No

Serotonin 5-HT_1D Receptor Agonist

Acute treatment of migraine with or without aura

C

Prior hypersensitivity to rizatriptan; documented ischemic heart disease or Prinzmetal's angina; uncontrolled hypertension; basilar or hemiplegic migraine; during or within 2 weeks of MAO inhibitors

Use only in patients with a clear diagnosis of migraine; use with caution in elderly or patients with hepatic or renal impairment, history of hypersensitivity to sumatriptan or adverse effects from sumatriptan, and in patients at risk of coronary artery disease. Do not use with ergotamines. May increase blood pressure transiently; may cause coronary vasospasm (less than sumatriptan); avoid in patients with signs/symptoms suggestive of reduced arterial flow (ischemic bowel, Raynaud's) which could be exacerbated by vasospasm. Phenylketonurics (tablets contain phenylalanine).

Caution in dialysis patients or hepatically impaired. Reconsider diagnosis of migraine if no response to initial dose. Long-term effects on vision have not been evaluated.

1% to 10%:

Cardiovascular: Systolic/diastolic blood pressure increases (5-10 mm Hg), chest pain (5%)

Central nervous system: Dizziness, drowsiness, fatigue (13% to 30% - dose related)

Dermatologic: Skin flushing

Endocrine & metabolic: Mild increase in growth hormone, hot flashes

Gastrointestinal: Nausea, vomiting, abdominal pain, dry mouth (<5%)

Respiratory: Dyspnea

<1%: Syncope, facial edema, tachycardia, palpitation, bradycardia, chills, hangover, decreased mental activity, neurological/psychiatric abnormalities, pruritus, neck pain/stiffness, muscle weakness, myalgia, arthralgia, blurred vision, dry eyes, eye pain, tinnitus, polyuria, nasopharyngeal irritation, heat sensitivity, diaphoresis

Use within 24 hours of another selective 5-HT₁ agonist or ergot-containing drug should be avoided due to possible additive vasoconstriction

Propranolol: Plasma concentration of rizatriptan increased 70%

SSRIs: Rarely, concurrent use results in weakness and incoordination; monitor closely

MAO inhibitors and nonselective MAO inhibitors increase concentration of rizatriptan

Store in blister pack until administration

Selective agonist for serotonin (5-HT_1D receptor) in cranial arteries to cause vasoconstriction and reduce sterile inflammation associated with antidromic neuronal transmission correlating with relief of migraine

Onset of action: Within 30 minutes

Duration: 14-16 hours

Protein binding: Minimal (14%)

Metabolism: Substantial nonrenal clearance by monoamine oxidase-A; undergoes first-pass metabolism

Bioavailability: 40% to 50%

Half-life: 2-3 hours

Time to peak concentration: 1-1.5 hours

Elimination: 8% to 16% excreted unchanged in urine; parent and metabolites eliminated (82%)

Oral: 5-10 mg, repeat after 2 hours if significant relief is not attained; maximum: 30 mg in a 24-hour period (Use 5 mg dose in patients receiving propranolol with a maximum of 15 mg in 24 hours)

Food delays the absorption

Headache severity, signs/symptoms suggestive of angina; consider monitoring blood pressure, heart rate, and/or EKG with first dose in patients with likelihood of unrecognized coronary disease, such as patients with significant hypertension, hypercholesterolemia, obese patients, diabetics, smokers with other risk factors or strong family history of coronary artery disease

Drowsiness and dizziness are common

Contraindicated with other serotonin agonists (SSRIs) and MAOIs

No information available to require special precautions

No effects or complications reported

Administration of orally disintegrating tablets: Do not open blister pack before using. Open with dry hands. Do not crush, chew, or swallow tablet; allow to dissolve on tongue. Take as prescribed; do not increase dosing schedule. May repeat one time after 2 hours, if first dose is ineffective. Do not ever take more than two doses without consulting prescriber. You may experience dizziness or drowsiness (use caution when driving, climbing stairs, or engaging in tasks requiring alertness until response to drug is known); skin flushing or hot flashes (cool clothes or a cool environment may help); mild abdominal discomfort or nausea or vomiting. Report severe dizziness, acute headache, chest pain or palpitation, stiff or painful neck or facial swelling, muscle weakness or pain, changes in mental acuity, blurred vision, eye pain, or excessive perspiration or urination. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Breast-feeding is not recommended.

Tablet, as benzoate:

Maxalt-MLT™ (orally disintegrating): 5 mg, 10 mg