Rizatriptan
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Rizatriptan (benzoate)
Maxalt (tablet), Maxalt-MLT (orally disintegrating tablet)
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Summary
Common uses
Acute migraine with or without aura (FDA; adult and pediatric ages 6+)0
Pharmacy
Starting dose
5-10 mg PO at migraine onset; may repeat after 2 hours, maximum 30 mg/24 hours
Preparations
Tablets 5, 10 mg; ODT (Maxalt-MLT) 5, 10 mg
US FDA Max
30 mg/24 hours
Pharmacology
Routes
Oral
Onset
30 minutes for migraine relief
Duration
4-6 hours; headache recurrence is common
Half-life
2-3 hours[1]
Bioavailability
~45% (oral; substantially higher than sumatriptan's ~14%)[1]
Pregnancy
Limited human data; pregnancy registry data have been broadly reassuring across the triptan class.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Selective 5-HT1B and 5-HT1D receptor agonist (the triptan-class signature). Compared to sumatriptan, oral bioavailability is substantially higher (~45% vs ~14%) and onset is faster, with similar headache-recurrence rates. The 5-HT1B effect produces cranial vasoconstriction reversing the neurogenic vasodilation of migraine; the 5-HT1D effect inhibits CGRP release at trigeminal nerve terminals.0 Propranolol substantially raises rizatriptan exposure (~70% increase) via MAO-A inhibition of rizatriptan metabolism; the 5 mg dose is required when used with propranolol. Same triptan-class contraindications: coronary artery disease, vasospastic angina, uncontrolled hypertension, ischemic stroke history, hemiplegic or basilar migraine[1].
References
- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Maxalt (rizatriptan benzoate), Merck, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/020864s022,020865s024lbl.pdf