Intranasal zolmitriptan for the treatment of acute migraine

Headache. 2013 Sep;53 Suppl 2:62-71. doi: 10.1111/head.12181.


Objective: To review the pharmacokinetics, efficacy, tolerability, and patient acceptance of zolmitriptan nasal spray (NS).

Background: Gastroparesis may delay or diminish the absorption of oral triptans, and nausea or vomiting may do the same and/or make it difficult to take a tablet. Some migraineurs require or prefer faster relief than oral medications provide. Injectable triptans provide the fastest drug delivery into the bloodstream, but many patients are reluctant to use them. Nasal sprays may address some of the problems with tablets and injectables while still providing rapid absorption of drug.

Methods: Non-systematic review.

Results: Significant levels of zolmitriptan NS are detectable in plasma within 2-5 minutes, and the rapid absorption is due to early uptake through the nasal mucosa. In 2 randomized trials, users of zolmitriptan NS were significantly more likely than placebo recipients to be pain-free at 15 minutes post-dose, the first time point measured, and about half of patients had sustained response at 24 hours. Studies in which patients could treat a migraine of any severity have documented significant headache response or relief with zolmitriptan NS at 10 minutes. In one trial, the rate of total symptom relief was significantly better with the NS than with placebo from 30 minutes post-dose. The most common side effect of zolmitriptan NS is unusual taste. Patient satisfaction studies indicate that zolmitriptan NS is appreciated for its speed of onset, ease of use, reliability, and overall efficacy.

Conclusions: Zolmitriptan NS provides onset of headache relief within 10 minutes for some patients and quickly abolishes some of the major migraine symptoms. Good candidates are migraineurs whose episodes rapidly escalate to moderate-to-severe pain and those who have morning migraine, have a quick time to vomiting, or have failed oral triptans.

Keywords: headache; migraine treatment; onset of action; serotonin 5-HT1B/1D receptor agonist; triptan; zolmitriptan nasal spray.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review
  • Systematic Review

MeSH terms

  • Administration, Intranasal
  • Animals
  • Clinical Trials as Topic / methods
  • Humans
  • Migraine Disorders / drug therapy*
  • Migraine Disorders / metabolism
  • Oxazolidinones / administration & dosage*
  • Oxazolidinones / pharmacokinetics
  • Serotonin 5-HT1 Receptor Agonists / administration & dosage*
  • Serotonin 5-HT1 Receptor Agonists / pharmacokinetics
  • Treatment Outcome
  • Tryptamines / administration & dosage*
  • Tryptamines / pharmacokinetics


  • Oxazolidinones
  • Serotonin 5-HT1 Receptor Agonists
  • Tryptamines
  • zolmitriptan