Anti-Coagulants

Question 1

Aspirin

Answer 1

MOA: irreversible (covalent) COX-2 inhibitor
Effect: 👇🏽TXA2 synthesis = inhibition of platelet aggregation (prolongs bleeding time)
Use: prophylaxis for transient CVA, reduce risk of recurrent MI, decreases mortality in post-MI pt

Question 2

Clopidogrel

Answer 2

MOA: inhibition of P2Y12 (ADP receptor)
Effect:
Metabolism: prodrug activated by CYP2C19
Use: reduce rate of CVA, MI and death in pt w/ recent MI/CVA
SE: fewer bad things so its preferred
*Omeprazole (inhibits CYP2C19) will reduce plasma levels of the active metabolite

Question 3

Ticlopidine

Answer 3

P2Y12 inhibitor

SE: more bad things happen with this so you use Clopidogrel instead

Question 4

Dipyridamole

Answer 4

MOA: phosphodiesterase inhibitor
Effect: 👆🏽cAMP, coronary vasodilator
Use: prophylactically to tx angina pectoris but has little effect alone so used as adjunct w/ Warfarin or Aspirin

Question 5

Abciximab

Answer 5

Monoclonal Ab directed against GPIIb/IIIa receptor

Use: reduce thrombotic events in pts w/ non-ST elevation acute coronary syndrome (NSTE-ACS)

Question 6

Eptifibatide

Answer 6

Cyclic peptide, reversible antagonist of GPIIb/IIIa receptor

Use: reduce thrombotic events in pts w/ non-ST elevation acute coronary syndrome (NSTE-ACS)

Question 7

Tirofiban

Answer 7

Nonpeptide reversible antagonist of GPIIb/IIIa receptor

Use: reduce thrombotic events in pts w/ non-ST elevation acute coronary syndrome (NSTE-ACS)

Question 8

Unfractionated Heparin (UFH)

Answer 8

Higher molecular weight than LMWH

MOA: inhibits thrombin and factor Xa

Question 9

Enoxaparin / Dalteparin / Tinzaparin

Answer 9

LMWHs (low molecular weight heparins)
MOA: inhibition of factor Xa (little effect on thrombin)
Compared to UFH: higher bioavailability, longer t1/2, less frequent dosing requirements

Question 10

Fondaparinux

Answer 10

Synthetic pentasaccharide
MOA: specific inhibitor of Xa
Use: prevention and tx of DVT

Question 11

Lepirudin

Answer 11

IV Direct thrombin inhibitor
MOA: inactivates fibrin-bound thrombin in a thrombus
Labs: monitored by aPTT
Use: HIT

Question 12

Bivalirudin

Answer 12

IV DTI (synthetic)
Lab: monitored by aPTT
Use: pt’s undergoing PCI

Question 13

Argatroban

Answer 13

IV DTI (small)
Labs: monitored by aPTT
Use: pt’s undergoing PCI

Question 14

Dabigatran Etexilate

Answer 14

Oral DTI
MOA: prodrug is converted to active metabolite
Use: prevent thromboembolic stroke in pt w/ a-fib, prevent and tx of DVT and PE

Question 15

Apixaban / Rivatoxaban

Answer 15

Oral direct factor Xa inhibitors

Use: prevention and tx of DVT and PE

Question 16

Warfarin

Answer 16

MOA: inhibits vitamin K epoxide reductase
Effect: decrease of clotting factor 2, 7, 9, 10, anticlotting proteins C and S
Labs: monitor with PT aka INR
Use: prevent/tx DVT and PE following initial heparinization and prevention of thromboembolisms in A-fib pt’s
SE: bleeding, cutaneous necrosis (d/t decreased Protein C activity bc its t1/2 is super short)
CI: Category X (crosses the placenta so never give in pregnancy)

Question 17

Streptokinase

Answer 17

Fibrinolytic/thrombolytic
Protein produced by group A and B Streptococci
Not used anymore

Question 18

Urokinase

Answer 18

Fibrinolytic/thrombolytic

Use: lysis of PE

Question 19

Alteplase

Answer 19

Fibrin-selective thrombolytic
(Recombinant t-Pa)
Use: management of acute MI and acute CVA

Question 20

Reteplase

Answer 20

Fibrin-selective thrombolytic
(Modified recombinant human t-Pa)
Use: management of acute MI

Question 21

Tenecteplase

Answer 21

Fibrin-selective thrombolytic
(Mutant form of t-Pa)
Use: management of acute MI

Question 22

Aminocaproic acid

Answer 22

Inhibits plasminogen activation

Use: adjunct in hemophilia pt and tx bleeding from fibrinolytic therapy

Question 23

Protamine Sulfate

Answer 23

Heparin antagonist
MOA: high in arginine so it’s cationic and it interacts with anionic heparin to form complex which stops the effect of heparin

Question 24

Vitamin K

Answer 24

Use: prevention of vitamin K deficiency bleeding in newborns - all babies should receive vitamin K at birth via IM administration

Question 25

Heparin (UFH and LMWH)

Answer 25

Activates antithrombin III
Effect: rapid inhibition of thrombin, IXa and Xa clotting factors
Use: DVT, PE, MI, DOC during pregnancy
SEs: bleeding, HS rxn, HIT

Question 26

HIT Type II

Answer 26

Pathogenesis: IgG binds the Fc receptor of the PF4/heparin platelet/complex forming an IC resulting in degranulation and aggregation of platelets
ROS: thrombocytopenia and thrombosis
Tx: d/c heparin and give DTI or Fondaparinux, *give Protamine sulfate if bleeding occurs