• Monday July 13,2020

rizatriptan

Rizatriptan is a drug of the drug class of triptans. This stimulates the serotonin receptors and is used in moderate to severe forms of migraine. It not only relieves pain but also has a positive effect on symptoms such as photosensitivity.

What is Rizatriptan?

Rizatriptan is used for moderate to severe forms of migraine.

The drug rizatriptan is a selective serotonin agonist for the treatment of cluster headache and migraine. Selective serotonin agonists are substances of pharmacology that can activate serotonin receptors. They thereby support the tissue hormones and neurotransmitters.

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

Rizatriptan is prescribed for the treatment of migraine and cluster headache. It does not only have a positive effect on the state of pain, but also relieves the other symptoms such as photosensitivity and eye flickering. This is achieved by narrowing the blood vessels in migraine-like headache (vessel angulation).

Pharmacological action

Rizatriptan is an approved drug in the triptans class of drugs. Triptans are called serotonin agonists. Serotonin agonists act by their pharmacological substance activating the signal transmission of the receptors of a cell. In rizatriptan, these are the 5-HT1D receptors. The irritation to these receptors leads to a narrowing of the intracranial (within the skull lying) blood vessels.

Furthermore, the activated stimulus transmission of receptors inhibits the secretion of vasoactive neuropeptides and inhibits central pain transmission in the brainstem. Neuropeptides are messengers in nerve tissue.

The drug intake of the drug rizatriptan is comparatively fast to other triptans. Within about 50 minutes, the maximum active ingredient is distributed in the blood plasma. As a result, the rizatriptan remains unchanged at about 45 percent in the systemic blood circulation and is absorbed from the circulation after two to three hours (half-life). When taking the drug 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 given to adults. It is taken in an acute attack and not as a prophylactic therapy for headache and migraine.

Rizatriptan is taken as tablets or sublingual tablets. A sublingual tablet is a tablet that is placed underneath the tongue and dissolves there. This has the advantage that the active ingredient is absorbed directly via the mucous membranes and thus reaches the bloodstream more quickly.

The standard dose of rizatriptan is about 10 milligrams, in disorders of liver or kidney function should be prescribed only 5 milligrams. If the first symptoms of an imminent migraine attack appear, an application should be taken immediately. Signs can be, for example, tiredness, photosensitivity or an aura. At these first signs, a single dose of 10 milligrams should be taken. If pain or other symptoms persist 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.

In about 10-20 percent of patients, they may not respond to rizatriptan. In this case, the treating physician should consider an alternative medicine.

Risks & Side Effects

Compared to other drugs in this class of active ingredients, rizatriptan is considered to be well tolerated. The most common side effects may include nausea, dry mouth and thirst, hot flashes, tiredness, dizziness, muscle weakness, or even generalized weakness. Occasionally, unwanted side effects such as palpitations and respiratory distress may occur. Rarely occurring, but life-threatening, side effects can be cardiac infarction provocation and severe cardiac arrhythmias.

Basically, rizatriptan should always be taken with due consideration of the patient's individual history and health history. If there are pre-existing conditions such as high blood pressure, diabetes mellitus, peripheral vascular diseases or disorders of the liver and kidney function, the intake of the drug is associated with significantly increased risks. Even women who are in the menopause or smokers belong to this risk group.

The drug is considered to be absolutely contraindicated in angina pectoris and patients who have suffered a heart attack or a stroke. Due to a lack of studies, the drug rizatriptan should not be prescribed in children, adolescents, in adults over the age of 65 and in pregnant women and nursing mothers.

The use of different drugs of the same class of drugs and in combination with ergotamine derivatives increase the effect of uncontrolled and increase the risk of side effects.

Even when discontinuing such a pharmacological substance there is always a potentially increased risk of serotonin syndrome. Serotonin syndrome is characterized by symptoms such as general agitation, hallucinations, loss of coordination, increased heart rate, blood pressure fluctuations, increased reflexes, nausea, vomiting, diarrhea and increased body temperature.

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