Selective 5-HT1B/1D serotonin receptor agonist
ATC code: N02CC04 (Rizatriptan)
Brand names
Maxalt-MLT, Maxalt, Rizalt
A selective 5-HT1B and 5-HT1D agonist. Via 5-HT1B it constricts dilated cranial vessels; via 5-HT1D it blocks release of inflammatory neuropeptides (CGRP, substance P) from trigeminal nerve endings. Onset 30–60 minutes after orally disintegrating tablets (MLT) or 60–90 minutes after standard tablets. Half-life 2–3 hours.
First line
First-line for acute moderate-to-severe migraine per AHS 2024 and EFNS 2022. The 2014 Cochrane meta-analysis showed pain-free response at 2 hours with rizatriptan 10 mg in 40% versus 19% on placebo. Among triptans, one of the fastest onsets (especially the MLT orally disintegrating tablet when nausea is present). Take at the first sign of pain, not during aura. If no response at 2 hours, repeat dosing is not recommended.
Sources
Second line
Migraine in nursing mothers. Per AHS 2024 – alternative to sumatriptan during breastfeeding. Dose 5-10 mg orally, repeat at 2 h. Max 30 mg/day. Fast onset (30 min).
The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.
Not recommended
Rizatriptan is a triptan with indications similar to sumatriptan. It is prescribed for migraine and cluster headache ( NG150 2021 and AHS 2021 guidelines). For severe tension-type headache, premenstrual headache, or hangover headache without confirmed migraine, rizatriptan is not used: regular use for non-migraine pain provokes medication-overuse headache. Triptans are contraindicated in ischemic heart disease, prior stroke, and uncontrolled hypertension. If rizatriptan was prescribed for any severe headache without confirmed migraine, consider seeking a second opinion.
2 pairs found. Sorted from critical to minor.
Mechanism
Rizatriptan is a MAO-A substrate. With phenelzine accumulation and fatal serotonin syndrome.
Symptoms
Agitation, tachycardia, hyperthermia, myoclonus, hyperreflexia within hours.
Management
Combination contraindicated. 14 days after MAOI withdrawal before starting triptan.
Mechanism
MAO-A inhibition by tranylcypromine + rizatriptan – fatal serotonin syndrome.
Symptoms
Agitation, tachycardia, hyperthermia, myoclonus, hyperreflexia within hours.
Management
Combination contraindicated. 14 days after MAOI withdrawal before starting triptan.
Opens the checker prefilled with this drug. Pick the second one from your regimen.
Direct links to regulator labels. Open in a new tab.
FDA category C. Limited pregnancy data. Avoid in T1 where possible. For severe migraine in pregnancy, first-line abortive is paracetamol; with insufficient effect under physician supervision, sumatriptan (which has more pregnancy data) is preferred.
Compatible. Hale L3, limited RID data. Short T½ 2 h gives rapid clearance. Wait 4-8 h before feeding to minimize exposure.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Rizatriptan is evaluated for the following indications with varying evidence strength: Acute migraine attack (evidence tier A), Migraine during breastfeeding (evidence tier B), Memory and concentration enhancement (evidence tier F). See the full indication matrix with dosing and citations above on this page.
Common side effects of Rizatriptan (≥ 1 in 100): Drowsiness, Dizziness, Chest, neck, or jaw tightness or pressure, Nausea, Dry mouth, Flushing. See the Safety section for uncommon and serious reactions.
FDA category C. FDA category C. Limited pregnancy data. Avoid in T1 where possible. For severe migraine in pregnancy, first-line abortive is paracetamol; with insufficient effect under physician supervision, sumatriptan (which has more pregnancy data) is preferred.
Compatible. Hale L3, limited RID data. Short T½ 2 h gives rapid clearance. Wait 4-8 h before feeding to minimize exposure.
Rizatriptan is contraindicated in: Rizatriptan hypersensitivity; Coronary artery disease, prior MI; Uncontrolled hypertension; History of cerebrovascular events (stroke, TIA); Peripheral arterial disease. Full list in the Safety section.