Ticagrelor is an antiplatelet drug that prevents heart attacks and strokes in those who are at high risk for heart disease. It helps to avoid blood clots in those who have acute coronary syndrome and have had stents placed in their heart arteries. A heart attack occurs when a blood clot blocks blood flow to the heart. This type of arterial blockage is typically caused by the accumulation of cholesterol, fat, and other compounds that form plaque in the arteries that supply the heart. A heart attack can include chest discomfort, upper body pain, sweat, nausea, tiredness, and trouble breathing.
It prevents blood clots from developing in blood arteries by acting as a blood thinner. In the arteries, clots are created when platelets, a kind of blood cell, group together. On the other hand, those who are prone to heart attacks or strokes may have a clot formed when platelets aggregate within blood vessels that are already congested. When a clot blocks blood flow to the brain or heart, it can cause a heart attack or stroke. By making platelets less sticky, ticagrelor slows down the blood clotting process. It was approved by the European Medicines Agency in 2010 and the Food and Drug Administration in 2011.
BRAND NAMES:
Brilique – Ticagrelor is one of its active components. It comes in tablet form and is used to lower the risk of heart attacks and strokes as well as prevent blood clots.
MECHANISM OF ACTION
Ticagrelor inhibits platelet activation and aggregation by reversibly interacting with the platelet P2Y12 adenosine diphosphate receptor to prevent signal transduction.
PHARMACOKINETICS
ABSORPTION
After oral administration of ticagrelor, the bioavailability is 36%. The active metabolite of ticagrelor reaches a Tmax of 3.0 hours.
DISTRIBUTION
The volume of distribution of ticagrelor is 88L.
METABOLISM
Ticagrelor was metabolized largely by CYP3A4 to produce the primary active metabolite. CYP3A5 metabolizes it to a lower amount. Ticagrelor and its primary active metabolite are limited P-gp substrates and inhibitors.
EXCRETION
Ticagrelor is excreted through urine and feces.
PHARMACODYNAMICS
Ticagrelor is a P2Y12 receptor antagonist that prevents the formation of a thrombus, lowering the risk of myocardial infarction and ischaemic stroke. It has a modest duration of effect because it is administered twice a day and a broad therapeutic index due to high single doses are easily tolerated.
DOSAGE AND ADMINISTRATION
Ticagrelor comes as a tablet that can be taken orally. It is usually taken with or without food two times a day.
Ticagrelor is available in the form of a tablet with strengths of 60 mg and 90 mg.
DRUG INTERACTIONS
Drug interactions with ticagrelor may include
- Antidepressants: citalopram, nefazodone
- Blood thinners—Warfarin
- Antibiotics: rifampicin, clarithromycin
- HIV drugs: ritonavir
- Anti-epileptic drugs—phenytoin
- Heart problems: digoxin
CONTRAINDICATIONS
Contraindications of ticagrelor were hypersensitivity, a history of intracranial hemorrhage, and active pathologic bleeding.
SIDE EFFECTS
Side effects of ticagrelor may include
- Nausea
- Dizziness
Serious side effects of ticagrelor may include
- Rash
- Chest pain
- Shortness of breath
- Swelling of the face
- Irregular heartbeat
OVERDOSE
Symptoms of overdose may include
- Irregular heartbeat
- Diarrhea
- Nausea
- Vomiting
- Bleeding
TOXICITY
ECG monitoring is one of the supportive and symptomatic treatments for overdose. Due to its high protein binding, ticagrelor is unlikely to be eliminated from the blood by dialysis.
