Frovatriptan

(R) -6 - ( methylamino) -5,6,7,8 - tetrahydrocarbazol -3- carboxamide

N02CC07

Triptan

Selective 5 - HT1 receptor agonist

Template: Infobox chemical / molecular formula search available

Frovatriptan is a serotonin receptor agonist is selected from the group of triptans, which is approved as a drug for acute treatment of migraine. He also shows efficacy in the prophylactic treatment of cluster headache. Frovatriptan was developed by Vernalis and is offered in Germany by Berlin-Chemie. It is subject to medical prescription.

Chemistry

Frovatriptan group of triptans belongs to. It is a ring- closed derivative of 5-HT1/7-Rezeptoragonisten 5 - carboxamidotryptamine and is structurally similar to serotonin.

Pharmacology

Mechanism of Action

Frovatriptan is a highly potent agonist of 5- HT1B and 5- HT1D, which occur at the serotonin receptors in cerebral blood vessels and on presynaptic neurons. Activation of these receptors by frovatriptan thus performs during a migraine attack on the one hand to a constriction of the dilated cerebral blood vessels and also to a reduction in the release of inflammatory mediators. Activation of 5 - HT1B receptors, however, also associated with cardiovascular side effects.

With a half -life of 26 h frovatriptan has within the group of triptans by far the longest duration of action. Therefore, during treatment with frovatriptan, the repetition rate of migraine attacks could be reduced more than with other triptans.

In addition, activated frovatriptan in high doses and 5- HT7 receptors. On the basis of this additional mechanism of a more favorable risk-benefit ratio was expected prior to launch, which, however, was not confirmed.

Side effects

More common ( 1 in 100 people) nausea, dry mouth, indigestion, and abdominal pain may be observed. Also common are headaches, dizziness, and paresthesia in the arms and legs, and altered sense of touch and extreme sleepiness. Also, hot flashes, possibly with erythema and increased sweating are often observed.

Uncommon (affects 1 in 1000 people) it comes to taste disturbances, tremors, lack of concentration, lethargy, increased touch sensation and involuntary muscle contractions. Also, stomach problems such as diarrhea or bloating in the stomach and / or intestine can be observed.

At this point it must be mentioned that many of these side effects often can not be clearly attributed to the drug, as well as the migraine itself includes similar or congruent symptoms.

One of the characteristic but rare side effects of the application of frovatriptan are of angina pectoris -like pressure and feeling of constriction of the chest, which are attributed to constriction of the coronary vessels. A blood pressure increase is also observed in some patients.

Interactions

Frovatriptan should not be used in combination with ergotamine, there is an increased risk of coronary artery spasm is. Concomitant use with serotonin reuptake inhibitors (SSRIs ), such as Fluoxetine, paroxetine, sertraline and citalopram selective serotonin and norepinephrine reuptake inhibitors ( SNRIs) or the herbal antidepressant St. John's wort can increase the effects and side effects of frovatriptan. The American FDA warns in this regard against the potentially life-threatening interaction of serotonin syndrome ( = the body accumulates too much serotonin in the nervous system). Symptoms of serotonin syndrome may restlessness, hallucinations, loss of coordination, fast heartbeat, changes in blood pressure, increased body temperature, increased reflexes, nausea, vomiting and diarrhea include. Absolute Caution should also be exercised when co-administering of frovatriptan with MAO inhibitors.