Classifications: serotonin 5-ht1 receptor agonist; Therapeutic:antimigraine
Pregnancy Category: C
5 mg, 10 mg tablets; 5 mg, 10 mg disintegrating tablets
Selective (5-HT1B/1D) receptor agonist. The agonist effects at 5-HT1B/1D reverse the vasodilation of cranial blood vessels associated with a migraine.
Activation of the 5-HT1B/1D receptors reduces the pain pathways associated with the migraine headache as well as reversing vasodilation of cranial
Acute migraine headaches with or without aura.
Hypersensitivity to rizatriptan; CAD; Prinzmetal's angina (potential for vasospasm); ischemic heart disease; risk factors
for CAD such as hypertension, hypercholesterolemia, obesity, diabetes, smoking, and strong family history; concurrent administration
with ergotamine drugs or sumatriptan; concurrent administration with MAOIs; basilar or hemiplegic migraine; pregnancy (category C).
Hypersensitivity to sumatriptan; renal or hepatic impairment; lactation; hypertension; asthmatic patients. Safety and effectiveness
in patients <18 y are not established.
Route & Dosage
Adult: PO 510 mg, may repeat in 2 h if necessary (max: 30 mg/24 h); 5 mg with concurrent propranolol (max: 15 mg/24 h)
- Give any time after symptoms of migraine appear. If symptoms return, a second tablet may be given but no sooner than 2 h
after the first.
- Do not exceed 30 mg (three doses) in any 24 h period.
- Do not give within 24 h of an ergot-containing drug or another 5-HT1 agonist.
- Store at 15°30° C (59°86° F) and protect from light and moisture.
Adverse Effects (≥1%) Body as a Whole:
, pain, pressure sensation, paresthesias, throat pressure, warm/cold sensations. CNS:
Somnolence, dizziness, headache, hypesthesia, decreased mental acuity, euphoria, tremor. CV:
Coronary artery vasospasm, transient myocardial ischemia, MI,
ventricular tachycardia, ventricular fibrillation, chest pain/tightness/heaviness, palpitations. GI:
Dry mouth, nausea, vomiting, diarrhea. Respiratory:
may increase concentrations of rizatriptan, use smaller rizatriptan doses; dihydroergotamine, methysergide,
other 5-ht1 agonists
may cause prolonged vasospastic reactions; ssris
have rarely caused weakness, hyperreflexia, and incoordination; maoi
s should not be used with 5-HT1 agonists
. Herbal: St. John's wort
may increase triptan toxicity.
45% of oral dose reaches systemic circulation. Peak:
11.5 h for oral tabs; 1.62.5 h for orally disintegrating tablets. Metabolism:
Via oxidative deamination by monoamine oxidase A. Elimination:
Primarily in urine (82%). Half-Life:
Assessment & Drug Effects
- Monitor cardiovascular status carefully following first dose in patients at risk for CAD (e.g., postmenopausal women, men
>40 y, persons with known CAD risk factors) or coronary artery vasospasms.
- ECG is recommended following first administration of rizatriptan to someone with known CAD risk factors.
- Report immediately to physician: chest pain or tightness in chest or throat that is severe or does not quickly resolve.
- Monitor periodically cardiovascular status with continued rizatriptan use.
Patient & Family Education
- Do not exceed 30 mg (three doses) in 24 h.
- Allow orally disintegrating tablets to dissolve on tongue; no liquid is needed.
- Contact physician immediately if any of the following develop following rizatriptan use: symptoms of angina (e.g., severe
and/or persistent pain or tightness in chest or throat), hypersensitivity (e.g., wheezing, facial swelling, skin rash, or
hives), abdominal pain.
- Report any other adverse effects (e.g., tingling, flushing, dizziness) at next physician visit.