Frovatriptan
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| Non-proprietary name | Frovatriptan | ||||||||||||
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( R ) -6- (methylamino) -5,6,7,8-tetrahydrocarbazole-3-carbamide |
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| Molecular formula | C 14 H 17 N 3 O | ||||||||||||
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Selective 5-HT 1 receptor agonist |
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| Molar mass | 243.30 g · mol -1 | ||||||||||||
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| As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . | |||||||||||||
Frovatriptan is a serotonin receptor agonist from the group of triptans , which as a drug for acute treatment of migraine has been approved. In addition, it shows effectiveness in the preventive treatment of cluster headache . Frovatriptan was developed by Vernalis and is offered in Germany by Berlin-Chemie and Kohlpharma . It is subject to medical prescription .
chemistry
Frovatriptan belongs to the group of triptans . It is a ring-closed derivative of the 5-HT 1/7 receptor agonist 5-carboxamidotryptamine and is structurally similar to serotonin .
pharmacology
Mechanism of action
Frovatriptan is a highly potent agonist at the serotonin receptors 5-HT 1B and 5-HT 1D , which occur on cerebral blood vessels and presynaptically on neurons . Activation of these receptors by frovatriptan thus leads, on the one hand, to a constriction of the dilated cerebral blood vessels during a migraine attack and, on the other hand, to a reduction in the release of inflammatory mediators . However, activation of 5-HT 1B receptors has also been associated with cardiovascular side effects .
With a half-life of 26 hours, frovatriptan has by far the longest duration of action within the group of triptans. Therefore, under therapy with frovatriptan, the repetition rate of migraine attacks could be reduced more than with other triptans.
In addition, high doses of frovatriptan also activate 5-HT 7 receptors. Due to this additional mechanism of action, a more favorable risk-benefit ratio was expected before the market launch, but this was not confirmed.
Side effects
Nausea , dry mouth, indigestion, and abdominal pain are more common (in 1 in 100 people) . Also common are headaches , dizziness and paresthesia in the arms and legs and altered sense of touch and extreme sleepiness. Hot flashes, possibly with reddening of the skin, and increased sweating are also often observed.
Occasionally (in 1 in 1000 people) there are taste disorders , tremors , poor concentration , lethargy , increased sensitivity to touch and involuntary muscle contractions . Stomach problems such as diarrhea or flatulence in the stomach and / or intestines can also be observed.
At this point it must be mentioned that many of these side effects can often not be clearly attributed to the active ingredient, since the migraine itself also includes similar or congruent symptoms .
One of the characteristic, but rare, side effects of using frovatriptan is angina- like pressure and tightness in the chest, which is attributed to a constriction of the coronary arteries . An increase in blood pressure can also be observed in some patients.
Interactions
Frovatriptan should not be used in combination with ergotamine as there is an increased risk of coronary spasms. Concomitant use with serotonin reuptake inhibitors (SSRI) such as B. fluoxetine , paroxetine , sertraline and citalopram , selective serotonin and noradrenaline reuptake inhibitors (SNRI) or the herbal antidepressant St. John's wort can increase the effects and side effects of frovatriptan. In this context, the American health authority FDA warns of the potentially life-threatening interaction of the serotonin syndrome (= the body accumulates too much serotonin in the nervous system). Symptoms of serotonin syndrome can include restlessness, hallucinations, loss of coordination, rapid heartbeat, fluctuations in blood pressure, increased body temperature, increased reflexes, nausea, vomiting, and diarrhea. Extreme caution is also advised when frovatriptan is used concomitantly with MAOIs .
Trade names
Allegro (D), Eumitan (A), Frovamig (A), Menamig (CH)
Individual evidence
- ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
- ^ Siow HC, Pozo-Rosich P, Silberstein SD .: Frovatriptan for the treatment of cluster headaches. Cephalalgia. 2004; 24 (12): 1045-1048; PMID 15566418 ; doi : 10.1111 / j.1468-2982.2004.00734.x .
- ^ S1 guideline for cluster headaches and trigemino-autonomic headaches of the German Society for Neurology (DGN). In: AWMF online (as of 2015)
- ↑ Limmroth V: mechanism of action of triptans . In: Pharmacy in our time . 31, No. 5, 2002, pp. 458-61. doi : 10.1002 / 1615-1003 (200209) 31: 5 <458 :: AID-PAUZ458> 3.0.CO; 2-G . PMID 12369163 .
- ↑ Jähnichen S, Glusa E, Pertz HH: Evidence for 5-HT2B and 5-HT7 receptor-mediated relaxation in pulmonary arteries of weaned pigs . In: Naunyn Schmiedebergs Arch Pharmacol . 371, No. 1, January 2005, pp. 89-98. doi : 10.1007 / s00210-004-1006-6 . PMID 15726452 .
- ↑ FDA Public Health Advisory: Combined Use of 5-Hydroxytryptamine Receptor Agonists (Triptans), Selective Serotonin Reuptake Inhibitors (SSRIs) or Selective Serotonin / Norepinephrine Reuptake Inhibitors (SNRIs) May Result in Life-threatening Serotonin Syndrome , July 19, 2006 ( English).
