Zolmitriptan CAS NO.139264-17-8
Active Pharmaceutical Ingredients 2025-03-03
Catalog ID80017035
CAS NO.139264-17-8
Purity 95%
MDL NumberMFCD00871503
EINEC Molecular Formula C16H21N3O2
Molecular Weight 287.3568
| Aspect | Details |
|---|---|
| Definition | Zolmitriptan is a selective 5-hydroxytryptamine (5-HT) 1B/1D receptor agonist used to treat acute migraine attacks. |
| Mechanism of Action | – Binds with high affinity to 5-HT1B/1D receptors, causing vasoconstriction of intracranial blood vessels and inhibiting the release of pro-inflammatory neuropeptides.<br>- Penetrates the blood-brain barrier, providing both peripheral and central effects. |
| Clinical Uses | – FDA-approved for treating acute migraine with or without aura.<br>- Available in tablet, orally disintegrating tablet, and nasal spray forms.<br>- Off-label use for preventing menstrual migraines. |
| Pharmacokinetics | – Absorption: Rapidly absorbed orally, with linear kinetics over the dose range of 2.5 to 50 mg.<br>- Distribution: Plasma protein binding is 25%, with a volume of distribution of 7 L/kg.<br>- Metabolism: Primarily metabolized by CYP1A2 and MAO-A into an active N-desmethyl metabolite.<br>- Elimination: Elimination half-life is approximately 3 hours, primarily excreted renally. |
| Side Effects | – Common: Dizziness, somnolence, paresthesia, dry mouth.<br>- Serious: Hypersensitivity reactions, serotonin syndrome. |
| Contraindications | – Hypersensitivity to zolmitriptan.<br>- Ischemic heart disease, uncontrolled hypertension. |
| Storage Conditions | Store at room temperature, away from moisture and light. |
| Formulations | – Tablets: 2.5 mg (yellow) and 5 mg (pink).<br>- Orally Disintegrating Tablets: 2.5 mg and 5 mg.<br>- Nasal Spray. |
| Research Applications | Investigated for its efficacy and safety in treating migraine attacks, with studies demonstrating its effectiveness in reducing headache severity and associated symptoms. |
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