Last reviewed 2026-04-20 · How we verify

Zomig (ZOLMITRIPTAN)

Zolmitriptan works by binding to serotonin receptors in the brain to constrict blood vessels and block pain pathways.

Zomig (Zolmitriptan) is a serotonin-1b and serotonin-1d receptor agonist, a small molecule modality developed by IPR and currently owned by Astrazeneca. It targets the 5-hydroxytryptamine receptor 1D to treat migraine. Approved by the FDA in 1997, it is now off-patent with 18 generic manufacturers. Zomig is effective in relieving migraine symptoms, but its use should be cautious due to potential cardiovascular side effects. Its half-life is approximately 3.6 hours with a bioavailability of 45%.

At a glance

Mechanism of action

Mechanism of Action:. Zolmitriptan binds with high affinity to human recombinant 5-HT1D and 5-HT1B receptors. Zolmitriptan exhibits modest affinity for 5-HT1A receptors, but has no significant affinity (as measured by radioligand binding assays) or pharmacological activity at 5-HT2, 5-HT3, 5-HT4, alpha1-, alpha2-, or beta1- adrenergic; H1, H2, histaminic; muscarinic; dopamine1, or dopamine2 receptors. The N-desmethyl metabolite also has high affinity for 5-HT1B/1D and modest affinity for 5-HT1A receptors. Current theories proposed to explain the etiology of migraine headache suggest that symptoms are due to local cranial vasodilatation and/or to the release of sensory neuropeptides (vasoactive intestinal peptide, substance and calcitonin gene-related peptide) through nerve endings in the trigeminal system. The therapeutic activity of zolmitriptan for the treatment of migraine headache can most likely be attributed to the agonist effects at the 5-HT1B/1D receptors on intracranial blood

Approved indications

• Acute treatment of migraine

Common side effects

• unusual taste
• unusual taste
• hyperesthesia
• hyperesthesia
• paresthesia
• paresthesia
• warm sensation
• discomfort of nasal cavity
• discomfort of nasal cavity
• pain location specified
• pain location specified
• throat pain

Drug interactions

• cimetidine
• ergotamine-containing or ergot-type medications (like dihydroergotamine or methysergide)
• MAO-A inhibitors
• other 5-HT 1B/1D agonists (including triptans)
• selective serotonin reuptake inhibitors (SSRIs) or serotonin norepinephrine reuptake inhibitors (SNRIs)

Key clinical trials

• Quality Improvement and Practice Based Research in Neurology Using the EMR (PHASE4)
• Cocaine and Zolmitriptan (EARLY_PHASE1)
• Pharmacokinetics in Oral and Intranasal Formulations of Zolmitriptan. (PHASE1)
• Treatments of Migraine with Triptans in Individuals with Elevated Cardiovascular Risk and in Pregnant Women
• Efficacy of Zolmitriptan (Zomig) in the Treatment of Migraines in Adolescents (PHASE3)
• Double-Blind Comparison of the Efficacy and Safety of C213 to Placebo for the Acute Treatment of Cluster Headaches (PHASE2,PHASE3)
• A Four-way Crossover Study of 3 Formulations of M207 With Intranasal Zolmitriptan in Healthy Volunteers (PHASE1)
• Study of PK, Safety, and Tolerability of 2 Lots of M207 & Intranasal Zolmitriptan in Healthy Volunteers (PHASE1)

Primary sources

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