Anti-platelet agents Flashcards
Aspirin - Mechanism
Inhibits COX-1 synthesis of thromboxane A2
Low dose (81mg) is specific for anti-platelet activity - reaches highest concentrations in the portal vein, thus greater effect on circulating platelet COX-1 relative to tissue endothelial cell COX-2 (prostacyclin synthesis)
Aspirin - Pharmacokinetics
Once daily oral dosing
Hepatic elimination
Aspirin - Uses
Secondary prevention of MI and ischemic stroke
Acute MI & Unstable Angina (ACS)
Percutaneous Coronary Intervention
Aspirin - Adverse Reactions & DDIs
Dyspepsia
Nausea
Vomiting
GI bleeding
Increased bleeding risk with anticoagulants
Clopidrogel & Prasugrel - Mechanism
Platelet ADP P2Y12 receptor antagonist; interferes with ADP-induced platelet aggregation via irreversible receptor inhibition
Clopidrogel - Adverse Reactions & DDIs
Bleeding (P & T > C)
Dyspepsia
Gastritis
Headache
Use of proton pump inhibitors may decrease efficacy
Dipyridamole - Mechanism
Phosphodiesterase inhibitor; blocks degradation of cAMP - elevated cAMP levels potentiate prostacyclin’s anti-aggretory action
Aggrenox
Aspirin + Dipyridamole
Dipyridamole - Adverse Reactions
GI upset
Dizziness
Headache
Nausea
Abciximab - Mechanism
Fab fragment of humanized monoclonal antibody to IIb/IIIa receptors on platelets; prevents fibrinogen binding and subsequent platelet aggregation
Abciximab - Pharmacokinetics
Administered by continuous IV infusion
Ticagrelor - Mechanism
Reversible inhibition of platelet ADP (P2Y12) receptor; interferes with ADP-induced platelet aggregation
Clopidogrel, Prasugrel & Ticagrelor - Pharmacokinetics
Clopidogrel & Prasugrel - Once daily oral administration, hepatic metabolism to active metabolite via CYP450, renal/fecal elimination
Ticagrelor - Twice daily oral administration, hepatic metabolism to active metabolite
Ticagrelor - Adverse Reactions
Bleeding (P & T > C)
Dyspnea
Bradyarrhythmias
Clopidogrel, Prasugrel, and Ticagrelor - Uses
Acute MI & Unstable Angina (ACS)
Percutaneous Coronary Intervention
Eptifibatide
Cyclic peptide inhibitor platelet GIIb/IIIa receptor; prevents fibrinogen binding and subsequent platelet aggregation
Administered by IV infusion
Renal elimination
AR: Bleeeding
Use: Percutaneous Coronary Intervention
Dipyridamole - Uses
Secondary prevention of MI & Stroke
Tirofiban
Non-peptide inhibitor of Platelet IIb/IIIa receptor; prevents fibrinogen binding and subsequent platelet aggregation
Administered by IV infusion, renal elimination
AR: Bleeding
Use: Percutaneous Coronary Intervention