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Pronunciation
(rye za TRIP tan)
Generic Available (U.S.)
No
Index Terms
Brand Names: U.S.
Brand Names: Canada
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Acute treatment of migraine with or without aura
Pregnancy Risk Factor
C
Pregnancy Considerations
There are no adequate and well-controlled studies using rizatriptan in pregnant women. Use only if potential benefit to the mother outweighs the potential risk to the fetus. A pregnancy registry has been established to monitor outcomes of women exposed to rizatriptan during pregnancy (800-986-8999). In some animal studies, administration was associated with decreased weight gain, developmental toxicity and increased mortality in the offspring. Teratogenic effects were not observed.
Lactation
Excretion in breast milk unknown/use caution
Contraindications
Hypersensitivity to rizatriptan or any component of the formulation; documented ischemic heart disease or Prinzmetal's angina; uncontrolled hypertension; basilar or hemiplegic migraine; during or within 2 weeks of MAO inhibitors; during or within 24 hours of treatment with another 5-HT1 agonist, or an ergot-containing or ergot-type medication (eg, methysergide, dihydroergotamine)
Warnings/Precautions
Concerns related to adverse effects:
• Cardiac events: Coronary artery vasospasm, transient ischemia, myocardial infarction, ventricular tachycardia/fibrillation, cardiac arrest, and death have been reported with 5-HT1 agonist administration. Patients who experience 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 receiving additional doses; if dosing is resumed and similar symptoms recur, monitor with ECG.
• Cerebrovascular events: Cerebral/subarachnoid hemorrhage and stroke have been reported with 5-HT1 agonist administration.
• Elevated blood pressure: Significant elevation in blood pressure, including hypertensive crisis, has also been reported on rare occasions in patients with and without a history of hypertension.
• Vasospasm-related events: Peripheral vascular ischemia and colonic ischemia have been reported with 5-HT1 agonist.
Disease-related concerns:
• Coronary artery disease: Should not be given to patients who have risk factors for CAD (eg, hypertension, hypercholesterolemia, smoker, obesity, diabetes, strong family history of CAD, menopause, male >40 years of age) without adequate cardiac evaluation. Patients with suspected CAD should have cardiovascular evaluation to rule out CAD before considering use; if cardiovascular evaluation is “satisfactory,” first dose should be given in the healthcare provider's office (consider ECG monitoring). Periodic evaluation of cardiovascular status should be done in all patients.
• Hepatic impairment: Use with caution in patients with hepatic impairment; drug clearance may be reduced leading to increased plasma concentrations.
• Renal impairment: Use with caution in dialysis patients.
Concurrent drug therapy issues:
• Serotonin syndrome: Symptoms of agitation, confusion, hallucinations, hyper-reflexia, myoclonus, shivering, and tachycardia may occur with concomitant proserotonergic drugs (ie, SSRIs/SNRIs or triptans) or agents which reduce rizatriptan's metabolism. Concurrent use of serotonin precursors (eg, tryptophan) is not recommended. If concomitant administration with SSRIs is warranted, monitor closely, especially at initiation and with dose increases.
Dosage form specific issues:
• Phenylalanine: Maxalt-MLT® tablets contain phenylalanine.
Other warnings/precautions:
• Appropriate use: Only indicated for treatment of acute migraine; if a patient does not respond to the first dose, the diagnosis of migraine should be reconsidered.
Adverse Reactions
>10%:
Central nervous system: Fatigue (adults 7% to 30%, dose related; children >1%)
Gastrointestinal: Xerostomia (<5% to 13%)
1% to 10%:
Cardiovascular: Chest pain (<2% to 5%), flushing (>1%), palpitation (>1%), systolic/diastolic blood pressure increases (5-10 mm Hg)
Central nervous system: Dizziness (9%), somnolence (8%), headache (≤2%), euphoria (>1%), hypoesthesia (>1%), drowsiness
Dermatologic: Skin flushing
Endocrine & metabolic: Growth hormone increased (mild), hot flashes
Gastrointestinal: Nausea (3%), diarrhea (>1%), vomiting (>1%), abdominal pain
Neuromuscular & skeletal: Weakness (4% to 7%), paresthesia (3% to 4%); myalgia (3%); neck, throat, and jaw pain/tightness/pressure (≤2%), tremor (>1%)
Respiratory: Dyspnea (>1%)
Miscellaneous: Feeling of heaviness (<1% to 2%)
<1%, postmarketing, and/or case reports: Abdominal distention, agitation, akinesia, anaphylaxis/anaphylactoid reactions, angina, angioedema, arrhythmia, arthralgia, attention span decreased (children), blurred vision, bradycardia, bradykinesia, chills, cold extremities, confusion, coordination impaired (children), diaphoresis, diarrhea, dry eyes, dysgeusia, dyspepsia, eye pain, eye swelling, facial edema, hallucinations (children), hangover, headache exacerbation (overuse), hearing impairment (children), heat sensitivity, hypertensive crisis, insomnia, memory impairment, mental activity decreased, MI, muscle spasm, myocardial ischemia, nasopharyngeal irritation, neurological/psychiatric abnormalities, pharyngeal edema, pharyngitis, polyuria, pruritus, rash, seizures, stroke, syncope, tachycardia, tinnitus, toxic epidermal necrolysis, urticaria, vasospasm, vertigo, wheezing
Metabolism/Transport Effects
None known.
Drug Interactions
Antipsychotics: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Risk C: Monitor therapy
Ergot Derivatives: May enhance the vasoconstricting effect of Serotonin 5-HT1D Receptor Agonists. Serotonin 5-HT1D Receptor Agonists may enhance the vasoconstricting effect of Ergot Derivatives. Risk X: Avoid combination
MAO Inhibitors: May decrease the metabolism of Serotonin 5-HT1D Receptor Agonists. Management: If MAO inhibitor therapy is required, naratriptan, eletriptan or frovatriptan may be a suitable 5-HT1D agonist to employ. Risk X: Avoid combination
Metoclopramide: Serotonin Modulators may enhance the adverse/toxic effect of Metoclopramide. This may be manifest as symptoms consistent with serotonin syndrome or neuroleptic malignant syndrome. Risk C: Monitor therapy
Propranolol: May increase the serum concentration of Rizatriptan. Management: Rizatriptan adult dose should be reduced to 5 mg in patients who are also being treated with propranolol. Risk D: Consider therapy modification
Serotonin Modulators: May enhance the adverse/toxic effect of other Serotonin Modulators. The development of serotonin syndrome may occur. Risk D: Consider therapy modification
Ethanol/Nutrition/Herb Interactions
Food: Food delays absorption.
Storage
Store in blister pack until administration.
Mechanism of Action
Selective agonist for serotonin (5-HT1B and 5-HT1Dreceptors) in cranial arteries; causes vasoconstriction and reduces sterile inflammation associated with antidromic neuronal transmission correlating with relief of migraine
Pharmacodynamics/Kinetics
Onset of action: ~30 minutes
Duration: 14-16 hours
Protein binding: 14%
Metabolism: Via monoamine oxidase-A; first-pass effect
Bioavailability: 40% to 50%
Half-life elimination: 2-3 hours
Time to peak: 1-1.5 hours
Excretion: Urine (82%, 8% to 16% as unchanged drug); feces (12%)
Dosage
Note: In patients with risk factors for coronary artery disease, following adequate evaluation to establish the absence of coronary artery disease, the initial dose should be administered in a setting where response may be evaluated (physician's office or similarly staffed setting). ECG monitoring may be considered.
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)
Note: For orally-disintegrating tablets (Maxalt-MLT®): Patient should be instructed to place tablet on tongue and allow to dissolve. Dissolved tablet will be swallowed with saliva.
Monitoring Parameters
Headache severity, signs/symptoms suggestive of angina; consider monitoring blood pressure, heart rate, and/or ECG with first dose in patients with likelihood of unrecognized coronary disease, such as patients with significant hypertension, hypercholesterolemia, obese patients, patients with diabetes, smokers with other risk factors or strong family history of coronary artery disease
Dietary Considerations
Some products may contain phenylalanine.
Patient Education
This drug is to be used to reduce your migraine, not to prevent or reduce the number of attacks. For orally-disintegrating tablets (Maxalt-MLT®), do not open blister pack before using. Open with dry hands, place on tongue, and allow to dissolve (dissolved tablet will be swallowed with saliva). Do not crush, break, or chew. If first dose brings relief, second dose may be taken anytime after 2 hours if migraine returns. Do not take more than two doses without consulting prescriber. May cause dizziness, drowsiness, dry mouth, skin flushing or hot flashes, mild abdominal discomfort , nausea, or vomiting. Report immediately any chest pain, palpitations, or irregular heartbeat; severe dizziness, acute headache, stiff or painful neck or facial swelling; muscle weakness or pain; changes in mental acuity; blurred vision or eye pain; or excessive perspiration or urination.
Geriatric Considerations
Since the elderly often have cardiovascular disease, careful evaluation of the use of 5-HT agonists is needed to avoid complications with the use of these agents. The pharmacokinetic disposition of these agents is similar to that seen in younger adults.
Cardiovascular Considerations
5-HT1B/1D agonists have been associated with coronary vasospasm. These agents are contraindicated in patients with documented ischemic of vasospastic coronary artery disease. Patients with risk factors for CAD may receive these agents, provided a cardiovascular evaluation yields satisfactory evidence that the patient is free of cardiovascular disease. In patients with risk factors for CAD, administration of the initial dose in a medically staffed/equipped facility (ie, physician's office) is recommended. In addition, ECG monitoring after the initial dose should be considered. Patients who acquire risk factors for CAD, or long-term users of agents from this class of medications, should undergo periodic cardiovascular evaluation.
Dental Health: Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation).
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
Drowsiness and dizziness are common
Mental Health: Effects on Psychiatric Treatment
Contraindicated with other serotonin agonists (SSRIs) and MAO inhibitors
Nursing: Physical Assessment/Monitoring
For use only with clear diagnosis of migraine. Cardiovascular status should be evaluated prior to initiating medication and periodically thereafter. Monitor for drowsiness, nausea/vomiting, chest pain, and palpitations.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, oral:
Maxalt®: 5 mg, 10 mg
Tablet, orally disintegrating, oral:
Maxalt-MLT®: 5 mg [contains phenylalanine 1.05 mg/tablet; peppermint flavor]
Maxalt-MLT®: 10 mg [contains phenylalanine 2.1 mg/tablet; peppermint flavor]
Pricing: U.S. (www.drugstore.com)
Tablet, orally-disintegrating (Maxalt-MLT)
5 mg (3): $315.72
10 mg (3): $95.99
Tablets (Maxalt)
5 mg (12): $353.69
10 mg (18): $518.01
References
Boyer EW and Shannon M, “The Serotonin Syndrome,” N Engl J Med, 2005, 352:1112-20.
International Brand Names
Lexi-Comp.com
Last full review/revision March 2012
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