Zolmitriptan

Many people are plagued by migraines. Treating these effectively is sometimes not that easy in more severe cases. For severe migraines with or without aura, as well as for cluster headaches, triptans, descendants of serotonin, are preferred nowadays. The lead substance is sumatriptan, but there are now several successor substances on the market. That also counts Zolmitriptan, which is said to be more effective than the earlier substance classes.

What is zolmitriptan?

Zolmitriptan is a selective serotonin agonist from the triptan class, which is mainly used in acute therapy against migraines. However, it only works if the headache has already occurred, which means it cannot prevent a migraine attack. The drug is also said to provide relief for cluster headaches that occur much less frequently.

Zolmitriptan can be administered in the form of tablets or as a nasal spray, with the advantage that it is absorbed more quickly. In contrast to the original lead substance, sumatriptan, it gets through the blood-brain barrier more easily.

As an agonist on the serotonin receptors, the drug causes vasoconstriction of the cerebral blood vessels, which is said to improve the migraine.

Pharmacological effect

The action of zolmitriptan is based on selective binding to serotonin 5HT1D and -5HT1B receptors. These sit on the cerebral blood vessels and presynaptically on neurons. If they are activated, they cause the blood vessels to constrict, because the headache only occurs when the blood vessels dilate (widen). In addition, they ensure a reduced release of inflammatory mediators and a reduced transmission of pain.

The half-life of zolmitriptan is relatively short with a duration of 2.5 to 3 hours. In the liver, an additional active metabolite is formed during metabolism, which is also involved in the effects of the drug. It is mainly metabolized by the enzyme CYP1A2; to a lesser extent also from MAO-A.

As already mentioned, zolmitriptan crosses the blood-brain barrier very well because its molecular size is very small and it can therefore be easily absorbed into fatty tissue. At the same time, it is also absorbed very quickly via the gastrointestinal tract, which means that effective levels in the blood are reached after about an hour.

Not only the headache is alleviated, but also side effects of migraines such as nausea, vomiting and sensitivity to light are positively influenced. A consistently good effectiveness was also shown in long-term use.

Medical application & use

The mean dose of the application is an amount of 2.5 milligrams. If possible, the tablet should be taken at the first sign of a migraine attack. While the tablets cannot prevent the headache from occurring, taking them early will help provide faster relief.

However, the drug can still be taken during the seizure. If the dose is not sufficient, it can be increased to 5 milligrams in consultation with a doctor. More than 2 tablets within 24 hours should not be taken.

Use in the form of a nasal spray is particularly beneficial for those who suffer from severe nausea and vomiting, as well as in the case of severe cluster headache. Food consumed at the same time hardly affects absorption. The drug is also available as a short infusion during a hospital stay.

Risks & side effects

Side effects may occur from taking zolmitriptan. Common side effects include nausea, vomiting, dry mouth, dizziness, and drowsiness. In addition, headaches are one of the undesirable effects, especially with prolonged use.

Occasionally there is an increase in heart rate or a tightness in the chest. Rarely, itching of the skin or hives can occur. Heart attack, angina pectoris and an excessive urge to urinate are classified as very rare side effects.

It is also important to be aware of possible interactions when taking other drugs at the same time. Whether an interaction occurs depends on various factors, so you should always consult your doctor. In any case, the simultaneous intake with ergot alkaloids should be avoided, as the risk of spasms in the coronary arteries is greatly increased by their additional vasoconstricting effect.

The effect of zolmitriptan is increased by moclobemide, cimetidine, fluvoxamine, cigarette smoke and quinolones, which is why the dose of zolmitriptan must be reduced and adjusted in these cases.

If selective serotonin reuptake inhibitors are taken at the same time, caution is advised because there is a risk of dangerous serotonin syndrome, in which too much serotonin accumulates in the nervous system.

Due to its vasoconstrictive effect, zolmitriptan is contraindicated in existing coronary artery disease, hypertension and vascular diseases. The drug must also not be taken in the event of hypersensitivity, hemiplegic migraines or basilar migraines.

Dose adjustments should be made in the event of impaired renal function. Zolmitriptan should only be taken during pregnancy if the doctor considers it absolutely necessary.