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Sumatriptan

Sumatriptan is a drug from the group of triptans, and is used for the acute treatment of migraine and cluster headaches.

Indications
Sumatriptanhaltige drugs are approved for the acute treatment of migraine as an oral drug or as an injection dosage it is approved for the treatment of cluster headache.

Contraindications
Sumatriptan should not be used in patients who have had or are a high risk for heart attacks, suspected ischemic heart disease, coronary Sumatriptanvasospasm Prinzmetal angina, peripheral blood vessel disorders and moderate to severe or uncontrolled hypertension.

Patients with known severe liver dysfunction, and transient ischemic attacks in previous usage of the sumatriptan drug in their medical history should not be taking this drug.

Sumatriptan should not be taken simultaneously with ergot alkaloids and their derivatives, for example, ergotamine or dihydroergotamine, since it increases the risk of vasospasm, similarly, sumatriptan may be administered no sooner than two weeks after the end of a treatment with monoamine oxidase inhibitors, as these inhibit the degradation of the sumatriptan.

Sumatriptan should not be used with known hypersensitivity to the drug and special care must be taken if the patient shows symptoms of allergy to the sulfonamides offered.

Use during pregnancy and lactation
The experience gained and information at hand regarding administration of the drug during pregnancy are still inadequate, past experience does not indicate an increased risk of malformations in pregnancy, however animal studies on rabbits, have shown embryotoxic effect from sumatriptan use

Sumatriptan is excreted into breast milk, a potential danger to the child can be avoided by Sumatriptaneinnahme or by pumping and discarding the breast milk while undergoing treatment.

Side-effects
One of the most frequently discussed, though rare side effects from the use of sumatriptan, is angina and the pressure like feelings of chest tightness, which are attributed to a constriction of the coronary arteries.
In animal experiments, these symptoms could only be induced through much higher concentrations of the substance in the blood, to induce the narrowing of the coronary arteries.

Patients sometimes experience an increase in blood pressure, taken in high doses; the drug can alter the color of blood to a green-black colour. The effect is called Sulfhämoglobinämie and arises from the chemical reaction of the sulphur contained in the substance mixed with haemoglobin. In an average-sized adult male the dose would be approximately 200mg daily produce this color change.

Interactions
Although data is limited, there is the danger of reinforcing the effects of the drug and therefore sumatriptan should not be used concomitantly or in conjunction with ergotamine, see Contraindications. After an application of ergotamine, a minimum of 24 hours must be observed, before further doses of Sumatriptantherapie is administered, in the opposite case, the minimum time requirement should be 6 hours.

MAO inhibitors may increase, by an inhibition of the degradation of sumatriptan, and the body’s natural serotonin, the effects and side effects of these substances, therefore, concomitant use of sumatriptan and MAO inhibitors is contraindicated.

In rare cases, when a triptan is prescribed as antidepressant from the group of SSRIs, Selective Serotonin Reuptake Inhibitors or SNRIs, selective serotonin and norepinephrine reuptake inhibitors, potentially life-threatening interaction of serotonin syndrome can occur.

If there is an accumulation of too much serotonin in the nervous system and its effect is amplified by sumatriptan, the symptoms of serotonin syndrome may be exhibited as restlessness, hallucinations, loss of coordination, fast heart beat, blood pressure fluctuations, increased body temperature, increased reflexes, nausea, vomiting and diarrhoea.

Pharmacology

How it works
Sumatriptan is a selective agonist at the serotonin receptors 5-HT1B, 5-HT1D and 5-HT1F which act on cerebral blood vessels and occur presynaptically on neurons.

An activation of these receptors by sumatriptan leads to a constriction of cerebral blood vessels dilated during a migraine attack. On the other hand sumatriptan leads to a reduction of the distribution of blood vessel dilating and pain triggering inflammatory mediators, such as serotonin, calcitonin gene-related peptide CGRP and substance P.

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