Ticagrelor

Benjamin Clanner-Engelshofen is a freelance writer in the medical department. He studied biochemistry and pharmacy in Munich and Cambridge / Boston (USA) and noticed early on that he particularly enjoyed the interface between medicine and science. That is why he went on to study human medicine.

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The active ingredient ticagrelor is a so-called platelet aggregation inhibitor (TAH), i.e. it prevents the blood platelets (thrombocytes) from accumulating and blood clots from forming in the vessels. It is often combined with acetylsalicylic acid (ASA), which also inhibits blood clotting, but in a different way. This combination of active ingredients is called "dual platelet inhibition". Here you can read more about the effects and use of ticagrelor, dosage and side effects.

This is how ticagrelor works

When blood leaks from the body's vasculature, the body tries to stop the loss of blood. To do this, blood clotting is activated, which causes clots to form precisely at the affected area in order to seal the leak. The blood platelets, which make up the third type of blood cell in addition to the red and white blood cells, play an important role in this. The task of the blood platelets is to detect a vascular leak and subsequently initiate clotting. To do this, the platelets attach themselves to the injured area with the help of other proteins in the blood and are activated, thus initiating everything in order to close the vessel as quickly as possible. They also release messenger substances (such as thromboxanes and ADP) that attract and activate further blood platelets. The blood platelets that are released also have docking points (receptors) for these messenger substances - they activate themselves even more strongly. One speaks of a “positive feedback loop”. In the further course of this "coagulation cascade", the clot is cross-linked with the "adhesive" fibrin and thus strengthened.

If this process is disturbed by various factors, so that it can be activated excessively sensitively, one speaks of a coagulation disorder. Then larger clots can also form in the bloodstream, which then clog important vessels that supply the brain or the heart, for example.

To avoid this, medication - for example with ticagrelor - intervenes in the coagulation process, often specifically with the blood platelets because of their central role:

The anticoagulant ticagrelor specifically inhibits the receptor for ADP, which suppresses the activation of further blood platelets and the further "self-activation" of the platelets. The combination of ticagrelor with ASA (acetylsalicylic acid) in dual platelet inhibition also prevents the formation of thromboxanes, which further reduces the coagulation ability of the blood platelets.

Ticagrelor uptake, breakdown and excretion

After taking ticagrelor, about a third of the active ingredient is absorbed from the intestine into the bloodstream, where it reaches the maximum blood level after an hour and a half. The anticoagulant is partly converted in the liver by the cytochrome P450 enzyme system into another active substance. Both ticagrelor itself and its metabolite are excreted from the body to a small extent with the urine, but mainly with the stool. After seven to eight hours, the ticagrelor blood level will have fallen to about half the dose taken.

When is ticagrelor used?

The active ingredient ticagrelor is approved in combination with ASA for the prevention of clot formation in adult patients who have already had an occlusion (heart attack) or massive constriction (angina pectoris) of the coronary arteries.

Ticagrelor must be taken long-term in order to permanently suppress clot formation.

This is how ticagrelor is used

At the beginning of treatment with ticagrelor, 180 milligrams of the active ingredient are taken, then 90 milligrams twice a day with an interval of about twelve hours. It can be taken with or without a meal.

If the patient has difficulty swallowing or is fed through a gastric tube, the ticagrelor tablet can be crushed and given as a suspension in water.

If a dose is missed, it should not be taken afterwards. Just take the next dose at the usual time. It is not allowed to take two doses at the same time!

What side effects does ticagrelor have?

Ticagrelor causes nosebleeds, shortness of breath, bleeding in the gastrointestinal tract, bruising, bleeding of the skin and subcutaneous tissue in one to ten percent of patients.

Occasionally, ticagrelor side effects such as dizziness, headache, skull bleeding, eye bleeding, bloody cough, vomiting blood, gastrointestinal ulcer, oral bleeding, rash, itching, urinary tract and vaginal bleeding are also present Mucous membrane as well as a weakening of the immune system.

What should be considered when taking ticagrelor?

Because of the diverse interactions of ticagrelor with other drugs, the therapy should be checked accordingly before starting treatment.

Ticagrelor is broken down in the liver by the enzyme cytochrome P450 3A4, which also breaks down many other active substances in the body. Some of these agents can block the enzyme, which increases the levels of ticagrelor in your blood. These active ingredients include, for example, antibiotics (clarithromycin, metronidazole, chloramphenicol), anti-fungal agents (fluconazole, ketoconazole, itraconazole), HIV drugs (ritonavir, indinavir, nelfinavir) and many herbal remedies (ginseng, valerian, grapefruit juice).

Conversely, some substances can increase the amount of the enzyme cytochrome P450 3A4, thereby increasing the breakdown of ticagrelor. This applies, for example, to drugs against epilepsy and seizures (phenytoin, carbamazepine, phenobarbital), some foods (ginger, garlic, licorice) and the herbal antidepressant St. John's wort.

Since the data on the use of ticagrelor during pregnancy and breastfeeding are limited, the anticoagulant should not be used during this time. The same applies to children and young people under the age of 18.

How to get medication with ticagrelor

Preparations with the active ingredient ticagrelor require a prescription and are therefore only available in pharmacies after a doctor's prescription.

Since when is ticagrelor known?

The anticoagulant ticagrelor was developed by scientists at the pharmaceutical company AstraZeneca as the first active ingredient to inhibit the activation of blood platelets by ADP. It was launched on the European market in 2011. The novelty and the considerable additional benefit of the active ingredient were also recognized by the Federal Joint Committee, which sets the fixed prices for drugs in Germany. For this reason, preparations with the active ingredient ticagrelor are comparatively expensive, but have the advantage that they can reduce mortality after a heart attack more than previous therapies.

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