SketchyPharm Blood and Inflammation.pdf - 01 Anticoagulants...

  • Tel Aviv Uni.
  • MED 101
  • Notes
  • DeanCrab520
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01 - Anticoagulants and ThrombolyticsIndirect thrombin inh.: - Unfractionated heparin - LMWH - Fondaparinux Direct thrombin inh.: - Direct thrombin inhibitors (DTI) - Direct Xa inhibitors- Warfarin Antiplatelet agents: - Aspirin - ADP rec. inh. (Thienopyridines)(Clopidogrel, ticagrelor, prasugrel) (Ticlopidine) - GPIIb/IIIa inh. (Abciximab, eptifibatide, tirofiban) - Cilostazol - DipyridamoleThrombolytics: - Alteplase - Reteplase - Tenecteplase - Streptokinase - Aminocaproic acid
Heparin, LMWH, fondaparinux, DTI, Xa inh.Fibrin clotThrombin (II)Fibrinogen fibrinFactor IIFactor XII IIaHeparinBinds ATIII inactivate IIa & XaMonitor PTT w/ heparinPTT measures intrinsic pathwayHeps for acute DVT & prophylaxisHeps for acute PE & prophylaxisHeps for acute MIAdminister Hep by IVS/E: Anti-(Hep-PF4) in hep-induced thrombocytopenia (HIT)Paradoxical thrombosisS/E: hypoaldosteronism hyperkalemia (RTA 4)S/E: osteoporosisProtamine sulfate (+) to reverse heparin (-) by binding to it.LMWHBinds ATIIIOnly inhibits Longer t1/2Renal insufficiency prolongs t1/2Heparins for pregnancy(-parin)LMWH less likely to cause HITFondaparinuxHigh spec. for ATIII Xa onlyVery low risk for HITBivalirudin(DTIs) For HITArgatroban Rivaroxaban ApixabanArgatroban DabigatranBind & inhibit Xa directlyOral adm.For anticoagulation in A. fib.
WarfarinVit. K activates clotting factorsPromotes γ-carboxylation of factors at the glutamic acid (GL) residueFactor II (thrombin)Factor VII first to by warfarinFactor IXFactor XVit. K epoxide (inactive) Vit. K (active) by Vit. K epoxide reductase (VKOR)Vit. K promotes γ-carboxylation of proteins C & S (anti-coag factors)WarfarinInhibits VKOR →↓active Vit. KOnset of action 8-12hrsOral adm.Long t1/2Monitor extrinsic effect using PTINR also used to measure Goal INR 2-3 for Tx.1° For long term anticoagulation in A. fib.For DVT & PE prophylaxisS/E: teratogenic; hemorrhage & abnormal bone formationS/E: protein C early hypercoagulable state skin necrosisCoadm. w/ heparin to prevent early hyper- coagulable state (heparin bridge)Reversal with Vit. K (delayed)Reversal with fresh frozen plasma (FFP) (immediate)S/E: drug-drug interaction d/t p450
Antiplatelet agentsDamaged endothelium exposes collagen & vWFPlatelet adhesion & activation by GP1B rec.Activated platelet degranulation

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