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PBL 2.2.4 > Pharm 23: Clots and bleeds > Flashcards

Pharm 23: Clots and bleeds Flashcards

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1
Q

How does aspirin thin the blood

A

Inhibits the synthesis of prostaglandins, thereby inhibiting the platelet granule release reaction and interfering with normal platelet aggregation.

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2
Q

Aspirin inhibits (enzymes)

A

COX 1/2 non selective

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3
Q

In platelets, an increase in the concentration of intracellular ____ leads to a decrease in platelet _____

A

In platelets, an increase in the concentration of intracellular cAMP leads to a decrease in platelet aggregability

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4
Q

Inhibitors of platelet phosphodiesterase decrease platelet aggregability by inhibiting __________

A

Inhibitors of platelet phosphodiesterase decrease platelet aggregability by inhibiting cAMP degradation

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5
Q

Dipyridamole MOA

A

platelet phosphodiasterase inhibitor

decreased platelet aggregation

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6
Q

Dipyridamole is administered with _________

Why?

A

Warfarin/aspirin

kinda weak

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7
Q

Dipyridamole side effect

A

Vasodilation leading to angina

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8
Q

Drugs that inhibit ADP-dependent platelet activation

A

clopidogrel

ticlopidine

prasugrel

aka thienopyridines

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9
Q

Ticlopidine indications

A

1) Secondary prevention of strokes when aspirin allergy
2)Post stent thrombosis prophylaxis (with aspirin)

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10
Q

Clopidogrel metabolism

A

Prodrug via P450

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11
Q

Clopidogrel indications

A

Secondary stroke prevention post MI

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12
Q

Clopidogrel dosing considerations

A

Loading dose to achieve effect then maintanance

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13
Q

Prasugrel use

A

Acute coronary syndromes during PCI

Cath lab drug

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14
Q

Prasugrel major AE cosideration

A

Dont give to stroke bc of head bleed risk

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15
Q

Ticagrelor MOA

A

competitive P2Y12 ADP receptor antagonist

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16
Q

Tricagelor use

A

Acute coronary syndromes

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17
Q

Tricagelor route

A

Oral with no hepatic activation needed

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18
Q

Eptifibatide MOA

A

GPIIb–IIIa receptor antagonist

Platelet inhibition

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19
Q

Abciximab MOA

A

Chimeric mouse–human monoclonal antibody directed against the human GPIIb–IIIa receptor.

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20
Q

Tirofiban MOA

A

nonpeptide tyrosine analogue that reversibly antagonizes fibrinogen binding to the platelet GPIIb–IIIa receptor.

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21
Q

Eptifibatide, tirofiban and abxcimab how to reveres

A

Abxicimab: give more platelets

Others: Wait

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22
Q

Vorapaxar MOA

A

protease-activated receptor 1 (PAR-1) antagonist one of two major thrombin receptors

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23
Q

Warfarine MOA

A

Epoxide reductase inhibitor

vitamin K cant regenerate

24
Q

Warfarin dosing considerations

A

Delayed action takes many doses to reach effect

25
Q

Warfarin kinetics

A

100% orally bioavailable, peak 1-4 hours, 99% albumin bound

26
Q

Warfarin drug drug interactions

A

Inhibitted by P450 enzyme activators

Increased by P450 inhibittors or antibiotics (less vit K availability)

27
Q

γ-carboxilated antiguaolant think

A

warfarin

28
Q

Warfarin contraindications

A

Pregnancy (cross placenta and bleed fetus)

29
Q

With warfarin monitor

A

PT/INR

30
Q

Heparin MOA

A

Cofactor for antithrombin III

-it serves as a catalytic surface to which both antithrombin III and the serine proteases bind

-induces a conformational change in antithrombin III that makes the reactive site of this molecule more accessible to the attacking protease

31
Q

LMW Heparin are more efficient in ___ and less efficient in _______.

A

More efficient: Catalyze factor Xa inactivation

Less efficient: catalyze inactivation of thrombin

32
Q

Unfractionated heparin

A

Less selective.. catalyzes both thrombin and factor Xa inactivation

33
Q

Heparin structure

A

Pentasacchiride structure… super acidic

34
Q

fondaparinux

A

Binds antithrombin III to indirectly inhibit Xa

35
Q

Heparin effect monitored via

A

aPTT

36
Q

LMW heparin names

A

Enoxaparin
Dalteparin
Tinzaparin

37
Q

Rivaroxaban and apixaban MOA

A

Direcltly inhibit factor Xa by competitive inhibition

do not require antithrobin III

38
Q

Lepidurin MOA

A

Direct thrombin inhibitor

39
Q

Heparin Induced Thrombocytopenia HIT MOA

A

Antibodies to hapten when heparin molecules bind to platelet. Platelets then removed by body

40
Q

Desirudin use

A

DVT prophalaxis in hip replacement

41
Q

HIT treatment

A

lepirudin

42
Q

Bivalirudin MOA and use

A

Inhibits thrombin activity. Use in cath lab

43
Q

Argatroban MOA and use

A

Thrombin inhibitor. Used for patients wtih HIT.

Biliary excretion, use with bad kidneys

No exosite activity

44
Q

Dabigatran MOA and use

A

Oral direct thrombin inhibitor

Use in non valve afib, and as warfarin substitute for mechanical valve pts

45
Q

Dabigratan mechanics /monitoring

A

Prodrug… does not need to be monitored

46
Q

Recombinant activated protein C (r-APC) MOA and use

A

Used in septic shock by cleaving factors Va and VIIIa

47
Q

Streptokinase moa and use

A

1) Forms complex with plasminogen, exposing active site

2) Now active, plasminogen cleaves other plasminogens to plasmin

STEMI and PE

48
Q

t-PA MOA and use

A

Binds to fresh thrombus, causing fribinolysis. After binding, t-PA is conformationally changed and it can now activate plasminogen

Use in stroke, STEMI, PE

49
Q

Tenecteplase vs tPA

A

More resistant to plasminogen activator inhibitor 1

Longer half life

Admin as single weight based bolus

50
Q

Reteplase what to know

A

Re- use (2 boluses 30 min apart)

51
Q

Protamine MOA and use

A

Chemical antagonist to heparin. used when too much heparin

52
Q

Aprotinin MOA and use

A

Serine protease inhibitor: Plasmin, thrombin t-pa

not really used bc anaphylaxis

53
Q
A
54
Q
A
55
Q
A

PBL 2.2.4 (13 decks)

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