Half-Life of Ticagrelor (Brilinta)
The half-life of ticagrelor (Brilinta) is approximately 7 hours, while its active metabolite has a half-life of about 8.5 hours. 1, 2
Pharmacokinetic Properties
Ticagrelor has several important pharmacokinetic characteristics that distinguish it from other P2Y12 inhibitors:
- Absorption: Rapid absorption with median time to peak plasma concentration of 1.3-2 hours 2
- Active metabolite: AR-C124910XX forms quickly (peak at 1.5-3 hours) and contributes to the antiplatelet effect 2
- Linear pharmacokinetics: Both ticagrelor and its metabolite show dose-proportional increases in concentration 2
- Metabolism: Unlike thienopyridines (clopidogrel, prasugrel), ticagrelor:
- Does not require hepatic bioactivation
- Acts directly on the P2Y12 receptor
- Binds reversibly rather than irreversibly 3
Clinical Implications of Ticagrelor's Half-Life
Dosing Considerations
- Requires twice-daily dosing due to its relatively short half-life 1
- Missing doses significantly increases thrombotic risk due to the reversible binding mechanism 1
Perioperative Management
- Discontinuation timing: Unlike irreversible agents that require 5-7 days, ticagrelor should be discontinued 3-5 days before elective procedures 1, 3
- Bleeding management: The reversible nature of ticagrelor means:
Comparison to Other P2Y12 Inhibitors
| Agent | Mechanism | Binding | Half-life | Recovery Time |
|---|---|---|---|---|
| Ticagrelor | Direct-acting | Reversible | 7-8.5 hours | 3-5 days |
| Clopidogrel | Prodrug | Irreversible | Variable | ~5 days |
| Prasugrel | Prodrug | Irreversible | 7 hours (active metabolite) | ~7 days |
| Cangrelor (IV) | Direct-acting | Reversible | 3-5 minutes | 60 minutes |
Management Considerations
Bleeding Events
- The 1 exception among antiplatelet agents is ticagrelor, a reversible platelet inhibitor with a half-life of 7 to 9 hours 3
- For bleeding management:
- Consider tranexamic acid to reduce bleeding
- Apply local hemostatic measures appropriate to the bleeding site
- Avoid relying solely on platelet transfusions 1
Missed Doses
- If remembered within 12 hours of the usual time, take the missed dose immediately
- Resume regular twice-daily schedule
- If more than 12 hours have passed, skip the missed dose and take the next dose at the regular time 1
Practical Implications
The relatively short half-life of ticagrelor (7 hours) has important clinical implications:
- Requires strict adherence to twice-daily dosing
- Allows for faster recovery of platelet function compared to irreversible agents
- Enables more flexibility in perioperative management
- May provide advantages when rapid cessation of antiplatelet effect is needed (e.g., before urgent surgery)
The pharmacokinetic profile of ticagrelor represents an important advance in antiplatelet therapy, offering more predictable and consistent platelet inhibition with the potential for more flexible management in clinical settings.