A triptan is a drug used to treat cluster headaches and migraines. Triptans are particularly well suited to control moderate to severe migraine attacks.
What is triptan?
A triptan is a drug used to treat cluster headaches and migraines. Triptans belong to the group of migraine medications and are administered for acute migraines as well as cluster headaches. By constricting blood vessels, they can reduce inflammation and decrease discomfort. Medical science has known since the 19th century that migraine attacks are associated with the dilatation of cerebral and cranial blood vessels. The observation that the neurotransmitter serotonin also caused constriction of the abnormally dilated vessels led to the development of the drug triptan. However, serotonin was not suitable as a treatment for migraine due to its strong side effects on the heart, circulation and stomach. For this reason, medical researchers attempted to obtain a serotonin derivative that would make it possible to selectively contract cerebral blood vessels without causing systemic side effects. In the early 1980s, 5-carboxamidotryptamine was discovered as an agent that could selectively stimulate 5-HT1 receptors. However, this substance also showed systemic side effects on the cardiovascular system. Therefore, the substance was not clinically developed. Only a short time later, with the drug sumatriptan, a 5-HT1B/1D receptor agonist was discovered with which it is possible to selectively contract cerebral blood vessels. In December 1992, sumatriptan received approval from the U.S. Food and Drug Administration (FDA) as a migraine drug. However, sumtriptan had the disadvantage of having insufficient oral bioavailability. Another drawback was that the active ingredient could not sufficiently pass the blood-brain barrier. Therefore, medical researchers developed other 2nd generation triptans that had better pharmacokinetic properties. Then, in the late 1990s, the triptans zolmitriptan, rizatriptan, and naratriptan came onto the market. Later, frovatriptan, almotriptan, and eletriptan were developed.
Pharmacologic action
The action of each triptan is based on binding to the receptors 5-HT-1B, 5-HT1D, as well as 5-HT1F. This results in vasoconstriction (vasoconstriction) of cerebral blood vessels. At the same time, the release of inflammatory mediators such as CGRP and substance P is inhibited. The spread of pain stimuli via the cerebral cortex is slowed down by the triptans. Unfortunately, the triptans do not have the same positive effect in every patient. Roughly estimated, about one third of all migraine patients respond well to the active ingredient, while in another third at least a relief of the pain can be achieved. In the remaining third, the triptans have no effect at all. If a pain-relieving effect is seen, it usually sets in after three to four hours. However, many patients suffer from headaches again only a few hours after administration of the migraine medication. The mechanism of action of the various triptans is identical. However, there are differences in the pharmacokinetic properties. These include onset and duration of action and elimination time.
Medical application and use
Triptans are used to treat acute moderate and severe migraine attacks. However, they are not suitable for the prevention of migraine attacks. In addition, they can be used to treat cluster headaches. Triptans can be used in different ways. For example, conventional tablets, melting tablets, water-soluble tablets, nasal sprays, suppositories, pre-filled syringes, and needle-free injectors are available. It is recommended that triptans be taken after the auric phase, when the headache phase begins. The sooner they are taken then, the greater the chances of therapeutic success. However, the triptans should not be administered more than ten times a month, otherwise there is a risk of drug-induced headache. With the exception of naratriptan, the triptans are subject to prescription in Germany.
Risks and side effects
Taking triptans may be associated with adverse side effects.These primarily include dizziness, slight weakness, sensations such as tingling, slight nausea, and feelings of warmth. In some cases, a temporary increase in blood pressure or an angina attack are also possible. These side effects are thought to be due to stimulation of 5-HT1B/1D receptors in the cardiovascular system. Very rarely, skeletal muscle dysfunction, circulatory disturbances, or cardiac arrhythmias may occur. The use of triptans, due to their vasoconstrictive effects, is not suitable if the patient suffers from vascular diseases, hypertension or coronary heart disease (CHD). Other contraindications include Raynaud’s syndrome, prior myocardial infarction, and severe renal and hepatic dysfunction. Use of the triptans during pregnancy and lactation is not recommended. Caution is also advised against interactions with other drugs. For example, the joint use of ergot alkaloids such as ergotamine, which are also migraine medications, can cause coronary vasospasm. For this reason, joint use should be avoided. Administration of MAO inhibitors often results in slower clearance of triptans from the body.
