Dosing & Uses
Indicated for acute treatment of migraine headache
2.5 mg PO at onset; may repeat once after 2 hr
Not to exceed 7.5 mg/day
Dose adjustment not necessary
Mild to moderate hepatic impairment: Dose adjustment not necessary
Severe hepatic impairment: Safety and efficacy not established
Safety and efficacy not established
Migraine: See adult dosing
Serious - Use Alternative
Significant - Monitor Closely
Chest pain (>2%)
Frequency Not Defined
Hot or cold sensation
Myocardial infarction and coronary artery vasospasm in patients with CAD risk factors (extremely rare)
Hypersensitivity, severe hepatic or renal impairment, migraine prophylaxis
Ischemic heart disease, uncontrolled HTN, hemiplegic or basilar migraines, cluster headache, cerebrovascular syndromes, PVD
Do not use within 24 hr of another 5-HT1 agonist or ergot derivative, or within 2 weeks of MAOIs
Clear diagnosis of migraine headache must be established
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)
Serious cardiac and cerebrovascular events, including cerebral hemorrhage, subarachnoid hemorrhage, stroke, acute MI, arrhythmias, and death reported within a few hours after administration
Chest discomfort and jaw or neck tightness reported infrequently following intranasal administration (relatively common following SC injection)
Not for use with unrecognized CAD as predicted by risk factors (eg, hypertension, hypercholesterolemia, smoking, obesity, diabetes, strong family history of CAD, female with surgical or physiological menopause, male aged >40 yr)
Serotonin syndrome may occur, particularly when coadministered with SSRIs (eg, fluoxetine, paroxetine, sertraline, fluvoxamine, citalopram, escitalopram) or SNRIs (eg, venlafaxine, duloxetine)
May increased blood pressure, monitor
Pregnancy & Lactation
Pregnancy Category: C
Lactation: unknown; use caution
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 antidronic neuronal transmission associated with relief of migraine
Half-life: 26 hr
Peak plasma time: 2-4 hr
Distribution: 4.2 L/kg (male); 3 L/kg (female)
Protein binding: 15%
Bioavailability: 20% (male); 30% (female)
Excretion: Feces (62%); urine (32%)
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