Frovatriptan: Effects, Uses & Risks

The active ingredient frovatriptan is an antagonist of the serotonin receptors. The drug is classified in the category of triptans and has an approval for the treatment of acute migraine attacks. In addition, the drug frovatriptan is also used in some cases for preventive therapy of cluster headaches.

What is frovatriptan?

Originally, the drug frovatriptan was produced by the manufacturer Vernalis. Currently, it is available on the market in Germany from the pharmaceutical producers Kohlpharma and Berlin-Chemie. The active ingredient frovatriptan is generally available only on prescription. The substance is a so-called triptan and appears from a structural point of view as a ring-closed derivative. In its structure, it also resembles the hormone serotonin. The drug frovatriptan has an antagonistic effect on serotonin receptors.

Pharmacologic Action

Basically, the active substance frovatriptan is a strong antagonist for the receptors of the neurological messenger serotonin. In this regard, the substance acts precisely at the 5-HT1B and 5-HT1D receptors. These are located in the blood vessels of the brain and in the presynaptic area of neurons. In the majority of cases, the drug frovatriptan is used for acute migraine. If the drug frovatriptan is taken during such an attack, the corresponding receptors are activated. As a result, the blood vessels in the brain are affected and the production of special inflammatory substances is reduced. However, when 5-HT1B receptors are stimulated, various cardiovascular side effects are also possible, which must be weighed before the drug is used. The half-life of the active ingredient frovatriptan is relatively long at approximately 26 hours. This makes the substance the longest-acting triptan. For this reason, the drug is more effective in reducing the risk of recurrent migraine attacks than treatment with other types of triptans. In addition, the drug leads to activation of 5-HT7 receptors when used in high doses. In this context, lower side effects were expected, but this has not been confirmed so far. The bioavailability of the drug frovatriptan is between 20 and 30 percent. The substance is primarily metabolized in the liver. Later, most of the active substance is excreted from the human organism renally, i.e. via the kidneys. The drug frovatriptan reduces pain by binding to various serotonin receptors. In doing so, it activates significantly more receptors than other triptans. By connecting to these receptors, the drug dilates cerebral blood vessels, improving blood flow and reducing pain during migraine attacks.

Medical application and use

From a chemical perspective, the drug frovatriptan is one of the triptans. As such, it is used in the vast majority of cases as part of the therapy of acute migraine attacks. In this case, the drug frovatriptan unfolds its pain-relieving effects. The active ingredient can also be used for other types of headache. In addition, frovatriptan is also used to prevent cluster headache. Basically, the drug frovatriptan is taken orally in the form of tablets.

Risks and side effects

In the course of treatment with frovatriptan, attention should be paid to various undesirable side effects or other complaints. Side effects occur with varying frequency and in different combinations, varying from person to person. In principle, the active ingredient frovatriptan is a prescription drug. Before prescribing it, the treating physician thoroughly weighs up whether the potential side effects are acceptable in the individual case or whether the risk of complications is too high. The most common side effects from frovatriptan include nausea, digestive discomfort, and abdominal pain. Headache, dry mouth, dizziness, and paresthesias in the limbs are also possible. In some circumstances, the sensation of touch is affected and there is severe fatigue. In some cases, patients also suffer from hot flashes, redness of the skin and heavy sweating.Less frequently, people complain of disturbances in taste perception, tremor, lethargy, and reduced concentration after taking the drug frovatriptan. Sometimes involuntary contractions of the muscles occur. More rarely, there are feelings of pressure in the chest area similar to those of angina pectoris. However, this is a relatively rare side effect of the drug frovatriptan. The cause is an effect on the coronary vessels. In addition, some patients experience an increase in blood pressure (hypertension). In addition, while taking the drug frovatriptan, some potential interactions with other substances should be noted. For example, frovatriptan should not be taken together with the substance ergotamine, as the risk of coronary spasm increases (spasm of the coronary arteries). Serotonin reuptake inhibitors and St. John’s wort should also not be taken at the same time as frovatriptan. This is because these substances intensify the effect of the drug frovatriptan. In addition, joint use with MAO inhibitors is strongly discouraged. Contraindications to treatment with the drug frovatriptan are, for example, hypersensitivity to the substance, high blood pressure and liver function disorders. Caution should also be exercised in the event of a heart attack or vascular disease. In some rarely occurring types of migraine, the drug frovatriptan is not suitable for treatment. These include basilar migraine, ophthalmoplegic migraine and familial hemiplegic migraine. Any side effects that occur should always be reported to the treating physician.