Anticoagulants Flashcards by Kristin Baker

Anistreplase class

Thrombolytics activate plasmin

3degree hemostasis

How well did you know this?

Not at all

Perfectly

Anistreplase description

purified human plasminogen and bacterial streptokinase

How well did you know this?

Not at all

Perfectly

Alteplase, Reteplase, Tenecteplase class

Thrombolytics activate plasmin

3 degree hemostasis

How well did you know this?

Not at all

Perfectly

Alteplase, Reteplase, Tenecteplase description

recombinant t-PA
Less selective
Mutant t-PA

How well did you know this?

Not at all

Perfectly

Alteplase, Reteplase, Tenecteplase mechanism

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

How well did you know this?

Not at all

Perfectly

Alteplase, Reteplase, Tenecteplase indication

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

How well did you know this?

Not at all

Perfectly

Urokinase class

Thrombolytic

How well did you know this?

Not at all

Perfectly

Urokinase description

Human enzyme synthesized in kidney

How well did you know this?

Not at all

Perfectly

Urokinase mechanism

Direct conversion of plasminogen to plasmin

How well did you know this?

Not at all

Perfectly

Urokinase indication

lysis of PE

How well did you know this?

Not at all

Perfectly

Streptokinase class

Thrombolytic

How well did you know this?

Not at all

Perfectly

Streptokinase mechanism

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

How well did you know this?

Not at all

Perfectly

Streptokinase description

Protein made by beta hemolytic strep

How well did you know this?

Not at all

Perfectly

Streptokinase indication

Rarely used due to newer drugs

How well did you know this?

Not at all

Perfectly

Warfarin description

Coumarin anti-coag

Monitor every 2-4 weeks via PT (INR)

How well did you know this?

Not at all

Perfectly

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)

How well did you know this?

Not at all

Perfectly

Warfarin indication

Hypercoagulable states

Pregnancy category X

How well did you know this?

Not at all

Perfectly

Warfarin PK

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

How well did you know this?

Not at all

Perfectly

Warfarin adverse

Narrow therapeutic window
Many drug interactions
Hemorrhage

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

How well did you know this?

Not at all

Perfectly

Lepirudin, Bivalirudin, Argatroban description

Direct thrombin inhibitors (hirudin from leeches)

How well did you know this?

Not at all

Perfectly

Lepirudin, Bivalirudin, Argatroban mechanism

Direct binding to active site of thrombin

Inhibits thrombin and platelet aggragation

Lepirudin, Bivalirudin, Argatroban indication

Thrombosis related to HIT

Coronary angioplasty

Lepirudin, Bivalirudin, Argatroban PK

Parenteral

Monitored with PTT

Lepirudin, Bivalirudin, Argatroban adverse

No antidote

Fondaparinux description

synthetic pentasaccharide

Fondaparinux mechanism

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

Fondaparinux indication

Treatment and prevention of DVT

Heparin, Enoxaparin, Dalteparin, Tinzaparin description

UFH: mixture of straight chain anionic GAGs LMWH: has higher therapeutic index Pentasaccharide sequence binds ATIII

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

Heparin, Enoxaparin, Dalteparin, Tinzaparin indication

*DOC in pregnancy* DVT PE MI

Heparin, Enoxaparin, Dalteparin, Tinzaparin PK

Only given IV, never oral Rapid acting Monitored with PTT Excess heparin is treated with *protamine sulfate*

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****

Abciximad mechanism

Irreversible monoclonal Ab

Eptifibatide mechanism

Reversible cyclic peptide antagonist

Tirofiban mechanism

Non peptide reversible antagonist

Abciximab, Eptifibatide, Tirofiban description

GPIIb/IIIa blockers | Platelet aggregation inhibitors

Abciximab, Eptifibatide, Tirofiban indication

Acute coronary syndrome Angioplasty give parentally

Abciximab, Eptifibatide, Tirofiban adverse

Patients who lack GPIIb/IIIa have Glanzmann's Thrombasthenia

Dipyridamole, Cilostazol description

Platelet aggregation inhibitors PDE inhibitor Coronary vasodilation

Dipyridamole, Cilostazol mechanism

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

Dipyridamole, Cilostazol indication

Prophylaxis for angina

Clopidogrel, Ticlopidine description

Platelet aggregation inhibitors | ADP receptor blockers

Clopidogrel, Ticlopidine mechanism

Irreversible inhibition of P2Y12 receptor on platelets -> decreased aggregation

Clopidogrel, Ticlopidine indication

Recent stroke, MI or acute coronary syndrome Clopidogrel is preferred because is has fewer AE

Clopidogrel, Ticlopidine PK

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

Clopidogrel, Ticlopidine adverse

Inhibits CYP450 Thrombocytopenic purpura Ticlopidine causes neutropenia

Aspirin description

inhibits platelet aggregation | COX inhibitor

Aspirin mechanism

*Irreversible* acetylation of COX -> blocks TXA2 synthesis -> prolonged bleeding time TXA2 normally increases affinity for GPIIb/IIIa receptor to find fibrinogen

Aspirin indication

Cerebral ischemia | Stroke and MI

Aspirin PK

No nucleus = no new enzyme for 10 days