rizatriptan (Rx)

>10%

Drowsiness (13-30%, dose related)

Fatigue (13-30%, dose related)

Dizziness (11-15%)

1-10%

Dizziness (4-9%)

Somnolence (4-8%)

Fatigue (4-7%; dose related)

Nausea (4-6%)

Asthenia (1-5%)

Hot flashes (1-5%)

Paresthesia (3-4%)

Dry mouth (3%)

Chest pain (2-3%)

Pain/pressure in chest, neck, throat, jaw (<2%)

Headache (<2%)

Dyspnea (>1%)

Hypoesthesia (>1%)

Palpations (>1%)

Skin flushing (>1%)

<1%

Tachycardia

Angioedema

Wheezing

Hypertensive crisis

Bradycardia

Hallucination

Epidermal necrolysis

Hearing impairment

Arrhythmias

Myocardial infarction and coronary artery vasospasm in patients with CAD risk factors

Contraindications

Hypersensitivity

Ischemic heart disease, uncontrolled hypertension, or other significant cardiovascular disease

Coronary artery vasospasm

History of stroke or transient ischemic attack

Ischemic bowel

Peripheral vascular disease

Basilar or hemiplegic migraine

Within 24 hours of another 5-HT1 agonist or ergot derivative

Within 2 weeks of MAOI

Cautions

Use caution in hepatic/renal insufficiency

Overuse of acute migraine drugs (eg, ergotamine, triptans, opioids, or combination of these drugs for ≥10 days/month) may lead to exacerbation of headache (medication overuse headache)

Potentially life-threatening serotonin syndrome may occur, particularly during combined use with SSRIs (eg, fluoxetine, paroxetine, sertraline, fluvoxamine, citalopram, escitalopram) or SNRIs (eg, venlafaxine, duloxetine)

Coronary artery vasospasm, ventricular tachycardia/fibrillation, cardiac arrest, myocardial infarction, transient ischemia, and death reported with the use of 5-HT1 agonists

Cerebral/subarachnoid hemorrhage and stroke reported with the use of 5-HT1 agonists

Significant hypertension or hypertensive crisis reported in patients with and without history of hypertension

Not for use in the prevention of migraine or the treatment of cluster headaches

Maxalt-MLT tablets contain phenylalanine (not for use in patients with phenylketonuria)

Patients with sensations of chest pain/pressure/tightness or symptoms suggestive of angina following dosing should be evaluated for coronary artery disease or Prinzmetal’s angina before administering additional doses; monitor with ECG if dosing is resumed and similar symptoms occur

Peripheral vascular ischemia and colonic ischemia, gastrointestinal ischemia/infarction, splenic infarction, and Raynaud’s syndrome reported with 5-HT1 agonist

Transient or permanent partial vision loss and blindness reported (rare)

Not for administration to patients who have risk factors for coronary artery disease (CAD), including hypertension, obesity, hypercholesterolemia, diabetes, menopause, strong family history of CAD, male >40 years of age or is a smoker unless patient undergoes adequate cardiac evaluation; patients suspected of having CAD, should have CAD ruled out before considering use of drug; if evaluation satisfactory, first dose should be administered in the healthcare provider’s office; perform periodic evaluation of cardiovascular status in all patients

Pregnancy Category: C

Lactation: Unknown; use with caution in breastfeeding

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Selective 5-HT1 receptor agonist in cranial arteries; causes vasoconstriction and reduces inflammation associated with antidromic neuronal transmission linked to relief of migraine

Absorption

Bioavailability: 45-50%

Onset of action: Within 2 hr

Peak plasma time: 1-1.5 hr

AUC: 30% higher in females than in males

Distribution

Protein bound: 14%

Vd: 110 L (female); 140 L (male)

Metabolism

Metabolized by MAO-O

Metabolites: N-monodesmethyl-rizatriptan

Elimination

Half-life elimination: 2-3 hr

Excretion: Urine (82%); feces (12%)