Zolmitriptan

Zolmitriptan is a second-generation triptan for the treatment of acute migraine attacks. It is available in different dosage forms: as a regular tablet, orally disintegrating tablet, and nasal spray.

The nasal spray is particularly advantageous in cases of severe nausea or vomiting, since it is not absorbed through the stomach. The orally disintegrating tablet offers flexibility when you are on the go.

The well-known brand name is Ascotop®.

Zolmitriptan acts as a selective serotonin receptor agonist:

Mechanism of action:

• Binds to 5-HT1B/1D receptors
• Constricts dilated cranial blood vessels
• Inhibits the release of CGRP and other neuropeptides
• Blocks trigeminal pain transmission

Special features:

• Good CNS penetration
• Nasal spray acts partly directly via the nasal mucosa
• Active metabolite prolongs the effect

Onset of action:

• Tablets: 45-60 minutes
• Orally disintegrating tablet: 45 minutes
• Nasal spray: 15-30 minutes

Zolmitriptan is suitable for:

• Adults with acute migraine attacks
• Patients with pronounced nausea (nasal spray)
• When other triptans are not effective enough

Nasal spray particularly suitable for:

• Severe nausea and vomiting
• A desire for a fast onset of action
• When tablets are not tolerated

Not suitable for:

• Cardiovascular diseases
• Moderate or severe high blood pressure as well as inadequately controlled mild high blood pressure
• Wolff-Parkinson-White syndrome
• Hemiplegic or basilar migraine

Tablets:

• 2.5 mg
• 5 mg

Orally disintegrating tablets:

• 2.5 mg
• 5 mg

Nasal spray:

• 5 mg per spray

Recommended dosage:

• Standard dose: 2.5 mg
• If the effect is insufficient: 5 mg
• Can be repeated after 2 hours
• Maximum: 10 mg in 24 hours

Tablets:

• Swallow with water
• Take at the onset of headache

Orally disintegrating tablets:

• Place on the tongue and let dissolve
• Swallow with saliva
• No water needed

Nasal spray:

• Tilt your head slightly forward
• Spray into one nostril
• Do not inhale while spraying
• Keep your head lowered for a few seconds

General notes:

• Take at the first sign of headache
• Not during the aura
• Second dose only after 2 hours

Zolmitriptan must not be taken in cases of:

• Coronary heart disease
• History of heart attack, stroke, TIA
• Wolff-Parkinson-White syndrome or other conduction disorders
• Moderate or severe high blood pressure as well as inadequately controlled mild high blood pressure
• Severe hepatic insufficiency
• Hemiplegic or basilar migraine
• Concomitant use of ergotamine

Caution in cases of:

• Moderate hepatic impairment (lower dose)
• Cardiovascular risk factors
• SSRI/SNRI therapy
• MAO-A inhibitor therapy (max. 5 mg zolmitriptan in 24 hours)

Common (1-10%):

• Taste disturbances (especially with the nasal spray)
• Paresthesia (tingling)
• Dizziness
• Drowsiness
• Headache
• Dry mouth
• Nausea

Triptan-specific sensations:

• Feeling of warmth
• Feeling of pressure/tightness in the chest and throat
• Heaviness in the limbs
• Usually harmless!

Additionally with the nasal spray:

• Unpleasant taste
• Nasal irritation
• Nosebleeds (rare)

Rare:

• Allergic reactions
• Coronary spasms
• Serotonin syndrome

Do not combine with:

• Ergotamine (24 hours apart!)
• Other triptans on the same day
• Moclobemide at a dose higher than 150 mg twice daily

Dose reduction with:

• MAO-A inhibitors such as moclobemide (max. 5 mg/24h)
• Cimetidine use (max. 5 mg/24h)
• Fluvoxamine (max. 5 mg/24h)

Caution with:

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