Thrombolytics, Anticoagulants, Antiplatelet Drugs--Regal

Question 1

Acetylsalecylate

Answer 1

MOA: irreversibly binds COX 1/2

• platelets only express COX 1
• COX 2 absent on platelets

TU: anticoag (low dose), anti-inflammatory, anti-pyretic (high dose)

Adverse: bleeding, GI, tinnitus

Question 2

Clopidogren

Answer 2

MOA: ADP receptor antagonist

PK: irreversible, CYP2C19 activation, ADP receptors always present

Adverse: bleeding, severe leukopenia

Question 3

Prasugrel

Answer 3

MOA: ADP receptor antagonist

PK: irreversible, ADP receptors always present

Adverse: bleeding, severe leukopenia

Question 4

Ticlopidine

Answer 4

MOA: ADP receptor antagonist

PK: irreversible, ADP receptors always present

Adverse: TTP, bleeding, severe leukopenia

Question 5

Abciximab

Answer 5

MOA: antibody agianst GPIIb/IIIa

PK: IV

Adverse: bleeding, thrombocytopenia

Question 6

Eptifibatine

Answer 6

MOA: fibrinogen acitvator (GPIIb/IIIa receptor inhibitor)

PK: IV

Adverse: bleeding, thrombocytopenia

Question 7

Tirofiban

Answer 7

MOA: non-peptide competative inhibitor (GPIIb/IIIa receptor inhibitor)

PK: IV

Adverse: bleeding, thrombocytopenia

Question 8

Dipyrimadole

Answer 8

MOA: increases [cAMP] –> inhibitits platelet activation

phosphodiesterase 3 inhibitor

inhibits platelet uptake of adenosine

TU: combinatin w/ warfarin or aspirin

Adverse: headache, vasodilation

Question 9

Unfactionated Heparin

Answer 9

MOA: bind ATIII (anti-thrombin III) –> exposes active site –> increases efficacy of ATIII –> inactivates thrombin and Xa

PK: t_1/2 = 1 hr (close monitoring)

Adverse: bleeding, heprin-induced thrombocytopenia (IgG against Factor IV-platelet factor complex)

Question 10

Low MW Heparin

Answer 10

MOA: bind ATIII (anti-thrombin III) –> exposes active site –> increases efficacy of ATIII –> inactivates Xa and (some) thrombin

PK: t_1/2 = 4 hr (less monitoring)

Adverse: bleeding, heparin-induced thrombocytopenia (IgG against Factor IV-platelet factor complex)

Question 11

Fondaparinux

Answer 11

MOA: bind ATIII (anti-thrombin III) –> exposes active site –> increases efficacy of ATIII –> inactivates Xa (not thrombin)

PK: t_1/2 = 17 hr. (less monitoring, harder to reverse)

Adverse: bleeding, heparin-induced thrombocytopenia (IgG against Factor IV-platelet factor complex)

**pentasaccharide, small synthetic molecule**

Question 12

Bivalirudin

Answer 12

MOA: inhibit thrombin

PK: IV

Question 13

Argatroban

Answer 13

MOA: inhibit thrombin

PK: IV

Question 14

Dibigatran etexylate

Answer 14

MOA: inhibit thrombin

PK: PO** (unique)

Question 15

Warfarin

Answer 15

MOA: binds vitamin K (epoxide) reductase

• blocks (oxidized) vit. K epoxide –> (reduced) vit. K hydroquinone reaction
• Factors II, VII, IX, X, protein C* sythesis affected

PK: slow onset (days)–b/c affects synthesis

• INR monitors
• heparin used as bridge b/c protein C synthesis affected first (normally antithrombotic) –> hypercoagulable state
• VKORC1 polymorphisms = 30% of pt-pt variability
• 20-70% patient-patient variability

Adverse: bleeding

_**Vit. K is anecdote**_

Question 16

Apixaban

Answer 16

MOA: inhibits Xa

PK: no monitoring, rapid onset and short t_1/2

_**no antidote available**_

Question 17

Rivaroxaban

Answer 17

MOA: inhibits Xa

PK: no monitoring, short t_1/2

_**no antidote available**_

Question 18

Exodaban

Answer 18

MOA: inhibit Xa

PK: no monitoring

_**no antidote available**_

Question 19

Streptokinase

Answer 19

MOA: complexes w/ plasminogen –> plasmin

Adverse: bleeding, cost

Question 20

Urokinase

Answer 20

MOA: directly converts plasminogen –> plasmin

Adverse: bleeding, cost

Question 21

tPAs

(alteplase, reteplase, tenecteplase)

Answer 21

MOA: preferentially activates plasminogen bound to fibrin–preferentially active at site of clot

Adverse: bleeding, cost

**only thrombolytic approved to treat ischemic stroke