Please check your internet connection and try again.
# Ticagrelor
## Overview
Ticagrelor is a direct-acting, reversible P2Y12 receptor antagonist that inhibits platelet activation and aggregation.
## Primary Indications
* **Acute Coronary Syndromes (ACS):** In combination with aspirin, for the reduction of thrombotic cardiovascular events in patients with ACS (unstable angina, non-ST-elevation myocardial infarction, or ST-elevation myocardial infarction) [1].
* **Myocardial Infarction (MI):** In patients with a history of MI, ticagrelor in combination with aspirin is indicated to reduce the rate of cardiovascular death, myocardial infarction, and stroke [2].
## Adult Dosing
* **ACS:** 180 mg orally as a single loading dose, followed by 90 mg orally twice daily.
* **History of MI:** 60 mg orally twice daily.
* A daily maintenance dose of aspirin (75-100 mg) is recommended in combination with ticagrelor for both indications.
## Pediatric Dosing
Dosing for pediatric patients is not established.
## Dose Adjustments
* **Renal Impairment:** No dose adjustment is required in patients with mild, moderate, or severe renal impairment.
* **Hepatic Impairment:** No dose adjustment is required in patients with mild to moderate hepatic impairment. Ticagrelor has not been studied in patients with severe hepatic impairment.
## Contraindications
* **Hypersensitivity:** To ticagrelor or any excipient in the formulation.
* **Active Bleeding:** Patients with active pathological bleeding.
## Adverse Effects
* **Bleeding:** Dyspnea, bruising, epistaxis, gastrointestinal hemorrhage, hematuria.
* **Dyspnea:** Most commonly reported side effect, often transient.
* **Bradycardia:** Can occur.
* **Ventricular pauses:** May occur.
* **Hyperuricemia and renal dysfunction:** Can occur.
## Key Drug Interactions
* **CYP3A4 Inhibitors/Inducers:** Ticagrelor is a substrate of CYP3A4. Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) may increase ticagrelor plasma concentrations. Concomitant use with strong CYP3A4 inducers (e.g., rifampin, phenytoin) may decrease ticagrelor plasma concentrations.
* **CYP3A4 Substrates:** Ticagrelor is a moderate inhibitor of CYP3A4. Concomitant use with CYP3A4 substrates (e.g., simvastatin, lovastatin) may increase concentrations of these drugs.
* **Other Antiplatelet Agents:** Use with other antiplatelets (e.g., clopidogrel, aspirin) increases the risk of bleeding.
* **Anticoagulants:** Concomitant use with anticoagulants (e.g., warfarin, heparin) increases the risk of bleeding.
## Monitoring
* Monitor for signs and symptoms of bleeding.
* Assess for dyspnea.
* Consider baseline and periodic monitoring of uric acid and renal function.
## Clinical Pearls
* Ticagrelor is a reversible P2Y12 inhibitor, unlike clopidogrel which is irreversible. This may offer advantages in specific clinical situations, such as after a PCI or if surgery is planned.
* Due to the risk of bleeding, ticagrelor should be used cautiously in patients with a high risk of bleeding, such as those with a history of stroke or transient ischemic attack, or those taking concomitant anticoagulants.
* The 60 mg twice daily dose is indicated for long-term maintenance in patients with a history of MI, 1 year or more after ACS or after stent implantation, provided they have not had a recent ACS or stent implantation. Transition to the 60 mg dose should occur after at least 1 year of treatment with 90 mg twice daily, or earlier if clinically appropriate.
***
*Disclaimer: This information is intended for healthcare professionals and is not a substitute for professional medical advice. Always consult the most current prescribing information and clinical guidelines for complete details. Drug information can change rapidly, and it is the responsibility of the prescriber to ensure that the information used is current and accurate.*
