Anticoagulants Flashcards
Argatroban given
IV
Dabigatran given
orally
Argatroban and dabigatron active on
Free thrombin?
fibrin bound thrombin?
Both?
Both
Used for treatment and prophylaxis of HIT
Monitor with PTT
Argatroban
Prodrug converted by esterases to active glucuronides. Not a P450 substrate (so less drug-drug interactions). Substrate for p-glycoprotein transport (rifampin decreases its levels). Caution in renal problems
Dabigatran
Inhibits phosphodiesterase increasing cAMP.
Always used in combo, no effect if given alone
Dipyridamole
Warfarin usually given in combo with __________ for prosthetic heart valves
dipyridamole
Clopidogrel, ticlopidine, and cangelor are
P2Y12 receptor inhibitors
Block ADP binding at P2Y12 receptors
Ticlopidine and clopidogrel
Prodrugs. Metabolites are __________ inhibitors of P2Y12 receptor
Ticlopidine and clopidogrel
Irreversible
Reversible inhibitor of P2Y12 given IV
Cangrelor
Preferred. Better safety profile and shorter duration of action
Clopidogrel
Peak action takes 5 days. Residual action for 72 hrs after stopped.
New plts have to be made to regain normal plt fn, which normally takes 7-14 days
Ticlopidine
Increased risk of TTP and agranulocytosis with
ticlopidine
Abciximab and eptifibatide are
Glycoprotein 3A/2B inhibitors
Abciximab and eptifibatide are __________ inhibitors of gp 2B/3A
Competitive, noncompetitive?
Irreversible, reversible?
Competitive
Reversible
Abciximab and eptifibatide inhibit
platelet crosslinking via fibrinogen
Do not use if major surgery or trauma in past 6 weeks, or concurrently with warfarin
glycoprotein 2B/3A inhibitors
alpha2-antiplasm binds _________ plasmin to inactive it
circulating
Circulating plasmin > alpha2-antiplasmin
Lytic state
Derived from beta-hemolytic strep. Binds 1:1 with plasminogen. Causes conformational change exposing catalytic site for conversion of 2nd plasminogen > plasmin
Streptokinase
Acts on fibrin bound and circulating plasminogen. May cause lytic state
streptokinase
Do not use if surgery/trauma in past 10 days. Or have had intracranial trauma
Streptokinase
Streptokinase complexed with human lys-plasminogen. Active site blocked by acyl group, which is removed by plasma enzymes
Anistreplase
More specific binding to thrombin
anistreplase
Tissue type plasminogen activator. More selective for fibrin bound plasminogen, so less of a lytic state
Alteplase (rt-PA)
Genetic derivative of alteplase
Tenecteplase
Has longer t1/2, greater fibrin specificity, and slower inactivation by PAI-1.
Tenecteplase
Inhibits plasminogen activation.
Aminocaproic Acid
Lysine analog. Competes for lys binding site on plasminogen and plasmin
Aminocaproic Acid
Argatroban and Dabigatran are
Direct thrombin inhibitors
