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36 Cards in this Set

  • Front
  • Back

Aspirin

Controls the balance between TXA2 in platelet and PGI2 in endothelium


TXA2 - decrease


PGI2 - increase


Through the inhibition of COX --> less PGH2


inactivates platelets irreversibly

Aspirin different doses

low 180 mg - prevent mini stroke


335 mg - reduce heart attack risk


>1000mg no effect due to inhibition of COS



Clinical use of aspirin

After MI


used with fibrinolytic drugs

ADP receptor antagonists (P2Y12 selective)

Ticlopidine


Clopidogrel


Prasugrel


Ticagrelor

Ticlopidine

irreversible antagonist of P2Y receptor (ADP receptor)


slow onset (3-7 days)

clinical uses of Ticlopidine

Reducing stroke risk- efficacy like aspirin



side effects of Ticlopidine

unexplained - rash, diarrhoea, neutropenia (loss of blood cells)

Clopidogrel

irreversible antagonist of P2Y receptor (ADP receptor)


used in combination with aspirin



Clinical uses of Clopidogrel

with aspirin


Reducing ischeamic stroke, MI and vascular death

side effects of Clopidogrel

Less than others - especially less neutropenia

Prasugrel

irreversible antagonist of P2Y receptor (ADP receptor)


faster onset and more efficacious than clopidogrel


more easily metabolised into active


less resistance

Side effects of Prasugrel

higher risk of bleeding as more easily metabolised to active metabolite in liver

Ticagrelor

reversible antagonist of P2Y receptor (ADP receptor)


similar efficacy to

clinical use of Ticagrelor

Reversibility is a clincal asset in situations


stent clinic (CPCI)

IIb/IIIa receptor antagonists

Tirifiban/ Abciximab


Tirofiban/ Eptifbatide



Tirifiban/ Abciximab

antibody fragment directed against the IIb/IIIa receptor


single administration due to immunogenicity


platelet function recovery in days

Clinical uses of Tirifiban/ Abciximab

In patients with high risk coronary angioplasty with aspirin and heparin

Tirofiban/ Eptifbatide

cyclic peptides ligands at the IIb/IIIa receptor


platelet recovery in hours


IV - (not long term oral = harmful)

Prostaglandin agonist

Epoprostemol - chemically unstable --> IV



Phosphodiesterase inhibitor

Dipyridamole - increase platelet cAMP levels

clinical use of Epoprostemol

used in patients undergoing haemodialysis where heparin is contraindicated


Clinical use of Dipyridamole

in conjunction with aspirin

Antiplatelet drug groups?

Aspirin


ADP receptor (P2Y) Antagonists


IIb/IIIa receptor antagonists


phosphodiesterase inhibitors


Prostaglandin agonist

Clinical uses of antiplatelet drugs

acute MI


risk of MI


after coronary bypass


unstable coronary syndromes


after coronary artery angioplasty


Transient cerebral ischeamic attack/ thrombotic stroke

Fibrinolytic agents

streptokinase

Recombinant tPA


Streptokinase

Increase conversion of plasminogen --> plasmin


Produced from streptococci


Action blocked after 4 days due to antibody production


One year must relapse before reuse

Recombinant tPA

more active at fibrin bound plasminogen sites - clot specific


Alteplase - short half life = infusion


Reteplase - longer = bolus

contraindications of fibrinolytic agents

Absolute - recent/ active bleeding; recent cerebral accident; invasive procedures




Relative - pregnancy; cardiopulmonary resuscitation ; trauma; bacterial endocarditis

side effects of fibrinolytic agents

GI haemorrage , stroke


allergic reactions, fever


burst of plasmin created by streptokinase can cause kinins --> hypotension

Clinical uses of fibrinolytic agents

acute MI


acute thrombotic stroke


clearing thrombus shunts/ cannulae


acute arterial thromboembolism

antifibrinolytic drugs

Tranexamic acid


Aproxinin




inhibit the activation of plasminogen

Tranexamic acid

inhibits activation of plasminogen


Oral and iv


used when increased risk of bleeding - dental extraction


side effects - nausea and vomiting

Aproxinin

proteolytic enzyme inhibitor of plasmin/ kallilerech?


Slow iv


Used in patients with high risk of blood loss during and after open heart surgery

Arterial thrombis

Anti platelet drugs




Aspirin, clopidogrel, Abciximab




reduce platelet activation/ clotting

Venous thrombis

anticoagulants




Heparin, Warfarrin




reduce effectiveness of clotting cascade


reduce formation of fibrin



life threatening thrombis

fibrinolytic




Alteplase




Activate plasminogen


Increase fibrin breakdown