Active Ingredients

Rizatriptan – Effect, Application & Risks


Rizatriptan is a drug belonging to the triptan class of drugs . This stimulates the serotonin receptors and is used for moderate to severe forms of migraine . It not only has an analgesic effect, but also has a positive effect on symptoms such as photosensitivity .

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. They thereby support the tissue hormones and neurotransmitters .

Rizatriptan belongs to the active substance class of triptans, whose mechanism of action is generally based on the selective stimulation of the serotonin receptors . The drug was approved as a prescription drug in the United States by the Food and Drug Administration (FDA) and in Germany by the Federal Institute for Drugs and Medical Devices in 1998.

Rizatriptan is prescribed to treat migraines and cluster headaches. It not only has a positive effect on the pain condition, but also alleviates other symptoms such as sensitivity to light and flickering eyes . This is achieved by constricting the blood vessels in migraine headaches ( vasoconstriction ).

Pharmacological action

Rizatriptan is an approved drug from the triptan drug class. Serotonin agonists are called triptans. Due to their pharmacological substance, serotonin agonists have an activating effect on the signal transmission of the receptors of a cell . For rizatriptan, these are the 5-HT1D receptors. Stimulating these receptors causes the intracranial (located inside the skull) blood vessels to narrow.

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 brainstem . Messenger substances in nerve tissue are called neuropeptides .

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 from about 45 percent in the systemic bloodstream and is only absorbed from the circulation after two to three hours (half-life). When the drug is taken orally, the effect occurs after 30 minutes.

Medical Application & Use

Rizatriptan is indicated for severe headaches and migraine attacks. Basically, this drug should only be administered to adults. It is taken during an acute attack and not as a prophylactic therapy for headaches and migraines.

Rizatriptan is taken in tablet or sublingual tablet form. A sublingual tablet is a tablet that is placed under 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 dosage of rizatriptan is around 10 milligrams, with liver or kidney function disorders only 5 milligrams should be prescribed. If the first symptoms of an impending migraine attack appear, an application should be taken immediately. Signs can be, for example, tiredness , sensitivity to light or an aura. 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 maximum daily dose of 20 milligrams should not be exceeded.

About 10-20 percent of patients may not respond to rizatriptan. In this case, the attending physician should consider an alternative drug.

Risks & side effects

Compared to other drugs in this drug class, rizatriptan is described as well tolerated. The most common side effects are nausea, dry mouth and thirst , hot flashes , tiredness, dizziness , muscle weakness or general weakness. Occasionally, undesirable side effects such as tachycardia and shortness of breath may occur. Rarely occurring side effects that can be described as life-threatening can be heart attack provocation and severe cardiac arrhythmias .

In principle, rizatriptan should always be taken with the individual medical history and medical history of the patient in mind. If there are previous illnesses such as high blood pressure , diabetes mellitus , peripheral vascular diseases or disorders of 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 for 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 and for pregnant women and breastfeeding mothers.

Taking different drugs of the same class of active ingredients and in combination with ergotamine derivatives uncontrollably increase the effect and increase the risk of side effects.

Even when discontinuing such a pharmacological substance, there is always a potentially increased risk of serotonin syndrome . A serotonin syndrome manifests itself with symptoms such as general restlessness , hallucinations , loss of coordination , increased heartbeat, blood pressure fluctuations , increased reflexes, nausea, vomiting, diarrhea and increased body temperature .

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Hello! I am Lisa Newlon, and I am a medical writer and researcher with over 10 years of experience in the healthcare industry. I have a Master’s degree in Medicine, and my deep understanding of medical terminology, practices, and procedures has made me a trusted source of information in the medical world.