Rizatriptan

Rizatriptan is a selective 5-HT1B/1D receptor agonist (serotonin receptor agonist) — the same class of receptor targeted by other triptans (sumatriptan, eletriptan, zolmitriptan). By activating 5-HT1B receptors on cranial blood vessels, rizatriptan causes vasoconstriction of dilated intracranial vessels. By activating 5-HT1D receptors on trigeminal sensory nerve terminals, it inhibits the release of pro-inflammatory neuropeptides (including CGRP and substance P) that mediate migraine pain and neurogenic inflammation. These two mechanisms together abort the migraine attack at the vascular and neural level.¹

Rizatriptan has a relatively short half-life of approximately 2–3 hours. Onset of action is typically 30 minutes to 2 hours.

Rizatriptan is FDA-approved for the acute treatment of migraine attacks with or without aura in adults and in pediatric patients 6–17 years of age.¹

Important limitations: Rizatriptan is not indicated for prevention of migraines, for the treatment of cluster headache, or for use in patients with hemiplegic or basilar migraine.

Adults: 5 mg or 10 mg as a single dose at the onset of migraine. If the migraine returns after initial relief, a second dose may be administered after 2 hours. Maximum 30 mg in any 24-hour period.

The 5 mg dose is recommended for patients taking propranolol (a beta blocker that substantially increases rizatriptan levels via MAO-A inhibition).¹

Pediatric patients (6–17 years): Weight-based dosing — 5 mg for patients under 40 kg; 10 mg for patients 40 kg or over.

Oral tablets or orally disintegrating tablets (Maxalt-MLT — dissolves on the tongue without water).

Store at room temperature. Maxalt-MLT orally disintegrating tablets should be left in the blister pack until just before use. Contains aspartame — patients with phenylketonuria should be aware.¹

Cardiovascular warning: Triptans cause vasoconstriction. Rizatriptan is contraindicated in patients with ischemic coronary artery disease (including history of myocardial infarction or angina), coronary artery vasospasm (including Prinzmetal's angina), history of stroke or TIA, peripheral vascular disease, or uncontrolled hypertension. Rare but serious cardiac events including MI and stroke have been reported.¹

Critical drug interactions:

• Serotonin syndrome — CRITICAL: Rizatriptan combined with SSRIs (including sertraline), SNRIs, MAOIs, buspirone, or other serotonergic agents significantly increases the risk of serotonin syndrome. The sertraline FDA label explicitly lists triptans as a drug class that increases serotonin syndrome risk. Patients on sertraline who use rizatriptan should be aware of this interaction and discuss it with their prescribing physician.
• MAOIs: Rizatriptan is absolutely contraindicated with MAOIs (including linezolid and methylene blue IV). Rizatriptan is metabolized by MAO-A; MAO inhibition dramatically increases rizatriptan exposure.
• Propranolol: Propranolol inhibits MAO-A and significantly increases rizatriptan plasma concentrations (approximately 70%). Use the 5 mg dose of rizatriptan in patients taking propranolol.
• Ergotamine-containing medications: Do not use within 24 hours of ergotamine or ergot-type medications (dihydroergotamine, methysergide) due to additive vasospastic effects.
• Other triptans: Do not use within 24 hours of other triptan medications.
• Frequency of use: Using acute migraine treatments (including triptans) on 10 or more days per month can cause medication overuse headache (MOH), also called rebound headache — a chronic daily headache that is worse than the original migraines.