Rizatriptan

Rizatriptan is a modern triptan for the treatment of acute migraine attacks. It is characterized by a rapid onset of action and is available in a particularly convenient form as an orally disintegrating tablet that can be taken without water.

The rapid onset of action (within 30 minutes) makes rizatriptan a good choice when quick relief is needed. The orally disintegrating tablet is also advantageous in case of nausea or when no water is at hand.

The well-known brand name is Maxalt®.

Rizatriptan works through the same mechanism as other triptans:

Mechanism of action:

• Activation of 5-HT1B/1D serotonin receptors
• Constriction of dilated cranial blood vessels
• Inhibition of the release of vasoactive peptides (CGRP)
• Blockade of trigeminal pain transmission

Special features:

• Rapid onset of action: 30 minutes
• High lipophilicity – good CNS penetration
• Orally disintegrating tablet dissolves within seconds

Duration of action: The plasma half-life of rizatriptan averages 2 to 3 hours. If the headache returns within 24 hours after the first response, a second dose can be taken, at the earliest 2 hours after the first.

Rizatriptan is suitable for:

• Adults with acute migraine attacks
• Patients who need a rapid effect
• In cases of nausea/vomiting (orally disintegrating tablet)
• When no water is available

Particularly advantageous:

• With severe migraine-related nausea
• On the go
• For early intervention in the attack

Not suitable in cases of:

• Cardiovascular diseases
• Uncontrolled high blood pressure
• Hemiplegic or basilar migraine

Tablets:

• 5 mg
• 10 mg (standard dose)

Orally disintegrating tablets (Maxalt lingua):

• 5 mg
• 10 mg

Recommended dosage:

• Adults: 10 mg at the onset of an attack
• If needed, a second dose after 2 hours
• Maximum: 20 mg in 24 hours

When taking propranolol:

• Only 5 mg rizatriptan (half dose!)
• No more than 2 doses of 5 mg each within 24 hours, at least 2 hours apart
• At least 2 hours between taking rizatriptan and taking propranolol

Regular tablets:

• Swallow with water
• At the onset of headache, not during the aura

Orally disintegrating tablets:

• Place on the tongue
• Dissolves within seconds
• Swallow with saliva
• No water needed

Timing:

• Take as soon as the headache starts
• Taking it early is more effective
• Not during the aura phase

If the first dose does not work: No second dose for the same attack. Try again with the next attack.

Rizatriptan must not be taken in cases of:

• Coronary heart disease
• History of heart attack, stroke, TIA
• Severe or uncontrolled hypertension
• Peripheral arterial occlusive disease
• Severe hepatic or renal insufficiency
• Hemiplegic or basilar migraine
• MAO inhibitor therapy (or < 2 weeks afterward)
• Concomitant use of ergotamine

Caution in cases of:

• Propranolol therapy (half dose!)
• Cardiovascular risk factors
• Mild/moderate hepatic/renal insufficiency

Common (1-10%):

• Dizziness
• Lightheadedness
• Fatigue
• Asthenia (weakness)
• Nausea
• Palpitations
• Dry mouth
• Diarrhea

Triptan-specific sensations:

• Tingling, numbness
• Feeling of warmth or cold
• Feeling of pressure or tightness (chest, throat)
• Heaviness in the limbs

Rare:

• Allergic reactions
• Coronary spasms
• Serotonin syndrome

Note on orally disintegrating tablets: May contain aspartame – caution in phenylketonuria.

Important – propranolol:

• Rizatriptan levels rise by 70 to 80 % on average
• Only 5 mg rizatriptan when propranolol is taken at the same time!

Do not combine with:

• Ergotamine (24 hours apart)
• Other triptans on the same day
• MAO inhibitors

Caution with:

• SSRIs/SNRIs (risk of serotonin syndrome)
• St. John's wort
• Lithium