Rizatriptan
MAXALT
Pronunciation: rye-za-TRIP-tan
“RZA tripped (on) Max altitude”
RZA of Wu-Tang Clan, pronounced "rizza“, while the medication is spelled “Riza” and pronounced “RYE-za”
What it is5-HT1B, 5-HT1D and 5-HT1F agonist; abortive treatment of migraine.
Why this oneFaster oral onset than sumatriptan, and the dissolving wafer needs no water when nausea is prominent.
What limits itCoronary vasospasm makes it contraindicated in ischemic heart disease. Propranolol raises exposure; medication-overuse headache follows frequent use.
FDA-approved for
- migraine (1998)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Acute treatment of migraine | Adults | 5-10 mg | 5-10 mg; may repeat after 2 h | 30 mg/24 h |
| Acute treatment of migraine | Pediatric 6-17 yr | 5 mg if <40 kg; 10 mg if >=40 kg | single dose (repeat dose not established) | single dose/24 h |
Renal Undefined
Hepatic Undefined
Second dose no sooner than 2 h after the first; max 30 mg/24 h
Instructions
- ODT: peel blister with dry hands, place on tongue to dissolve, swallow with saliva; no liquid needed
- Do not exceed 30 mg in any 24-hour period; treat on average no more than 4 headaches per 30 days
- On propranolol: adults use 5 mg only (max 15 mg/24 h); pediatric >=40 kg single 5 mg; do not use in propranolol-treated pediatric patients <40 kg
- Contains phenylalanine (component of aspartame)
Available strengths
- tab 5, 10 mg
- ODT 5, 10 mg
- film 5, 10 mg
Contraindications
- MAOIs (concurrently or within 14 days)
- Ischemic coronary artery disease (angina, prior MI, silent ischemia) or other significant cardiovascular disease
- Coronary artery vasospasm, including Prinzmetal's angina
- History of stroke or transient ischemic attack
- Peripheral vascular disease
- Ischemic bowel disease
- Uncontrolled hypertension
- Recent use (within 24 h) of another 5-HT1 agonist, ergotamine, or ergot-type medication
- Hemiplegic or basilar migraine
- Concurrent use or recent discontinuation (within 2 weeks) of an MAO-A inhibitor
Cautions
- Myocardial ischemia, MI, and Prinzmetal's angina
- Life-threatening cardiac arrhythmias
- Chest/throat/neck/jaw pain, tightness, or pressure
- Cerebrovascular events (hemorrhage, stroke)
- Other vasospasm reactions (peripheral, GI ischemia, Raynaud's)
- Medication overuse headache
- Serotonin syndrome (with SSRIs, SNRIs, TCAs, MAO inhibitors)
- Increase in blood pressure, including hypertensive crisis
Adverse reactions
- Asthenia/fatigue
- Somnolence
- Pain/pressure sensations
- Dizziness
- Dry mouth
- Nausea
- Paresthesia
Pregnancy Insufficient human data; no clear drug-associated risk of birth defects.
Lactation Excreted in rat milk (~6x maternal plasma); no human data.
Cost
Generic entry2012
NO BOXED WARNINGS
Principal riskCoronary vasospasm; contraindicated in ischemic heart disease
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilityAgent-specific vascular, serotonergic or hepatic risks; acute overdose is usually limited outside ergot or cardiovascular agents.
Serotonicity
This drug is routinely called serotonergic. By Gillman’s human-effect criteria it does not raise serotonin in the synapse.
Triptan receptor agonism is not a mechanistic serotonin-toxicity interaction with SRIs.
Label contraindicationMAOIs (concurrently or within 14 days). The label governs prescribing; Gillman’s point concerns serotonin toxicity only.
Gillman’s four human testsA measurable SERT affinity that fails all four is not clinical serotonicity.
- Retarded orgasm
- Efficacy in OCD and cataplexy
- Clonus and hyperreflexia in single-drug overdose
- Serotonin toxicity when combined with an MAOI
Non-elevating action5-HT1B/1D agonist
Evidence confidenceHigh
Background: what serotonicity is · what is and is not an SRI · what counts as a relevant MAOI.
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