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Pharmacology > Anticoagulants > Flashcards

Anticoagulants Flashcards

1
Q

Anistreplase class

A

Thrombolytics activate plasmin

3degree hemostasis

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2
Q

Anistreplase description

A

purified human plasminogen and bacterial streptokinase

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3
Q

Alteplase, Reteplase, Tenecteplase class

A

Thrombolytics activate plasmin

3 degree hemostasis

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4
Q

Alteplase, Reteplase, Tenecteplase description

A

recombinant t-PA
Less selective
Mutant t-PA

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5
Q

Alteplase, Reteplase, Tenecteplase mechanism

A

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

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6
Q

Alteplase, Reteplase, Tenecteplase indication

A

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

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7
Q

Urokinase class

A

Thrombolytic

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8
Q

Urokinase description

A

Human enzyme synthesized in kidney

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9
Q

Urokinase mechanism

A

Direct conversion of plasminogen to plasmin

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10
Q

Urokinase indication

A

lysis of PE

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11
Q

Streptokinase class

A

Thrombolytic

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12
Q

Streptokinase mechanism

A

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

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13
Q

Streptokinase description

A

Protein made by beta hemolytic strep

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14
Q

Streptokinase indication

A

Rarely used due to newer drugs

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15
Q

Warfarin description

A

Coumarin anti-coag

Monitor every 2-4 weeks via PT (INR)

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16
Q

Warfarin mechanism

A

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)

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17
Q

Warfarin indication

A

Hypercoagulable states

Pregnancy category X

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18
Q

Warfarin PK

A

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

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19
Q

Warfarin adverse

A

Narrow therapeutic window
Many drug interactions
Hemorrhage

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

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20
Q

Lepirudin, Bivalirudin, Argatroban description

A

Direct thrombin inhibitors (hirudin from leeches)

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21
Q

Lepirudin, Bivalirudin, Argatroban mechanism

A

Direct binding to active site of thrombin

Inhibits thrombin and platelet aggragation

22
Q

Lepirudin, Bivalirudin, Argatroban indication

A

Thrombosis related to HIT

Coronary angioplasty

23
Q

Lepirudin, Bivalirudin, Argatroban PK

A

Parenteral

Monitored with PTT

24
Q

Lepirudin, Bivalirudin, Argatroban adverse

A

No antidote

25
Q

Fondaparinux description

A

synthetic pentasaccharide

26
Q

Fondaparinux mechanism

A

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

Negligible ATIII activity

27
Q

Fondaparinux indication

A

Treatment and prevention of DVT

28
Q

Heparin, Enoxaparin, Dalteparin, Tinzaparin description

A

UFH: mixture of straight chain anionic GAGs

LMWH: has higher therapeutic index
Pentasaccharide sequence binds ATIII

29
Q

Heparin, Enoxaparin, Dalteparin, Tinzaparin mechanism

A

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
Q

Heparin, Enoxaparin, Dalteparin, Tinzaparin indication

A

DOC in pregnancy

DVT
PE
MI

31
Q

Heparin, Enoxaparin, Dalteparin, Tinzaparin PK

A

Only given IV, never oral

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

32
Q

Heparin, Enoxaparin, Dalteparin, Tinzaparin adverse

A

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
Q

Abciximad mechanism

A

Irreversible monoclonal Ab

34
Q

Eptifibatide mechanism

A

Reversible cyclic peptide antagonist

35
Q

Tirofiban mechanism

A

Non peptide reversible antagonist

36
Q

Abciximab, Eptifibatide, Tirofiban description

A

GPIIb/IIIa blockers

Platelet aggregation inhibitors

37
Q

Abciximab, Eptifibatide, Tirofiban indication

A

Acute coronary syndrome
Angioplasty
give parentally

38
Q

Abciximab, Eptifibatide, Tirofiban adverse

A

Patients who lack GPIIb/IIIa have Glanzmann’s Thrombasthenia

39
Q

Dipyridamole, Cilostazol description

A

Platelet aggregation inhibitors
PDE inhibitor
Coronary vasodilation

40
Q

Dipyridamole, Cilostazol mechanism

A

Increases cAMP

Little effect alone -> coadminister with aspirin or warfarin

41
Q

Dipyridamole, Cilostazol indication

A

Prophylaxis for angina

42
Q

Clopidogrel, Ticlopidine description

A

Platelet aggregation inhibitors

ADP receptor blockers

43
Q

Clopidogrel, Ticlopidine mechanism

A

Irreversible inhibition of P2Y12 receptor on platelets -> decreased aggregation

44
Q

Clopidogrel, Ticlopidine indication

A

Recent stroke, MI or acute coronary syndrome

Clopidogrel is preferred because is has fewer AE

45
Q

Clopidogrel, Ticlopidine PK

A

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

46
Q

Clopidogrel, Ticlopidine adverse

A

Inhibits CYP450
Thrombocytopenic purpura
Ticlopidine causes neutropenia

47
Q

Aspirin description

A

inhibits platelet aggregation

COX inhibitor

48
Q

Aspirin mechanism

A

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

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

49
Q

Aspirin indication

A

Cerebral ischemia

Stroke and MI

50
Q

Aspirin PK

A

No nucleus = no new enzyme for 10 days

Pharmacology (24 decks)

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