Rizatriptan

Rizatriptan binds with high affinity to human cloned 5-HT 1B/1D receptors. Rizatriptan presumably exerts its therapeutic effects in the treatment of migraine headache by binding to 5-HT 1B/1D receptors located on intracranial blood vessels and sensory nerves of the trigeminal system.

• & USAGE Ri zatriptan benzoate tablets are indicated for the acute treatment of migraine with or without aura in adults and in pediatric patients 6 to 17 years old. Limitations of Use • Rizatriptan benzoate tablets should only be used where a clear diagnosis of migraine has been established.ICD-10: G43.909

• Rizatriptan benzoate tablets are contraindicated in patients with: • Ischemic coronary artery disease (angina pectoris, history of myocardial infarction, or documented silent ischemia), or other significant underlying cardiovascular disease [see Warnings and Precautions ( 5.1 )]. • Coronary artery vasospasm including Prinzmetal's angina [see Warnings and Precautions ( 5.1 )].contraindicated

DOSAGE & ADMINISTRATION Adults: 5 mg or 10 mg single dose; separate repeat doses by at least two hours; maximum dose in a 24-hour period: 30 mg (2.1) Pediatric patients 6 to 17 years: 5 mg single dose in patients less than 40 kg (88 lb); 10 mg single dose in patients 40 kg (88 lb) or more ( 2.2 ) Adjust dose if co-administered with propranolol ( 2.4 ) 2.1 Dosing Information in Adults The recommended starting dose of rizatriptan benzoate tablets is either 5 mg or 10 mg for the acute treatment of migraines in adults. The 10-mg dose may provide a greater effect than the 5-mg dose, but may have a greater risk of adverse reactions [see Clinical Studies (14.1) ]. Redosing in Adults Although the effectiveness of a second dose or subsequent doses has not been established in placebo-controlled trials, if the migraine headache returns, a second dose may be administered 2 hours after the first dose. The maximum daily dose should not exceed 30 mg in any 24-hour period. The safety of treating, on average, more than four headaches in a 30-day period has not been established. 2.2 Dosing Information in Pediatric Patients (Age 6 to 17 Years) Dosing in pediatric patients is based on the patient's body weight. The recommended dose of rizatriptan benzoate tablets is 5-mg in patients weighing less than 40 kg (88 lb), and 10 mg in patients weighing 40 kg (88 lb) or more. The efficacy and safety of treatment with more than one dose of rizatriptan benzoate tablets within 24 hours in pediatric patients 6 to 17 years of age have not been established.

• Myocardial ischemia, myocardial infarction, and Prinzmetal's angina: Perform cardiac evaluation in patients with multiple cardiovascular risk factors ( 5.1 ) • Arrhythmias: Discontinue dosing if occurs ( 5.2 ) • Chest/throat/neck/jaw pain, tightness, pressure, or heaviness; Generally not associated with myocardial ischemia; Evaluate patients at high risk ( 5.3 ) • Cerebral hemorrhage, subarachnoid hemorrhage, and stroke: Discontinue dosing if occurs ( 5.4 ) • Gastrointestinal ischemic events, peripheral vasospastic reactions: Discontinue dosing if occurs ( 5.5 ) • Medication overuse headache: Detoxification may be necessary ( 5.6 ) • Serotonin syndrome: Discontinue dosing if occurs ( 5.7 ) 5.1 Myocardial Ischemia, Myocardial Infarction, and Prinzmetal's Angina Rizatriptan benzoate should not be given to patients with ischemic or vasospastic coronary artery disease. There have been rare reports of serious cardiac adverse reactions, including acute myocardial infarction, occurring within a few hours following administration of rizatriptan benzoate. Some of these reactions occurred in patients without known coronary artery disease (CAD). 5-HT 1 agonists, including rizatriptan benzoate may cause coronary artery vasospasm (Prinzmetal's Angina), even in patients without a history of CAD. Triptan-naïve patients who have multiple cardiovascular risk factors (e.g., increased age, diabetes, hypertension, smoking, obesity, strong family history of CAD) should have a cardiovascular evaluation prior to receiving rizatriptan benzoate.

The following adverse reactions are discussed in more detail in other sections of the labeling: • Myocardial Ischemia, Myocardial Infarction, and Prinzmetal's Angina [see Warnings and Precautions ( 5.1 )]. • Arrhythmias [see Warnings and Precautions ( 5.2 )]. • Chest, Throat, Neck and/or Jaw Pain/Tightness/Pressure [see Warnings and Precautions ( 5.3 )]. • Cerebrovascular Events [see Warnings and Precautions ( 5.4 )]. • Other Vasospasm Reactions [see Warnings and Precautions ( 5.5 )]. • Medication Overuse Headache [see Warnings and Precautions ( 5.6 )]. • Serotonin Syndrome [see Warnings and Precautions ( 5.7 )]. • Increase in Blood Pressure [see Warnings and Precautions ( 5.8 )]. The most common adverse reactions in adults were (incidence ≥ 5% and greater than placebo): asthenia/fatigue, somnolence, pain/pressure sensation and dizziness (6.1) To report SUSPECTED ADVERSE REACTIONS, contact Macleods Pharma USA, Inc. at 1-888-943-3210 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of another drug and may not reflect the rates observed in practice. Adults Incidence in Controlled Clinical Trials Adverse reactions to rizatriptan benzoate were assessed in controlled clinical trials that included over 3700 adult patients who received single or multiple doses of rizatriptan benzoate tablets.

• Pregnancy: Based on animal data, may cause fetal harm (8.1) 8.1 Pregnancy Risk Summary Available human data on the use of rizatriptan benzoate in pregnant women are not sufficient to draw conclusions about drug-associated risk for major birth defects and miscarriage. In animal studies, developmental toxicity was observed following oral administration of rizatriptan during pregnancy (decreased fetal body weight in rats) or throughout pregnancy and lactation (increased mortality, decreased body weight, and neurobehavioral impairment in rat offspring) at maternal plasma exposures greater than that expected at therapeutic doses in humans [see Animal Data]. In the U.S. general population, the estimated background risk of major birth defects and of miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. The reported rate of major birth defects among deliveries to women with migraine range from 2.2% to 2.9% and the reported rate of miscarriage was 17%, which are similar to rates reported in women without migraine. Clinical Considerations Disease-Associated Maternal and/or Embryo/Fetal Risk In women with migraine, there is an increased risk of adverse perinatal outcomes in the mother, including pre-eclampsia and gestational hypertension.

Metabolism

Absorption Rizatriptan is completely absorbed following oral administration. The mean oral absolute bioavailability of the rizatriptan benzoate tablet is about 45%, and mean peak plasma concentrations (C max ) are reached in approximately 1 to 1.5 hours (T max ).

No overdoses of rizatriptan benzoate were reported during clinical trials in adults. Some adult patients who received 40 mg of rizatriptan benzoate either a single dose or as two doses with a 2-hour interdose interval had dizziness and somnolence. In a clinical pharmacology study in which 12 adult subjects received rizatriptan benzoate, at total cumulative doses of 80 mg (given within four hours), two of the subjects experienced syncope, dizziness, bradycardia including third degree AV block, vomiting, and/or incontinence. In the long-term, open label study, involving 606 treated pediatric migraineurs 12 to 17 years of age (of which 432 were treated for at least 12 months), 151 patients (25%) took two 10-mg doses of rizatriptan benzoate orally disintegrating tablets within a 24-hour period. Adverse reactions for 3 of these patients included abdominal discomfort, fatigue, and dyspnea. In addition, based on the pharmacology of rizatriptan benzoate, hypertension or myocardial ischemia could occur after overdosage. Gastrointestinal decontamination, (i.e., gastric lavage followed by activated charcoal) should be considered in patients suspected of an overdose with rizatriptan benzoate.

• Jun 29, 1998NDANDA020864Organon Llc
• Jun 29, 1998NDANDA020865Organon
• Dec 31, 2012ANDAANDA077263Teva Pharms
• Dec 31, 2012ANDAANDA202047Creekwood Pharms
• Dec 31, 2012ANDAANDA202490Aurobindo Pharma Ltd
• Dec 31, 2012ANDAANDA201967Glenmark Pharms Ltd
• Apr 14, 2023NDANDA205394Gensco
• Jan 30, 2025NDANDA215431Axsome

1. 1Drug Ineffective2,10313%
2. 2Nausea1,69311%
3. 3Headache1,58210%
4. 4Migraine1,4699.3%
5. 5Off Label Use1,1647.4%
6. 6Fatigue1,0526.7%
7. 7Pain9075.7%
8. 8Vomiting7484.7%
9. 9Dizziness7054.5%
10. 10Diarrhoea6864.3%
11. 11Product Use In Unapproved Indication6814.3%
12. 12Dyspnoea6133.9%
13. 13Arthralgia5873.7%
14. 14Anxiety5693.6%
15. 15Hyperhidrosis5603.5%

The 10 most recently updated of 42 ClinicalTrials.gov registrations naming Rizatriptan as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Initiating Early Control of Migraine Pain and Associated Symptoms
  Completed · Phase 3 · Interventional · 302 enrolled · Axsome Therapeutics, Inc.
  NCT04163185updated 2026-01-28
• Open-Label Study of AXS-07 for the Acute Treatment of Migraine in Adults With a Prior Inadequate Response to an Oral CGRP Inhibitor (EMERGE)
  Completed · Phase 3 · Interventional · 100 enrolled · Axsome Therapeutics, Inc.
  NCT05550207updated 2025-12-02
• A Comparison of Nurtec ODT to Maxalt MLT-ODT in Adult ED Patients With Migraine Headache
  Recruiting · Phase 4 · Interventional · 80 enrolled · Antonios Likourezos
  NCT06473597updated 2025-10-01
• Quality Improvement and Practice Based Research in Neurology Using the EMR
  Enrolling by invitation · Phase 4 · Interventional · 3,300 enrolled · Endeavor Health
  NCT02670161updated 2025-08-24
• Efficacy and Safety of Rizatriptan-Naproxen (10/550 Mg) in the Acute Treatment of Migraine
  Completed · Phase 3 · Interventional · 2,068 enrolled · Eurofarma Laboratorios S.A.
  NCT04384367updated 2025-02-14
• Treatments of Migraine with Triptans in Individuals with Elevated Cardiovascular Risk and in Pregnant Women
  Completed · Observational · 68,419 enrolled · Mayo Clinic
  NCT05854992updated 2024-12-02
• Study to Test a Marketed Drug in the Treatment of Menstrual Migraine (0462-072)
  Completed · Phase 3 · Interventional · 393 enrolled · Organon and Co
  NCT00111722updated 2024-08-14
• Study to Test an Approved Product in the Early Treatment of Migraine (0462-066)
  Completed · Phase 3 · Interventional · 167 enrolled · Organon and Co
  NCT00095004updated 2024-08-14
• Study to Test a Marketed Drug in the Treatment of Menstrual Migraine (0462-071)
  Completed · Phase 3 · Interventional · 393 enrolled · Organon and Co
  NCT00111709updated 2024-08-14
• Study to Test an Approved Product in the Early Treatment of Migraine (0462-065)
  Completed · Phase 3 · Interventional · 529 enrolled · Organon and Co
  NCT00092963updated 2024-08-14

Ranked by 2D fingerprint (Tanimoto) similarity over PubChem structures. Structural proximity only — not a claim of therapeutic equivalence.

• SumatriptanSerotonin-1b and Serotonin-1d Receptor Agonist79%

Frequently asked questions

How does Rizatriptan work?

Rizatriptan binds with high affinity to human cloned 5-HT 1B/1D receptors. Rizatriptan presumably exerts its therapeutic effects in the treatment of migraine headache by binding to 5-HT 1B/1D receptors located on intracranial blood vessels and sensory nerves of the trigeminal system.

What is Rizatriptan used for?

According to FDA labeling, Rizatriptan carries indications including: & USAGE Ri zatriptan benzoate tablets are indicated for the acute treatment of migraine with or without aura in adults and in pediatric patients 6 to 17 years old. Limitations of Use • Rizatriptan benzoate tablets should only be used where a clear diagnosis of migraine has been established.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Rizatriptan?

Rizatriptan is classified as Selective serotonin (5HT1) agonists, Serotonin-1b and Serotonin-1d Receptor Agonist, Monoamine Oxidase Inhibitors, Serotonin 1b Receptor Agonists, Serotonin 1d Receptor Agonists, Serotonin Agonists, Cerebral Arterial Vasoconstriction, Increased Central Nervous System Serotonin Activity.

What are the brand names for Rizatriptan?

Rizatriptan is marketed under brand names including Maxalt, Rizafilm, Symbravo.

What are the contraindications for Rizatriptan?

Rizatriptan labeling lists contraindications including: Rizatriptan benzoate tablets are contraindicated in patients with: • Ischemic coronary artery disease (angina pectoris, history of myocardial infarction, or documented silent ischemia), or other significant underlying cardiovascular disease [see Warnings and Precautions ( 5.1 )]. • Coronary artery vasospasm including Prinzmetal's angina [see Warnings and Precautions ( 5.1 )].. Always consult the full prescribing information and a clinician.