Blood drugs- Cardiovascular drugs ( Chapter 5/7) | Lipincott review
Thrombus=A clot that adheres to vessel wall
Embolus= intravascular clot that floats in the blood
Platelet aggregation inhibitor
Platelet Aggregation=Stimulation of Platelets by Thrombin, Collagen and ADP…
Activation of Phospholipase..liberate Arachidonic acid..Arachidonic acid convert into Prostaglandin H2(PG) by COX-1….PG H2 convert into TX A2 ..cause aggregation
Fibrinogen attach GP IIb/IIIa receptor..cross-linking..aggregation of platelets
Aspirin=inhibit COX1 by irreversible Acetylation of Serine…Arachidonic acid not
convert into TX A2…..inhibit aggregation
Also inhibit TX A2 Synthetase…activate Prostacyclin...furthur inhibition of
aggregation… Ibuprofen anatagonize platelet inhibition by Aspirin
Aspirin is only NSAID that irreversibly exhibit antithrombotic property…81mg of Aspirin
known as “Baby Aspirin”….S.E; bleeding time prolong
Clopidogrel, Ticlopidine, Prasugrul= MOA= irreversibly inhibit binding of ADP to
GP IIb/IIIa…inhibit activation of receptor…inhibit aggregation
T.E=Ticlopidine used in Ischemic attacks & Stroke prior to cerebral thrombotic..
Clopidogrel prevent Atherosclerosis after M.I, Stroke & best in ischemic disease
etc..Prasugrul in patients with unstable angina, non-ST elevated M.I, ST-elevated M.I
S.E= Ticlopidine cause TTP (thrombotic thrombocytopenia purpura),
Aplastic anemia(FDA black box warning), Neutropenia/Agranulocytosis
Clopidogrel=black box warning for poor metabolizer…prodrug
Prasugrul=Black Box warning for bleeding
Abciximab=monoclonal…inhibit GP llb/llla receptor…block binding of fibrinogen &
von Willebrand factor…inhibit aggregation…i.v for 24-48hr only
Eptifibatide &Tirofiban=Eptifibatide is Cyclic peptide….Tirofiban is non-peptide…
inhibit GP llb/llla receptor...inhibit aggregation..i.v …4hr effect
Dipyridamole= Coronory Vasodilator…increases cAMP…decrease
Phosphodiesterase.. DecreaseTxA2…inhibit aggregation...treat angina...inappropriate in elderly Pt.
Cilostazol=oral antiplatelet…Vasodilating…ϴ Phosphodiesterase lll….FDA approved for Intermittant Claudication…Non-FDA use in Beurger disease, Diabetes Mellitus with vascular sclerosis, Cerebral ischemia, ……..alter lipid profile..contra in C.H.F
BLOOD CO-AGULATION
Intrinsic pathway= XII XIIa , it activate XI XIa, it activate IX I IX a
It activate X Xa , it activate Prthrombin into Thrombin which convert
Fibrinogen into Fibrin
Extrinsic Pathway= VII VIIa X Xa Prothrombin thrombin Fibrinogen Fibrin
VIIa activate X, Xa activate Prothrombin into Thrombin, thrombin convert Fibrinogen into Fibrin
Inhibitors of Co-agulation
Protein C…Protein S….Antithrombin lll……Tissue factor
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