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

Anticoagulant, Antiplatelet, thromboltic agents 1 Flashcards

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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
warfarin is the drug of choice for what
oral anticoagulant
26
warfarin is used for what
anticoagulant venous thromboembolism PE prothetic heart valves
27
warfarin only works as an anticoagulant when administered how
in vivo
28
how is warfarin monitored
INR laboratory standardized quick one-stage prothrombin time
29
warfarin monitors what coagulation cascade pathway
extrinsic via prothrombin time
30
the goal for INR is what normally and what in prophylactic for heart valves
normal- 2.0-3.0 | prophylactic for heart valves- 2.5-3.0
31
what adverse reactions are there to warfarin
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)
32
genetic predisposition to warfarin are in what genes
CYP2C9 | VKORC1
33
what drugs or conditions increase warfarin response
``` vitamin K deficiency hepatic disease thyroid hormones cimetidine Aspirin Erythromycin cephalosporins ketoconazole ```
34
what drugs or conditions decrease warfarin response
cholestyramine oral contraceptives rifampin excess vitamin K
35
warfarin use in contraindicated in what patients
those with bleeding disorders or existing bleeding site | pregnant woman
36
what is used to treat warfarin overdose
``` whole blood or plasma vitamin K (phyonadione) ```
37
Direct Thrombin inhibitor are
Argatroban and dabigatran etexilate
38
direct thrombin inhibitors MOA
block active site of thrombin | active (free or fibrin bound thrombin)
39
argatroban is administered how
IV
40
argatroban is used for what
treatmetn and prophylaxis in thrombosis with heparin induced thromboytopenis
41
argatroban is monitored how
PTT
42
dabigatran is administed how
oral
43
dabigatran given how
a produg covered by esterase's to dabigatran
44
what drug is a substrate for p-glycoprotein transport
dabigatran
45
what is dabigatran used for
venous thrombosis prophylaxis | prevent stroke
46
caution must be used in what patients when administering dabigatran
diminished renal excretion
47
what are the side effects of dabigatran
bleedings
48
what is the goal of anti platelet drugs
diminish platelet function
49
antiplately drugs are used to treat what
arterial thrombotic diseases (TIA, unstable angina, history of MI)
50
Aspirin MOA
irreversible inhibitor COX, decreases TXA2 platelet aggregation
51
Adverse effects of aspirin
GI bleeding, pain and peptic ulcer | bleeding
52
Dipyridamole MOA
inhibits phosphodiesterase (increase platelet cAMP)
53
Dipyridamole use
given with warfarin for prevention of thromboembolism in patients with prosthetic heart valves
54
Clopidogrel, Ticlopidine, and cangelor are examples of what
P2Y12 receptor inhibitor
55
Clopidogrel, Ticlopidine, and cangelor MOA
ticlopidine and clopidogrel block ADP binding at the purinergic P2Y12 receptor
56
what P2Y12 receptor inhibitors are prodrugs
ticlopidine and clopidogrel
57
Clopidrogel metabolite and ticlopidine thiol metablolite work how
irreversible inhibitors of P2Y12 receptor
58
Cangrelor works how
reversible inhibitor | IV administration
59
ticlopidine and clopidogrel are used for what and which is preferred
reduced risk of thrombotic events in predisposed individuals | clopidogrel is preferred
60
Clopidogrel is used for what
reduce thrombotic events following MI, stroke, unstable angina, or peripheral arterial disease
61
major adverse effects of P2Y12 receptor inhibitors are
bleeding due to diminished platelet function thrombocytopenia purport ticlopidine can cause life threatening agranulocytosis
62
Abciximab and eptifibatide are examples
glycoprotein IIB/IIIA inhibitors
63
Abciximab and eptifibatide MOA
platelet glycoprotein IIb/IIIa receptor antagonists competitive reversible inhibitor inhibit platelet cross linking with fibrinogen monoclonal antibody Fab fragment
64
Abciximab and eptifibatide are used for what
acute coronary syndrome (unstable angina) prevent acute adjunct with angioplasty administered IV
65
Abciximab and eptifibatide adverse effects
bleeding | increased bruising
66
Abciximab and eptifibatide contraindications
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
glycoprotein IIb/IIIa inhibitors can't be used with what
warfarin
68
t-PA is inactivated by what
plasminogen activator inhibitor 1 (PAI-1)
69
alpha-2 antiplasmin does what
binds covalently to plasmin at a lysine rich binding site causing inactivation occurs only with circulating plasmin
70
streptokinase MOA
complexes with plasminogen promoting conformational change of plasminogen exposes catalytic site for conversion of a second plasminogen molecule to plasmin
71
streptokinase on what
fibrin bound and circulation plasminogen
72
therapeutic use of streptokinase
repercussion of occluded coronaries following acute MI PE arterial thrombosis
73
adverse effects of streptokinase
high antigenic activity | bleeding
74
contraindications of streptokinase
surgery or trauma in the past 10 days pre-exisiting bleeding disorder or episode intracranial trauma
75
antistreplase is what
streptokinase complexed with human lys-plasminogen: the active catalytic center is blocked by an acyl group (acyl group removed by plasma enzymes)
76
alteplase is what type of drug
tissue-type plasminogen activator (rt-PA)
77
alteplace is used for what
repercussion of coronary arteries in acute MI PE thrombotic stroke
78
tenecteplace is what type of drug
genetically engineered derivative of alteplace
79
tenecteplace is approved for
MI
80
tenecteplace is better than alteplace why
longer half-life greater fibrin specificity slower inactivation by PAI-1
81
minocaproic acid is what type of drug
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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