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# Ticagrelor (Brilinta)
## Overview
Ticagrelor is an orally active, direct-acting P2Y12 receptor antagonist. It reversibly binds to the P2Y12 receptor and prevents the activation of platelets by adenosine diphosphate (ADP).
## Primary Indications
* **Acute Coronary Syndrome (ACS):** To reduce the rate of thrombotic cardiovascular events, including cardiovascular death, myocardial infarction (MI), and stroke, in patients who have had an ACS.
* **Myocardial Infarction (MI):** In patients with a history of MI, ticagrelor is indicated to reduce the rate of thrombotic cardiovascular events in patients at high risk for such events.
## Adult Dosing
* **ACS:** 180 mg orally once as a loading dose, followed by 90 mg orally twice daily.
* **History of MI:** 60 mg orally twice daily.
## Pediatric Dosing
* The safety and efficacy of ticagrelor in pediatric patients have not been established.
## Dose Adjustments
* No dose adjustment is required for patients with hepatic impairment.
* No dose adjustment is required for patients with mild to moderate renal impairment.
* For severe renal impairment or end-stage renal disease (ESRD), consider the risks and benefits, as data are limited.
## Contraindications
* Hypersensitivity to ticagrelor or any component of the formulation.
* Active pathological bleeding.
## Adverse Effects
* **Bleeding:** The most common and serious adverse effect. This includes fatal bleeding, intracranial bleeding, and gastrointestinal bleeding.
* **Dyspnea:** May occur and can be severe.
* **Bradycardia:** Symptomatic bradycardia can occur.
* **Ventricular pauses:** Common and usually asymptomatic.
* **Hyperuricemia:**
* **Angioedema:**
## Key Drug Interactions
* **CYP3A4 Substrates:** Ticagrelor is a moderate inhibitor of CYP3A4. Avoid coadministration with strong CYP3A4 substrates with narrow therapeutic indices (e.g., simvastatin, lovastatin, atorvastatin, cyclosporine, tacrolimus, sirolimus). If coadministration is unavoidable, consider a lower dose of the CYP3A4 substrate.
* **CYP3A4 Inhibitors/Inducers:** Avoid strong CYP3A4 inhibitors. Use caution with strong CYP3A4 inducers.
* **Aspirin:** Concurrent use with aspirin is recommended in ACS patients, but increases bleeding risk. For patients with a history of MI, aspirin is used as an alternative to clopidogrel.
* **Other Antithrombotics:** Increased risk of bleeding.
* **UGT1A1 Inhibitors:** Ticagrelor is a substrate of UGT1A1. Avoid concomitant use with strong UGT1A1 inhibitors.
## Monitoring
* **Bleeding:** Monitor for signs and symptoms of bleeding (e.g., hematuria, melena, bruising, epistaxis).
* **Renal Function and Electrolytes:** Especially in patients with risk factors for renal impairment.
* **Uric Acid Levels:**
## Clinical Pearls
* Ticagrelor is a P2Y12 inhibitor and should be used in combination with aspirin unless contraindicated.
* The maintenance dose of 90 mg twice daily for ACS should be continued for at least 12 months.
* The maintenance dose of 60 mg twice daily for patients with a history of MI should be continued long-term.
* Discontinuation of ticagrelor therapy can increase the risk of thrombotic events. If ticagrelor must be discontinued, consider the risks and benefits of stopping therapy early.
* Ticagrelor does not require a loading dose for the 60 mg twice daily indication.
* Ticagrelor should be initiated as soon as ACS is diagnosed.
**Educational Disclaimer:** Always consult the most current prescribing information for ticagrelor to ensure the accuracy and completeness of this drug information. Local protocols and institutional guidelines may also apply.
