Migraines are likely due to local cranial vasodilatation and/or to the release of sensory neuropeptides through nerve endings in the trigeminal system. The therapeutic activity of Zolmitriptan for the treatment of migraine headache is thought to be due to the agonist effects at the 5-HT_1B/1D receptors on intracranial blood vessels and sensory nerves of the trigeminal system which results in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release.

Zolmitriptan is indicated for the acute treatment of migraines with or without aura in adults.

Tablet: The recommended starting dose of Zolmitriptan is 2.5 mg tablet. Maximum recommended single dose is 5 mg. If the migraine has not resolved by 2 hours after taking Zolmitriptan, or returns after a transient improvement, a second dose may be administered at least 2 hours after the first dose. The maximum daily dose is 10 mg in any 24-hours period.

Nasal Spray: Administer one dose of Zolmitriptan Nasal Spray 5 mg for the treatment of acute migraine. If the headache returns the dose may be repeated after 2 hours. The maximum daily dose should not exceed 10 mg in any 24-hour period. In controlled clinical trials, single doses of 5 mg zolmitriptan nasal spray were administered into one nostril and were effective for the treatment of acute migraines in adults. Individuals may vary in response to Zolmitriptan Nasal Spray. The pharmacokinetics of a 5 mg nasal spray dose is similar to the 5 mg oral formulations. Doses lower than 5 mg can only be achieved through the use of an oral formulation. The choice of dose, and route of administration should therefore be made on an individual basis. The effectiveness of a second dose has not been established in placebo-controlled trials. The safety of treating an average of more than four headaches in a 30 day period has not been established.

Contraindicated in patients with ischemic coronary artery disease, history of stroke, concurrent or recent use of a monoamine oxidase inhibitor and known hypersensitivity to Zolmitriptan.

Most common adverse reactions were neck/throat/jaw pain or pressure, dizziness, paresthesia, asthenia, somnolence, warm/cold sensation, nausea, heaviness sensation, and dry mouth.

There have been rare reports of serious cardiac adverse reactions, including acute myocardial infarction, occurring within a few hours following administration. Sensations of tightness, pain, and pressure may occur in the chest, throat, neck, and jaw after treatment with Zolmitriptan.

Use in Special Populations

Pediatric Use: Not recommended for use in patients under 18 years of age.

Pregnancy & Lactation

Pregnancy Category C. Zolmitriptan should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is not known whether Zolmitriptan is excreted in human milk. A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.