Rizatriptan with Propranolol Interaction Details

Brand Names Associated with Rizatriptan

Brand Names Associated with Propranolol

Medical Content Editor Dr. Brian Staiger, PharmD
Last updated Nov 19, 2023

Interaction Effect

Increased rizatriptan exposure

Interaction Summary

Concomitant use of propranolol and rizatriptan has resulted in increased rizatriptan AUC and Cmax values. The mechanism of action for this interaction is unknown; however, it is postulated that inhibition of monamine oxidase A by propranolol increases concentrations of rizatriptan. Administration of propranolol with rizatriptan may also lead to increased propranolol blood levels and/or toxicity . In adults treated with propranolol, rizatriptan 5 mg (maximum of 3 doses in a 24-hour period) is recommended. In pediatric patients treated with propranolol, only a single 5 mg dose of rizatriptan is recommended (maximum dose 5 mg within 24 hours). Rizatriptan should not be administered in propranolol-treated pediatric patients weighing less than 40 kg . Also, since propranolol increases the exposure of rizatriptan and dosage adjustment is not possible with rizatriptan oral film, concomitant use of rizatriptan oral film with propranolol is contraindicated .

Severity

Contraindicated

Onset

Rapid

Evidence

Established

How To Manage Interaction

Concomitant use of propranolol and rizatriptan has resulted in increased rizatriptan plasma concentrations. Therefore, in adults treated with propranolol, rizatriptan 5 mg (maximum of 3 doses in a 24-hour period) is recommended. In pediatric patients treated with propranolol, a single 5 mg dose of rizatriptan is recommended for patients weighing 40 kg or more (maximum of 5 mg within 24 hours). Do not administer rizatriptan in propranolol-treated pediatric patients weighing less than 40 kg. Also, since propranolol increases the exposure of rizatriptan and dosage adjustment is not possible with rizatriptan oral film, concomitant use of rizatriptan oral film with propranolol is contraindicated .

Mechanism Of Interaction

Unknown

Literature Reports

A) Propranolol increased plasma concentrations of rizatriptan in 4 double-blind, placebo-controlled, randomized, crossover studies including 51 subjects. Propranolol 60 and 120 mg twice daily, nadolol 80 mg twice daily, metoprolol 100 mg twice daily, or placebo were administered with rizatriptan. Rizatriptan AUC and Cmax were increased 67% and 75%, respectively, with concomitant propranolol therapy. There was no significant change in rizatriptan pharmacokinetics occurring with a reduction in the dose of propranolol to 60 mg twice daily. Rizatriptan pharmacokinetics were also not significantly changed when propranolol was given 1 or 2 hours before or after rizatriptan administration. Administration of rizatriptan with nadolol 80 mg twice daily or metoprolol 100 mg twice daily for 7 days did not significantly change the pharmacokinetics of rizatriptan. It is postulated that inhibition of monoamine oxidase A by propranolol increases concentrations of rizatriptan .

B) Rizatriptan AUC increased by 70% when propranolol 240 mg/day was coadministered with a single dose of rizatriptan 10 mg in a study of 11 healthy volunteers. One subject experienced a four-fold increase in the rizatriptan AUC. The AUC of the active N-monodesmethyl metabolite of rizatriptan was not altered .

Rizatriptan Overview

• Rizatriptan is used to treat the symptoms of migraine headaches (severe, throbbing headaches that sometimes are accompanied by nausea and sensitivity to sound and light). Rizatriptan is in a class of medications called selective serotonin receptor agonists. It works by narrowing blood vessels in the brain, stopping pain signals from being sent to the brain, and blocking the release of certain natural substances that cause pain, nausea, and other symptoms of migraine. Rizatriptan does not prevent migraine attacks or reduce the number of headaches you have.

Propranolol Overview

• Propranolol is used to treat high blood pressure, irregular heart rhythms, pheochromocytoma (tumor on a small gland near the kidneys), certain types of tremor, and hypertrophic subaortic stenosis (a heart muscle disease). It is also used to prevent angina (chest pain), migraine headaches, and to improve survival after a heart attack. Propranolol is in a class of medications called beta blockers. It works by relaxing blood vessels and slowing heart rate to improve blood flow and decrease blood pressure.

• High blood pressure is a common condition and when not treated, can cause damage to the brain, heart, blood vessels, kidneys and other parts of the body. Damage to these organs may cause heart disease, a heart attack, heart failure, stroke, kidney failure, loss of vision, and other problems. In addition to taking medication, making lifestyle changes will also help to control your blood pressure. These changes include eating a diet that is low in fat and salt, maintaining a healthy weight, exercising at least 30 minutes most days, not smoking, and using alcohol in moderation.

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Definitions

Severity Categories

Contraindicated

These drugs, generally, should not be used together simultaneously due to the high risk of severe adverse effects. Combining these medications can lead to dangerous health outcomes and should be strictly avoided unless otherwise instructed by your provider.

Major

This interaction could result in very serious and potentially life-threatening consequences. If you are taking this drug combination, it is very important to be under close medical supervision to minimize severe side effects and ensure your safety. It may be necessary to change a medication or dosage to prevent harm.

Moderate

This interaction has the potential to worsen your medical condition or alter the effectiveness of your treatment. It's important that you are monitored closely and you potentially may need to make adjustments in your treatment plan or drug dosage to maintain optimal health.

Minor

While this interaction is unlikely to cause significant problems, it could intensify side effects or reduce the effectiveness of one or both medications. Monitoring for changes in symptoms and your condition is recommended, and adjustments may be made if needed to manage any increased or more pronounced side effects.

Onset

Rapid: Onset of drug interaction typically occurs within 24 hours of co-administration.

Delayed: Onset of drug interaction typically occurs more than 24 hours after co-administration.

Evidence

Level of documentation of the interaction.

Established: The interaction is documented and substantiated in peer-reviewed medical literature.

Theoretical: This interaction is not fully supported by current medical evidence or well-documented sources, but it is based on known drug mechanisms, drug effects, and other relevant information.

How To Manage The Interaction

Provides a detailed discussion on how patients and clinicians can approach the identified drug interaction as well as offers guidance on what to expect and strategies to potentially mitigate the effects of the interaction. This may include recommendations on adjusting medication dosages, altering the timing of drug administration, or closely monitoring for specific symptoms.

It's important to note that all medical situations are unique, and management approaches should be tailored to individual circumstances. Patients should always consult their healthcare provider for personalized advice and guidance on managing drug interactions effectively.

Mechanism Of Interaction

The theorized or clinically determined reason (i.e., mechanism) why the drug-drug interaction occurs.

Disclaimer: The information provided on this page is for informational purposes only and should not be considered medical advice. Always consult with a qualified healthcare professional regarding your specific circumstances and medical conditions.

Where Does Our Information Come From?

Information for our drug interactions is compiled from several drug compendia, including:

• Gold Standard Drug Database
• Micromedex
• Lexicomp
• DrugBank

The prescribing information for each drug, as published on DailyMED, is also used. 

Individual drug-drug interaction detail pages contain references specific to that interaction. You can click on the reference number within brackets '[]' to see what reference was utilized.

The information posted is fact-checked by HelloPharmacist clinicians and reviewed quarterly.