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Pharmacology of Ticagrelor; Overview, Pharmacology, Dosage, Uses, Mechanism of action, Effects
Ticagrelor is an antiplatelet medication used to reduce the risk of cardiovascular events in patients with acute coronary syndrome (ACS) or a history of myocardial infarction (MI)
. Here's a detailed overview of its pharmacology:
Mechanism of Action
Ticagrelor is a P2Y12 receptor antagonist that works by inhibiting platelet activation and aggregation
. Unlike clopidogrel, ticagrelor is a direct-acting, reversible inhibitor that does not require metabolic activation
.
Pharmacokinetics
Absorption: Ticagrelor is rapidly absorbed after oral administration
.
Distribution: It has a volume of distribution of approximately 87 liters
.
Metabolism: Ticagrelor is metabolized in the liver primarily by the enzyme CYP3A4
.
Elimination: The half-life of ticagrelor is about 7 hours, and its active metabolite has a half-life of about 9 hours3
. Approximately 26% of the drug is excreted in urine, and 58% in feces
.
Indications
Ticagrelor is indicated for:
Reduction of cardiovascular death, MI, and stroke in patients with ACS or a history of MI
Reduction of the risk of a first MI or stroke in high-risk patients with coronary artery disease (CAD)
.
Dosage and Administration
Loading Dose: 180 mg orally, followed by a maintenance dose
.
Maintenance Dose: 90 mg orally twice daily for the first year after an ACS event, then 60 mg orally twice daily thereafter
.
Combination with Aspirin: It is usually administered with a daily maintenance dose of aspirin (75-100 mg)
.
Side Effects
Bleeding: The most common side effect, which can be severe
.
Dyspnea: Shortness of breath is a distinctive adverse effect associated with ticagrelor
.
Allergic reactions: Including rash and pruritus.
Contraindications
Active bleeding or history of bleeding disorders.
Severe hepatic impairment.
Pregnancy and breastfeeding (unless the potential benefit outweighs the risk).
#Ticagrelor
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