Indications
Ticagrelor is prescribed for patients to mitigate the risk of cardiovascular events. Specifically, it is indicated for individuals with acute coronary syndrome or those with a history of myocardial infarction in order to reduce the likelihood of cardiovascular death, myocardial infarction, and stroke. Additionally, ticagrelor is used to lower the risk of an initial myocardial infarction or stroke in high-risk patients suffering·harmacodynamics
Ticagrelor functions as a P2Y12 receptor antagonist, playing·hibiting·hrombus formation, thereby decreasing·he risk of myocardial infarction and ischemic stroke. The medication has a moderate duration of action, necessitating·herapeutic index, as evidenced by the tolerability of high sing·hould be advised of potential side effects, including·he risk of bleeding·hythmias.
Absorption
When taken orally, ticagrelor demonstrates 36% bioavailability. Following·he maximum concentration (Cmax) of ticagrelor in the blood is 923 ng·hed within 1.5 hours (Tmax), and has an area under the curve (AUC) of 6675 ng·h/mL. Its active metabolite achieves a Cmax of 264 ng·h a Tmax of 3.0 hours and an AUC of 2538 ng·h/mL.
Metabolism
The metabolic pathways of ticagrelor involve several processes, although the complete structures of all metabolites are not entirely defined. Ticagrelor is primarily metabolized through dealkylation at position 5 of the cyclopentane ring·he active metabolite AR-C124910XX. This metabolite can undergo further glucuronidation or hydroxylation, affecting·her the cyclopentane ring·he alkyl chain. Additionally, ticagrelor itself can be subjected to glucuronidation, hydroxylation, and N-dealkylation to form AR-C133913XX, which can also be glucuronidated or hydroxylated.
Mechanism of Action
Ticagrelor functions as a P2Y12 receptor antagonist, engaging with the P2Y12 receptor which typically couples with Gαi2 and other Gi proteins to inhibit adenylyl cyclase activity. This receptor coupling plays a critical role in activating several pathways, including PI3K, Akt, Rap1b, and potassium channels, all of which contribute to hemostasis and facilitate platelet aggregation. By antagonizing the P2Y12 receptor, ticagrelor effectively decreases the formation of occlusive thromboses, thereby reducing the risk of myocardial infarction and ischemic stroke.
