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Zolmitriptan – Effect, Application & Risks


Many people are plagued by migraines . Treating this effectively in more severe cases is sometimes not that easy. In the case of severe migraines with or without aura, as well as cluster headaches , triptans , derivatives of serotonin , are preferably used today. The lead substance is sumatriptan , but there are now several successor substances on the market. This also includes zolmitriptan , which is said to be more effective than previous substance classes.

What is zolmitriptan?

Zolmitriptan is a selective serotonin agonist from the triptan class, which is mainly used in the acute therapy of migraine. However, it only works when the headache has already set in, which means it cannot prevent a migraine attack. The drug is also said to help with cluster headaches, which 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. It crosses the blood-brain barrier more easily than the original lead compound, sumatriptan .

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

Pharmacological action

Zolmitriptan acts by selectively 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 narrow, because the headache only occurs when the blood vessels dilate. They also ensure a reduced release of inflammatory mediators and reduced pain transmission.

The half-life of zolmitriptan is relatively short, lasting 2.5 to 3 hours. Metabolism in the liver produces an additional active metabolite, which also contributes to 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 is therefore well absorbed into fatty tissues . At the same time, it is also very quickly absorbed via the gastrointestinal tract , which means that effective levels in the blood are reached after about an hour.

Not only are headaches relieved, but side effects of migraines such as nausea , vomiting and sensitivity to light are also positively influenced. Consistently good effectiveness was also demonstrated in long-term use.

Medical Application & Use

The average dose of the application is an amount of 2.5 milligrams. If possible, it should be taken at the first sign of a migraine attack. Although the tablets cannot prevent the headache from occurring, taking them in good time will help to achieve faster relief.

However, the drug can still be taken during the attack. If the dose is not sufficient, it can also 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 especially beneficial for those suffering from severe nausea and vomiting and in cases of severe cluster headaches. Food taken at the same time has little effect on absorption . During a hospital stay, the drug is also available as a short infusion.

Risks & side effects

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

Occasionally there is an increase in heart rate or chest tightness. Rarely, itching on 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 medicines at the same time. Whether an interaction occurs depends on various factors, so you should always consult your doctor. However, the simultaneous intake with ergot alkaloids should be avoided in any case , since the risk of spasms of the coronary arteries increases greatly due to their additional vasoconstrictive effect.

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

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

Due to the vasoconstrictive effect, zolmitriptan is contraindicated in existing coronary artery disease , hypertension and vascular disease. The drug should also not be taken in cases of hypersensitivity, hemiplegic migraine or basilar migraine.

In the case of impaired renal function, the dose should be adjusted. During pregnancy , zolmitriptan should only be taken if the doctor considers it absolutely necessary.

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Hello! I am Lisa Newlon, and I am a medical writer and researcher with over 10 years of experience in the healthcare industry. I have a Master’s degree in Medicine, and my deep understanding of medical terminology, practices, and procedures has made me a trusted source of information in the medical world.