Block 3 Pro And Anti Coagulants

Front 1

What types of anticoagulant drugs do we know?

Back 1

direct and indirect thrombin inhibitors, vitamin K antagonist

Front 2

Direct thrombin inhibitors?

Back 2

argatroban, dabigatran
Bivalent: Bivalrudin, leprudin, Hirudin,

Front 3

Indirect thrombin inhibitors?

Back 3

Heparin (UFH,LMWH), Fondaparinux

Front 4

Vitamin K antagonists?

Back 4

Warfarin

Front 5

UFH's MOA?

Back 5

interacts w/ AT to inactivate thrombin (IIa), IXa (plasma thromboplastin component/christmas factor), Xa (stuart prower), XIa (plasma thromboplastin antecedent), XIIa (hageman)

Front 6

LMWH's MOA? Administration?

Back 6

Inhibits Xa>thrombin; Weight based

Front 7

What are the LMWH? How dosed?

Back 7

enoxaprin(mg); dalteparin & tinzaparin: (anti factor Xa units)

Front 8

UFH vs LMWH

Back 8

LMWH less tox and dose frequency, only monitored in special populations

Front 9

How is UFH administerd? what route should be avoided?

Back 9

given IV,SC; avoid IM: risk of hematoma
short t1/2 (1hr)

Front 10

Which heparin needs close monitoring? How?

Back 10

UFH, aPTT(intrinsic) or protamin titration or anti-Xa units

Front 11

What drug should be used if HIT occurs? Which heparin is HIT most commonly associated?

Back 11

Discontinue heparin and use DTI or fondaparainux; UFH

Front 12

Symptoms of HIT? Cause?

Back 12

decrease platelet count, new thrombus, thrombocytopenia, bleeding;
Antibodies against heparin/platelet factor 4cplx

Front 13

What is heparin? Where does it come from?

Back 13

Mixture of sulfated mucopolysaccharides extracted from porcine gut or bovine lung

Front 14

How do Indirect thrombin inhibitors work?

Back 14

Use AT to Inactivate(2,9,10,11,12) thrombin IIa, plasma thromboplastin components/ chritmas factor IXa, stuart prowerXa, plasma thromboplastin antecedent XIa, hageman XIIa
Also, Heparin increases lipoprotein lipase(clear lipemia)

Front 15

How to reverse UFH?

Back 15

Protamine sulfate

Front 16

Can protamin sulfate reverse fondaparinux?

Back 16

No Ineffective reversal for fondaparinux

Front 17

Can protamin sulfate reverse LMWH?

Back 17

Yes, but incompletlly for LMWH

Front 18

fondaparinux MOA?

Back 18

identical to UFH, inactivates IIa, IXa, Xa, XIa, XIIa through interactions w/ AT

Front 19

Fondaparinux Adminstration?

Back 19

once daily SC long t1/2;

Front 20

Fondaparinux indications?

Back 20

the synthetic pentasaccharide is a prophylaxis/treatment of venous thromboemobolism, alternate for HIT

Front 21

What are the Univalent DTI's?

Back 21

argatroban, dabigatran

Front 22

What is argatroban and dabigatran MOA?

Back 22

Bind to the active site of the thrombin enzyme

Front 23

Which DTIs are bivalent and what is there MOA?

Back 23

Hirudin, lepirudin, bivalirudin; bind to thrombin and the substrate site (site which molecules that interact w/ thrombin use to bind)

Front 24

Which Bivalent DTI is irreversible?

Back 24

Hirudin

Front 25

Which bivalent DTI inhibits platelet activation?

Back 25

Bivalirudin

Front 26

Which bivalent DTI prefered for HIT?

Back 26

Lepirudin

Front 27

Which bivalent DTI has rapid on/off action and is given IV?

Back 27

Bivalirudin

Front 28

What is the oral prodrug to argatroban?

Back 28

dabigatran

Front 29

Univalent used for HIT?

Back 29

argatroban

Front 30

argatroban administration?

Back 30

IV

Front 31

What should be monitored w/ agatroban?

Back 31

aPTT

Front 32

What is dabigatran the oral prodrug for?

Back 32

argatroban

Front 33

What is the oral prodrug to argatroban?

Back 33

dabigatran?

Front 34

Argatroban increases ___ and has inhibitory effects on____?

Back 34

Increases INR and inhibits Protein C and platelet aggregation through thrombin

Front 35

what enzyme does warfarin inhibit?

Back 35

Vitamin K epoxide reductase. so there is no vit k reduced for gamma glutamyl carboxylase to act on

Front 36

Warfarin MOA?

Back 36

Block gamma carboxylation of glutamate residue in prothrombin, VII, IX, X protein C & S

Front 37

What is the delay before warfarin acts

Back 37

8-12 hour delay

Front 38

What does vitamin K do?

Back 38

carboxylate glutamic acid

Front 39

What are the substrates for Vit K glutamic acid carboxylation?

Back 39

vit k carboxylated glutamic acid on II,VII,IX,X

Front 40

Which warfarin enantomer is more potent

Back 40

S

Front 41

does warfarin have a long half life?

Back 41

yes 36hr

Front 42

What is the largest loading does that can facilitate onset of warfarin?

Back 42

.75mg/kg

Front 43

Above .75mg/kg loading dose what is the effect?

Back 43

NO increase in onset, only prolonged action

Front 44

should warfarin be used for pregnant women?

Back 44

No crosses placenta, fetal hemorrhage, birth defects (blood bone proteins)

Front 45

Anticoagulant used in pregnant?

Back 45

Heparin, dose not cross placenta

Front 46

Warfarin adverse reactions?

Back 46

Skin necrosis aka WISN, venous thrmonisis (decrease protein C) worse w/ large loading dose

Front 47

warfarin adminstration?

Back 47

oral typically std dose 5-10mg then increased acording to PT to maintain 25% normal or 2-3 INR. Avoid going below 20%

INR= p’t PT/mean of normal PT for lab

Front 48

Reduces warfarin effect?

Back 48

Inducers of P450
barbiturates, cholestyramine, rifampin, diuretics, vit K

Front 49

Reverse warfarin?

Back 49

Vit k1(phytonadione, fresh frozen plasma, prothrombin cplx concentrates, rFVIIa

Front 50

Stop warfarin

Back 50

excessive anticoaglulant w/ or w/o bleeding

Front 51

Streptokinase MOA

Back 51

catalyst: plasminogen to plasmin via cplx w/ proactivator plasminogen

Front 52

Urokinase MOA

Back 52

Converts plasminogen to plasmin

Front 53

Thrombolytic drug categories?

Back 53

Plasminogen activators,
Recombinant tPA

Front 54

Streptokinase origin

Back 54

bacterial protein streptococci

Front 55

Urokinase Origin

Back 55

synthesized in human kidney

Front 56

Recombinant tissue plasminogen activators (t-PAs)

Back 56

Alteplase & reteplase

Front 57

Mutant recombinant t-PA

Back 57

Tenecteplase

Front 58

Preferentially activate fibrin bound plasminogen

Back 58

alteplase and reteplase

Front 59

Thrombolytic drugs clinical uses?

Back 59

IV, pulmonary embolism w/ hemodynamic instability, deep venous thrombosis, & ascending thrombophlebitis w severe lower extremity edema;
acute MI

Front 60

r t-PA unique use?

Back 60

acute ischemic stroke

Front 61

______ by ADP (blocked by clopidogrel) leads to a conformational change in platelet gpIIb/IIIa receptors that induces binding to fibrinogen

Back 61

Platelet activation

Front 62

r t-PA MOA

Back 62

activates plasminogen to release enzyme plasmin

Front 63

ADP R antagonist?

Back 63

clopidrogel, ticlopidine

Front 64

Thromboxane inhibitor?

Back 64

Asprin

Front 65

GPIIIa/IIb R antagonist

Back 65

abciximab, eptifibatide, tirofiban

Front 66

Antiplatelet categories?

Back 66

ADP R antagonist, Thromboxane inhibitor, GPIIIa/IIb R antagonist

Front 67

Asprin antiplatelet MOA

Back 67

irreversibly inhibits TXA2 synthesis via acetylation of COX enzyme

Front 68

Primary prophylazis of MI

Back 68

325 mg/dl asprin

Front 69

PAR1

Back 69

thrombin receptor protease activated

Front 70

P2Y12 & 1

Back 70

ADP receptor: g protein bound

Front 71

Clopidrogel, ticlopidine MOA

Back 71

Inhibitt P2Y12 on platelet

Front 72

Prodrug useful for patients who cant tolerate asprin

Back 72

Clopidrogel

Front 73

Clopidrogel, ticlopidine Uses?

Back 73

prevent thrombosis

Front 74

Ticlopidine> clopidrogel toxicity?

Back 74

Gi tox, hemorrahge, thrombotic thrombocytopenic purpura TTP, neutropenia

Front 75

Proton pump inhibitors (omeprazole)

Back 75

should be avoided w/ clopidrogel, reduces antiplatelet activty

Front 76

activators of GPIIb/IIIa that aid activation of platelet aggregation

Back 76

ADP, serotonin, shear forces, epinepherin, plasmin, thrombin, collagen, PAF, TXA2

Front 77

Abciximab MOA?

Back 77

Chimeric mAB that blocks gpIIb/IIIa & vibronectin

Front 78

Eptifibatide MOA?

Back 78

fibrinogen delta chain analog block binding of fibrinogen to IIb/IIIa

Front 79

Tirofiban MOA?

Back 79

similar to eptifabitide

Front 80

vibronectin

Back 80

extracellular matrix protein on endothelial and platelets.
adhesion molecule in the integrin family.

Front 81

Types of drugs that facilitate clotting?

Back 81

Vit K, clotting factors, fibrinolytic inhibitors, serine protease inhibitors

Front 82

Factor VIII deficiency

Back 82

Hemophilia A

Front 83

Factor VIII

Back 83

antihemophilic factor

Front 84

Christmas disease

Back 84

Hemophilia B

Front 85

Factor Ix deficiency

Back 85

Hemophilia B

Front 86

comsumption coagulopathy

Back 86

DIC (disseminated intravascular coagulation disorder)

Front 87

Lab findings to diagnose DIC

Back 87

Fibrin degredation products

Front 88

DIC natural course

Back 88

hypercoagulability succeeded by deficiency in clotting factors w/ hypocoagulability and hemorrhaging

Front 89

Factor XI deficiency

Back 89

hemophilia C

Front 90

Factor VII deficiency

Back 90

aka serum prothrombin conversion accelerator (SPCA) deficiency

Front 91

Types used to facilitate clotting

Back 91

Vit K, antiplasmin, clotting factors

Front 92

Antiplasmin drugs

Back 92

aminocaproic acid, aprotinin

Front 93

Clotting factors used to facilitate clotting clinically

Back 93

VII, VIII, IX,X, fresh frozen plasma (FFP) cryoprecipitate

Front 94

antiplasmin drugs are?

Back 94

fibrinolytic inhibitors

Front 95

Vit K is?

Back 95

fat soluble, K1 (phytonadione):leafy green veggies, K2(menaquinone): human intestinal bacteria
K3:menadione not for therapeutic use (water soluble)

Front 96

What to avoid w/ vitamin K?

Back 96

rapid infusion ( dyspnea, chest/back pain, SC-erratic bioavailability

Front 97

Vit K clinical use?

Back 97

depression of prothrombin by warfarin, vit K deficiency; Given to all newborns as prophylaxis

Front 98

protein C is a?

Back 98

Vit K dependent serine protease.

Front 99

Protein C is activated by?

Back 99

Activated by thrombin to APC.

Front 100

Protein C degrades?

Back 100

Degrades cofactor Va & VIIIa

Front 101

Protein C deficiency can lead to?

Back 101

Increased thrombis

Front 102

Protein S is a?

Back 102

Vit K dependent glycoprotein

Front 103

The two forms of protein S?

Back 103

Free and C4b bound