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20003 > haemostasis and thrombosis pharmacology > Flashcards

haemostasis and thrombosis pharmacology Flashcards

1
Q

what is haemostasis

A

the arrest of blood loss from damaged vessels

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2
Q

how does the body stop/ reduce blood loss

A
  • vascular spasm
  • platelet plug formation
  • clotting/ coagulation
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3
Q

what is the mechanism of action of antiplatelets (aspirin)

A
  • irreversibly inactivates COX1
  • stops thromboxane A2 synthesis
  • 7 days
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4
Q

what are the adverse effects of asprin

A

increase haemorrhagic stroke and GI bleeding

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5
Q

what is the mechanism of action of ADP-induced platelet aggregation inhibition

A
  • P2Y12 = purine receptor of ADP
  • inhibits activation of GP IIb/IIIa receptors
  • needed for platelets and fibrinogen to bind
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6
Q

why are clopidogrel and aspirin used together

A
  • anticoagulants
  • work in conjunction with one another
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7
Q

what is the mechanism of action of GP IIb/IIIa receptor blockers

A
  • bind to GP IIb/IIIa
  • block fibrinogen binding
  • stops aggregation
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8
Q

when are GP IIb/IIIa receptor blockers used

A
  • with aspirin
  • prevent clotting before invasive heart procedures
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9
Q

what are the side affects of GP IIb/IIIa receptor blockers

A
  • bleeding
  • thrombocytopenia
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10
Q

what are the 2 different ways that anticoagulants can work

A
  1. inhibiting action of coagulation factors
  2. inhibiting synthesis of coagulation factors
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11
Q

what anticoagulants inhibit synthesis of coagulation factors

A

vitamin K antagonists

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12
Q

what are parental anticoagulants that inhibit action of coagulation factors

A
  1. thrombin inhibitors (direct & indirect)
  2. factor x inhibitors
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13
Q

what are direct oral anticoagulants that inhibit action of coagulation factors

A
  1. thrombin inhibitor
  2. factor X inhibitors
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14
Q

what are examples of parental indirect thrombin inhibitors

A
  • heparin
  • low molecular weight heparins
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15
Q

what is the mechanism of action of parental indirect thrombin inhibitors

A
  • speed up antithrombin interaction
  • inhibits thrombin and factor X
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16
Q

what is the pharmacokinetics of parental indirect thrombin inhibitors

A
  • renal elimination
  • LMWH half life > heparin half life
  • IV and subcut
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17
Q

what are the adverse effects of parental indirect thrombin inhibitors

A
  • bleeding
  • hypersensitivity
  • thrombocytopenia
  • thrombosis
  • osteoporosis
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18
Q

what are the reversal agents of heparin

A
  • protamine sulfate
  • ciraparantag
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19
Q

what are the reversible agents of low molecular weight heparins

A
  • andexanet
  • ciraparantag
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20
Q

what is an example of parental direct thrombin inhibitors

A

bivalirudin

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21
Q

what is the mechanism of action of parental direct thrombin inhibitors

A

direct thrombin inhibitor

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22
Q

what is the pharmacokinetics of parental direct thrombin inhibitors

A

IV administration

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23
Q

what are the adverse effects of parental direct thrombin inhibitors

A

bleeding

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24
Q

what is an example of parental factor X inhibitor

A

fondaparinux

25
Q

what is the mechanism of action of parental factor X inhibitors

A
  1. binds to antithrombin III
  2. selectively neutralises factor Xa by antithrombin III
26
Q

what is the pharmacokinetics of parental factor X inhibitors

A
  • SC administration
  • eliminated unchanged in urine
27
Q

what are the adverse effects of parental factor X inhibitors

A

bleeding

28
Q

what is dabigatran etexilate

A

prodrug of active moiety dabigatran to overcome poor bioavailability

29
Q

what is the therapeutic use of dabigatran etexilate

A
  • prevention of stroke & systemic embolism in af
  • DVT and PE treatment
30
Q

what are the adverse effects of dabigatran etexilate

A
  • bleeding
  • GI effects
31
Q

what are the reversal agents of dabigatran etexilate

A
  • idarucizumab
  • ciraparantag
32
Q

what are examples of direct oral anticoagulant thrombin inhibitors

A
  • dabigatran etexilate
  • edoxaban
  • apixaban
  • rivaroxaban
  • betrixaban
33
Q

what is the mechanism of action of vitamin K antagosist

A
  • inhibit factors 2,7,9,10
  • need vit K for synthesis
  • reductase inhibited > reduced vitamins > no vit K > no clotting of factors needing K
34
Q

what is an example of vitamin K antagonists

A

warfarin

35
Q

what is the therapeutic use of vitamin K antagonists

A
  • prevent & treat DVT, PE
  • stroke prevention in af
  • venous thromboembolism prevention
36
Q

what is the pharmacokinetics of warfarin

A
  • 99% bound to plasma
  • crosses placental barrier
  • low therapeutic index
37
Q

what are the adverse effect of vitamin K antagonists

A

bleeding

38
Q

what is the reversal agent to vitamin K antagonists - warfarin

A

vitamin K1

39
Q

what does a low therapeutic index mean

A

high levels can be reached very quickly and become toxic

40
Q

what is the international normalized ration

A

INR = (patient PT/ mean normal PT)^ISI

41
Q

what is the international sensitivity index

A

sensitivity of the thromboplastin reagent compare to WHO standards

42
Q

what is the action of thrombolytic drugs

A
  • fibrinolysis
    1. activates plasminogen
    2. activated to plasma
    3. degrades fibrin
43
Q

when is reperfusion therapy used

A
  • STEMI pts
  • aims to restore blood flow to infarct
44
Q

what is alteplase

A

tissue plasminogen activator

45
Q

how doe alteplase and Tenecteplase work

A

activate plasminogen bound to the fibrin clot

46
Q

what is the therapeutic use of alteplase

A
  • STEMI
  • acute ischemic stroke
  • massive PE
47
Q

what is the therapeutic use of Tenecteplase

A

STEMI

48
Q

what are the adverse effects of firbrinolytics

A
  • bleeding complications
  • angioedema
49
Q

what are the reversable agents for firbinolytics

A

TXA

50
Q

what may cause bleeding problems

A
  • haemophilia
  • VW disease
  • severe liver disease
  • reduce vit K absorption
  • GI surgery - fibrinolytic state
  • anticoagulants
51
Q

what does TXA do

A

inhibits plasminogen activation

52
Q

what is TXA used to treat

A
  • bleeding conditions
  • menorrhagia
  • life threatening bleeding
53
Q

why is desmopressin used as an antifibrinolytic agent

A

increase plasma concentration for factor VIII and vWF

54
Q

why is vitamin K used as an anti-fibrinolytic agent

A
  • fat soluble vitamin
  • forms clot factors II, VII. IX, X
55
Q

what does factor VIII do

A

accelerates the process of fibrin formation

56
Q

what does vWF do

A

enhances platelet adhesion to subendothelial tissue

57
Q

what drugs can be used as anti-fibrinolytic agents

A
  • desmopressin
  • vitamin K
  • TXA
58
Q

what are thrombolytic drugs

A
  • alteplase
  • tenecteplase

20003 (17 decks)

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