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MED 4 > Anticoagulants, Antiplatelets, Fribriolytic Drug > Flashcards

Anticoagulants, Antiplatelets, Fribriolytic Drug Flashcards

1
Q

What are the ADP inhibitors P2Y12 Inhibitors?
Hint: CPT

A

Clopidogrel
Prasugrel
Ticagrelor

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2
Q

GPIIb/IIIa Inhibitors
Hint: ATE

A

Abciximab
Tirofiban
Eptifibatide

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3
Q

Platelet adenosine uptake inhibitor

A

Dipyridamole

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4
Q

PDE3 inhibitor

A

Cilostazol

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5
Q

Protease-activated receptor-1
inhibitor

A

Vorapaxar

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6
Q

Thromboxanes A2 inhibitor

A

Aspirin

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7
Q

Blocks production of TXA2, by irreversibly
Acetylating COX1 receptors in platelets
Prophylaxis in MI and stroke
Adverse effects: GI upset and bleeding

A

Aspirin

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8
Q

MOA: Block ADP receptors which lead to inactivation of P2Y12 receptors and INCREASE in cAMP causing inhibition of platelets aggregation

Clinical Use: Treatment of ACS and prevention of Stroke
DAPT (dual antiplatelet therapy) for drug eluted stent
Adverse effect: Bleeding

A

Antiplatelets that Inhibit ADP receptors (P2Y12 inhibitors)
Clopidogrel
Prasugrel
Ticagrelor
Ticlopidine: Not used in the US due to life threatening aplastic anemia.

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9
Q

Durg MOA: Antiplatelets that inhibit Glycoprotein IIB/IIIA

A

Prevent platelets aggregation by inhibiting fibrinogen from
Binding to IIb/IIIa receptors

Clinical use: ACS
PCI (angioplasty)

Adverse effect: Bleeding

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10
Q

Antiplatelets that inhibit
Phosphodiesterase

A

Dipyridamole
Cilostazol

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11
Q

What is the drug given: —-Thromboembolism prophylaxis
Cardiac stress test for patients who cannot use the treadmill

A

Dipyridamole:

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12
Q

What drug is given that:
Inhibits PDE3
Indication: Treatment of intermittent claudication (PVD)

A

Cilostazol

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13
Q

What is a Protease-activated receptor-1 inhibitor

A

Voraparar

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14
Q

What is the DRUG?
Mechanism of action:
Inhibits protease-activated receptor-1 (PAR-1), inhibits platelet aggregation induced by thrombin and thrombin receptor agonist peptide (TRAP)

Indication: Thrombotic event prevention

Adverse reaction:
Bleeding
Depression
Rash

A

Vorapaxar

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15
Q

Anticoagulate _________ and Antiplatelet ___________

A

Venous, Arterio

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16
Q

Vit K Antagonist

A

Warfarin

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17
Q

Potentiator of Antithrombin

A
  1. Unfractionated Heparin
  2. LMWHs: Low molecular weight heparin
    * Enoxaparin
    *Dalteparin
    *Fondaparinux
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18
Q

Direct Thrombin inhibitors
HINT: BADL

A

Lepirudin
*Bivalirudin
*Argatroban
*Dabigatrin (Oral)

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19
Q

Active Factor Xa Inhibitors

A

Apixaban
*Rivaroxaban

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20
Q

Flow chart of coagulation pathway and drug interactions

A
21
Q

What drug inhibits the hepatic synthesis of Vitamin K factors: II, VII, IX, X by blocking the gamma carboxyation of clotting factors site of action: LIVER: Only effective in Vivo
Indications: ambulatory anticoagulation
Contraindicated in pregnancy. Why?
It crosses the placenta.
“Adverse effects”
-Bleeding
-Skin necrosis (more in people with decrease in protein C)
-Purple toe syndrome (in 3-8 weeks)
-Teratogenic (bone defects)

A

Warfarin

22
Q

Why may Skin Necrosis occur with Warfarin Therapy?

A

Protein C and S are brakes in the clotting cascade. They
Inactivate the intrinsic pathway.
They have a shorter half life than IXa, Xa, and IIa and they
depend on γ-carboxylation to work
Warfarin can cause a transient protein C deficiency and
Hypercoagulability which lead to dermal vascular thrombosis
(skin necrosis)

23
Q

Warfarin is contraindicated for Pregnancy because it crosses the placenta. What is the alternate drug to give?

A

Heparin

24
Q

What drug is given?
Activates the plasma antithrombin III by enhancing the serine
Protease activity.
Antithrombin III will cause inactivation of factorsIIa, IXa, Xa, XIa, and XIIa.
Site of action Circulating blood
Effective in vivo and in vitro
Safe in Pregnancy: Doesn’t cross the placenta
Adverse effects: Heparin induced Thrombocytopenia (HIT) Osteoporosis

A

Unfractionated Heparin

25
Q

MOA of Low Molecular weight Heparins: Enoxaparin, Dalteparin

A

High activity against factor X
Longer half life than heparin
Less thrombocytopenia
No effect on PT and PTT (levels determined by Anti-Xa assay)
Side effects: Hemorrhage, thrombocytopenia, local irritation
Enoxaparin is contraindicated in prosthetic valve due to
High risk of thromboembolism

26
Q

True or False
Enoxaparin is contraindicated in prosthetic valve due to
High risk of thromboembolism

A

True

27
Q

MOA of synthetic Heparinoids : Fondaparinux

A

*Selective antithrombin III medicated Xa inhibition
*Safer in heparin induced thrombocytopenia

28
Q

Prosthetic Valve what drugs to give?

A

Warfarin

29
Q

Direct Thrombin Inhibitors
Hirudin Family: Lepirudin, Bivalirudin

A

Lepirudin: recombinant hirudin obtained from yeast cells

Bivalirudin: Synthetic derivative of hirudin

Indication: To prevent thrombosis in patients with unstable Angina and acute MI

Adverse effect: bleeding

30
Q

Fribinolytic (Thrombolytics)
1. Tissue plasminogen activator (tPA drugs)
Alteplase
Reteplase
Tenecteplase

A

Recombinant DNA
Clot specific
No allergy or hypersensitivity reactions

31
Q

Clinical use of Fibrinolytics (Thrombolytics) and Mechanism of Actions

A

Clinical Use:
Acute MI
Acute PE
Deep vein thrombosis
Thromboembolic stroke

Mechanism of action:

Activate conversion of plasminogen to plasmin which causes
lysis of fibrin clot to degradation products
Plasmin is a serine protease and is inhibited by α2 antiplasmin

32
Q

(Fibrinolytics)
Protein obtained from B hemolytic streptococci (antigenic)
Non-specific
Allergic reactions and hypotension
Antibodies may decrease activity after recent use

A

Streptokinase

33
Q

Prodrug, anisoylated streptokinase
Slowly release streptokinase

A

Anistreplase

34
Q

Enzyme obtained from human neonatal kidney
Reapproved by FDA only for treatment of Pulmonary Embolism

A

Urokinase

35
Q

Adverse Effects and Contraindications of Fibrinolytics (Thrombolytics)

A

Adverse effects

Bleeding and Hemorrhage
Additive with antiplatelets and anticoagulants

Contraindications:

Serious GI bleed
Active bleeding or hemorrhagic disorder
Surgery planned within 10 days
Aortic dissection

36
Q

Antidote to Fribrinolytics (Treatment or bleeding)

A

Aminocaproic acid
Adverse Effects: Thrombosis, hypotension and arrhythmias

37
Q

Treatment of heavy menstrual
bleeding

A

Antifibrinolytic drug: Tranexamic acid
Adverse effects: Thrombotic events which is increased in obese
women who smoke Cigarettes and use hormonal contraceptives.

38
Q

Potentiator of Antithrombin Heparin- A synthetic Direct Thrombin Inhibitor given IV
Indication: Treatment of thrombosis in Patients with HIT

A

Argatroban

39
Q

What Potentiator of Antithrombin Heparin is a FIRST ORAL DIRECT Thrombin inhibitor
Indication: reduce the risk of stroke in patients with Afib.
Prevent thrombotic complications of hip and knee replacement Surgery
Adverse effects: Bleeding, gastritis like symptoms
Interactions: Dabigatran is a substrate for P-Glycoprotein (Pgp)
Contraindication with Pgp inducers as Rifampin
Given with caution with Pgp inhibitors: Verapamil, amiodarone, clarithromycin

A

Dabigatran

40
Q

What are the Active Factor Xa Inhibitors and their Adverse Effect and Indication?

A

Apixaban: (Eliquis) Oral direct factor Xa inhibitor
Indication: Afib to reduce risk of stroke
Prevention and treatment of venous thromboembolism

Rivaroxaban: (Xarelto) Oral direct factor Xa inhibitor
Indication: DVT, blood clots and Pulmonary embolism
After knee replacement.

Adverse effect: bleeding

41
Q

Indications for Anticoagulants

A
  1. Thromboembolic disorders: DVT, PE and Afib
  2. Unstable angina undergoing PCI
42
Q

Contraindications of Anticoagulants

A

Hypersensitivity
Underlying coagulation disorder
Ulcer disease
Severe thrombocytopenia
Active bleeding

43
Q
A
44
Q

Antidote to Heparin

A

Protamine Sulfate

45
Q

Antidote to Warfarin

A

Buzzword Vit. K (Phytonadione)

46
Q

True or False:
Warfarin affects PT and INR (Prothrombin time and
International normalized ratio

What is PT and INR
PT and INR measures the extrinsic pathway of coagulation
INR monitor warfarin therapy

A

True

47
Q

True or False

A

Heparin affects PTT ( Partial thromboplastin time)

What is PTT?
PTT measures the intrinsic pathway of coagulation
aPTT: Monitor heparin therapy

48
Q

Cautions with Anticoagulants:

A
  1. Heparin is given IV or SC
  2. Heparin is given first then warfarin for maintenance
    3.Goal with heparin: PTT > 1.5 to 2.5 times normal
  3. Goal with warfarin: INR > 2.5 times normal
  4. Normal PTT: 21-35 seconds
  5. Normal INR: 1
49
Q

Clinical Uses and MOA of Fibrinolytics (Thrombolytics)

A

Clinical Use:
Acute MI
Acute PE
Deep vein thrombosis
Thromboembolic stroke

Mechanism of action:

Activate conversion of plasminogen to plasmin which causes
lysis of fibrin clot to degradation products
Plasmin is a serine protease and is inhibited by α2 antiplasmin

MED 4 (4 decks)

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