Ticagrelor
General
- Type: Antiplatelet
- Dosage Forms: Pill
- Common Trade Names: Brilenta
Adult Dosing
- ACS: 180mg (two 90mg tablets) loading dose
- PO vs OG vs NG (depending on mental status)
- ACS patients who have received a loading dose of Clopidogrel may be started on Ticagrelor
- Maintenance: 90mg twice daily
Pediatric Dosing
- Undetermined
Special Populations
- Pregnancy Rating: Category C
- Lactation: Undetermined
- Renal Dosing
- Adult
- No adjustment necessary
- Pediatric
- Adult
- Hepatic Dosing
- Adult
- Mild impairment - no adjustment necessary
- Moderate impairment - not defined but use caution as undergoes hepatic metabolism
- Severe impairment - avoid use
- Pediatric
- Adult
Contraindications
- Allergy to class/drug
- History of:
- Intracranial hemorrhage
- Active pathological bleeding, such as peptic ulcer or intracranial hemorrhage
- Severe hepatic impairment
Adverse Reactions
Serious
- Major coronary artery bypass graft (CABG)–related bleeding (86%)[1]
- Digoxin: Because of inhibition of the P-gp transporter, digoxin concentrations may be elevated, increasing the risk of toxicity.
- Monitor digoxin concentrations with initiation of, or any change in, ticagrelor therapy
Common
- Cardiovascular
- Ventricular pause (6%)
- Atrial fibrillation
- Hypertension (4%)
- Chest pain
- Hypotension(3%)
- CNS
- Headache (7%)
- Dizziness (5%)
- Fatigue (3%)
- Syncope/pre-syncope/loss of consciousness (2%)
- GI
- Diarrhea, nausea (4%).
- Hematologic
- Non–CABG-related bleeding (9%)
- Pulmonary
- Dyspnea (14%)
- Cough (5%)
Pharmacology
- Half-life: 7 hours (ticagrelor) and 9 hours (active metabolite)
- Metabolism: liver (CYP3A4)
- Excretion: 26% excreted in urine (less than 1% as ticagrelor and the active metabolite); 58% excreted in feces
- Mechanism of Action: Reversibly binds to the P2Y 12 class of adenosine diphosphate (ADP) receptors on platelets to prevent signal transduction and platelet activation
See Also
References
- ↑ http://www.drugs.com/cdi/ticagrelor.html -- Accessed April 2015
Ticagrelor: Drug information. UpToDate. www.uptodate.com. Accessed April 2, 2019.