Brand name: Maxalt
Drug class: Selective Serotonin Agonists
- Antimigraine Agents
- Selective Vascular Serotonin Type 1-Like Receptor Agonists
- 5-HT1 Agonists
VA class: CN105
Chemical name: N,N-Dimethyl-5-(1H-1,2,4-triazol-1-yl-methyl)-1H-indole-3-ethanamine monobenzoate
Molecular formula: C₁₅H₁₉N₅•C₇H₆O₂
CAS number: 145202-66-0

Medically reviewed by Drugs.com on Jul 26, 2024. Written by ASHP.

Introduction

Selective serotonin (5-hydroxytryptamine; 5-HT) type 1B and 1D receptor agonist (“triptan”).

Uses for Rizatriptan

Vascular Headaches

Acute treatment of migraine attacks with or without aura in adults and pediatric patients 6–17 years of age. Efficacy in reducing migraine-associated symptoms (nausea, photophobia, phonophobia) in pediatric patients not established.

Not recommended for management of hemiplegic or basilar migraine or for prophylaxis of migraine.

Safety and efficacy not established for management of cluster headaches.

Rizatriptan Dosage and Administration

Administration

Oral Administration

Administer orally as conventional or orally disintegrating tablets without regard to meals.

Just prior to administration of orally disintegrating tablet, remove blister from aluminum pouch; with dry hands, peel open blister package, place tablet on tongue to dissolve, and swallow with saliva.

Administration of orally disintegrating tablet with liquid is not necessary.

Dosage

Available as rizatriptan benzoate; dosage is expressed in terms of rizatriptan.

Pediatric Patients

Vascular Headaches

Migraine

Oral

Pediatric patients 6–17 years of age: 5 mg as a single dose in patients weighing <40 kg, 10 mg as a single dose in those weighing ≥40 kg.

Efficacy and safety of >1 dose within any 24-hour period not established.

Adults

Vascular Headaches

Migraine

Oral

5 or 10 mg as a single dose; 10-mg dose may provide greater effect than 5-mg dose, but may be associated with increased risk of adverse effects.

If headache recurs, a second dose may be administered 2 hours after the first dose; maximum dosage of 30 mg in any 24-hour period.

Prescribing Limits

Pediatric Patients

Vascular Headaches

Migraine

Oral

Efficacy and safety of >1 dose (5 mg in patients weighing <40 kg, 10 mg in those weighing ≥40 kg) in any 24-hour period not established.

Adults

Vascular Headaches

Migraine

Oral

Maximum 30 mg in any 24-hour period.

Safety of treating an average of >4 headaches per 30-day period has not been established.

Special Populations

Geriatric Patients

Select dosage with caution, usually starting at the low end of the dosage range, because of greater frequency of decreased hepatic, renal, or cardiac function and of concomitant disease or other drug therapy.

Cautions for Rizatriptan

Contraindications

• Ischemic heart disease (e.g., angina pectoris, history of MI, documented silent ischemia).

• Coronary artery vasospasm (e.g., Prinzmetal variant angina).

• Uncontrolled hypertension.

• Other serious underlying cardiovascular disease.

• History of stroke or TIA.

• Peripheral vascular disease or ischemic bowel disease.

• Hemiplegic or basilar migraine.

• Treatment within previous 24 hours with another 5-HT₁ receptor agonist or an ergot alkaloid. (See Specific Drugs under Interactions.)

• Concurrent or recent (within 2 weeks) treatment with an MAO-A inhibitor. (See Specific Drugs under Interactions.)

• Known hypersensitivity to rizatriptan or any ingredient in the formulation.

Warnings/Precautions

Careful Diagnosis of Migraine

Use only in patients in whom a clear diagnosis of migraine has been established.

If first migraine attack treated with rizatriptan fails to respond to the drug, reconsider diagnosis before administering rizatriptan to treat subsequent attacks.

Exclude other potentially serious neurologic disorders before administering rizatriptan to patients not previously diagnosed with migraine or to those with atypical symptoms.

Cardiac Effects

Possible myocardial ischemia and/or infarction and coronary vasospasm, even in patients without a history of CAD. Contraindicated in patients with ischemic or vasospastic heart disease.

Possible fatal or life-threatening cardiac rhythm disturbances (e.g., ventricular tachycardia or fibrillation). Discontinue if such disturbances occur.

Tightness, pain, pressure, and heaviness in the precordium, throat, neck, and jaw occur frequently but usually are noncardiac in origin. Manufacturer states that cardiovascular evaluation should be performed if a cardiac origin is suspected.

Patients at Risk for CAD

Perform cardiovascular evaluation prior to initiating therapy in patients with multiple cardiovascular risk factors (e.g., postmenopausal women; men >40 years of age; patients with risk factors such as hypertension, hypercholesterolemia, smoking, obesity, diabetes, family history of CAD) who have not previously received 5-HT₁ receptor agonist therapy.

If evaluation provides evidence of CAD or coronary vasospasm, do not administer the drug.

If results of evaluation are satisfactory, consider administering the initial dose in a medically supervised setting followed immediately by an ECG.

Periodic cardiovascular evaluation recommended in patients with risk factors for CAD if receiving intermittent long-term therapy.

Cerebrovascular Events

Possible cerebral or subarachnoid hemorrhage and stroke, sometimes fatal. (See Careful Diagnosis of Migraine under Cautions.) Discontinue therapy if a cerebrovascular event occurs.

Risk of certain cerebrovascular events (e.g., stroke, hemorrhage, TIA) may be increased in patients with migraine.

Other Vasospastic Effects

Possible noncoronary vasospastic reactions (e.g., peripheral vascular ischemia, GI ischemia and infarction with abdominal pain and bloody diarrhea, splenic infarction, Raynaud’s syndrome); transient or permanent blindness and partial vision loss reported in patients receiving 5-HT₁ receptor agonists.

If signs or symptoms suggestive of vasospasm occur following administration, evaluate patient to rule out vasospastic reaction before administering additional doses.

Hypertensive Effects

Substantial increases in BP, including hypertensive crisis with acute impairment of organ systems, reported rarely with 5-HT₁ receptor agonists in patients with or without history of hypertension.

Serotonin Syndrome

Potentially life-threatening serotonin syndrome reported in patients receiving 5-HT₁ receptor agonists, particularly in those receiving SSRIs or SNRIs concomitantly. (See Specific Drugs under Interactions.) Also may occur in patients receiving MAO inhibitors or tricyclic antidepressants concomitantly.

Symptoms may include mental status changes (e.g., agitation, hallucinations, coma), autonomic instability (e.g., tachycardia, labile BP, hyperthermia), neuromuscular aberrations (e.g., hyperreflexia, incoordination), and/or GI symptoms (e.g., nausea, vomiting, diarrhea).

If manifestations of serotonin syndrome occur, discontinue rizatriptan and any concurrently administered serotonergic agents and initiate supportive and symptomatic treatment.

Medication Overuse Headache

Overuse of drugs indicated for management of acute migraine attacks (e.g., use of 5-HT₁ receptor agonists, ergotamine, opiates, or certain analgesic combinations on a regular basis for ≥10 days per month) may result in migraine-like daily headaches or a marked increase in frequency of migraine attacks.

Detoxification, including withdrawal of overused drugs; treatment of withdrawal symptoms (e.g., transient worsening of headaches); and consideration of prophylactic migraine therapy may be necessary.

Sensitivity Reactions

Hypersensitivity reactions (e.g., angioedema, anaphylaxis, wheezing, toxic epidermal necrolysis) reported.

Phenylketonuria

Advise individuals who must restrict phenylalanine intake that each 5- or 10-mg Maxalt-MLT orally disintegrating tablet contains aspartame, which is metabolized in GI tract to provide 1.1 or 2.1 mg of phenylalanine, respectively. Conventional tablets do not contain aspartame.

Generic preparations of rizatriptan also may contain aspartame; consult the manufacturer’s prescribing information.

Specific Populations

Pregnancy

Category C. Pregnancy registry at 800-986-8999.

Lactation

Distributed into milk in rats; not known whether distributed into milk in humans. Caution advised if rizatriptan is used.

Pediatric Use

Safety and efficacy not established in children <6 years of age. Adverse effects in pediatric patients expected to be similar to those in adults.

Geriatric Use

No substantial differences in pharmacokinetic profile relative to younger adults; however, clinical studies did not include sufficient numbers of patients ≥65 years of age to determine whether response is different. Select dosage with caution.

Hepatic Impairment

Not studied in patients with severe hepatic impairment.

Common Adverse Effects

Pain/pressure sensations (i.e., chest pain [tightness/pressure/heaviness], pain/tightness/pressure in neck/throat/jaw, regional pain [tightness/pressure/heaviness], pain at location not specified), asthenia/fatigue, dizziness, headache, somnolence, dry mouth, nausea, paresthesia.

Drug Interactions

Metabolized by MAO-A.

Does not inhibit CYP3A4/5, 1A2, 2C9, 2C19, or 2E1; inhibits CYP2D6 only at high concentrations.

Specific Drugs

Rizatriptan Pharmacokinetics

Absorption

Bioavailability

Completely absorbed from GI tract, but absolute bioavailability (as conventional tablet) is 45%, indicating first-pass metabolism. Bioavailability is similar for orally disintegrating tablets.

Peak plasma concentrations attained within 1–1.5 hours when administered as conventional tablets; peak concentrations are delayed by up to 0.7 hour when administered as orally disintegrating tablets.

AUC and peak plasma concentration are approximately 30 and 11% higher, respectively, in females than in males.

Exposure in pediatric patients 6–17 years of age receiving a single dose at recommended dosage levels is similar to that in adults receiving a single 10-mg dose.

Food

Food does not substantially affect bioavailability but may delay time to peak concentration by 1 hour.

Distribution

Extent

Crosses placenta and is distributed into milk in animals; no studies in pregnant or nursing women.

Plasma Protein Binding

14%.

Elimination

Metabolism

Metabolized principally via oxidative deamination by MAO-A to an inactive indole acetic acid metabolite. Other minor metabolites, including an N-monodesmethyl derivative with similar activity to the parent compound, have been identified.

Elimination Route

Excreted principally in urine (14% of dose as unchanged drug, 51% as indole acetic acid metabolite).

Half-life

Approximately 2–3 hours.

Special Populations

In patients with moderate hepatic impairment, plasma rizatriptan concentrations are approximately 30% higher than in healthy individuals.

In hemodialysis patients, AUC is approximately 44% greater than in patients with normal renal function. AUC in patients with CL_cr of 10–60 mL/minute per 1.73 m² is similar to that in healthy individuals.

Pharmacokinetic profile in healthy geriatric individuals is similar to that in younger adults.

Stability

Storage

Oral

Tablets

15–30°C.

Orally Disintegrating Tablets

15–30°C.

Actions

• Binds with high affinity to 5-HT_1B and 5-HT_1D receptors.

• Structurally and pharmacologically related to other selective 5-HT_1B/1D receptor agonists (e.g., almotriptan, eletriptan, frovatriptan, naratriptan, sumatriptan, zolmitriptan).

• Precise mechanism of action not established; may ameliorate migraine through selective constriction of certain intracranial blood vessels, inhibition of neuropeptide release, and reduced transmission in trigeminal pain pathway.

Advice to Patients

• Risk of serious cardiovascular or cerebrovascular events (e.g., MI, stroke) or other vasospastic reactions. Importance of seeking medical care if symptoms of such reactions (e.g., shortness of breath, weakness, slurring of speech, sudden or severe abdominal pain, difficulty in seeing, or tightness, pain, pressure, or heaviness in chest, throat, neck, or jaw) occur and of not taking rizatriptan again until evaluated by clinician.

• Importance of taking rizatriptan exactly as prescribed.

• Importance of providing patient a copy of manufacturer’s patient information.

• Risk of dizziness, somnolence, and fatigue; importance of exercising caution when driving or operating machinery.

• For patients taking orally disintegrating tablets, importance of not removing the blister from the outer pouch until just before administering dose; importance of opening blister pack with dry hands and of placing tablet on tongue to dissolve and be swallowed with saliva.

• Importance of informing patients with phenylketonuria that orally disintegrating tablets contain aspartame.

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and herbal supplements, as well as any concomitant illnesses (e.g., cardiovascular disease).

• Importance of informing patients of risk of serotonin syndrome, particularly with concurrent use of rizatriptan and an SSRI or SNRI. Importance of seeking immediate medical attention if symptoms of serotonin syndrome develop.

• Overuse of drugs indicated for the management of acute migraine attacks may exacerbate headaches; importance of recording headache frequency and drug use to monitor effectiveness of treatment.

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Reload page with references included

Frequently asked questions

• How often can you take Maxalt?
• How long does it take for Maxalt to work?
• Does Maxalt have caffeine in it?

Medical Disclaimer