Anti-Thrombotics (Anti-Coagulants & Anti-Platelets) Flashcards
Anti-Coagulants
= Blood thinners that delay blood clotting
DOACS = Warfarin, Rivaroxaban/Apixaban, Dabigatran
PARENTERAL = Heparin, LMWH (Dalteparin, Enoxaparin), Fondaparinux
* DOACS*
Direct Factor Xa (Protease) Inhibitors
Drugs = Rivaroxaban, Apixaban
Mechanism = inhibit liver-made Factor Xa (protease)
Factor Xa = cleaves prothrombin –> thrombin (CF)
Uses = VTE, PE, DVT, AF/Stroke
+ No blood test required for PT
- INC. risk of GI bleed = dark brown/black/red stools
Vitamin K Antagonist
Drug = Warfarin
Mechanism:
= Inhibits enzyme Vitamin K epoxide reductase
= Carboxylation of glutamic acid residues
= Inhibits PT (Factor II), CF’s (VI, IX, X) activation
Uses = DVT, PE, AF, Heart Valve replacement
+ Vitamin K antagonist
- INC. risk in bleeding (provide VK antidote)
- Low VK = high PT = INC. bleeding risk
PARENTERAL
Unfractioned Heparin (UFH)
= Mucopolysaccharides (short duration, rapid onset)
Mechanism:
= Bind to activate Factor Xa + thrombin
= Activate anti-thrombin III by INC. affinity for serine proteases
LMWH
Drugs = Enoxaparin, Dalteparin, Fondaparinux (SC injection)
Mechanism = bind to Factor Xa but not thrombin
Uses = VTE, DVT, hospital prophylaxis, PE, ACS
Difference between UFH & LMWH?
= UFH binds to Factor Xa and thrombin
= LMWH binds to Factor Xa only
Ant-Platelets
= Keep clots from forming by keeping blood clots from sticking together
Uses = MI, stent, CABG, TIA, Stroke
Aspirin
Mechanism:
= Irreversible COX-inhibitor (acetylates COX enzymes)
= Selectively inhibit thromboxane production
= Reduces platelet aggregation ability
Dose = 75mg/day
Uses = ACS, MI (75mg daily + 300mg LD), stroke
- GI tract irritation (give with PPI for long term)
- Increased bleeding risk
- Hypersentivity reactions
Clopidogrel
Mechanism:
= Irreversible purine antagonist
= Prodrug activated by CYP2C19 in liver
= Binds to P2Y2 receptor to block calcium induced release of ADP
Uses = ACS, stents, CVS, AF
- Bleeding, dyspepsia, diarrhoea
- (Prodrug) CYP2C19 interactions = DEC. efficacy (thus ovoid Omeprazole)
Ticagrelor
Mechanism:
= Reversible purine antagonist
= Binds to P2Y2 receptor at allosteric site
= Not a prodrug, so doesn’t need hepatic activation
+ Faster onset than Clopidogrel
+ First choice
+ Easier to stop pre-surgery
- Dyspnea, bleeding
Thrombolytics
Drugs = Alteplase, Streptokinase
Mechanism = convert plasminogen to plasmin (degrades fibrin strands)
Alteplase = selective for fibrin bound plasminogen
Statins
Drugs = Simvastan, Atorvastatin Mechanism: = Inhibit HMG-CoA Reductase = Prevents HMG-CoA --> Mevalonic acid conversion = Reduce cholsterol levels
+ Effective in evening time (once in evening)
- Muscle pain/cramps
- DON’T TAKE CLARYTHROMYCIN!
Which of the following drugs could be used to treat deep vein thrombosis?
Dalteparin