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Anticoagulant, Antiplatelet, thromboltic agents > Anticoagulant, Antiplatelet, thromboltic agents 1 > Flashcards

Anticoagulant, Antiplatelet, thromboltic agents 1 Flashcards

1
Q

Heparin MOA

A

binds reversibly to Antithrombin-III
accelerates inactivation by AT-III of intrinsic and common pathway
Thrombin, IXa, Xa bind irreversibly to Arg-Ser site on AT-III

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2
Q

what drug has anticoagulant activity both in vitro and in vivo

A

heparin

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3
Q

heparin has what clinical uses

A

venous thrombosis
pulmonary embolism
patency of IV cannulas

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4
Q

what anticoagulant can be used in pregnancy

A

Heparin and low molecular weight heparin (discontinue use 24 hour prior to induction of labor)

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5
Q

what method of administration is contraindicated for heparin use and why

A

intramuscular

induces painful hematoma

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6
Q

what effect other than anticoagulant does heparin have

A

lipid clearing effect by activating lipoprotein lipase (cleave TG from VLDL)

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7
Q

how does one monitor heparin

A

activated partial thromboplastin time (PTT)

this monitors the common and intrinsic pathway

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8
Q

what are the adverse effects associated with heparin use

A

bleeding- Heparin Induced Thrombocytopenia (type 1 non immune mediated and type 2 immune mediated)
osteoporosis (if given for more than 6 months)

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9
Q

treatment of excess hemorrhage due to heparin can be done how

A

protamine sulfate- the heparin-protamine complex cannot bind to AT-III
administer plasma or blood containing coagulation factors

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10
Q

what is protamine sulfate

A

heparin-protamine complex cannot bind to AT-III

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11
Q

Heparin use is contraindicated for use in what

A

bleeding disorder

pre-existing bleeding sites

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12
Q

Enoxaparin, dalteparin, and tinzaparin are examples of what

A

low molecular weight heparin

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13
Q

low molecular weight heparin have what MOA

A

higher specificity for enhanced antithrombin III inactivation of Xa

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14
Q

low molecular weight heparin is used for what

A

prophylaxis and acute deep vain thrombosis, pulmonary embolism, orthopedic abdominal surgery
unstable angina or non-Q-wave MI

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15
Q

how is low molecular heparin administered

A

sub-cutaneous

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16
Q

how does one monitor low molecular weight heparin

A

anti-Xa activity

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17
Q

LMW heparin is better than unfractioned heparin why

A

longer half life
can be used outpatient
lower incidence of thrombocytopenia (less binding to platelet proteins)
predicable response

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18
Q

what does one need to monitor in long term use of unfractioned heparin

A

platelet count

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19
Q

Fondaparinux MOA

A

synthetic pentasaccharide binds to ATIII to accelerate only factor Xa inactivation

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20
Q

Fondaparinux is used for what

A

DVT acute and postoperative
PE
can be used in pregnancy (stope 24 hours b4 labor)

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21
Q

adverse effects of Fondaparinux

A

bleeding

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22
Q

contraindications of Fondaparinux

A

active bleeding

severe renal impairment

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23
Q

warfarin MOA

A

inhibits conversion of vitamin K epoxide reductase

inhibits hepatic synthesis of biologically active vitamin K-dependent clotting factors, protein C and S

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24
Q

biological activity of warfarin requires what

A

gamma-carboxyglutamyl residues on clotting factors

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25
Q

warfarin is the drug of choice for what

A

oral anticoagulant

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26
Q

warfarin is used for what

A

anticoagulant
venous thromboembolism
PE
prothetic heart valves

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27
Q

warfarin only works as an anticoagulant when administered how

A

in vivo

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28
Q

how is warfarin monitored

A

INR laboratory standardized quick one-stage prothrombin time

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29
Q

warfarin monitors what coagulation cascade pathway

A

extrinsic via prothrombin time

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30
Q

the goal for INR is what normally and what in prophylactic for heart valves

A

normal- 2.0-3.0

prophylactic for heart valves- 2.5-3.0

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31
Q

what adverse reactions are there to warfarin

A

hemorrhage (more likely to occur if changes in absorption or metabolism of warfarin or vitamin K, alteration occurs in synthesis or catabolism of coagulation factors)

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32
Q

genetic predisposition to warfarin are in what genes

A

CYP2C9

VKORC1

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33
Q

what drugs or conditions increase warfarin response

A 
vitamin K deficiency
hepatic disease
thyroid hormones
cimetidine
Aspirin
Erythromycin
cephalosporins
ketoconazole
34
Q

what drugs or conditions decrease warfarin response

A

cholestyramine
oral contraceptives
rifampin
excess vitamin K

35
Q

warfarin use in contraindicated in what patients

A

those with bleeding disorders or existing bleeding site

pregnant woman

36
Q

what is used to treat warfarin overdose

A 
whole blood or plasma
vitamin K (phyonadione)
37
Q

Direct Thrombin inhibitor are

A

Argatroban and dabigatran etexilate

38
Q

direct thrombin inhibitors MOA

A

block active site of thrombin

active (free or fibrin bound thrombin)

39
Q

argatroban is administered how

A

IV

40
Q

argatroban is used for what

A

treatmetn and prophylaxis in thrombosis with heparin induced thromboytopenis

41
Q

argatroban is monitored how

A

PTT

42
Q

dabigatran is administed how

A

oral

43
Q

dabigatran given how

A

a produg covered by esterase’s to dabigatran

44
Q

what drug is a substrate for p-glycoprotein transport

A

dabigatran

45
Q

what is dabigatran used for

A

venous thrombosis prophylaxis

prevent stroke

46
Q

caution must be used in what patients when administering dabigatran

A

diminished renal excretion

47
Q

what are the side effects of dabigatran

A

bleedings

48
Q

what is the goal of anti platelet drugs

A

diminish platelet function

49
Q

antiplately drugs are used to treat what

A

arterial thrombotic diseases (TIA, unstable angina, history of MI)

50
Q

Aspirin MOA

A

irreversible inhibitor COX, decreases TXA2 platelet aggregation

51
Q

Adverse effects of aspirin

A

GI bleeding, pain and peptic ulcer

bleeding

52
Q

Dipyridamole MOA

A

inhibits phosphodiesterase (increase platelet cAMP)

53
Q

Dipyridamole use

A

given with warfarin for prevention of thromboembolism in patients with prosthetic heart valves

54
Q

Clopidogrel, Ticlopidine, and cangelor are examples of what

A

P2Y12 receptor inhibitor

55
Q

Clopidogrel, Ticlopidine, and cangelor MOA

A

ticlopidine and clopidogrel block ADP binding at the purinergic P2Y12 receptor

56
Q

what P2Y12 receptor inhibitors are prodrugs

A

ticlopidine and clopidogrel

57
Q

Clopidrogel metabolite and ticlopidine thiol metablolite work how

A

irreversible inhibitors of P2Y12 receptor

58
Q

Cangrelor works how

A

reversible inhibitor

IV administration

59
Q

ticlopidine and clopidogrel are used for what and which is preferred

A

reduced risk of thrombotic events in predisposed individuals

clopidogrel is preferred

60
Q

Clopidogrel is used for what

A

reduce thrombotic events following MI, stroke, unstable angina, or peripheral arterial disease

61
Q

major adverse effects of P2Y12 receptor inhibitors are

A

bleeding due to diminished platelet function
thrombocytopenia purport
ticlopidine can cause life threatening agranulocytosis

62
Q

Abciximab and eptifibatide are examples

A

glycoprotein IIB/IIIA inhibitors

63
Q

Abciximab and eptifibatide MOA

A

platelet glycoprotein IIb/IIIa receptor antagonists
competitive reversible inhibitor
inhibit platelet cross linking with fibrinogen
monoclonal antibody Fab fragment

64
Q

Abciximab and eptifibatide are used for what

A

acute coronary syndrome (unstable angina)
prevent acute adjunct with angioplasty
administered IV

65
Q

Abciximab and eptifibatide adverse effects

A

bleeding

increased bruising

66
Q

Abciximab and eptifibatide contraindications

A

history of hemorrhagic stroke
active internal bleeding or GI/genitourinary bleeding in the past 6 weeks
thrombocytopenia
major surgery or trauma in past 6 weeks

67
Q

glycoprotein IIb/IIIa inhibitors can’t be used with what

A

warfarin

68
Q

t-PA is inactivated by what

A

plasminogen activator inhibitor 1 (PAI-1)

69
Q

alpha-2 antiplasmin does what

A

binds covalently to plasmin at a lysine rich binding site causing inactivation occurs only with circulating plasmin

70
Q

streptokinase MOA

A

complexes with plasminogen promoting conformational change of plasminogen exposes catalytic site for conversion of a second plasminogen molecule to plasmin

71
Q

streptokinase on what

A

fibrin bound and circulation plasminogen

72
Q

therapeutic use of streptokinase

A

repercussion of occluded coronaries following acute MI
PE
arterial thrombosis

73
Q

adverse effects of streptokinase

A

high antigenic activity

bleeding

74
Q

contraindications of streptokinase

A

surgery or trauma in the past 10 days
pre-exisiting bleeding disorder or episode
intracranial trauma

75
Q

antistreplase is what

A

streptokinase complexed with human lys-plasminogen: the active catalytic center is blocked by an acyl group (acyl group removed by plasma enzymes)

76
Q

alteplase is what type of drug

A

tissue-type plasminogen activator (rt-PA)

77
Q

alteplace is used for what

A

repercussion of coronary arteries in acute MI
PE
thrombotic stroke

78
Q

tenecteplace is what type of drug

A

genetically engineered derivative of alteplace

79
Q

tenecteplace is approved for

A

MI

80
Q

tenecteplace is better than alteplace why

A

longer half-life
greater fibrin specificity
slower inactivation by PAI-1

81
Q

minocaproic acid is what type of drug

A

inhibitor of plasminogen activation

lysine analog, compete for lysine binding site on plasminogen and plasmin

Anticoagulant, Antiplatelet, thromboltic agents (1 decks)

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