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Sumatriptan

This is how sumatriptan works

Migraines differ from normal headaches in that they are usually one-sided, strong and pulsating to throbbing. The causes of migraines are not fully understood. Experts are currently assuming several complementary factors in the development of migraines:

  • During an acute migraine attack, blood vessels in the brain have been shown to dilate, which means that the affected parts of the brain are supplied with more blood. In the vessel wall there are receptors that transmit pain and the distension of the vessels to the brain.
  • Experts suspect that certain parts of the brain may be over-excited in migraine patients. The same is the case with epileptic seizures, to which migraines have some parallels.

Triptans such as sumatriptan reach the brain via the blood and activate certain docking points (receptors) for the neurotransmitter serotonin (5-HT) on the surface of nerve cells and blood vessels in the brain1-Receptor). As a result, the blood vessels that widen during an attack constrict and, moreover, fewer inflammatory messengers are released by nerve cells.

Sumatriptan also has an effect on cluster headaches. These are strictly one-sided, very strong pain attacks that occur primarily in the area of ​​the temples and eyes.

Sumatriptan uptake, breakdown and excretion

Sumatriptan is quickly absorbed through the mouth, but only in small amounts (around ten to twenty percent) through the intestinal wall into the blood. It reaches its site of action via the blood-brain barrier. Sumatriptan is then largely converted in the liver into degradation products that are no longer effective and excreted via the kidneys. About two hours after ingestion, half of the original amount of active ingredient has already left the body.

When is sumatriptan used?

The active ingredient sumatriptan is approved for the treatment of acute migraine attacks with and without aura as well as cluster headaches.

This is how sumatriptan is used

The migraine drug sumatriptan is usually taken as a tablet at the beginning or during an acute migraine attack. The usual dosage is 50 to 100 milligrams of sumatriptan, higher dosages do not show any increased effect. If the pain returns after a few hours after the first tablet has been taken, a second tablet can be taken within a day (but not earlier than two hours after the first). If the first tablet does not work, however, no more should be taken, but other painkillers (ASA, ibuprofen, paracetamol) should be used instead.

Since sumatriptan is poorly absorbed in the intestine, there are several other dosage forms on the market that enable a faster onset of action:

  • Sumatriptan nasal spray is sprayed once into one nostril.
  • Sumatriptan injection solution is injected into the subcutaneous fat tissue.

All of these dosage forms are dosed lower than the tablets in order to do justice to the improved absorption. They are particularly suitable for patients who suffer from nausea and vomiting during migraine attacks and who therefore find it difficult to take tablets.

What are the side effects of sumatriptan?

Sumatriptan causes side effects such as dizziness, sleepiness, weakness, heaviness, sensory disturbances, rise in blood pressure, hot flashes, shortness of breath, nausea, vomiting and muscle pain in one in ten to one hundred people treated.

What should be considered when taking sumatriptan?

If sumatriptan is combined with other medicines used to treat migraines (such as other triptans or ergotamine), undesirable effects such as spasms of the coronary arteries may increase. Such combinations of active ingredients must therefore be avoided.

MAO-type antidepressants (monoamine oxidase inhibitors such as tranylcypromine, moclobemide) can slow down the breakdown of sumatriptan so that its blood levels rise sharply. The same applies to other active ingredients that affect the serotonin balance, such as other antidepressants (SSRI - selective serotonin reuptake inhibitors, St. John's wort, tricyclic antidepressants, 5-hydroxytryptophan), light sleep aids (tryptophan), opioid pain relievers (tramadol, fentanyl) ) and especially addictive substances (amphetamines, cocaine, MDMA).
They must therefore not be combined with the migraine drug sumatriptan.

Use in pregnant women should be avoided due to the limited amount of studies available, but is possible in the second and third trimester of pregnancy under medical supervision and a strict risk-benefit assessment.

Sumatriptan passes into breast milk, but only for about twelve hours after ingestion. If the milk produced during this time is pumped out and discarded, it can then be breastfed.

Since the effectiveness in children and adolescents has not been proven, they should not use sumatriptan for migraine therapy.

Basically nothing speaks against the use of sumatriptan in elderly patients. However, as there is little data available, use is not recommended.

How to get sumatriptan medication

Preparations with the active ingredient sumatriptan are currently still subject to prescription in all doses and pack sizes, but a release from the prescription requirement (for low dosages and small pack sizes) is being discussed. Newer triptans such as naratriptan and almotriptan are only available from pharmacies in small packs.

How long has sumatriptan been known?

After scientific studies in the 1960s showed that the vasoconstriction in the brain caused by various serotonin derivatives and analogues led to an improvement in migraine attacks, the pharmaceutical company Glaxo (now GlaxoSmithKline) began looking specifically for new active ingredients for this purpose from 1972. The newly developed active ingredient sumatriptan was approved in the Netherlands in 1991 and in Germany and the USA in 1992. Since the patent protection expired in 2006, numerous generics came with the active ingredient Sumatriptan on the market.

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