Zolmitriptan – the comprehensive one

The development of zolmitriptan (AscoTop) was also guided by the goal of having a substance available that was even more effective and more reliable than previous classes of substances. The mechanism of action of Zolmitriptan:

Zolmitriptan leads to vasoconstriction of dilated cerebral vessels. The substance blocks the release of inflammatory substances from the nerve fiber endings. In addition, excessive nerve activity is inhibited.

Finally, nerve centers in the central nervous system are also inhibited in their excessive activity during the migraine attack. This is particularly true for nerve switching centers in the brain stem, which are responsible for the numerous accompanying symptoms.

Compared to sumatriptan, zolmitriptan is able to cross the so-called blood-brain barrier to a greater extent. The reason for this is that the substance has a much smaller molecular size and can be absorbed much more easily into fatty tissue. However, this can lead to more pronounced side effects such as tiredness or dizziness. At the same time, the substance is able to be absorbed very quickly in the gastrointestinal tract. Effective blood levels can be achieved within an hour. Another advantage is that these blood levels last for over 6 hours and are therefore effective for a long time even during longer headache attacks. Not only are headache symptoms reduced, but accompanying disorders such as nausea, vomiting, sensitivity to noise and light are also positively influenced.

The average dose in use is 2.5 mg. Zolmitriptan is currently available as a regular oral tablet and as a 2.5 mg and 5 mg orodispersible tablet. The orodispersible tablet dissolves very quickly on the tongue and, in addition to being pleasant to take (orange taste), leads to a quick substance effect. However, it is important that the orodispersible tablet must also be swallowed with enough water! The active ingredient is not absorbed through the oral mucosa, but, like the other tablets, only in the intestine.

In addition, a nasal spray with 5 mg was introduced in autumn 2002. Its use is beneficial for patients who suffer from severe nausea or vomiting. A chewable tablet is currently in development. Clinical studies show that when zolmitriptan is used in a dose of 5 mg, headaches can be significantly reduced in up to 80 percent of patients, and in around 55 percent of attacks the headaches subside completely.

Bioequivalent and surcharge-free generics have been on the market since March 2012, while the first-party preparation is priced above the fixed price.


  • Even in long-term use, it shows consistently good effectiveness.
  • With mild pain intensity, 78 percent of attacks can be treated successfully, with moderate intensity 76 percent and with very severe pain intensity 67 percent.
  • From this data it follows that for more severe migraine attacks, 5 mg should be taken right at the beginning.
  • At this dose, even severe migraine attacks can be treated very successfully.
  • It is particularly advantageous that patients who have not responded successfully to previous drug therapies now have effective migraine therapy available with zolmitriptan.
  • A controlled study confirmed that 82 to 85 percent of patients who were previously unable to achieve sufficient relief can achieve significant improvement with zolmitriptan.