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Ticagrelor- Structure and Mechanism of Action

Ticagrelor is a medication used by patients with heart diseases for the prevention of stroke, heart attack, and other life-threatening events. This drug is commonly used by people with acute coronary syndrome showing problems in blood supply to the coronary arteries. Ticagrelor is prescribed in cases where the chances for a heart bypass surgery are minimal.

Structure of the Ticagrelor compound

The Ticagrelor structure consists of a triazolopyrimidine that is an adenosine isostere. The ring of cyclopentane resembles ribose and the nitrogen-rich triazolo pyrimidine is similar to the nucleobase adenine.

The molecular formula of Ticagrelor is C23H28F2N6O4S and its molecular weight is 522.6.

A platelet aggression inhibitor is used to prevent thromboembolic events from occurring in patients with the acute coronary syndrome. Ticagrelor was developed for its P2Y12 receptor antagonist as an ADP derivative. It is an aryl sulfide, a hydroxy ether, a secondary amino compound, an organofluorine compound and a member of triazolopyrimidines.

Ticagrelor has a water solubility of approximately 10 ug/ml. It is also highly soluble in ethyl acetate. It is commonly sold in a solid form as a crystalline powder. It is observed that the Ticagrelor compound is canonicalized.

The Mechanism of Action of Ticagrelor

Similar to the clopidogrel, thienopyridines prasugrel and ticlopidine, the compound of Ticagrelor works by blocking the adenosine diphosphate receptors of the P2Y12 subtype. In contrast to several other antiplatelet drugs, the binding site of Ticagrelor is different from ADP. This makes it an allosteric antagonist, the blockage of which is irreversible.

Ticagrelor is a fast-action drug that is quickly absorbed from the gut and reaches its peak concentration after a period of 1.5 hours. The primary metabolite,  AR-C124910XX, quickly takes form via CYP3A4 by de-hydroxyethylation in the cyclopentane ring, which peaks at 2.5 hours.

Both Ticagrelor and AR-C124910XX are bound to proteins of plasma and are pharmacologically active. These plasma concentrations are linearly dependent on the sevenfold daily dose of 1260 mg. The metabolite is able to reach about 30 to 40 percent of Ticagrelor’s plasma concentration.

With the reversible Ticagrelor mechanism of action, it is known to act faster and shorter than Clopidogrel, which is also an oral antiplatelet medication. This means that it has to be taken twice a day instead of just once which poses a threat of compliance. But since its effects are quickly reversible, it can prove to be useful before surgery or in case any side effects are experienced.

 

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