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HLSC 220 Pharmacotherapeutics for Health Professionals 💊 > Hemostasis Modifier Drugs - Ch. 55 > Flashcards

Hemostasis Modifier Drugs - Ch. 55 Flashcards

1
Q

What is hemostasis?

A

Process that halts bleeding after injury to a blood vessel
1. Forms a platelet plug
2. Fibrin produced (clotting cascade, plasma proteins)

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1
Q

What are hemostasis modifier agents?

A

Anticoagulants
Antiplatelet drugs
Thrombolytic drugs
Hemostatic agents

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2
Q

What do anticoagulants do?

A

Inhibit the action or formation of clotting factors
Prevent clot formation

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3
Q

What do anti platelet drugs do?

A

Inhibit platelet aggregation
Prevent platelet plugs

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4
Q

What do thrombolytic drugs do?

A

Lyse existing/preformed clots

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5
Q

What do hemostatic agents do?

A

Promote blood coagulation

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6
Q

What is the final product of the clotting cascade?

A

Fibrin

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7
Q

What is the clotting/coagulation cascade divided into?

A

Intrinsic pathway
Extrinsic pathway

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8
Q

What is the other name for anticoagulants?

A

Blood thinners

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9
Q

How are anticoagulants used?

A

Prophylactically

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10
Q

What are anticoagulants used to prevent?

A

Clot formation (thrombus)
Emboli (dislodged clots)

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11
Q

What are anticoagulants not used for?

A

Do not use to lyse/break down existing clots

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12
Q

In what settings are anticoagulants used to prevent clot formation?

A

MI
Unstable angina
Atrial fibrillation
DVT e.g, major orthopaedic surgery
Indwelling devices (e.g, mechanical heart valves)
Pulmonary embolism

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13
Q

Examples of anticoagulants that all prevent clot formation?

A

Heparin and low molecular weight heparins (LMWH)
Warfarin -oral
Direct-Acting Oral Anticoagulants (DOACs)
-Direct factor X & Thrombin inhibitors

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14
Q

When is anticoagulant use contraindicated?

A

Known drug allergy
Acute bleeding process
Thrombocytopenia

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15
Q

What adverse effects are associated with anticoagulants?

A

Bleeding risk
-gums bleed
-nosebleeds
-unusual bruising
-anemia/low Hct
-tarry stools

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16
Q

What is the mechanism of action of Heparin?

A

Indirectly inhibits activity of multiple proteins on cascade

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17
Q

What proteins are inhibited by heparin?

A

-Thrombin (II)
-Factor Xa
-Intrinsic pathway factors

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18
Q

What is natural heparin?

A

Obtained from animal sources

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19
Q

how is heparin monitored because of its unpredictable dosage?

A

Activated partial thromboplastin times (aPTT)

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20
Q

What pathway does aPTT measure?

A

Intrinsic pathway

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21
Q

What do aPTTs need to be?

A

1.5 - 2.5 x greater than 40 sec (control)

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22
Q

How is Heparin administered?

A

Parenteral (IV or SC)

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23
Q

How long does it take for Heparin to be effective?

A

Seconds

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24
Q

What is the half life of Heparin?

A

Short half life
1-2 hours

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25
Q

What adverse effects are associated with Heparin?

A

Heparin-induced thrombocytopenia (HIT)
Hypersensitivity reactions

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26
Q

What is Heparin-induced thrombocytopenia (HIT)?

A

The body reacts to heparin in a way that causes platelets to clot instead of preventing them
-Increases blood clots
-1-5% population (>4 days of administration)
-stop heparin administration and use an alternative

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27
Q

What hypersensitive reactions does Heparin cause?

A

Urticaria (hives)
Fever
Chills

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28
Q

What is the antidote for heparin?

A

protamine sulfate

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29
Q

What does protamine sulphate do?

A

Reverses anticoagulant effects

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30
Q

Examples of low-molecular-weight heparins (LMWHs)?

A

Enoxaparin
Tinzaparin
Dalteparin

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31
Q

What do Low-molecular-weight heparins (LMWHs) have that heparins don’t?

A

More predictable anticoagulant response

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32
Q

low-molecular-weight heparins (LMWHs) do not require what?

A

Frequent lab monitoring
-Often given at home

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33
Q

How are low-molecular-weight heparins (LMWHs) administered?

A

SC q12h

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34
Q

What is the mechanism of action of low-molecular-weight heparins (LMWHs)?

A

Indirectly inhibits Factor X only

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35
Q

What antidote is used for low-molecular-weight heparins (LMWHs)?

A

Protamine sulfate
(same as heparin)

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36
Q

What are some other anticoagulant drugs?

A

Danaparoid
Fondaparinux

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37
Q

What is Danaparoid?

A

anticoagulant that is structurally distinct from heparin
Alternative to heparin

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38
Q

How is Danaparoid administered?

A

SC or IV

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39
Q

What is Fondaparinux?

A

Synthetic anticoagulant

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40
Q

How is Fondaparinux administered?

A

SC or IV

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41
Q

Subcutaneous LMWH doses should be injected only in what area?

A

Abdomen only
-Rotate sites around abdomen

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42
Q

What is an oral anticoagulant?

A

Warfarin (Coumadin)

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43
Q

What is warfarin?

A

Modified coumarin

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44
Q

What is the mechanism of action of Warfarin?

A

Vitamin K “antagonist”
-Reduces ‘ready for action” clotting factors in plasma so clotting time is extended

45
Q

What is Vitamin K used for?

A

Production of several clotting factors (VII, IX, X, prothrombin) in liver cells

46
Q

What do Warfarin effects depend on?

A

Clotting factors turnover (proteins degradation)

47
Q

How long may Warfarin’s max effect take?

A

3-5 days
-effects start within 24 hours

48
Q

Patients may be started on 5 days on a combination of what anticoagulants?

A

LMWHs + warfarin
-then LMWH is withdrawn

49
Q

How is warfarin monitored?

A

Clotting lab test
-Prothrombin time (PT)
INR (international normalization reference ratio)

50
Q

What pathway does PT/INR measure?

A

Extrinsic

51
Q

For the drug to be therapeutic, PT needs to be within what range?

A

1.3-1.5 times the normal (control) level

52
Q

What is the normal target INR range?

A

2 to 3 x control
Some need to be 2.5 to 3.5 (normal is 0.8 to 1.2) eg mechanical heart valves

53
Q

If excessive PT/INR during Warfarin, use of what can begin?

A

Vit K

54
Q

How can Vitamin K be administered if excessive PT/INR?

A

IV (slow infusion) 4-8h effect
PO effect within 24 hours

55
Q

When is Warfarin use contraindicated?

A

Pregnancy
-Risk for fatal bleeding, teratogenicity and spontaneous abortion

-Use LMWH instead

56
Q

What should someone do is they are taking Warfarin?

A

Maintain intake of vitamin K
-Tomatoes, dark leafy green veggies)

Wear medical alert bracelet

Consult physician before taking other drugs because warfarin has many drug-drug interactions

57
Q

Warfarin administration may be started while the client is still on what drug?

A

Heparins
-until prothrombin times/INR indicate adequate anticoagulation

58
Q

How long does it take for the full therapeutic effect of warfarin ?

A

several days

59
Q

What are the advantages of Direct-Acting Oral Anticoagulants (DOACs) over Warfarin?

A

Rapid onset and offset
Fixed doses
No blood test
Few drug-drug interactions
no dietary concerns
Lower risk of bleeds

60
Q

Example of Direct-Acting Oral Anticoagulants (DOACs)??

A

dabigatran
rivaroxaban
apixaban
betrixaban
edoxaban

61
Q

What is the mechanism of action of Dabigatran?

A

Directly inhibits thrombin

62
Q

How is dabigatran administered?

A

PO

63
Q

Adverse effects associated with dabigatran?

A

GI disturbances
-Nausea, vomiting, abdominal pain, bloating

64
Q

What is the mechanism of action of rivaroxaban
apixaban, betrixaban and edoxaban?

A

Directly inhibit Factor Xa

65
Q

How is rivaroxaban, apixaban, betrixaban and edoxaban adminsitered (Factor X inhibitor DOACs)?

A

PO

66
Q

What is the antidote for dabigatran?

A

Idarucizumab (antibody)

67
Q

What is the antidote for Factor X inhibitor DOACs?

A

andexanet alfa (modified factor X)

68
Q

All DOACs use required what?

A

Annual renal function test
- if below min function, changed to Vit K antagonist

69
Q

All anticoagulants increase the risk for what?

A

Bleeding
-Mild to life-threatening

70
Q

What are signs of abnormal bleeding?

A

bleeding of gums while brushing teeth
unexplained nosebleeds
bruising
heavier menstrual bleeding
bloody or tarry stools, vomiting blood
bloody urine or sputum
abdominal pain

71
Q

What are some anti platelet agents?

A

Acetylsalicyclic acid (Aspirin) - 81 mg EC
Pentoxifylline
Clopidogrel (plavix), prasurgel, ticlopidine
ticagrelor
GPIIb/IIIa antagonists

72
Q

What is the mechanism of action of Aspirin?

A

Inhibits COX enzyme pathway in platelets (irreversible)

73
Q

What is the mechanism of action of clopidogrel?

A

Irreversible ADP receptor blocker
-effects last the entire life-time of the platelet

74
Q

What is the mechanism of action of ticagrelor?

A

Reversible ADP receptor blocker

75
Q

What are anti platelet drugs used for?

A

Antithrombotic effects
-Reduce risk of MI
-Reduce risk of stroke

76
Q

The combination of anti platelet drugs, Aspirin + clopidogrel produces what effects?

A

Additive anti platelet activity but increased bleeding potential

77
Q

Where are the receptors for GPIIb/IIIa antagonists?

A

On platelets

78
Q

What activates GPIIb/IIIa receptors?

A

TXA2, ADP and 5-HT

79
Q

What are Glycoproteins IIb/IIIa used for?

A

Required for fibrinogen cross-linking = platelet aggregation

80
Q

What do GPIIb/IIIa antagonists do?

A

Prevent fibrinogen cross linking
-no platelet aggregation

81
Q

Example of GPIIb/IIIa antagonists?

A

Abciximab
Tirofiban

82
Q

How does Abciximab bind to GPIIb/IIIa receptors on platelets?

A

Irreversibly binds
-Is an antibody

83
Q

How does Tirofiban bind to GPIIb/IIIa receptors on platelets?

A

Reversibly binds

84
Q

Clients taking anti platelet drugs should be taught the same things as those taking what kind of drugs?

A

Anticoagulation drugs

85
Q

What is a group of thrombolytic agents?

A

Recombinant tissue plasminogen activator (tPA)

86
Q

Examples of tPA drugs?

A

Alteplase
Tenecteplase
reteplase

87
Q

How is Alteplase administered?

A

Slow infusion

88
Q

Describe the half life of alteplase?

A

short

89
Q

How is tenectephase administered?

A

Single bolus

90
Q

Describe the half life of tenectephase?

A

Long

91
Q

How is Reteplase administered?

A

2x bolus

92
Q

Describe the half life of Reteplase?

A

long

93
Q

What is the mechanism of action of thrombolytic agents?

A

Activate fibrinolytic system to break down clot in blood vessel

94
Q

What enzyme do thrombolytic agents activate to cause fibrinolysis?

A

Plasminogen which converts to Plasmin
-Plasmin digests fibrin, dissolves clot

95
Q

When thrombolytic agents lyse existing clots, what happens?

A

Blood flow is re-established
e.g, Heart muscle via coronary arteries (MI)
broin (stroke)

96
Q

What are thrombolytic agents used for?

A

Acute MI
Arterial thrombolysis
DVT
Occlusion of shunts or catheters
Pulmonary embolus

97
Q

When os thrombolytic agent use contraindicated?

A

Allergy
Concurrent use of other anticoagulation

98
Q

What adverse effects are associated wit thrombolytic agents?

A

Bleeding
Nausea, vommiting
Hypotension
Anaphylactoid reactions
Dysrhythmias

99
Q

What kind of bleeding is associated with thrombolytic agents?

(adverse effects)

A

Internal
Intracranial
Superficial

100
Q

What do antifibrinolytic agents do?

A

Some prevent the lysis of fibrin in an existing clot so clot remains

-

101
Q

What do antifibrinolytic agents promote?

A

Promote clot formation and/or clot maintenance
-improve clotting factor survival

102
Q

Examples of Antifibrinolytic agents?

A

Aminocaproic acid
tranexamic acid (TXA)
Desmopressin

103
Q

What is the mechanism of action of aminocaproic acid, tranexamic acid (TXA)?

A

Inhibits fibrinolysis by blocking plasminogen activation

104
Q

What is aminocaproic acid and tranexamic acid (TXA) used for?

A

Trauma (bleeding)
Antidote to thromolytic agents e.g, alteplase

105
Q

What is desmopressin?

A

Synthetic pituitary hormone similar to Vasopressin (ADH)

106
Q

What is desmopressin used for?

A

Diabetes insipidus
Mild hemophilla A (VIII deficiency)

107
Q

What does desmopressin do to plasma concentration of factor VIII?

A

Increases plasma concentration of factor VIII by von Willibrand factor release from endothelial cells

108
Q

What are antifibrinolytic agents used to prevent and treat?

A

Excessive bleeding
-Hyperfibronolysis
-Surgical complications
-Excessive oozing from surgical sites e.g, chest tubes
-reduces total blood loss and duration of bleeding in post op period

109
Q

When is antifibrinolytic drug use contraindicated?

A

Allergy
Never used in DIC (disseminated intravascular coagulation)
-very rare but critical
-uncontrolled clotting

110
Q

What adverse effects are associated with antifibrinolytic agents?

A

Uncommon and mild
Rare reports of thrombotic events

HLSC 220 Pharmacotherapeutics for Health Professionals 💊 (31 decks)

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