Ticagrelor
Class
P2Y12 receptor antagonist
Indications
- Prevention of atherothrombotic events
- ACS – DAPT with aspirin
- Revascularization procedures
Pharmaceutics
Tablet 60mg/90mg
Dose
PO: 180mg load then 90mg BD
Offset
Discontinue 5 days prior to surgery
MoA
Reversible, non-competitive binding to P2Y12 receptor
Prevents ADP-mediated P2Y12 dependent platelet activation and aggregation
Increases local endogenous adenosine levels by inhibition of equilibrative nucleoside transporter-1 (ENT-1)
PD
CVS
Platelet aggregation inhibition
PK
A
PO absorption within 2-4hrs, OBA 36%
D
99% protein bound, VD 87.5L
M
Extensive metabolism by CYP3A4 with active metabolites
E
Minimal renal elimination, mainly biliary elimination of active metabolite, t½ ~8hrs
No dose adjustment required for renal impairment
Adverse Effects
Bleeding, TTP, hyperuricaemia, dyspnea, gout, bradyarrhythmias, syncope, hypotension, GIT effects – nausea, diarrhoea, hypersensitivity reactions including angioedema, central sleep apnea
Interference with platelet function test for HITS – false negative results due to inhibition of P2Y12 receptor
Contraindications
Active pathological bleeding, history of intracranial haemorrhage, severe hepatic impairment
Discontinue 5-7 days prior to surgery
Drug Interactions
Co-administration with strong CYP3A4 inhibitors (diltiazem, ketaconazole) → ↑effects of ticagrelor
NSAIDS/anticoagulant/PPI – decrease its efficacy
Monitoring
Generally not performed
Reversal
Not dialysable
Platelet transfusion