Anti-coagulant (week 7) Drugs

Question 1

Aspirin

Answer 1

anti-platelet: COX inhibitor
irreversibly acetylates COX1--/ PG, TXA2
prevent TXA platelet aggreg
(PK) oral upper GI effect 
~10 day effect
(X) 1o prevention - reduce MI mortality
(X) 2o prevention - hx of MI, angina, stroke- reduce MI, stroke, death
(-1) bleeding
(-2) GI irritation (ulcer)

Question 2

Clopidogrel

Answer 2

anti-platelet: ADP:P2Y12 
Inhibitor 
inhibit ADP from binding to P2Y12R (platelet)
(PK) cyP2C19
(O) proton pump inhib 
(-1) bleeding
(-2) severe neutropenia

Question 3

Prasugrel

Answer 3

anti-platelet: ADP:P2Y12 
inhibit ADP from binding to P2Y12R (platelet)
(PK) cyP2C19
(O) proton pump inhib 
(-1) bleeding
(-2) severe neutropenia

Question 4

Ticlopidine

Answer 4

anti-platelet: ADP:P2Y12 inhib
inhibit ADP from binding to P2Y12R (platelet)
(PK) cyP2C19
(O) proton pump inhib 
(-1) bleeding
(-2) severe neutropenia

Question 5

Ticagrelor*

Answer 5

anti-platelet: ADP:P2Y12 inhib
REVERSIBLE 
inhibit ADP from binding to P2Y12R (platelet)
(PK) cyP2C19
(O) proton pump inhib 
(-1) bleeding
(-2) severe neutropenia

Question 6

Abcximab

Answer 6

anti-platelet: GpIIb/IIIa inhibitor
Non-competitive
Fab chimeric human-murine monoAb
bind (platelet) GPIIb/IIIa-R --/ fibrinogen cross-link
(PK) IV , bi-phasic t 1/2 
(X) PCI 
(-1) bleeding
(-2) thrombocytopenia
(-3) hyp-O- tension
(-4) bradycardia

Question 7

Eptifibatide

Answer 7

anti-platelet: GpIIb/IIIa inhibitor
Competitive, reversible 
prevent fibrinogen cross-link of platelets
Lys-Gly-Asp (KGD) seq= ^ specificity for R
(PK) IV, renal clearance
(X) 2o prevention
(X) unstable angina
(X) NSTEMI
(O) renal dysfunction
(-1) bleeding

Question 8

Heparin

Answer 8

anti-thrombotic: parenteral 
bind antithrombin
--/ thrombin + F Xa
(PK) parenteral NOT abs in GI (^ size and charge) , immediate onset 
(X) Coronary Artery Disease
(X) prevention of death, AMI, refract angina, 
(X) PCI 
(-1) bleeding
(-2) heparin-induced thrombocytopenia

Question 9

Enoxaparin

Answer 9

anti-thrombotic: parenteral LMWH 
^ inhib of FXa (less thrombin)
(PK) parenteral (NOT abs in GI)
longer t 1/2> heparin
(X) 1st line subQ for UA or AMI
(X) IV for STEMI or PCI
(O) renal impairment 
(-1) bleeding
(-2) LMWH-induced thrombocytopenia (less than< heparin)

Question 10

Dalteparin

Answer 10

anti-thrombotic: parenteral LMWH
^ inhib of FXa (less thrombin)
(PK) parenteral (NOT abs in GI)
longer t 1/2> heparin
(X) 1st line subQ for UA or AMI
(X) IV for STEMI or PCI
(O) renal impairment 
(-1) bleeding
(-2) LMWH-induced thrombocytopenia (less than< heparin)

Question 11

Bivalirudin

Answer 11

anti-thrombotic: parenteral direct thrombin inhib
Phe-Pro-Arg-Pro 
bind/occupy catalytic site of thrombin
(PK) t 1/2 = 25 min
    IV, kidney excr
(X) 2nd line (to heparin) angioplasty, CABG
(O) renal failure
(-1) bleeding

Question 12

Lepirudin

Answer 12

anti-thrombotic: parenteral direct thrombin inhib
bind/occupy exosite 1 and catalytic site of thrombin
(PK) t 1/2 = 1.3hr
IV, kidney excr
(X) 2nd line (to heparin) angioplasty, CABG
(O) renal failure
(-1) bleeding

Question 13

Fondaparinux

Answer 13

anti-thrombotic: direct FXa inhibitor
anti-thrombin-mediated --/FXa
(PK) subQ , renal excr, t 1/2 = 17hr
(X) ACS (UA, NSTEMI, STEMI)
(O) renal failure
(-1) heparin-induced thrombocytppenia
(-2) catheter-related thrombosis

Question 14

Warfarin

Answer 14

(oral)anti-thrombotic: oral anti-vit K
inhib epoxide reductase –/ F II, VII, IX, X
(X) 2o prevention after STEMI
(X) AF mechan/ prosthetic heart valve

Question 15

Dabigatran

Answer 15

(oral)anti-thrombotic: oral thrombin
direct thrombin inhibitor
free + fibrin-bound

Question 16

Rivaroxiban

Answer 16

(oral)anti-thrombotic: oral anti FXa

Question 17

Dipyridamole

Answer 17

(oral) anti-thrombotic: oral –/PDE
^^cAMP–/platelet aggreg + vasoDILATE
(X) use + clopidogrel or Aspirin

Question 18

Alteplase

Answer 18

thrombolytic (tPA) 
activate plasminogen
bind fibrin (clot)- activate plasminogen> plasmin*--> clot dissolve 
(PK) (1) bolus dose 1 min
(2) infusion 
(X) AMI (STEMI or L bundle block) 
within 3 HOURS! 
(-1) bleeding= intracranial hemorrhage