardiac events including acute myocardial infarction, arrhythmia, cardiac arrest, and death have been reported within a few hours following the administration of 5-HT1 agonists, in some cases even in patients with no prior history or findings of coronary artery disease (CAD).

Significant elevation in blood pressure, including hypertensive crisis, has also been reported on rare occasions in patients with and without a history of hypertension, as have transient increases in blood pressure and peripheral vascular resistance.

In general, patients with potentially unrecognized CAD as predicted by the presence of risk factors (e.g., hypertension, hypercholesterolemia, tobacco use, obesity, diabetes, strong family history of CAD, female with surgical or physiological menopause, or male over 40 years of age) should not be administered 5-HT1 agonists unless a cardiovascular evaluation provides satisfactory clinical evidence indicating the lack of CAD, ischemic heart disease, or other significant underlying cardiovascular disease.

As a precaution, the manufacturers recommend that the first dose be administered under medical surveillance in such patients, and that electrocardiographic monitoring be considered during the interval immediately following administration to help detect any asymptomatic cardiac ischemia that may occur.

Periodic cardiovascular evaluations should be performed during intermittent, long-term use.

Naratriptan Drug Interaction

Major: duloxetine, duloxetine, ondansetron, ondansetronUnknown: diphenhydramine, diphenhydramine, galcanezumab, galcanezumab, pregabalin, pregabalin, rimegepant, rimegepant, topiramate, topiramate, cyanocobalamin, cyanocobalamin, cholecalciferol, cholecalciferol, cetirizine, cetirizine

Naratriptan Disease Interaction

Major: CAD risk factors, cardiovascular disease, liver disease, renal dysfunction

Volume of Distribution

• 170 L

Elimination Route

Well absorbed (74% oral biovaility), absorption is rapid with peak plasma concentrations after 2-5 hours. The rate of absorption is slower during a migraine attack.

Half Life

5-8 hours

Clearance

• 6.6 mL/min/kg

Innovators Monograph

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