Zolmitriptan – the Comprehensive
The development of zolmitriptan (AscoTop) was also driven by the goal of providing a substance with even better efficacy and higher reliability than previous classes of drugs. The mechanism of action of zolmitriptan:
Zolmitriptan causes vasoconstriction of dilated cerebral blood vessels. The substance blocks the release of inflammatory substances from nerve endings. Additionally, it inhibits excessive nerve activity.
Finally, during a migraine attack, nerve centers in the central nervous system are also inhibited from excessive activity. This applies particularly to nerve relay centers in the brainstem, which are responsible for the numerous accompanying symptoms.
Compared to sumatriptan, zolmitriptan is able to cross the blood-brain barrier to a greater extent. This is because the substance has a significantly smaller molecular size and is absorbed much more readily into fatty tissue. However, this can lead to more pronounced side effects such as fatigue or dizziness. At the same time, the substance is absorbed very quickly in the gastrointestinal tract. Effective blood levels can be reached within one hour. Another advantage is that these blood levels persist for over six hours, thus providing long-lasting relief even during prolonged headache attacks. It not only reduces headache symptoms but also positively influences accompanying symptoms such as nausea, vomiting, and sensitivity to noise and light.
The average dose is 2.5 mg. Zolmitriptan is currently available as a regular tablet to be swallowed and as a orally disintegrating tablet in 2.5 mg and 5 mg strengths. The orally disintegrating tablet dissolves very quickly on the tongue and, in addition to being pleasant to take (orange flavor), leads to a rapid onset of action. It is important, however, that the orally disintegrating tablet must also be swallowed with sufficient water! The active ingredient is not absorbed through the oral mucosa, but, like the other tablets, only in the intestine.
In addition, a 5 mg nasal spray was introduced in autumn 2002. Its use is beneficial for patients suffering from severe nausea or vomiting. A chewable tablet is also currently under development. Clinical studies have shown that zolmitriptan at a dose of 5 mg can significantly reduce headaches in up to 80 percent of patients, and completely eliminates headaches in approximately 55 percent of attacks.
Since March 2012, bioequivalent and co-payment-free generic drugs have been on the market, while the original brand-name drug is priced above the fixed reimbursement amount.
Special features
- Even in long-term use, consistently good effectiveness is evident.
- With mild pain intensity, 78 percent of attacks can be successfully treated, with moderate intensity 76 percent, and with very severe pain intensity 67 percent.
- These data suggest that 5 mg should be taken right at the beginning of severe migraine attacks.
- Even severe migraine attacks can be treated very successfully at this dose.
- A particular advantage is that patients who have not responded successfully to previous drug therapies now have an effective migraine therapy available through zolmitriptan.
- A controlled study confirmed that 82 to 85 percent of patients who had previously been unable to achieve sufficient relief could achieve significant improvement with zolmitriptan.