Rizatriptan

What is rizatriptan?

Rizatriptan is part of a class of medications called ‘triptans’, which belong to a group of drugs called serotonin agonists. Triptans were specifically developed as an acute migraine treatment, targeting the underlying processes that cause symptoms during a migraine attack.

Migraine is a complex brain disorder that causes recurrent attacks involving head pain, nausea, and/or sensitivity to light and sound. Attacks can last between 4–72 hours when untreated, and are often disabling.

Rizatriptan can be taken to reduce symptoms when you start to experience a migraine attack. Your doctor may recommend trying rizatriptan if you do not respond to over-the-counter medications.

Rizatriptan at a glance

Cost and access in Australia

Rizatriptan is available in Australia for people who are diagnosed with migraine. It is available over the counter and on prescription.

Since February 2021, lower strengths and quantities of rizatriptan have been permitted to be supplied as a Schedule 3 (pharmacist-only) medication. Patients are now able to purchase 2 x 5 mg wafers without a prescription, after speaking to a pharmacist. This is helpful in a number of situations:

• If over-the-counter analgesics alone are inadequate in treating your migraine symptoms and;
  • While travelling;
  • If you run out of medication before your next appointment;
  • If you experience migraine very rarely;
  • Or any other time that you don’t have your medication with you / aren’t able to access a prescription.
    

These smaller packets are not covered under the PBS and are approximately $10–$15 depending on the pharmacy.

Multiple strengths and greater quantities of rizatriptan tablets and wafers are available on prescription only, which you will need to get from your doctor. These doses and quantities are covered under the PBS, and the cost depends on various factors e.g. patient copayment.

Learn more about triptans without a prescription in this recorded webinar from Professor and pharmacist Dr. Jacinta Johnson-  Triptans Without A Prescription.

How rizatriptan works

Rizatriptan belongs to a class of drugs called ‘triptans’, which are acute medications developed specifically to treat migraine pain. However, they aren’t ‘painkillers’ in the same way as paracetamol, ibuprofen, or other non-steroidal anti-inflammatory drugs (NSAIDs).

Triptans target the underlying processes that cause migraine symptoms. In the 1990s, researchers discovered that serotonin played a pivotal role in migraine attacks. This led to the development of triptans, which selectively activate the 5-HT1B and 5-HT1D receptors. This stops two of the processes that occur during a migraine attack:

• Dilation of blood vessels: Dilated blood vessels contribute towards the pain of a migraine attack. When the 5-HT1B receptor is activated, it helps to constrict (narrow) your blood vessels.
• Activation of trigeminovascular system: The trigeminal nerves usually release proinflammatory proteins during a migraine attack, which causes migraine pain. Activation of the 5-HT1D receptor stops these proinflammatory proteins from being released.

Rizatriptan is only effective for migraine attacks and can’t be used to treat other conditions or other headache disorders. Triptans also can’t be used to prevent migraine attacks from occurring.

Dosage and administration

Dosage

Rizatriptan is available as tablets and orally disintegrating wafers in 5 mg and 10 mg strengths. The recommended dosing instructions are as follows:

• Take 1 tablet or wafer of rizatriptan 5 mg or 10 mg.
• If the migraine returns after initial relief, a second dose may be taken at least 2 hours after the first dose.
• Do not take more than 30 mg in a 24-hour period.^[1]

Administration

It is generally recommended to take rizatriptan as soon as possible after the start of the migraine attack. If you experience migraine aura, you should wait until the headache phase begins, as it may be ineffective if taken during the aura phase. However, if you aren’t able to take it at the beginning of your attack, it will still provide some relief if taken later.

Other important guidelines for when and how to take rizatriptan include:

• Swallow the tablets whole with a full glass of water, either with or without food.
• Orally disintegrating wafers should be placed on the tongue and allowed to dissolve.
• Do not take a second dose of rizatriptan within 2 hours of taking the first dose.
• If rizatriptan does not relieve your migraine, do not take a second dose for the same attack.
• You may take something else for the pain, but do not take medicine containing ergotamine, dihydroergotamine, or methysergide for at least 24 hours before or after taking rizatriptan.

Rizatriptan is not available in other formulations such as nasal spray or injection. If you experience severe nausea due to the migraine attack and find it difficult to take tablets or wafers, you should speak to your doctor about other medication options or combining rizatriptan with an anti-nausea medication.

How effective is rizatriptan?

Rizatriptan has demonstrated consistent and significant clinical efficacy for migraine treatment in multiple clinical trials. It has been tested in different dosages against placebo and other medications.

There are few studies that directly compare different types of acute medications for migraine, and there are important reasons that you should not try to compare response rates between clinical trials directly. If you are reading several articles on different ‘triptan’ medications, try and avoid the temptation of looking just for the medication with the highest number, and speak with your doctor about different options!

Systematic reviews are one way of trying to indirectly compare different treatments. One such study evaluated the efficacy of different types and formulations of triptans. The table below shows the proportion of patients achieving specific pain outcomes for rizatriptan compared to placebo, paracetamol, and non-steroidal anti-inflammatories (NSAIDs).

Source: C Cameron et al, 2015, Triptans in the Acute Treatment of Migraine: A Systematic Review and Network Meta-Analysis. DOI: 10.1111/head.12601

If you don’t find rizatriptan effective, try not to be discouraged. Most people with migraine will respond to at least one type of triptan medication, with trials suggesting that it is worth trying other types if the first one doesn’t work. Even though all triptans work broadly in the same way, they each have some inherent differences and people may also respond differently to the same triptan. These factors will play a role in which triptan works for you.

Side effects

Like most medications, rizatriptan may cause side effects. In most cases, they will be minor and temporary. However, more serious complications or reactions are possible that require immediate medical attention. Side effects can also vary depending on your age, other health conditions you have, and other medications you take.

Some of the side effects are summarised below. However, other side effects not listed here may occur in some people. You should always tell your doctor or pharmacist if you notice anything that is making you feel unwell.

Warnings & risks

Medication overuse headache

Rizatriptan is not addictive, but it is associated with medication overuse headache (MOH), a condition that can result from taking acute migraine medications too frequently. MOH can increase the number of headache days and reduce the effectiveness of both acute and preventive migraine treatments.

To reduce the risk of MOH, it is generally recommended that triptans such as rizatriptan are not used on more than 10 days per month. Your doctor or pharmacist can help you monitor your usage and determine whether preventive treatments may be appropriate.

Health conditions that are not appropriate for rizatriptan

All triptans, including rizatriptan, can cause narrowing (constriction) of blood vessels. For this reason, they may not be appropriate for people with existing or suspected cardiovascular disease or risk factors. You should speak with your doctor if you have any of the following conditions or risk factors:

• History of heart attack or stroke
• Uncontrolled high blood pressure
• Peripheral vascular disease
• Prinzmetal’s angina or other forms of angina
• Severe liver or kidney problems
• High cholesterol
• Diabetes
• Strong family history of heart disease
• Smoking
• Postmenopausal (for women) or over 40 years old (for men)

Rizatriptan is also not suitable for people who are allergic to rizatriptan or any of the ingredients in its formulations. Some products may contain lactose, which may be unsuitable for people with lactose intolerance.

If you experience allergic symptoms such as rash, itching, swelling, or difficulty breathing, discontinue use immediately and seek urgent medical attention.

Interactions 

Certain medications can interact with rizatriptan, affecting how well it works or increasing the risk of side effects. You should always inform your doctor or pharmacist of all medications you are taking, including over-the-counter medicines, vitamins, and herbal supplements.

Speak to your doctor if you are also taking or have recently taken:

Storage

Rizatriptan tablets and wafers should be stored in a cool, dry place below 30°C and out of direct sunlight. Keep them in their original packaging until ready to use, and ensure they are kept out of reach of children.

Further information & resources

If you would like to learn more about migraine or different treatment options, you may find the following articles helpful.

• Migraine – a comprehensive article about migraine symptoms, causes, treatments, and more.
• Acute Migraine Medication – article summarising other types of acute migraine medication, including a general overview of other triptans.
• Treatment directory – overview article including a brief explanation of the medications available to treat migraine and different classes of treatment.
• Sumatriptan – medication review for sumatriptan, another medication in the same class as rizatriptan.
• Eletriptan – medication review for eletriptan, another medication in the same class as rizatriptan.
• Zolmitriptan – medication review for zolmitriptan, another medication in the same class as rizatriptan.

References

1. Goadsby PJ et al, 2017, Pathophysiology of Migraine: A Disorder of Sensory Processing, Physiological Reviews. DOI: 10.1152/physrev.00034.2016
2. Therapeutic Goods Administration, 2023, Product Information (Summary) [for each product containing rizatriptan benzoate on the ARTG]. Retrieved from: https://www.ebs.tga.gov.au
3. C Cameron et al, 2015, Triptans in the Acute Treatment of Migraine: A Systematic Review and Network Meta-Analysis. DOI: 10.1111/head.12601
4. B Gilmore & M Michael, 2011, Treatment of Acute Migraine Headache, American Family Physician, 83(3):271–280. PMID: 21302868
5. Organon, 2023, Maxalt Consumer Medicine Information (CMI). Retrieved from: https://www.medsinfo.com.au/
6. Australian Medicines Handbook, 2024, Rizatriptan. Retrieved from: https://amhonline.amh.net.au/