Dosing & Uses
Dosage Forms & Strengths
tablet
- 6.25mg
- 12.5mg
Migraine
Indicated for acute treatment of migraine attacks in patients with a history of migraine with or without aura
Initial 6.25-12.5 mg PO at onset; may repeat once after 2 hours
Not to exceed 25 mg/day
Renal Impairment, Severe
CrCl <30 mL/min: Initial 6.25 mg PO
Not to exceed 12.5 mg/day
Hepatic Impairment
Initial: 6.25 mg PO
Not to exceed 12.5 mg/day
Dosage Forms & Strengths
tablet
- 6.25mg
- 12.5mg
Migraine
Indicated for acute treatment of migraine headache pain in adolescents with a history of migraine attacks with or without aura usually lasting ≥4 hr (when untreated)
<12 years: Safety and efficacy not established
≥12 years: 6.25-12.5 mg PO at onset of headache; may repeat once after 2 hr
Not to exceed 25 mg/day
Migraine: See adult dosing
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
1-10%
Somnolence (1-5%)
Dizziness (3-4%)
Nausea (1-3%)
Vomiting (2%)
Dry mouth (1-2%)
Headache (1-2%)
Nausea (1-2%)
Paresthesia (1-2%)
Paresthesia (1%)
Somnolence (>1%)
<1%
Infrequent (0.01-0.001%)
- Anxiety, asthenia, chills, CNS stimulation, fatigue, hypesthesia, tremor
- Pruitus, rash
- Diaphoresis, dysmenorrhea, hyperglycemia, increased thirst
- Abdominal cramp, gastroenteritis
- Back pain, myalgia, neck pain, rigid neck, Increased CPK
- Bronchitis, chest pain, dyspnea, pharyngitis, rhinitis, sinusitis
- Conjunctivitis, tinnitis, vertigo
Rare (<0.001%)
- Hypertension, syncope
- Fever, insomnia, nervousness, nightmares
- Erythema, photosensitivity
- Colitis, esophegeal reflux, gastritis
- Arthralgia, arthritis, muscle weakness, myopathy
- Laryngitis, sneezing
- Eye abnormalities, nystagmus
- Hypercholesteremia, hyperventilation, increased gamma glutamyl transpeptidase, increased salvation
Postmarketing Experience
Hypersensitivity reactions (including angioedema, anaphylactic reactions and eye disorders including visual impairment, vision blurred) reported
Warnings
Contraindications
Hypersensitivity, severe hepatic or renal impairment, migraine prophylaxis
Ischemic heart disease, uncontrolled HTN, hemiplegic or basilar migraines, cluster HA, cerebrovascular syndromes, PVD
Do not use within 24 hr of another 5-HT1 agonist or ergot derivative, or within 2 weeks of MAOIs
Cautions
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); detoxification of patients, including withdrawal of overused drugs, and treatment of withdrawal symptoms (often includes a transient worsening of headache) may be necessary
After dose is administered, patients who experience angina symptoms or chest pain, pressure, and tightness, should be evaluated for coronary artery disease or Prinzmetal's angina before receiving additional doses
Hemorrhage and stroke have been reported with 5-HT1 agonist administration
Significant increase in blood pressure has been reported with 5-HT1 agonists
Transient and permanent blindness and partial vision loss have been reported with 5-HT-1 agonisits
Serotonin syndrome may develop if administered concomitantly with proserotonergic drugs
Pregnancy & Lactation
Pregnancy Category: C
Lactation: excretion in milk unknown; use with caution
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.
Pharmacology
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
Pharmacokinetics
Half-Life: 3-4 hr
Peak Plasma Time: 1-3 hr
Bioavailability: 70%
Protein bound: 35%
Vd: 180-200 L
Absorption: Well absorbed
Metabolism: CYP3A4, CYP2D6
Excretion: Urine (75%)
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Patient Handout
Formulary
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