Zolmitriptan is a selective serotonin (5-HT1B/1D) receptor agonist, commonly known as a 'triptan'. It is a second-generation agent specifically designed for the acute treatment of migraine with or without aura in adults. It is not intended for prophylactic use. In the Indian context, it is a widely prescribed, effective, and well-tolerated option for aborting migraine attacks, available in both conventional tablet and orally disintegrating tablet (ODT) formulations.
Adult: Initial dose: 2.5 mg or 5 mg at the onset of migraine. If headache recurs, a second dose may be taken after 2 hours. Maximum daily dose: 10 mg in 24 hours. The 5mg dose may provide greater efficacy but with a slightly higher incidence of side effects.
Note: Tablet: Swallow whole with a glass of water. Can be taken with or without food. Orally Disintegrating Tablet (ODT): Place on tongue, allow to disintegrate, and swallow with saliva. No water needed. Do not break or crush the ODT. Take at the earliest sign of a migraine headache. If no response to the first dose, do not take a second dose for the same attack. A second dose may be taken for a recurrent headache, but only after a minimum 2-hour interval.
Zolmitriptan exerts its therapeutic effects by binding with high affinity to serotonin 5-HT1B and 5-HT1D receptors. This agonism leads to cranial vasoconstriction of painfully dilated cerebral and dural blood vessels, inhibition of pro-inflammatory neuropeptide release (like CGRP and substance P) from perivascular trigeminal sensory nerves, and reduction of pain signal transmission in the trigeminal nucleus caudalis.
Pregnancy: Pregnancy Category C (US FDA). Animal studies have shown adverse effects (embryolethality, teratogenicity). No adequate, well-controlled studies in pregnant women. Use only if the potential benefit justifies the potential risk to the fetus. Should not be used for incidental headaches; reserved for severe, disabling migraine attacks.
Driving: May cause dizziness, somnolence, or visual disturbances. Patients should be cautioned about driving or operating machinery until they are certain they are not affected.
| Monoamine Oxidase-A Inhibitors (Moclobemide, Clorgyline) | Markedly increased zolmitriptan plasma levels (up to 8-fold) and reduced metabolite formation. Risk of serotonin syndrome. | Contraindicated |
| Selective Serotonin Reuptake Inhibitors (SSRIs: Citalopram, Escitalopram, Fluoxetine, etc.) | Increased risk of serotonin syndrome (weakness, hyperreflexia, incoordination). | Major |
| Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs: Venlafaxine, Duloxetine) | Increased risk of serotonin syndrome. | Major |
| Ergot Alkaloids (Ergotamine, Dihydroergotamine, Methysergide) | Prolonged vasospastic reactions. Additive vasoconstriction. | Contraindicated (within 24 hours) |
| Other Triptans (Sumatriptan, Rizatriptan, etc.) | Additive vasoconstriction and increased risk of adverse effects. | Contraindicated (within 24 hours) |
| CYP1A2 Inhibitors (Ciprofloxacin, Fluvoxamine) | Increased plasma concentration of zolmitriptan. Reduce zolmitriptan dose. | Moderate |
| Oral Contraceptives | May increase the bioavailability of zolmitriptan by ~25%. Clinical significance is low. | Minor |