Chapter 16 xD Flashcards
Warfarin- MoA
Blocks reduction of oxidized vitamin K and prevents the post translational carboxylation of coagulation factors 2,7,9 and 10
Warfarin- Clinical use
Longterm treatment of thromboembolic disorders:
- DVT
- Thrombosis in pt with atrial fibrillation and artificial valve
- Treatment of MI
Warfarin- Adverse effects
- Bleedings
- Fetal warfarin syndrome
Warfarin- interactions
- Salicylates potentiate anticoagulant effect
- Rifampin and barbiturates induce CYP enzymes and decrease anticoagulant effect
- Cholestyramine decrease absorption
- GIMS FACE inhibit metabolism and increase risk of bleeding
Warfarin- Contraindication
Pregnancy
Heparin and related drugs- MoA
Heparin->Potentiate activity of endogenous antithrombin 3, an inhibitor of factor 2 and active factor 10
LMWHs and Fondaparinux->Inactivate factor 10
Heparin- Clinical use
- Acute thromboembolic disorders (Pulmonary or peripheral embolism, DIC, and DVT)
- Prevention of clotting (in arterial and heart surgery, blood transfusions, renal dialysis and during blood sample collection)
- Prevention of stroke due to emboli from acute atrial fibrillation
LMWHs- Clinical use
- Prevention of venous thromboembolism (associated with abdominal surgery or knee-or-hip replacement surgery)
- Prevent ischemic complication of unstable angina or NSTEMI
- Used in acute coronary syndrome and angioplasty
Fondaparinux- Clinical use
-Prevention of DVT in pt with hip-fracture, or hip-or knee replacement surgery
Heparin and related drugs- Adverse effects
Heparin->Bleeding, thrombocytopenia, and hyperkalemia
LMWHs->Bleeding, and thrombocytopenia
Fondaparinux-> Bleeding
Bivalirudin, Argatroban and Dabigatran- MoA
Inhibit thrombin
Bivalirudin- Clinical use
Prevent thrombosis in pt with UA or acute MI (including those undergoing coronary angioplasty and stent insertion)
Argatroban- Clinical use
Treatment of thrombosis in Pt with HIT or undergoing PCIs for MI
Dabigatran- Clinical use
- Reduce risk of stroke and PE in pt with nonvalvular atrial fibrillation
- Prevention of DVT in pt undergoing hip-replacement surgery
Dabigatran- Adverse effect
- Increased risk of bleeding
- Dyspepsia and gastritis
Apixaban, Edoxaban and rivaroxaban- MoA
Inhibit active factor 10
Apixaban, Edoxaban and rivaroxaban- Clinical use
- Reduce risk of stroke and systemic embolization in pt with nonvalvular atrial fibrillation
- Prevention of DVT and PE in pt undergoing knee-or hip replacement surgery
Apixaban, Edoxaban and rivaroxaban- Adverse effects
Bleeding
Aspirin- MoA
Irreversible inhibition of COX and the synthesis of prostaglandins from arachidonic acid
Aspirin- Clinical use
-Prevention of thromboembolic diseases (MI, stroke,
chronic limb ischemia etc.)
Aspirin- adverse effects
GI bleeding and peptic ulcers, renal and hepatic dysfunction, lithium toxicity, hyperkalemia, platelet inhibition, premature closure of ductus arteriosus and Reye syndrome
Aspirin- interactions
- Increases hypoglycemic effect of sulfonylureas
- Increases risk of GI bleeding and ulcers associated with methotrexate and valproate
- Inhibits uricosuric effect of probenecid
Dipyridamole- MoA
It leads to coronary vasodilation and inhibition of platelet aggregation by blocking platelet uptake of adenosine
Dipyridamole- Clinical use
- Used with aspirin in stroke prevention
- Produce vasodilation in myocardial perfusion imaging in pt with CAD
Dipyridamole- Adverse effects
GI distress, headache and rash
Cilostazol- MoA
Vasodilation and platelet inhibition by inhibition of type 3 PDE and thus inhibition of cAMP breakdown
Cilostazol- Clinical use
-Treatment of intermittent claudication (pain and weakness in limbs due to arterial occlusion)
Cilostazol- Adverse effects
Headache
Clopidogrel, prasugrel, ticagrelor and cbangrelor- MoA
Inhibit platelet ADP receptors which inhibit activation of GP-2b/3a receptors and prevents ADP-induced platelet aggregation
Clopidogrel, prasugrel, ticagrelor and cbangrelor- Clinical use
- Prevention of MI and stroke
- Prevention of thrombosis in sickle cell anemia, PCI and claudication
Clopidogrel, prasugrel, ticagrelor and cbangrelor- Adverse effects
Bleeding, GI distress, hypercholesterolemia and neutropenia
Clopidogrel- interactions
-PPIs (Omeprazole) inhibit clopidogrel activation by CYP
Abciximab, Tirofiban and Eptifibatide- MoA
Inhibitors of platelet GP-2b/3a receptors and platelet aggregation
Abciximab, Tirofiban and Eptifibatide- Clinical use
Prevent thrombosis in pt undergoing angioplasty and stent replacement
Abciximab, Tirofiban and Eptifibatide- Adverse effects
Bleeding
Vorapaxar- MoA
Occupies PAR-1 receptors, and inhibits thrombin access to its target receptor and thus prevents thrombin-mediated platelet aggregation
Vorapaxar-Clinical use
Reduce thrombotic cardiovascular events
Vorapaxar-Adverse effects
Bleeding
Thrombolytic agents- names and MoA
Reteplase, alteplase, streptokinase, tenecteplase and anistreplase
-They are recombinant forms of human t-PA which convert plasminogen to plasmin. Plasmin lead to clot dissolution
Thrombolytic agents- Clinical use and adverse effects
- Used to treat thromboembolic diseases
- Adverse effect is bleeding
Stop bleedings caused by:
-Warfarin, Heparins, Dabigatran and Fibrinolysis
Warfarin->Phytonadione
Heparins->Protamine sulfate
Dabigatran->Idarucizumab
Fibrinolysis->Aminocaproic acid
Contraindications to thrombolytics
Hemorrhage, hemophilia, hypertension, hypersensitivity, pregnancy, and Trauma/surgery (HHHHPT)
