Name Zolmitriptan
Classes Analgesic / Pain Killer
Central Nervous System Agent
Antimigraine Agent
Diseases CNS Disorder
Migraine

Zolmitriptan

Zolmitriptan is a 5-HT1B/1D receptor agonist used to treat migraine. Zolmitriptan's therapeutic activity in migraine is most likely due to agonist effects at 5-HT1B/1D receptors on extracerebral, intracranial blood vessels that dilate during a migraine attack, as well as nerve terminals in the trigeminal system. When these receptors are activated, cranial vessels constrict, neuropeptide release is inhibited, and transmission in trigeminal pain pathways is reduced.

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

  • Zolmitriptan's recommended starting dose is 1.25 mg or 2.5 mg. Zolmitriptan's 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-hour period.  

The most common side effects associated with Zolmitriptan are-

  • Nausea
  • Asthenia
  • Sleepiness/ drowsiness/ somnolence
  • Tingling or burning feeling (paresthesia)
  • Headache
  • Dry mouth
  • Zolmitriptan should only be used where a clear diagnosis of migraine has been established. 
  • Zolmitriptan should not be given to patients with documented ischemic or vasospastic coronary artery disease because this class of compounds (5-HT1B/1D agonists) has the potential to cause coronary vasospasm.
  • As with other 5-HT1B/1D agonists, sensations of tightness, pain, pressure, and heaviness in the precordium, throat, neck, and jaw have been reported after treatment with Zolmitriptan.
  • Within a few hours of receiving Zolmitriptan, serious adverse cardiac events, including acute myocardial infarction, have been reported.
  • Cerebral hemorrhage, subarachnoid hemorrhage, stroke, and other cerebrovascular events have been reported in patients receiving other 5-HT1 agonists, with some resulting in death.
  • Significant increases in systemic blood pressure, including hypertensive crisis, have been reported in patients with and without a history of hypertension treated with other 5-HT1 agonists on rare occasions.
  • Triptans, including Zolmitriptan, have been linked to the development of a potentially fatal serotonin syndrome.

Contraindication

  • Zolmitriptan is contraindicated in patients who are hypersensitive to Zolmitriptan or any of its ingredients. 
  • Zolmitriptan should not be administered within 24 hours of treatment with another 5-HT1 agonist, or an ergotamine-containing or ergot-type medication like-

Zolmitriptan should not be given to patients with-

  • ischemic heart disease (angina pectoris, history of myocardial infarction, or documented silent ischemia), or to patients who have symptoms or findings consistent with ischemic heart disease, coronary artery vasospasm, including Prinzmetal's variant angina, or other significant underlying cardiovascular disease.
  • uncontrolled hypertension.
  • hemiplegic or basilar migraine.