In short
Zolmitriptan is a serotonin (5-HT) 1B/1D receptor agonist, a type of medicine known as a triptan, used for the acute treatment of migraine with or without aura in adults. One completed Phase 1 trial in the EU Clinical Trials Information System (CTIS) compared an orally disintegrating tablet and a nasal spray in 8 healthy volunteers to understand how the body processes the drug.
Zolmitriptan is a medicine belonging to the triptan class, which acts on serotonin (5-HT) 1B/1D receptors. It is authorised for the acute treatment of migraine with or without aura in adults. One completed Phase 1 trial, registered in the EU Clinical Trials Information System (CTIS) under number 2023-504492-24-00, investigated two formulations of zolmitriptan in 8 healthy volunteers.
Key points
- Zolmitriptan is a triptan medicine approved for the acute treatment of migraine with or without aura in adults.
- The EU trial was a Phase 1 study completed with 8 healthy volunteers.
- It compared an orally disintegrating tablet (5 mg) with a nasal spray (5 mg).
- Researchers measured pharmacokinetic parameters such as Cmax, Tmax, and AUC over 24 hours.
- Effects on heart rate and blood pressure were also assessed as pharmacodynamic endpoints.
What is zolmitriptan?
Zolmitriptan is a serotonin (5-HT) 1B/1D receptor agonist, a class of medicines commonly called triptans. The prescribing information states that zolmitriptan orally disintegrating tablets received initial U.S. approval in 1997 and are indicated for the acute treatment of migraine with or without aura in adults. The medicine is not indicated for the preventive treatment of migraine or for the treatment of cluster headache. In the EU trial record, zolmitriptan appears as the active substance in two marketed products: Zolmitriptán Normon 5 mg comprimidos bucodispersables and Zomig 5 mg solución para pulverización nasal.
How does zolmitriptan work?
Zolmitriptan works by stimulating serotonin (5-HT) 1B/1D receptors. The prescribing information identifies this mechanism as the basis for its use in migraine. The trial record adds that the study measured pharmacodynamic effects of zolmitriptan on heart rate and blood pressure, which are physiological responses relevant to how the medicine acts in the body.
Which conditions is zolmitriptan used or studied for?
- Migraine with or without aura in adults — zolmitriptan is authorised for the acute treatment of migraine attacks in adults.
- Healthy volunteers — the EU trial enrolled healthy people, not patients, to study how the body processes the medicine.
How is zolmitriptan given?
The EU trial compared two pharmaceutical forms: an orally disintegrating tablet taken by mouth and a nasal spray. The prescribing information describes zolmitriptan orally disintegrating tablets for oral use, available in 2.5 mg and 5 mg strengths, with a recommended starting dose of 1.25 mg or 2.5 mg and a maximum single dose of 5 mg. A dose may be repeated after 2 hours if needed, but no more than 10 mg should be taken in any 24-hour period.
What do the clinical trials show?
One Phase 1 trial is registered for zolmitriptan in the CTIS dataset, with status completed and an enrollment of 8 healthy volunteers. The study was interventional and investigated the pharmacokinetics of oral and intranasal zolmitriptan formulations. Pharmacokinetics describes how a medicine is absorbed, distributed, metabolised, and eliminated by the body.
What are the trials measuring?
The trial measured pharmacokinetic parameters in blood samples collected at multiple time points over 24 hours after dosing. These included the maximum concentration reached in the blood (Cmax), the time to reach that maximum (Tmax), the area under the concentration-time curve (AUC), which reflects total drug exposure, and the terminal elimination half-life (t1/2), which indicates how long the medicine stays in the body. The trial also assessed the effects of zolmitriptan on heart rate and blood pressure as pharmacodynamic endpoints.
Who can take part in these trials?
The completed Phase 1 trial enrolled healthy volunteers, meaning people without the condition the medicine treats. The trial record does not list additional eligibility criteria in the data provided. The prescribing information notes that zolmitriptan should not be used by people with a history of coronary artery disease, stroke, transient ischemic attack, peripheral vascular disease, ischemic bowel disease, or uncontrolled hypertension.
What side effects are known?
The prescribing information lists contraindications, which are conditions that make use of the medicine unsafe, including a history of coronary artery disease or coronary vasospasm, symptomatic Wolff-Parkinson-White syndrome, history of stroke or transient ischemic attack, hemiplegic or basilar migraine, peripheral vascular disease, ischemic bowel disease, and uncontrolled hypertension. The source provided does not include a full list of adverse reactions, so side effects are not described here.