Thrombolytics Flashcards
Therapeutic uses
- Venous thromboembolism
- Unstable angina
- Acute MI
- Stroke
- Prevent thrombosis during angioplasty
Aspirin MOA
- Acetylsalicylate
- Irreversible COX inhibitor
- Antipyretic, analgesic and anti-inflammatory
Aspirin adverse effects
- Bleeding
- GI disturbances
- Tinnitus
- :Low dose (anti-platelet effect) vs. high dose (anti-platelet, anti-inflammatory)
ADP Receptor antagonists
Clopidogrel, Prasugrel, Ticlopidine
ADP receptor antagonists MOA
-Irreversible ADP receptor antagonists that prevent activation of ADP receptor
ADP receptor antagonist distribution
- Lasts the life of the platelet
- Oral drugs w/duration of days
ADP receptor antagonist uses
- During stenting
- For patients that don’t tolerate aspirin
ADP receptor antagonist adverse effects
- BLEEDING
- Nausea, diarrhea
- Rash
- Severe leuopenia
- THROMBOTIC THROMBOCYTOPENIC PURPURA (TTP) (Rare)
Which of the ADP receptor antagonists have fewer side effects
Clopidogrel and prasugrel
Which ADP receptor antagonist requires activation via CYP2C19
Clopidogrel
GPIIb/IIIa receptor inhibitors MOA
- Prevent binding of adhesive glycoproteins (ex. fibrinogen and vWF) to activated platelets.
- Inhibits the final common pathway for platelet aggregation
GPIIb/IIIa receptor names inhibitor
Abciximab
Eptifibatide
Tirofiban
GPIIb/IIIa receptor inhibitors uses and given via?
- Used with aspirin and heparin during angioplasty
- For acute coronary syndromes
- Given IV
GPIIb/IIIa receptor inhibitors adverse effects
- Bleeding
- Thrombocytopenia
Dipyridamole
Increases cAMP and inhibits platelet aggregation
- Little or no benefits by itself 9used in combination w/ aspirin or warfarin)
- Vasodilator
- Adverse effect: headache
Thrombin inhibitors given?
Paraenterally (except Dabigatran etexylate given orally!!)
Indirect Thrombin inhibitors drug names
- Unfractionated heparin (high molecular weight)
- Low molecular weight heparin
- Fondaparinux
Direct thrombin inhibitors
Bivalrudin
Argatroban
Dabigatran etexylate
Indirect thrombin inhibitors MOA
- Bind to antithrombin to have effect
- Allows antithrombin to do a better job
- activity against thrombin is size dependent
Antithrombin
Inactivates both thrombin and factor Xa
Heparin
- Binding to plasma proteins, platelets, macrophages, and endothelial cells limit bioavailability to account for variable anticoagulant response.
- Stabilizes Xa and thrombin and prevent them from doing their job.
Heparin MOA
- Binds antithrombin
- Induces conformational change in reactive center loop of antithrombin
- Accelerates interaction with factor Xa.
- Heparin must simultaneously bind antithrombin and thrombin
