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# Ticagrelor
## Overview
Ticagrelor is an orally administered, direct-acting, reversible P2Y12 receptor antagonist used to prevent thrombotic events. It is a member of the cyclopentyltriazolopyrimidine (CPTP) class.
## Primary Indications
* **Acute Coronary Syndrome (ACS):** In combination with aspirin, to reduce the rate of cardiovascular events (including myocardial infarction and cardiovascular death) in patients with ACS.
* **Myocardial Infarction (MI):** Following MI with ST-elevation (STEMI) treated with percutaneous coronary intervention (PCI), in combination with aspirin, to reduce the rate of thrombotic cardiovascular events.
## Adult Dosing
* **ACS:**
* **Loading Dose:** 180 mg orally once.
* **Maintenance Dose:** 90 mg orally twice daily.
* Dosing should be continued for at least 12 months, or longer based on individual patient risk assessment and clinical guidance.
* **MI (STEMI) post-PCI:**
* **Loading Dose:** 180 mg orally once.
* **Maintenance Dose:** 90 mg orally twice daily.
* Dosing should be continued for at least 12 months, or longer based on individual patient risk assessment and clinical guidance.
## Pediatric Dosing
Dosing in pediatric patients has not been established.
## Dose Adjustments
* **Hepatic Impairment:** No dose adjustment is recommended in patients with mild to moderate hepatic impairment. Use with caution in severe hepatic impairment due to lack of data.
* **Renal Impairment:** No dose adjustment is recommended in patients with mild to severe renal impairment.
## Contraindications
* Active pathological bleeding.
* History of transient ischemic attack (TIA) or stroke.
* Known hypersensitivity to ticagrelor or any of its excipients.
## Adverse Effects
* **Most Common:** Bleeding (including fatal bleeding), dyspnea, bradycardia.
* **Serious:** Hemorrhage, ventricular pauses.
* **Other:** Bruising, contusion, increased creatinine, hyperuricemia.
## Key Drug Interactions
* **CYP3A4 Substrates/Inhibitors/Inducers:** Ticagrelor is a substrate of CYP3A4. Coadministration with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin) may increase ticagrelor exposure. Coadministration with strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin) may decrease ticagrelor exposure.
* **CYP3A4 Substrates with Narrow Therapeutic Index:** Avoid coadministration with potent CYP3A4 substrates with a narrow therapeutic index (e.g., simvastatin, atorvastatin).
* **P-glycoprotein (P-gp) Inhibitors:** Coadministration with P-gp inhibitors may increase ticagrelor exposure.
* **Aspirin:** Concomitant use is indicated for ACS and MI, but prolonged use beyond 12 months may increase bleeding risk without additional cardiovascular benefit. Low-dose aspirin is generally recommended, but higher doses may increase bleeding.
* **Other Antithrombotics:** Concomitant use with other antithrombotic agents (e.g., anticoagulants, other P2Y12 inhibitors, NSAIDs) increases the risk of bleeding.
## Monitoring
* **Bleeding:** Monitor closely for any signs or symptoms of bleeding.
* **Renal Function:** Periodic monitoring of serum creatinine may be useful, particularly in patients with renal impairment.
* **Cardiac Rhythm:** Assess for bradycardia, particularly in patients with pre-existing risk factors.
## Clinical Pearls
* Ticagrelor is a reversible P2Y12 inhibitor, unlike clopidogrel or prasugrel, which are irreversible. This reversibility may be beneficial in patients requiring urgent surgery.
* The maintenance dose of 90 mg twice daily should be taken for at least 12 months post-ACS or MI. Lowering the dose to 60 mg twice daily is approved for long-term secondary prevention in patients who have completed 12 months of treatment with 90 mg twice daily and are at high risk for ischemic events but low risk for bleeding.
* Dyspnea is a common side effect and is typically mild and transient. It does not necessitate discontinuation unless severe.
* Aspirin dose should be minimized when used concurrently, typically 75-100 mg daily, unless otherwise specified by clinical guidelines.
**Disclaimer:** This information is intended for healthcare professionals and does not substitute for professional medical advice. Always consult the most current prescribing information and relevant clinical guidelines for complete details.
