Anti-coagulants

Question 1

Drug list?

Answer 1

Aspirin, Clopidogrel, Ticlopidine, Abciximab, Eptifibatide, Dipyridamole, Dabigatran etexilate, Hirudin, Argatroban, Bivalirudin, Rivaroxaban, HMW-Heparin, LMW-Heparin, Warfarin, Streptokinase, Alteplase, tPA, Activase, Reteplase, Tenecteplase

Question 2

Aspirin (MoA)

Answer 2

Irreversibly acetylates Cox-1 and Cox-2&raquo_space; TxA2 formation is inhibited.

Inhibits PGI2 (prostacycline) at higher doses, which lessens the effect

Question 3

Clopidogrel (MoA)

Answer 3

Prodrug (CYP2C19)

Irreversibly inhbits P2Y12 (ADP receptor)

Question 4

Ticlopidine (MoA)

Answer 4

Prodrug (CYP2C19)

Irreversibly inhbits P2Y12 (ADP receptor)

Question 5

Abciximab (MoA)

Answer 5

Fab frag against GPIIB/IIIA

Question 6

Eptifibatide (MoA)

Answer 6

Peptide antagonist at fibrinogen binding site on GPIIB/IIIA

Question 7

Dipyridamole (MoA)

Answer 7

Phosphodiesterase inhibitor (cAMP>AMP). cAMP levels rise > Ca decreases > platelet activation decreases.

Inhibits adenosine uptake

Question 8

Dabigatran Etexilate (MoA)

Answer 8

Directly inhibits thrombin

Question 9

Hirudin (MoA)

Answer 9

Irreversibly inhibits thrombin

Question 10

Argatroban (MoA)

Answer 10

Reversibly inhibits thrombin

Question 11

Bivalirudin (MoA)

Answer 11

Reversibly inhibits thrombin

Question 12

Rivaroxaban (MoA)

Answer 12

Used for DVT pts

Inhibits factor 10

Question 13

HMW-heparin (MoA)

Answer 13

Inhibits factors 9, 10, and thrombin by greatly increasing Anti-thrombin III activity

Question 14

LMW-heparin (MoA)

Answer 14

Inhibits factor 10 via anti-thrombin, but not the others

Question 15

Warfarin (MoA)

Answer 15

Blocks vit k epoxide reductase and prevents maturation of prothrombin, factors 7, 9, and 10

Question 16

Streptokinase (MoA)

Answer 16

Combines with plasminogen to make an active complex for the conversion to plasmin

Question 17

Alteplase (MoA)

Answer 17

Directly converts plasminogen to plasmin

Question 18

tPA (MoA)

Answer 18

Directly converts plasminogen to plasmin

Question 19

Activase (MoA)

Answer 19

Directly converts plasminogen to plasmin

Question 20

Releplase (MoA)

Answer 20

Directly converts plasminogen to plasmin

Question 21

Tenecteplase (MoA)

Answer 21

Directly converts plasminogen to plasmin

Question 22

What are the anti-platelet drugs we need to know?

Answer 22

Prevent platelet activation/aggregation:

Aspirin, Clopidogrel/Ticlopidine, Abciximab/eptifibatide, and dipyridamole

Question 23

What are the anti-coagulants that we need to know?

Answer 23

Inhibit clotting cascade to prevent fibrin clot formation:

Dabigatran etexilate, HMW/LMW-heparin, Warfarin, Rivaroxaban

Question 24

What are the thrombolytics that we need to know?

Answer 24

Activate plasmin to break up clots:

Streptokinase, Alteplase (tPA), Reteplase, Tenecteplase

Question 25

Aspirin - adverse effects

Answer 25

1) 30% resistance in population 2) Bleeding (stroke, GI) 3) Tinnitus 4) Reye's syndrome (multiorgan symptoms, but brain and liver get affected most. Hypoglycemia present)

Question 26

Clopidogrel/Ticlopidine - adverse effects

Answer 26

1) Prolonged bleeding 2) TTP 3) Poor metabolizers (Cyp2c19*2 or *3) cant convert the prodrug 4) Ticlo - nausea/vomiting, SEVERE neutropenia

Question 27

Abciximab/Eptifibatide - adverse effects

Answer 27

1) 10% major hemorrhagic event 2) Thrombocytopenia 3) Epti is renal metabolism, so use abciximab for renal disease

Question 28

Dipyridamole - adverse effects

Answer 28

1) Coronary steal 2) Hypotension 3) Bleeding

Question 29

Dabigatran etexilate - adverse effects

Answer 29

1) Hemorrhage 2) Heartburn, GI upset 3) MI risk

Question 30

Hirudin, Argatroban, Bivalirudin - adverse effects

Answer 30

Bleeding

Question 31

HMW/LMW-Heparin - adverse effects

Answer 31

1) thrombocytopenia Overdose treated with protamine sulfate (not as effective for LMW)

Question 32

Rivaroxaban- adverse effects

Answer 32

Bleeding

Question 33

Warfarin - adverse effects

Answer 33

1) bleeding 2) crosses placenta and causes hemorrhage Increased potency with cimetidine aspirin, vit k def, steroids, tamoxifen, oral hypoglycemics Decreased potency with contraceptives, barbiturates CYP2C9 induced with barbiturates, rifampicin CYP2C9 inhibited with cimetidine

Question 34

Thrombolytics - adverse effects

Answer 34

1) hemorrhage Do not use with prior hemorrhage of any kind