Anticoagulants, antiplatelets, and fibrinolytics

Question 1

ADP and P2Y12 inhibitors

Answer 1

Clopidogrel
Prasugrel
Ticagrelor
Ticlopidine - not in US (aplastic anemia)

Question 2

Mechanism of ADP and P2Y12 inhibitors

Answer 2

Block ADP receptors which lead to inactivation of P2Y12 receptors, leading to an increase in cAMP to inhibit platelet aggregation

Question 3

Clinical uses of ADP and P2Y12 inhibitors

Answer 3

Treatment of ACS
Stroke prevention
Dual antiplatelet therapy

Question 4

Adverse effect of ADP and P2Y12 inhibitors

Answer 4

Bleeding

Question 5

GP IIb/IIIa inhibitors

Answer 5

Abciximab
Tirofiban
Eptifibatide

Question 6

Mechanism of GP IIb/IIIa inhibitors

Answer 6

Inhibit binding of fibrinogen to IIb/IIIa receptors to prevent platelet aggregation

Question 7

Clinical uses of GP IIb/IIIa inhibitors

Answer 7

ACS
PCI

Question 8

Adverse effect of GP IIb/IIIa inhibitors

Answer 8

Bleeding

Question 9

Platelet adenosine uptake inhibitor that works by inhibiting phosphodiesterase

Answer 9

Dipyridamole

Question 10

Clinical uses of dipyridamole

Answer 10

Thromboembolism prophylaxis
Pharmacologic cardiac stress test

Question 11

PDE3 inhibitor that inhibits phosphodiesterase for an antiplatelet action

Answer 11

Cliostazol

Question 12

Use of cliostazol

Answer 12

Intermittent claudication (PVD)

Question 13

Protease-activated receptor 1 (PAR-1) inhibitor that inhibits platelet aggregation induced by thrombin and thrombin receptor agonist peptide (TRAP)

Answer 13

Vorapaxar

Question 14

Clinical use of vorapaxar

Answer 14

Thrombotic event prevention

Question 15

Adverse effects of vorapaxar

Answer 15

Bleeding
Depression
Rash

Question 16

Thromboxane A2 (TXA2) inhibitor that irreversible acetylates COX1 receptors in platelets

Answer 16

Aspirin

Question 17

Prophylactic use of aspirin

Answer 17

MI and CVA

Question 18

Adverse effects of aspirin

Answer 18

GI upset
Bleeding

Question 19

Vit K antagonist that inhibits the hepatic synthesis of vit K clotting factors (II, VII, IX, and X) by blocking the gamma-carboxylation of clotting factors

Answer 19

Warfarin

Question 20

Bleeding values affected by warfarin use

Answer 20

INR and PT –> extrinsic pathway

Question 21

Indication for warfarin use

Answer 21

Ambulatory anticoagulation

Question 22

Contraindication of warfarin

Answer 22

Pregnancy –> crosses placenta –> teratogenic –> bone defects

Question 23

Adverse effects of warfarin

Answer 23

Bleeding
Skin necrosis
Purple toe syndrome (3-8 wks)

Question 24

Increased risk for developing skin necrosis with warfarin use

Answer 24

Pts with decreased protein C

Question 25

Antidote to warfarin

Answer 25

Vit K1 (phytonadione)

Question 26

Activates the plasma antithrombin III by enhancing serine protease activity to cause inactivation of clotting factors IIa, IXa, Xa, XIa, and XIIa

Answer 26

Heparin

Question 27

Bleeding values affected by heparin

Answer 27

PTT --> intrinsic pathway

Question 28

Adverse effects of heparin

Answer 28

Heparin induced thrombocytopenia (HIT) Osteoporosis

Question 29

Antidote to heparin

Answer 29

Protamine sulfate

Question 30

Low molecular weight heparins with a higher half-life than heparin and less risk of thrombocytopenia. Higher activity against factor X and no impact on PT or PTT.

Answer 30

Enoxaparin Dalteparin

Question 31

Contraindication of enoxaparin

Answer 31

Prosthetic valve

Question 32

Synthetic heparinoid with selective antithrombin III mediated Xa inhibition. Safer to use in heparin induced thrombocytopenia.

Answer 32

Fondaparinux

Question 33

Recombinant hirudin obtained from yeast cells with direct thrombin inhibitory action

Answer 33

Lepirudin

Question 34

Synthetic derivative of hirudin with direct thrombin inhibitory action

Answer 34

Bivalirudin

Question 35

Indications for use of hirudin family drugs

Answer 35

Prevent thrombosis in pts with unstable angina and acute MI

Question 36

Adverse effect of the hirudin family of drugs

Answer 36

Bleeding

Question 37

Synthetic direct thrombin inhibitor indicated for use in treatment of thrombosis in pts with HIT

Answer 37

Argatroban (IV)

Question 38

First oral direct thrombin inhibitor used to reduce risk of stroke in A fib and prevent thrombotic complications after joint replacement surgeries.

Answer 38

Dabigatran/Pradexa

Question 39

Adverse effects of dabigatran/Pradexa

Answer 39

Bleeding Gastritis-like symptoms

Question 40

Interactions of dabigatran/Pradexa

Answer 40

Substrate for P-glycoprotein --> contraindicated in Pgp inducers (rifampin) Caution with Pgp inhibitors (verapamil, amiodarone, clarithromycin)

Question 41

Active factor Xa inhibitors

Answer 41

Apixaban/Eliquis Rivaroxaban/Xarelto

Question 42

Uses of apixaban

Answer 42

In A fib to reduce stroke risk Prevention and treatment of venous thromboembolism

Question 43

Uses of rivaroxaban

Answer 43

DVT Blood clots PE After knee replacement

Question 44

Adverse effect of active factor Xa inhibitors

Answer 44

Bleeding

Question 45

Indications for anticoagulant therapy

Answer 45

Thromboembolic disorders --> DVT, PE, A fib Unstable angina undergoing PCI

Question 46

Only anticoagulant approved for use with synthetic valves

Answer 46

Warfarin

Question 47

General contraindications for anticoagulant therapy

Answer 47

Hypersensitivity Underlying coagulation disorder Ulcer disease Severe thrombocytopenia Active bleeding

Question 48

General adverse reactions to anticoagulant therapy

Answer 48

Hyperlipidemia Thrombocytopenia Pain at site of injection Spinal and/or epidural hematoma

Question 49

Heparin goal --> bleeding values

Answer 49

PTT > 1.5-2.5x normal Normal PTT of 21-35 sec

Question 50

Warfarin goal --> bleeding values

Answer 50

INR > 2.5x normal Normal INR is 1

Question 51

Clinical uses of fibrinolytics/thrombolytics

Answer 51

Acute MI Acute PE DVT Thomboembolic stroke

Question 52

Drug class that works by activating conversion of plasminogen to plasmin, causing lysis of fibrin clot to degradation products

Answer 52

Fibrinolytics/thrombolytics

Question 53

Serine protease inhibited by alpha-2 antiplasmin

Answer 53

Plasmin

Question 54

Tissue plasminogen activators --> recombinant DNA and clot specific

Answer 54

Altepase Reteplase Tenecteplase

Question 55

Protein obtained by beta-hemolytic strep that can be used as a non-specific fibrinolytic

Answer 55

Streptokinase

Question 56

Adverse effects of streptokinase fribinolytic

Answer 56

Allergic reaction Hypotension Decreased antibody activity after recent use

Question 57

Prodrug of isolated streptokinase that acts as a slow release

Answer 57

Anistreplase

Question 58

Fibrinolytic enzyme obtained from human neonatal kidney only approved for use in PE

Answer 58

Urokinase

Question 59

Adverse effects of fibrinolytic therapy

Answer 59

Bleeding and hemorrhage --> additive

Question 60

Contraindications of fibrinolytic therapy

Answer 60

Serious GI bleed Active bleeding or hemorrhagic disorder Surgery within 10 days Aortic dissection

Question 61

Antidote for fibrinolytic therapy

Answer 61

Aminocaproic acid

Question 62

Adverse effects of aminocaproic acid

Answer 62

Thrombosis Hypotension Arrhythmias

Question 63

Anti-fibrinolytic drug used to treat heavy menstrual bleeding

Answer 63

Tranexamic acid

Question 64

Increased risk factors for thrombotic adverse effect with tranexamic acid

Answer 64

Obese Cigarette smoking OCP