What is Rizatriptan (Maxalt), a selective 5-hydroxytryptamine (5-HT)1 receptor agonist?

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From the Guidelines

Rizatriptan is a recommended medication for the treatment of migraine headaches with or without aura in adults, with a standard dose of 5-10 mg taken orally at the onset of migraine symptoms, and a maximum of 30 mg in a 24-hour period 1.

Key Points

  • Rizatriptan belongs to the triptan class of drugs and works by narrowing blood vessels in the brain and blocking pain signals.
  • The medication is available as regular tablets or as orally disintegrating tablets (Maxalt-MLT) that dissolve on the tongue without water.
  • Patients should take only one dose for each migraine attack, and if symptoms return, a second dose may be taken after 2 hours.
  • Rizatriptan should not be used for prevention of migraines or for other types of headaches.
  • Common side effects include dizziness, drowsiness, fatigue, and dry mouth.
  • The medication should be avoided by patients with certain cardiovascular conditions, uncontrolled hypertension, or those taking monoamine oxidase inhibitors (MAOIs) 1.

Important Considerations

  • Rizatriptan is contraindicated in patients with risk for heart disease, basilar or hemiplegic migraine, or uncontrolled hypertension.
  • The medication works by stimulating serotonin receptors, which reduces inflammation and constricts blood vessels that become abnormally dilated during migraine attacks, thereby relieving pain and associated symptoms.
  • Patients should be advised to consult their healthcare provider before taking rizatriptan, especially if they have any underlying medical conditions or are taking other medications 1.

From the FDA Drug Label

Rizatriptan binds with high affinity to human cloned 5-HT1B/1D receptors. Rizatriptan presumably exerts its therapeutic effects in the treatment of migraine headache by binding to 5-HT1B/1D receptors located on intracranial blood vessels and sensory nerves of the trigeminal system. The mechanism of action of Rizatriptan is through binding to 5-HT1B/1D receptors.

  • The therapeutic effects are presumed to be due to this binding, which affects intracranial blood vessels and sensory nerves of the trigeminal system. The question about Rizatriptan does not specify what information is being asked, therefore, no conclusion can be drawn. 2

From the Research

Efficacy of Rizatriptan

  • Rizatriptan is effective in relieving the symptoms of migraine, with the 10 mg dose providing faster pain relief than other medications such as sumatriptan, naratriptan, and ergotamine/caffeine 3.
  • Clinical trials have shown that rizatriptan is at least as effective or superior to other oral migraine-specific agents in the acute treatment of migraine 4.
  • Rizatriptan has been shown to be effective in treating acute migraine, with a dose-related increase in efficacy 5.

Tolerability and Safety

  • Rizatriptan is generally well tolerated, with adverse events usually being mild and transient 6.
  • The most common adverse events associated with rizatriptan are asthenia/fatigue, dizziness, somnolence, and nausea 6.
  • Rizatriptan has a favorable tolerability profile, with patients reporting greater satisfaction and a preference for rizatriptan over other migraine-specific agents 4.

Timing of Medication Use

  • Taking rizatriptan at the onset of headache is associated with more rapid relief of headache and reversal of functional disability 7.
  • Rizatriptan is equally effective in relieving acute migraine headache by 2 hours postdose, whether taken at headache onset or later in the attack 7.

Cost-Effectiveness

  • Rizatriptan is cost-effective compared to usual care, with an incremental cost per quality-adjusted life-year (QALY) gained of 31,845 Can dollars (2002 values) 3.
  • Rizatriptan is more cost-effective than ergotamine/caffeine, simple analgesics, naratriptan, zolmitriptan, and sumatriptan 3.

References

Guideline

Guideline Directed Topic Overview

Dr.Oracle Medical Advisory Board & Editors, 2025

Research

Rizatriptan in the treatment of migraine.

Neuropsychiatric disease and treatment, 2006

Research

Rizatriptan for acute migraine.

The Cochrane database of systematic reviews, 2001

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Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

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