Generic Name

Ticagrelor

Precaution

Patients w/ increased risk of bleeding (e.g. patients who are likely to undergo surgery or invasive procedures). Patients at risk of bradycardic events; w/ history of asthma or COPD, hyperuricaemia or gouty arthritis. Pregnancy and lactation. Lactation: Unknown whether distributed in human breast milk; potential for serious adverse reactions in breastfed infants, a decision should be made whether to discontinue nursing or to discontinue drug, taking into account the importance of the drug to the mother

Indication

Prevention of thrombotic events, [cardiovascular death (CV), myocardial infarction (MI) and stroke] in patients with acute coronary syndromes (ACS) [unstable angina, non-ST elevation myocardial infarction (NSTEMI) or ST elevation myocardial infarction (STEMI)]; including patients managed with percutaneous coronary intervention (PCI), coronary artery bypass grafting (CABG).

Contra Indication

History of Intracranial Hemorrhage: Ticagrelor is not recommended in patients with a history of intracranial hemorrhage (ICH) due to a high risk of recurrent ICH in this population. Active Bleeding: Patients with active pathological bleeding eg, peptic ulcer or intracranial hemorrhage. Severe Hepatic Impairment: Patients with severe hepatic impairment because of a probable increase in exposure, and it has not been studied in these patients. Severe hepatic impairment increases the risk of bleeding because of reduced synthesis of coagulation proteins. Hypersensitivity (eg, angioedema) to ticagrelor or to any of the components.

Dose

N/A

Side Effect

>10% Dyspnea (13.8%),Bleeding 1-10% Headache (6.5%),Cough (4.9%),Dizziness (4.5%),Nausea (4.3%),Atrial fibrillation (4.2%),Hypertension (3.8%),Noncardiac chest pain (3.7%),Diarrhea (3.7%),Back pain (3.6%),Hypotension (3.2%),Fatigue (3.2%),Chest pain (3.1%),Syncope (1.7%) <1% Dyspena (0.9%) Bleeding Non-CABG related bleeds Total bleeds (major + minor) (8.7%) Major bleeds (4.5%) Fatal/life-threatening (2.1%) Fatal (0.2%) Intracranial (fatal/life-threatening) (0.3%) CABG related bleeds Total major bleeds (85.8%) Major bleeds when antiplatelet therapy stopped 5 days before CABG (75%) Fatal/life-threatening (48.1%) Fatal (0.9%)

Pregnancy Category

Mode of Action

Ticagrelor and its major metabolite reversibly interact with the platelet P2Y12 ADP-receptor to prevent signal transduction and platelet activation. Ticagrelor and its active metabolite are approximately equipotent.

Interaction

Aminocaproic acid or tranexamic acid &/or recombinant clotting factor VIIa may augment haemostatis. NSAIDs, oral anticoagulants &/or fibrinolytics, ketoconazole, clarithromycin, nefazodone, ritonavir, atazanavir, rifampin, dexamethasone, phenytoin, carbamazepine, phenobarb, simvastatin >40 mg, digoxin. Increased Cmax & AUC w/ cyclosporine.

Pregnancy Category Note

Pregnancy Available data from case reports on use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes Animal data Drug given to pregnant rats and pregnant rabbits during organogenesis caused structural abnormalities in the offspring at maternal doses about 5 to 7 times maximum recommended human dose (MRHD) based on body surface area; when given to rats during late gestation and lactation, pup death and effects on pup growth were seen at ~10 times the MRHD Lactation There are no data on presence of drug or metabolites in human milk, effects on breastfed infant, or on milk production Ticagrelor and its metabolites were present in rat milk at higher concentrations than in maternal plasma; when a drug is present in animal milk, it is likely that the drug will be present in human milk Breastfeeding is not recommended during therapy

Adult Dose

Oral Acute coronary syndrome Adult: Loading dose (following ACS event): 180 mg PO (two 90 mg tablets) Maintenance dose (for first year following ACS event): 90 mg PO BID Maintenance dose (after 1 year with history of MI): 60 mg PO BID Administer with aspirin: Initial aspirin loading dose of 325 mg, then maintenance dose of aspirin of 75-100 mg/day; DO NOT exceed aspirin dose of 100 mg/day. Hepatic Impairment Moderate to severe: Contraindicated.

Child Dose

N/A

Renal Dose

Renal impairment No dosage adjustment needed

Administration

May be taken with or without food.