Anticoagulants Flashcards Preview

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Flashcards in Anticoagulants Deck (50):
1

Anistreplase class

Thrombolytics activate plasmin
3degree hemostasis

2

Anistreplase description

purified human plasminogen and bacterial streptokinase

3

Alteplase, Reteplase, Tenecteplase class

Thrombolytics activate plasmin
3 degree hemostasis

4

Alteplase, Reteplase, Tenecteplase description

recombinant t-PA
Less selective
Mutant t-PA

5

Alteplase, Reteplase, Tenecteplase mechanism

t-PA is a serine protease produced by human endothelial cells that activates plasminogen bound to fibrin (selective)

6

Alteplase, Reteplase, Tenecteplase indication

2nd line therapy after angioplasty for treatment of acute MI and ischemic stroke

7

Urokinase class

Thrombolytic

8

Urokinase description

Human enzyme synthesized in kidney

9

Urokinase mechanism

Direct conversion of plasminogen to plasmin

10

Urokinase indication

lysis of PE

11

Streptokinase class

Thrombolytic

12

Streptokinase mechanism

Catalyzes degradation of PF-V and VII in addition to activation of plasmin

13

Streptokinase description

Protein made by beta hemolytic strep

14

Streptokinase indication

Rarely used due to newer drugs

15

Warfarin description

Coumarin anti-coag
Monitor every 2-4 weeks via PT (INR)

16

Warfarin mechanism

Inhibits Vit K epoxide reductase -> can't gamma carboxylate factors II, VII, IX and X

Factor VII is the first to go -> monitor PT

Can reverse action with Vit K (24 hrs)

17

Warfarin indication

Hypercoagulable states

Pregnancy category X

18

Warfarin PK

Oral
Several hours to take effect; single dose lasts for 2-5 days
Monitor with INR

19

Warfarin adverse

Narrow therapeutic window
Many drug interactions
Hemorrhage

Cutaneous necrosis** ->decreased activity of protein C -> paradoxical hypercoagulability

20

Lepirudin, Bivalirudin, Argatroban description

Direct thrombin inhibitors (hirudin from leeches)

21

Lepirudin, Bivalirudin, Argatroban mechanism

Direct binding to active site of thrombin
Inhibits thrombin and platelet aggragation

22

Lepirudin, Bivalirudin, Argatroban indication

Thrombosis related to HIT
Coronary angioplasty

23

Lepirudin, Bivalirudin, Argatroban PK

Parenteral
Monitored with PTT

24

Lepirudin, Bivalirudin, Argatroban adverse

No antidote

25

Fondaparinux description

synthetic pentasaccharide

26

Fondaparinux mechanism

*Selective PF-10 inhibitor* -> binds anti-thrombin III allowing it inhibit PF-10

Negligible ATIII activity

27

Fondaparinux indication

Treatment and prevention of DVT

28

Heparin, Enoxaparin, Dalteparin, Tinzaparin description

UFH: mixture of straight chain anionic GAGs

LMWH: has higher therapeutic index
Pentasaccharide sequence binds ATIII

29

Heparin, Enoxaparin, Dalteparin, Tinzaparin mechanism

UFH: binds to anti-thrombin III -> increased activity -> inhibits thrombin by forming a ternary complex along with factors IX and X

LMWH:inhibits factor X, with less of an effect on thrombin than UFH due to lack of ternary complex formation

30

Heparin, Enoxaparin, Dalteparin, Tinzaparin indication

*DOC in pregnancy*

DVT
PE
MI

31

Heparin, Enoxaparin, Dalteparin, Tinzaparin PK

Only given IV, never oral

Rapid acting
Monitored with PTT
Excess heparin is treated with *protamine sulfate*

32

Heparin, Enoxaparin, Dalteparin, Tinzaparin adverse

Bleeding
HIT (Type 2):
IgG binds to heparin/PF-4 complex -> binding to FcR on platelets ->degranulation and more PF-4 release -> thrombosis and thrombocytopenia

Tx. -> disocntinue use and give DTI or fondaparinux****

33

Abciximad mechanism

Irreversible monoclonal Ab

34

Eptifibatide mechanism

Reversible cyclic peptide antagonist

35

Tirofiban mechanism

Non peptide reversible antagonist

36

Abciximab, Eptifibatide, Tirofiban description

GPIIb/IIIa blockers
Platelet aggregation inhibitors

37

Abciximab, Eptifibatide, Tirofiban indication

Acute coronary syndrome
Angioplasty
give parentally

38

Abciximab, Eptifibatide, Tirofiban adverse

Patients who lack GPIIb/IIIa have Glanzmann's Thrombasthenia

39

Dipyridamole, Cilostazol description

Platelet aggregation inhibitors
PDE inhibitor
Coronary vasodilation

40

Dipyridamole, Cilostazol mechanism

Increases cAMP
Little effect alone -> coadminister with aspirin or warfarin

41

Dipyridamole, Cilostazol indication

Prophylaxis for angina

42

Clopidogrel, Ticlopidine description

Platelet aggregation inhibitors
ADP receptor blockers

43

Clopidogrel, Ticlopidine mechanism

Irreversible inhibition of P2Y12 receptor on platelets -> decreased aggregation

44

Clopidogrel, Ticlopidine indication

Recent stroke, MI or acute coronary syndrome

Clopidogrel is preferred because is has fewer AE

45

Clopidogrel, Ticlopidine PK

Clopidogrel is a prodrug activated by CYP2C19 ... DO NOT use with omeprazole which inhibits CYP2C19

46

Clopidogrel, Ticlopidine adverse

Inhibits CYP450
Thrombocytopenic purpura
Ticlopidine causes neutropenia

47

Aspirin description

inhibits platelet aggregation
COX inhibitor

48

Aspirin mechanism

*Irreversible* acetylation of COX -> blocks TXA2 synthesis -> prolonged bleeding time

TXA2 normally increases affinity for GPIIb/IIIa receptor to find fibrinogen

49

Aspirin indication

Cerebral ischemia
Stroke and MI

50

Aspirin PK

No nucleus = no new enzyme for 10 days