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AnticoagAntithrombo
lecture 20 thorpe
| Question | Answer |
|---|---|
| aspirin | oral drug that inhibits plt aggregation by irreversible acetylation of COX1, blocks synthesis of TXA2 and inhibits endothelial COX and production of PGI2 which inhibits plt aggregation but those cells just make more b/c they are nucleated |
| therapeutic uses of ASA | MI prophylaxis in ppl 45 y/o and older, prevention of stroke in pts with h/o TIA, preventing occlusive CV dz in pts recently recovered from MIs or with unstable angina |
| clopidogrel (Plavix) | inhibit P2Y-12 ADP receptors irreversibly, disallows activation of GPIIb/IIIa by ADP. results in reduced fibrinogen/vWF binding, reduced plt aggregation |
| ticagrelor (Brilinta) | bind reversibly and directly to ADP receptors, thus has rapid onset and offset of action if pt needs to be discontinued quickly for surg |
| adverse effects of clopidogrel and prasugrel | rashes, diarrhea and neutropenia |
| therapeutic uses of clopidogrel and like drugs | reduces MI, stroke and vascular death in pts with ACS aka unstable angina and prior MIs |
| heparin | relatively strong sulfated mucopolysaccharide that interacts with antithrombin III and increases ability of it to neutralize factor Xa and thrombin; given IV when needed immediately, otherwise SQ with delay of 20 min to 1 hr |
| LMWH aka low molecular weight heparin | binds antithrombin III to inhibit factor X specifically; same as Lovenox or enoxaparin; used for prophylaxis NOT emergencies, given SQ every 12-15 hrs |
| protamine sulfate | reverses bleeding, which is known adverse effect of heparin or Lovenox use, by immediately killing heparin and somewhat LMWH |
| heparin-induced thrombocytopenia (HIT) | serious complication caused by generation of Ab to PF-4/heparin binding complex and causes plt activation and thrombocytopenia but life-threatening thrombosis |
| warfarin (Coumadin) | vit K antagonist that only works in vivo, inhibits synthesis of factors II, VII, IX, X in the liver; takes 48 hrs to reach full effect and lasts 2-5 days |
| drug interactions of Coumadin | cholestyramine resin interrupts enterohepatic circulation = small half-life; phenylbutazone displaces it from albumin in blood; P450 induces like barbiturates cause rapid clearance whereas acetaminophen lowers clearance; diuretics increase clearance |
| relationship btwn cephalosporins and Coumadin | kill off vitamin K producing bacteria in the gut and increase anticoagulant effect |
| reversal of Coumadin | give FFP immediately and vit K slowly |
| therapeutic uses of Coumadin | prevents venous thromboses, PEs after trauma or surg, tx for overt thrombosis, stop coagulation on artificial surfaces like prostheses |
| lepirudin | thrombin-binding protein, similar to what leech secreates into skin --> anticoagulant effect; approved for tx of HIT |
| tPA | recombinant human thrombolytic protein that stimulates the conversion of plasminogen that's bound to fibrin clots into plasmin that exerts its fibrinolytic activity; must be IV not oral |
| reversal of tPA | epsilon-aminocaproic acid (Amicar) or tranexamic acid, which are lysine analogs that block binding of plasmin to fibrin |