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Anticoagulants & Antiplatelets Flashcards

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1
Q

What are the 4 main types of anti platelets

A

Aspirin (COX inhibitor)

Clopidogrel, Ticagrelor, Prasugrel, Ticlopidine (ADP receptor antagonist)

Abciximab, Tirofiban, Eptifibatide (Glycoprotein 2b/3a inhibitor)

Dipyridamole, Cilostazol (PDE & Adenosine uptake inhibitor)

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2
Q

Aspirin MOA

A

Irreversibly inhibits COX1 and COX2.

COX1 is responsible for converting arachidonic acid to prostaglandin H2 Which is converted to TXA2

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3
Q

Aspirin SIDE EFFECTS

A 
Gastrointestinal toxicity,
nephrotoxicity, 
hyperventilation, 
hypothermia, 
coma in over dose
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4
Q

Aspirin C/Is

A 
Hypertension, 
kidney dysfunction, 
Stomach ulcers, 
Asthma.
known hypersensitivity to NSAIDs 
Rhinitis
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5
Q

Aspirin USE

A

Antiplatet effect
Analgesic
Antiinflammatory

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6
Q

Aspirin SIDE EFFECTS

A

Fatal hepatotoxicity with overdose

treat w/active charcoal

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7
Q

Glycoprotein 2b/3a Inhibitor EXAMPLES

A

Abciximab
Tirofiban
Eptifibatide

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8
Q

GLYCOPROTEIN IIb/IIIa INHIBITOR: MOA

A

Abciximab Tirofiban Eptifibatide

● These agents prevent platelet aggregation by binding to the glycoprotein 2b/3a and hence prevent cross link between platelet Glycoprotein 2b/3a and fibrinogen
● Hence prevents platelet aggregation
● They are reversible Inhibitors of fibrin
● They are administered only intravenously.
● Clinical application: Acute coronary syndrome
● Prevents restenosis after coronary angioplasty

GP 2a/3b Inhibition means no fibrin links which means no clots

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9
Q

ADP RECEPTOR ANTAGONIST

EXAMPLES

A

Clopidogrel
Ticagrelor
Prasugrel
Ticlopidine

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10
Q

Clopidogrel
Ticagrelor
Prasugrel
Ticlopidine

MOA

A

They block the ADP receptor (specifically P2Y12)
● Activated platelet release another chemical mediator called ADP
● ADP binds to P2Y12 and that leads to the activation of Glycoprotein IIb/IIIa which are
required for fibrin mediated crosslink.
● Thus by blocking P2Y12 ADP receptors, these drugs effectively block the formation of
platelet aggregation
● Clinical application: Acute coronary syndrome, prevention and treatment for arterial
thrombosis
● Prevents transient ischemic attacks and strokes, Clopidogrel is used to prevent
thrombosis in patients who have received coronary artery Stent, and in patients who can’t tolerate aspirin.

In summary P2Y12 receptor inhibitor means ADP can’t bind which means no clot

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11
Q

Clopidogrel
Ticagrelor
Prasugrel
Ticlopidine

ADVERSE EFFECT

A

bleeding,

gastrointestinal disturbances

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12
Q

Clopidogrel
Ticagrelor
Prasugrel
Ticlopidine

CONTRAINDICATIONS

A

Anaplastic anemia

TTP ( Thrombotic thrombocytopenic purpura )

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13
Q

PDE AND ADENOSINE UPTAKE INHIBITOR/PHOSPHODIESTERASE INHIBITOR:

EXAMPLES

A

Dipyridamole

Cilostazol

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14
Q

PDE AND ADENOSINE UPTAKE INHIBITOR/PHOSPHODIESTERASE INHIBITOR:

MOA

A

Inhibit enzyme called phosphodiesterase
● Phosphodiesterase is responsible for breaking down of cAMP to AMP
● By blocking phosphodiesterase, there is
, which

inturn leads to
● This automatically leads to inhibition of platelet activation.
● These agents also inhibit phosphodiesterase in the vascular wall as well as uptake of
adenosine which promotes vasodilation
● Cilostazol and Dipyridamole gives headache (adverse effect)
● Clinical application: prevention of thromboembolic complications of cardiac valve
replacement

IN SUMMARY inhibits cAMP–>AMP conversion by enzyme phosphodiesterase meaning increased cAMP—> Leading to increased Calcium intracellularly so less is to be used in plt activation

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15
Q

Dipyridamole
Cilostazol

ADVERSE EFFECTS

A

Headache,

Palpitation

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16
Q

PDE AND ADENOSINE UPTAKE INHIBITOR/PHOSPHODIESTERASE INHIBITOR:

Contraindications

A

heart failure

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17
Q

ADVERSE EFFECTS OF ANTIPLATELET DRUGS:

A

● Bleeding

● Headache (Cilostazol and Dipyridamole)

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18
Q

Heparin USE

A

Acute treatment of DVTs,
pulmonary embolism,
Acute myocardial infarction

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19
Q

Heparin MOA

A

Binds to antithrombin 3 which is responsible for degrading several activated clotting factors like thrombin and factor 10a.

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20
Q

HEPARIN S/E

A

Bleeding
HIT
Allergic reactions Can treat excessive bleeding caused by heparin with protamine sulfate!

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21
Q

HEPARIN CONTRAINDICATIONS

A

Hypersensitivity
History of HIT
Active bleeding

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22
Q

NOACS:

Direct inhibitor thrombin:

A

DABIGATRAN

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23
Q

NOACS

Direct inhibitor of X

A

RIVAROXABAN

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24
Q

NOACS USE

A

Acute and chronic anticoagulation needs

Used instead of Warfarin in certain patients.

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25
Heparin EXAMPLES
Enoxaparin Dalteparin Fondaparinux
26
DIRECT FACTOR X INHIBITORS | EXAMPLES
Apixaban- Rivaroxaban- Edoxaban-
27
Direct thrombin inhibitors: EXAMPLES
Bivalirudin Argatroban dabigatran
28
Heparin MOA
● Binds to natural anticoagulant called antithrombin III. ● Primary function of antithrombin is to inactivate factor Xa and thrombin. ● Drugs bind to antithrombin and accelerate its activity ● Heparin binds to factor Xa and thrombin and rapidly inactivated them ● Low molecular weight heparin finds it hard to inactivate thrombin hence it radipdly inactivates factor Xa ● Fondaparinux also finds it hard to inactivate thrombin hence it radipdly inactivates factor Xa Side effect is bleeding, HIT(heparin induced thrombocytopenia), osteoporesis ● Bleeding is stopped by Protamine Sulfate (only for heparin) (binds with heparin and forms stable inactive complex) (no antidote for fondaparinux) ● Clinical application: venous thrombosis, myocardial infarction
29
Direct Factor X Inhibitors MOA Apixaban Rivaroxaban Edoxaban
Apixaban ● NOAC Rivaroxaban ● NOAC Edoxaban ● Binds to active site of factor Xa and prevents conversion of prothrombin to thrombin ● Available orally ● Clinical application: venous thrombosis, pulmonary embolism ● Adverse effect - bleeding (no antidote)
30
DIRECT THROMBIN INHIBITORS: | MOA
Directly inhibit thrombin, thereby interfering w/ intrinsic and extrinsic factors. Humanized antibody fragment (Fab) designed as a specific reversal agent for the anticoagulant effect of dabigatran. ● Idarucizumab binds free and thrombin-bound dabigatran and neutralizes its activity.
31
DIRECT THROMBIN INHIBITORS: | Side effects:
``` ● Low blood potassium (hypokalemia) ● Delirium. ● Constipation. ● Fever. ● Pneumonia. ● Headache ```
32
Subclasses of direct thrombin inhibitors
a) univalent direct thrombin inhibitors | b) bivalent direct thrombin inhibitors
33
Univalent Direct Thrombin Inhibitors:
Binds only to the active site ● Drugs:argatroban,dabigatran(NOAC) (Treatment for overdose of dabigatran - Idarucizumab)
34
Bivalent Direct Thrombin Inhibitors:
Binds to active site and exosite of thrombin ● Drugs:bivalirudin ● Advantage: Does Not join with factor IV and hence good for treatment of HIT(heparin induced thrombocytopenia) Clinical application: HIT patients Adverse effect = bleeding
35
Warfarin is a
Vitamin K antagonist
36
Warafrin is used in
Chronic anticoagulation in patients at risk for thromboembolic events
37
Warfarin MOA
Vitamin K is needed for the synthesis of f ● Factors II (thrombin), VII, IX, X are inactive and by vitamin K(reduced form of vitamin K) ● Vitamin K reduced is converted to Vitamin K epoxide in presence of oxygen and carbon dioxide ● Hence fully active clotting factors Vitamin K is needed for the synthesis of f ● Factors II (thrombin), VII, IX, X are inactive and by vitamin K(reduced form of vitamin K) ● Vitamin K reduced is converted to Vitamin K epoxide in presence of oxygen and carbon dioxide ● Hence fully active clotting factors IN SUMMARY, Inhibits the synthesis of Vit. K dependent factors: 2, 7, 9, and 10 thus increasing bleeding
38
Warfarin SE
Bleeding Skin changes Teratogen
39
Warfarin Contraindication
Open wounds Uncontrolled HTN Active ulcer disease
40
Clopidogrel Ticagrelor Prasugrel Ticlopidine USE
Treat acute coronary syndrome w/aspirin. Prevent thrombosis Patients who can’t tolerate aspirin
41
ABCIXIMAB (IV) EPTIFIBATIDE TIBROFIBIAN USE
Acute coronary syndromes
42
ABCIXIMAB (IV) EPTIFIBATIDE TIBROFIBIAN MOA
Binds to glycoprotein 2b3a located on the surface of platelets, prevents fibrinogen from binding and crosslinking, thus hindering platelet aggregation
43
ABCIXIMAB (IV) EPTIFIBATIDE TIBROFIBIAN SE
Bleeding Thrombocytopenia Diffuse alveolar hemorrhage
44
ABCIXIMAB (IV) EPTIFIBATIDE TIBROFIBIAN | Contraindications
Hypersensitivity Internal bleeding past 6 weeks
45
Phosphodiesterase: | EXAMPLES
DIPYRIDAMOLE | CILOSTAZOL
46
DIPYRIDAMOLE CILOSTAZOL USE
Treat claudication symptoms in patients with peripheral arterial disease.
47
DIPYRIDAMOLE CILOSTAZOL MOA
Inhibits the enzyme cyclic AMP phosphodiesterase 3, an enzyme involved in breakdown of cAMP, so ↑cAMP → inhibits TxA2 synthesis and ↑prostacyclin production. Platelet aggregation is thus inhibited.
48
DIPYRIDAMOLE CILOSTAZOL SEs
Headache Palpitations Gi upset
49
DIPYRIDAMOLE CILOSTAZOL SE
Headache Palpitations Gi upset
50
DIPYRIDAMOLE CILOSTAZOL contraindications
Congestive HF
51
LMWH heparin: | EXAMPLES
ENOXAPARIN | DALTEPARIN
52
ENOXAPARIN DALTEPARIN use
Acute treatment of DVTs Pulmonary embolism MI
53
ENOXAPARIN DALTEPARIN MOA
Inactivates both 10 and 2a. They bind to natural anticoagulants circulating in blood - Antithrombin 3. By binding they accelerate its activity.
54
ENOXAPARIN DALTEPARIN SEs
Bleeding | HIT
55
ENOXAPARIN | DALTEPARIN
Active major Gi bleed History of HIT within last 100 days.
56
ACETAMINOPHEN PARACETAMOL USE
Antipyretic | Analgesic
57
ACETAMINOPHEN PARACETAMOL MOA
BlocksCOX1&2 permanently, thus blocking TxA2 → bleeding
58
ACETAMINOPHEN/ PARACETAMOL S/Es
Fatal hepatotoxicity with overdose Treat paracetamol overdose with activated charcoal & acetylcysteine.
59
ACETAMINOPHEN/ PARACETAMOL | Contraindication
Known hypersensitivity to NSAIDs Asthma | Rhinitis
60
What is the first line treatment of MI in ED?
Aspirin
61
How do we control warfarin levels
Using INR
62
What is the normal INR range
2-3
63
What is the antidote for heparin overdose
Protamine Sulfate
64
How do we control heparin dose
By checking APTT levels, it should be 1.5-2.5
65
What kind of block does aspirin have to cox 1
Ireversible
66
What do medical professionals do in an aspirin overdose ?
Platelet infusion because aspirin effect last 7-12 days so we cannot wait
67
What is the recommended aspirin level
300mg
68
What is the MOA of heparin
Heparin catalyses the formation of antithrombin 3 which blocks factor 10 and 2
69
What are the types of heparin?
Unfractioned (Huge Monoamers) - Used in hospitals. | Fractioned/Standard (Smaller)- Used at home ie LMWH
70
What is the indication of use of heparin and warfarin
PE, Pregnancy, Immobilisation after surgery Past covid patient (to reduce d-dimer and due to cytokine storm)
71
What is heparin measured in?
Units are the safest dose | b/c they are many ways used by companies to process and produce heparin
72
What is the anticoagulant of choice in pregnancy and why?
Heparin because it does not cross the placenta
73
Four S/Es of Heparin
1. Bleeding 2. Thrombocytopenia/HIT 3. Osteoporosis 4. Necrosis at site of injection
74
Antidote for heparin overdose
Protamine Sulfate
75
List 2 Vitamin K antagonist
warfarin & Acenocrumorol
76
List the Vitamin K dependent factors
2, 7, 9, 10
77
Disadvantage of vitamin K antagonist
Metabolised via Cytochrome 450 therefore there are many interactions with drugs and food, it also stays in the body longer leading to an increased bleeding risk.
78
What do we do in the case of a warfarin overdose
Give the patient vitamin k or in emergencies give then 2,7,9,10
79
How long should we wait to se factors after Vit.k Administration
Up to 72 hours
80
MOA of vitamin k antagonist | warfarin
Blocks enzyme vitamin k epoxide reductase which allows the reduced form of vitamin k to be recycled
81
What class of drug is dabigatran and rivaroxoban
New oral anticoagulant
82
MOA of Dabigatran
Inhibits thrombin ---> No coagulation
83
MOA of Rivaroxaban
Inhibits factor X---> No coagulation
84
Should INR be checked?
In any case of bleeding
85
Warfarin food and drug interactions
Alcohol Aspirin Fluoroquinolones Grapefruit/ Fruit
86
What things may affect the treatment of Vitamin K antagonists
``` Wrong diet Hepatocellular disorder Viral Infection Chronic alcoholism Hepatic congestion Increased catabolism of coagulation/ clotting factors Hepatitis ```
87
Describe the effect of cimetidine on Warfarin

Pharmacology (22 decks)

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