Ticagrelor

Ticagrelor is an active substance that is used to treat thromboembolic events such as a heart attack or stroke. It is a platelet aggregation inhibitor and belongs to the group of P2Y12 antagonists. It is usually administered in combination with acetylsalicylic acid. The advantage of ticagrelor is that it acts more quickly than other active substances.

Ticagrelor works by binding to the P2Y12-ADP receptor in the blood platelets (thrombocytes) and thus blocking the binding of ADP (adenosine diphosphate) to this receptor (antagonism). The binding of ADP to this receptor causes the blood platelets to clump together, thereby "thickening" the blood, which can be observed in cuts or small wounds and is also desirable. After activation of the receptor by ADP, the platelets change their shape and form protrusions (pseudopodia), whereby they adhere to each other and can thus cause blood to stop flowing in small wounds. This effect is disadvantageous in the blood vessels because clot formation (thrombus formation) in the blood vessels should be prevented so that they do not become blocked. In the case of a heart attack or stroke, however, it is precisely this thrombus formation that occurs and the blood vessel is partially(angina pectoris) or completely(heart attack or stroke) blocked by this clot (thrombus). However, this is prevented by blocking the P2Y12 receptor with ticagrelor. Ticagrelor is not only used in acute cases, but can also be used as a long-term therapy to minimize risk.

Ticagrelor is metabolized in the liver and excreted via faeces and urine. The bioavailability of the active ingredient, i.e. the percentage of the active ingredient available in the blood, is 36%. The half-life, i.e. the time the body needs to excrete half of the active substance, is around 8 hours. The maximum plasma concentration (Cmax), i.e. the maximum concentration of the active substance in the blood plasma (liquid cell-free part of the blood) is reached after about 1.5 hours.

Always take Ticagrelor exactly as described in the package leaflet or as advised by your doctor.

The usual recommended dose in acute cases is 180 mg once.

The recommended dose for long-term therapy is 90 mg twice daily in the first year after the thromboembolic event.

After one year, the recommended dose is 60 mg twice a day.

The following side effects may occur:

Very common:

• High uric acid levels in the blood
• Bleeding
• Feeling of shortness of breath

Common:

• Bruising
• Headache
• Dizziness
• Diarrhea
• Nausea
• constipation
• skin rash
• itching
• joint pain
• nosebleeds
• Increased and more frequent bleeding after operations or cuts
• Bleeding from the stomach lining
• Bleeding from the gums

Occasionally:

• allergic reactions
• Confusion
• Visual disturbances
• Bleeding from the vagina (independent of menstrual bleeding)
• Increased or prolonged menstrual bleeding
• Bleeding in joints and/or muscles
• Blood in the ear
• Internal bleeding

Frequency unknown:

• slowed heartbeat (bradycardia)

If the following side effects occur, please seek medical help immediately:

• Bleeding into the brain or inside the brain skull
  • Symptoms:
    • sudden possibly one-sided numbness in arms, legs or face
    • sudden confusion and speech difficulties
    • sudden coordination problems
    • sudden dizziness
• bleeding
  • Symptoms:
    • Unstoppable or prolonged bleeding
    • pink, red or brown urine
    • vomiting blood
    • Red or black stool
    • hemoptysis
• fainting
• Thrombotic thrombocytopenic purpura

Interactions may occur if the following medicines are taken at the same time:

• rosuvastatin
• simvastatin or lovastatin
• rifampicin
• phenytoin, carbamazepine and phenobarbital
• digoxin
• Ciclosporin
• Quinidine and diltiazem
• Beta-blockers and verapamil
• Morphine and other opioids
• "Blood thinners"
• Non-steroidal anti-inflammatory drugs (NSAIDs)
• Selective serotonin reuptake inhibitors (SSRIs)
• Ketoconazole
• Clarithromycin
• Nefazodone
• Ritonavir
• Atazanavir
• cisapride
• Ergot alkaloids

Ticagrelor must NOT be taken in the following cases

• in case of allergy to ticagrelor
• in case of acute bleeding
• previous cerebral hemorrhage
• severe liver disease
• if you are taking ketoconazole
• when taking clarithromycin
• when taking nefazodone
• when taking ritonavir and atazanavir

Ticagrelor is NOT recommended under the age of 18.

Ticagrelor should NOT be taken during pregnancy and breastfeeding unless your doctor considers it absolutely necessary.

Ticagrelor was first prescribed in 2003. The drug is marketed by the pharmaceutical company AstraZeneca. The active ingredient was approved in the EU in December 2010 and in the USA in July 2011.