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Pharmacology > Blood Coagulation/Anticoagulants > Flashcards

Blood Coagulation/Anticoagulants Flashcards

1
Q

what is the role of thromboxane A2 in platelet aggregation

A

stimulates aggregation

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2
Q

what is the role of prostacyclin in platelet aggregation

A

inhibition of aggregation

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3
Q

heparin and warfarin mainly target factors __ and __

A

II
X

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4
Q

what is the function of proteins C and S

A

act as anticoagulants

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5
Q

antithrombin inactivates what clotting factors

A

IIa, IXa, Xa, XIa, and XIIa

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6
Q

protein C and S inhibit coagulation by inactivation of what clotting factors

A

Va and VIIIa

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7
Q

parenteral anticoagulants can either be indirect or direct acting. indirect acting include what 2 main classes

A

unfractionated (high molecular weight) heparin
low molecular weight heparin

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8
Q

what is the mechanism of action of unfractionated (high molecular weight) heparin

A

activates antithrombin III which inactivates factors IIa, IXa, and Xa

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9
Q

thrombin is clotting factor __

A

IIa

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10
Q

what is the mechanism of action of low molecular weight heparin

A

inhibits factor Xa by activation of antithrombin III

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11
Q

heparin shouldn’t be administered by what route

A

IM injection

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12
Q

why shouldn’t heparin be administered by IM injection

A

it causes hematoma in muscles

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13
Q

what is the preferred method of delivery of heparin

A

IV

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14
Q

unfractionated heparin is preferred over low molecular weight heparins in patients with compromised __ function

A

renal

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15
Q

in a rapid onset emergency condition, is warfarin or heparin used

A

heparin

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16
Q

is high or low molecular weight heparin preferred to prevent DVT and PE during prolonged bed rest/surgery

A

low

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17
Q

if severe bleeding occurs after discontinuing heparin, what can be used to neutralize heparin anticoagulant activity

A

protamine sulfate

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18
Q

what occurs in heparin induced thrombocytopenia (HIT)

A

heparin, platelet factor, and Ab immune complex and destroy platelets leading to ischemia of limbs, MI, stroke, and skin necrosis

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19
Q

what is used for treatment of heparin induced thrombocytopenia (HIT)

A

direct thrombin inhibitor such as Argatroban

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20
Q

what are some adverse reactions of heparin usage

A

osteoporosis
aldosterone synthesis inhibition
hypersensitivity/allergic reactions
increased hair loss

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21
Q

can heparin be used in pregnancy

A

yes- doesn’t cross BBB

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22
Q

is heparin safe to use in those with kidney disease

A

yes, it is metabolized in the liver and excreted in bile

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23
Q

what are some contraindications for heparin usage

A

heparin induced thrombocytopenia
hemophilia
ulcer lesions in GIT
dissecting aortic aneurysm
recent surgery (eye, brain, or spinal cord)

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24
Q

what is the mechanism of action of the synthetic heparin derivative fondaparinux

A

inhibition of factor Xa by antithrombin III

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25
Q

what is the preferred substitute to heparin in heparin induced thrombocytopenia

A

argatroban

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26
Q

what is the mechanism of action of warfarin

A

inhibition of synthesis of vitamin K dependent clotting factors

inhibition of vitamin K epoxide reductase

inhibition of anticoagulant proteins C and S

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27
Q

what are the 4 vitamin K dependent clotting factors

A

II, VII, IX, X

(2, 7, 9, 10)

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28
Q

why is warfarin not used for emergency situations

A

effect is not observed until after 3-5 days

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29
Q

since warfarin effect isn’t observed until 3-5 days after administration, what is given in the meantime

A

low molecular weight heparin

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30
Q

warfarin is metabolized by what enzyme

A

CYP450

31
Q

what is the international normalized ratio for warfarin monitoring

A

prothrombin time observed/normal prothrombin time

32
Q

what is recommended for the international normalized ratio for warfarin monitoring

A

2-3

> 3= bleeding complications
<2= no effect

33
Q

what is the effect of fetal warfarin syndrome

A

fetal hemorrhage
IUD
teratogenicity

34
Q

what is used instead of warfarin in the pregnant

A

heparin

35
Q

prolonged use of warfarin suppresses the synthesis of __ and __

A

protein C and S

36
Q

skin necrosis is a common effect of __ usage

A

warfarin

37
Q

what is the effect of cephalosporins on warfarin activity

A

cephalosporins destroy vitamin K producing bacteria–>
increased inhibition of vitamin K epoxide reductase by warfarin

38
Q

what is the affect of aspirin usage with warfarin

A

increased warfarin activity

39
Q

is warfarin or heparin preferred in atrial flutter and fibrillation and patients on prosthetic heart valves

A

warfarin

40
Q

what is the mechanism of action of direct acting oral anticoagulants

A

direct factor Xa inhibitor

41
Q

rivaroxaban, apixaban, and edoxaban are what kind of anticoagulant drugs

A

direct acting factor Xa inhibitors

42
Q

what drugs can be used for both treatment and prophylactic of acute DVT, PE, and venous thromboembolic disease

A

rivaroxaban
apixaban
edoxaban

(direct acting factor Xa inhibitors)

43
Q

what is an-dexa-net alfa used for

A

reversal of anti factor Xa effects (to stop uncontrolled bleeding in those taking factor Xa inhibitors)

44
Q

what is the mechanism of action of an-dexa-net alfa

A

it prevents factor Xa inhibiting drugs from binding to and inhibiting factor Xa

45
Q

what is the mechanism of action of direct thrombin inhibitors

A

directly bind to active site of thrombin

46
Q

what is the preferred drug for use in heparin induced thrombocytopenia

A

argatroban ( a direct thrombin inhibitor

47
Q

what is the mechanism of action of dabigatran

A

direct inhibitor of thrombin and fibrinogen (both bound and free forms)

48
Q

dabigatran is inhibited by what drug

A

ketoconazole

49
Q

dabigatran, an oral direct thrombin inhibitor is used to reduce the risk of recurrent __

A

venous thromboembolic disease

50
Q

what is the effect of idarucizumab on dabigatran

A

it irreversibly binds and rapidly reverses the anticoagulant effect

51
Q

what are the advantaes of dabigatran usage over warfarin

A

lower bleeding rate
rapid effects
no monitoring required
fewer drug+food interactions

52
Q

streptokinase and urokinase are enzymes used for what type of drug

A

fibrinolytic drugs (thrombolytics)

53
Q

what is the mechanism of action of fibrinolytic drugs

A

activate plasminogen that is bound to fibrin

54
Q

what type of drug is alteplase

A

fibrinolytic (thrombolytic)

55
Q

what is the advantage of reteplase and tenecteplase over alteplase as a fibrinolytic (thrombolytic) drugs

A

reteplase and tenecteplase have:
longer half life
a bolus dose is enough
no maintenance dose is required

56
Q

what is the mechanism of action of fibrinolytic drugs (thrombolytic)

A

convert plasminogen to plasmin
plasmin then degrades the fibrin and fibrinogen, causing clot dissolution

57
Q

what drug is used for clot dissolution in acute myocardial infarction

A

fibrinolytic agents such as streptokinase and urokinase

58
Q

what is the benefit of using fibrinolytic agents for acute myocardial infarction

A

more beneficial in ST-segment elevation

59
Q

what is an adverse effect of streptokinase use as a fibrinolytic (thrombolytic)

A

it can induce a hypersensitivity reaction

60
Q

in what situations are fibrinolytics contraindicated

A

prior intracranial hemorrhage
cerebral vascular lesion
malignant intracranial neoplasm
ischemic stroke within 3 months
suspected aortic dissection
significant closed-head trauma or facial trauma within 3 months

61
Q

what is the function of fibrinolytic inhibitors

A

block the activation of plasminogen to plasmin to prevent fibrinolysis (helps blood clot)

62
Q

what are fibrinolytic inhibitors used for

A

control post-surgery bleeding
heavy menstrual flow

63
Q

what is the mechanism of action of aspirin

A

irreversibly inhibit COX-1 inhibiting thromboxane A2 synthesis and prevents platelet activation

64
Q

low dose aspirin is recommended for patients age __ with high risk heart issues

A

40-70

65
Q

what is the mechanism of action of the antiplatelet drugs Ticlopidine, Clopidogrel, and Prasugrel

A

inhibition of P2Y12 ADP induced activation of GPIIb/IIIa receptors required for binding with fibrinogen and other platelets

66
Q

what is the advantage of Clopidogrel over Ticlopidine

A

more potent
rarely associated with neutropenia, leukopenia, and thrombocytopenia

67
Q

what antiplatelet drug is used as prophylaxis with warfarin in patients with prosthetic heart valves

A

dipyridamole

68
Q

what is the mechanism of action of dipyridamole

A

increases level of cAMP in platelets

69
Q

what is the action of abciximab

A

it’s an antibody against GPIIb/IIIa that prevents the binding of fibrinogen to GPIIa/IIIb

70
Q

when are GPIIb/IIIa receptor antagonists used

A

unstable angina
post MI
patients undergoing percutaneous coronary intervention

71
Q

thrombin activates platelets through _____ receptors

A

protease activated

72
Q

what is the mechanism of action of vorapaxar

A

competitive antagonist of PAR-1 and inhibits thrombin induced platelet aggregation

73
Q

what is the mechanism of action of cilostazol

A

phosphodiesterase III inhibitor

74
Q

what is the main use of cilostazol

A

treatment of intermittent claudication

Pharmacology (16 decks)

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