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24 terms

anti-thrombotic drugs

clot this!!
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aspirin
MOA: irreversible plt effect; dec plt aggregation by stopping thromboxane a2-> stops vasoconstriction
USE: analgesia, anti pyretic, ami prophylaxis, ACS, TIA/CVA
ADRs: dyspesia, GI ulceration; bleeding (dbls gi bleed risk); hepatotoxicity, SNHL, ARF, bronchospasm, reye's syndrome
don't use H2RAs to stop ulcers; use PPIs instead
ticlopidine
anti-plt;
OFF MARKET
clopidogrel (plavix)
anti-plt, prodrug
MOA: irreversible plt effect; knocks out ADP receptor-> dec plt aggregation/adhesion
consider genotyping 2C19 (not efficacious in ~20%)
-less efficacious then prasugrel
INTERACTIONS: PPIs, cimetidine, fluoxetine, fluconazole, other antiplts/anticoags, NSAIDS
ADRs: GI intolerance, flu-like illness, TTP, bleeding
stop 5 days prior to surgery
-only give PPIs if high bleeding risk OR multiple risk factors
prasugrel
anit-plt, prodrug (not as dependent on metabolism)
MOA: prevents plt activation (more so than clopidogrel)
USE: ACS
INTERACTIONs: other antiplts/anticoags, NSAIDS
ADRs: GI intolerance, flu-like illness, TTP, bleeding
stop 7 days before surgery
ticagrelor
anti-plt (new)
MOA: same as clopidogrel/prasugrel but REVERSIBLE
MONITOR: H/H, uric acid, renal fcn
ADRs: bleeding, dyspnea, inc [UA], bradyarrhythmias
abciximab
IV antiplatelet drug
MOA: glycoprotein IIb/IIIa receptor antagonist
ADRs: immune mediated thrombocytopenia
just like eptifibatide and tirofiban
eptifibatide
IV antiplatelet drug
MOA: glycoprotein IIb/IIIa receptor antagonist
ADRs: immune mediated thrombocytopenia
just like abciximab and tirofiban
tirofiban
IV antiplatelet drug
MOA: glycoprotein IIb/IIIa receptor antagonist
ADRs: immune mediated thrombocytopenia
just like abciximab and eptifibatide
dipyridamole
anti-plt
MOA: anti-plts; vasodilation
USE: post CVA/TIA (esp w/asa combo aggrenox)
ADRs: severe HA, angina, dizziness, hypotension
warfarin
coumarin, taken qday
MOA: antagonized vit K epoxide reductase complex (VKORC1)-> hypofcn clotting factors accumulate (protein C&S also inhibited)
-metabolized by 2C9 (highly variable), consider genotyping
S-warfarin clinically important (it is a racemic mix)
USE: prevent/tx venous thrombosis/emobli; *preferred anticoagulant for Afib w/CAD; recurrent TIA.
DOSING: start 5-10mg for 2 days, t1/2= 40hrs (takes 2 days to see effect); Loading >10mg could cause hypercoagulable state
MONITOR: extrinsic pathway/common path (PT/INR),qday until stable -> q3-4wks
REVERSAL:
1.) Vit K: oral if non-life threatening (~24hrs); IV slowly if life threatening
2.) PCC prothrombin complex concentrates (S.O.C), lowers INR fastest
3.) FFP
4.) rVIIa (expensive)
INTERACTIONS: antacids, bile acid sequesterants, FQs, other antiplt/coags
ADRs: bleeding
heparin
MOA: indirect thrombin inhibitor (supercharges anti-thrombin)
USE: DVT prophylaxis (SQ q8hrs); anti-coag; ACS; use w/in 24hrs
LIMITS: doesn't break up clots (may still grow)
MONITOR: aPTT (intrinsic pathway); plt counts (therapeutic dose=qod; prophylactic dose=q3-4days)
REVERSAL: non-urgent=stop; urgent= protamine slowly. *FFP does NOT reverse*
ADRs: hemorrhage (esp post eye/spinal/brain surg), osteoporosis (>6months)
ADRs:
1.) HIT (type 1 and 2(worse))), antibody driven process->plts don't work
2.) HTTS heparin induced thromboytopenia and thrombosis syndrome
rivaroxaban
factor Xa inhibitor; very new
MOA: inhibits free & clot bound factor Xa
PEARLS: start 6-10hrs post surg, don't use if CrCl<30
ADRs: bleeding, can't be turned off, protamine doesn't work, not dialyzable
enoxaparin
LMWH; "parins" (Lovenox)
MOA: antithrombin mediated inhibition of factors Xa>IIa
USE: DVT prophlx; DVT/PE tx; ACS
PROS: fixed dose, no lab monitoring, less thrombocytopenia, hemorrhage, and bone loss
DOSING: adjust for CrCl, PT wt, situation specific have pharm dose it
MONITOR: none, except preggers, renal dysfcn, obese
REVERSAL: partially with protamine, *FFP does NOT reverse*
ADRs: injection site pain/hematoma, thrombocytopenia, hemorrhage
-used more than dalteparin
dalteparin
LMWH; "parins" (Fragmin)
MOA: antithrombin mediated inhibition of factors Xa>IIa
USE: DVT prophlx; DVT/PE tx; ACS
PROS: fixed dose, no lab monitoring, less thrombocytopenia, hemorrhage, and bone loss
DOSING: adjust for CrCl, PT wt, situation specific have pharm dose it
MONITOR: none, except preggers, renal dysfcn, obese
REVERSAL: partially with protamine, *FFP does NOT reverse*
ADRs: injection site pain/hematoma, thrombocytopenia, hemorrhage
-used less than enoxaparin
fondaparinux
synthetic analog of heparin;
MOA: Xa inhibitor
can't be reveresed, do NOT USE
-long 1/2life
-monitor: CBC, SOB, SCr, anti-Xa assay
dabigatran
direct thrombin inhibitor; tablet BID
MOA: dec thrombin stimulated plt aggregation
MONITOR: SCr annually
PEARLS: no antidote, effect wears off in 2 days
1.) sensitve to moisture
2.) can't dbl up doses, take asap if missed
3.) stop 2 days prior to surg, start 24hrs after
4.) transition from warfarin: stop warfarin until INR <2
ADRs: bleeding, dyspesia/gastritis has acid to inc absorption
lepirudin
injected direct thrombin inhibitor; recombinant hirudin
USE: approved for anticoagulation w/ HITTS
CANT REVERSE
argatroban
injected direct thrombin inhibitor; recombinant hirudin
USE: approved for anticoagulation w/ HITTS
CANT REVERSE
-very short 1/2 life
desirudin
injected direct thrombin inhibitor; recombinant hirudin
USE: approved for DVT prophylx in THA
CANT REVERSE
bivalirudin
injected direct thrombin inhibitor; synthetic analog of hirudin
USE: ACS; approved for anticoagulation w/ HITTS
CANT REVERSE
streptokinase
urokinase
old fibrinolytics
alteplase
older fibrinolytic; tPA (recombinant tissue-type plasminogen activator)
MOA: binds fibrin and converts trapped plasminogen to plasmin
USE: STEMI, acute PE, ischemic stroke, etc
ADR: bleeding
use this if no PCI
LIMITATIONs: 15-20% failure, 5-15% reocclusion
reteplase
newer fibrinolytic; rPA
longer 1/2 life then alteplase, less fibrin selective
USE: STEMI
tenecteplase
newer fibrinolytic tPA
14x more fibrin specific; SINGLE iv bolus
USE: STEMI