Dosing & Uses
Dosage Forms & Strengths
1-2.5 mg PO at onset; may repeat once after 4 hours
Not to exceed 5 mg/day
Mild-to-moderate: Not to exceed 2.5 mg/day
Severe (<15 mL/min); Do not administer
Safety and efficacy not established
Serious - Use Alternative
Significant - Monitor Closely
Coronary artery vasospasm in pts with CAD risk factors
Hypersensitivity, including angioedema and anaphylaxis
Severe hepatic or renal impairment
Wolff-Parkinson-White syndrome or arrhythmias associated with other cardiac accessory conduction pathway disorders
Ischemic heart disease (angina pectoris, history of myocardial infarction, or documented silent ischemia) or coronary artery vasospasm, including Prinzmetal’s angina)
History of stroke or TIA, or history of hemiplegic or basilar migraine because such patients are at a higher risk of stroke
Peripheral vascular disease
Ischemic bowel disease
Do not use within 24 hr of another 5-HT1 agonist or ergot derivative
Decrease dose with mild-moderate renal impairment
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)
Serotonin syndrome: 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)
Myocardial infarction, cardiac arrest, transient ischemia, coronary artery vasopasm reported
Significant increase in blood pressure including hypertensive crisis with acute impairment of organ systems reported
Anaphylaxis/anaphylactoid and hypersensitivity reactions, including angioedema reported (see Contraindications)
May cause dizziness, weakness, or drowsiness (infrequent)
Pregnancy & Lactation
Pregnancy Category: C
Lactation: unknown; use with caution in breastfeeding
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
Peak Plasma Time: 3-4 hr
Peak Plasma Concentration: 50-1,000 ng/ml; 50% higher in women
Protein Bound: 28-31%
Vd: 170 L
Via hepatic CYP450 enzymes
Half-Life: 6 hr
Excretion: Urine 50%
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|1||This drug is available at the lowest co-pay. Most commonly, these are generic drugs.|
|2||This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.|
|3||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.|
|4||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.|
|5||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.|
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