Rizatriptan is a drug belonging to the triptans class. This stimulates the serotonin receptors and is used in moderate to severe forms of migraine. Not only does it relieve pain, but it also has a positive effect on symptoms such as sensitivity to light.
What is rizatriptan?
The drug rizatriptan is a selective serotonin agonist used to treat cluster headaches and migraines. Substances from pharmacology that can activate serotonin receptors are referred to as selective serotonin agonists. Thereby they support the tissue hormones and neurotransmitters.
Rizatriptan belongs to the triptan class of active ingredients, the mechanism of which is generally based on the selective stimulation of the serotonin receptors. The drug was approved as a prescription drug by the Food and Drug Administration (FDA) in the United States and by the Federal Institute for Drugs and Medical Devices in Germany.
Rizatriptan is used to treat migraines and cluster headaches. It not only has a positive effect on the state of pain, but also relieves other symptoms such as sensitivity to light and eye flicker. This is achieved by narrowing the blood vessels in migraine headaches (vascular constriction).
Pharmacological effect
Rizatriptan is an approved drug from the class of triptans. Serotonin agonists are called triptans. Serotonin agonists have an activating effect on the signal transmission of the receptors of a cell through their pharmacological substance. In rizatriptan, these are the 5-HT1D receptors. The stimulation of these receptors leads to a narrowing of the intracranial (inside the skull) blood vessels.
Furthermore, the activated stimulus transmission of the receptors has an inhibiting effect on the release of vasoactive neuropeptides and inhibits the central transmission of pain in the brain stem. Neuropeptides are messenger substances in nerve tissue.
The absorption of the drug rizatriptan is very fast compared to other triptans. The maximum active ingredient is distributed in the blood plasma within about 50 minutes. As a result, the rizatriptan remains unchanged by around 45 percent in the systemic blood circulation and is only absorbed from the circulation after two to three hours (half-life). If the drug is taken orally, the effect occurs after just 30 minutes.
Medical application & use
The rizatriptan is indicated for severe headaches and migraine attacks. Basically, this drug should only be given to adults. It is taken during an acute attack and not as a prophylactic therapy for headaches and migraines.
Rizatriptan is taken as tablets or sublingual tablets. A sublingual tablet is a tablet that is placed below the tongue and dissolves there. This has the advantage that the active ingredient is absorbed directly through the mucous membranes and thus gets into the bloodstream more quickly.
The standard dose of rizatriptan is around 10 milligrams, and only 5 milligrams should be prescribed for liver or kidney disorders. If the first symptoms of an impending migraine attack appear, an application should be taken immediately. Signs can be tiredness, light sensitivity or an aura, for example. At these first signs, a single dose of 10 milligrams should be taken. If pain or other symptoms are still present after about 2 hours, a second application of 10 milligrams can be taken. However, the daily dose of a maximum of 20 milligrams should not be exceeded.
About 10-20 percent of people may experience no response to rizatriptan. In this case, the attending physician should consider an alternative drug.
Risks & side effects
Compared to other drugs in this class of active ingredients, rizatriptan is said to be well tolerated. The most common side effects are nausea, dry mouth and thirst, hot flashes, tiredness, dizziness, muscle weakness or general attacks of weakness. Occasionally, unwanted side effects such as palpitations and shortness of breath can occur. Side effects that occur rarely but are life-threatening can be heart attack provocation and severe cardiac arrhythmias.
Basically, rizatriptan should always be taken with consideration of the patient's individual medical history and health history. If there are previous illnesses such as high blood pressure, diabetes mellitus, peripheral vascular diseases or disorders of the liver and kidney function, taking the drug is associated with significantly increased risks. Women who are in the menopause or smokers also belong to this risk group.
The active ingredient is absolutely contraindicated in angina pectoris and patients who have suffered a heart attack or stroke. Due to a lack of studies, the drug rizatriptan should not be prescribed for children, adolescents, adults over 65 years of age, pregnant women and nursing mothers.
Taking different drugs of the same class of active ingredients and in combination with ergotamine derivatives intensifies the effect in an uncontrolled manner and increases the risk of side effects.
Even if such a pharmacological substance is discontinued, there is always a potentially increased risk of serotonin syndrome. Serotonin syndrome manifests itself with symptoms such as general restlessness, hallucinations, loss of coordination, increased heartbeat, fluctuations in blood pressure, increased reflexes, nausea, vomiting, diarrhea and an increased body temperature.
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