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Pharmacology > Anticoagulants, Antiplatelets, Thrombolytics > Flashcards

Anticoagulants, Antiplatelets, Thrombolytics Flashcards

1
Q

Define hemostasis (patho)

A

a process used by the body to stop bleeding by method of clot formation

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2
Q

Coagulation cascade

A

Series of events that take place in the formation of a clot. Anticoagulants, antiplatelets and thrombolytics all work at different points in the cascade

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3
Q

Define anticoagulant

A

disrupt coagulation cascade (before it can start taking place)

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4
Q

Define antiplatelet

A

disrupt platelet aggregation (sticking together)

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5
Q

Define thrombolytic

A

breakdown of formed clots

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6
Q

Which clotting factors rely on vitamin k in order to be synthesized by the liver?

A

Seven, Nine, Ten and Two (SNTT)

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7
Q

Anticoagulant General Info

A

Reduce formation of fibrin

May be given p/o or parenterally

For both treatment and prevention of thromboembolism

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8
Q

3 Heparin Derivative Groups

A
  1. Unfractionated heparin
  2. Low molecular weight heparin
  3. Fondaparinux

Mech: enhance activity of antithrombin III

**These drugs have the same mechanism of action, but do not have equal effects on factor Xa and factor IIa (thrombin)

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9
Q

Unfractionated Heparin (UFH)

SQ

A

Mech: Antithrombin III undergoes a conformation change that enhances its binding capability

Indication: Treatment of venous thromboembolism (VTE), prophylaxis of VTE< myocardial infarction, atrial fibrilation

Adverse Effects: hemmorhage, spinal/epidural hematoma, heparin-induced thrombocytopenia (HIT)

Lab Monitoring: Activated partial thromboplastin time (aPTT), Anti-factor assay

** anti-factor assay is more accurate than aPTT

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10
Q

What is thrombocytopenia?

A

Reduced platelet count

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11
Q

What medication is used in the reversal of unfractionated heparin or low molecular weight heparin?

A

Protamine

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12
Q

Protamine (SLOW IV push or rapid admin for hypotension)

A

Indication: binds with heparin to inactivate, used in unfractionated heparin reversal

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13
Q

What is the ratio of protamine to heparin in neutralizing/reversal of heparin or low molecular weight heparin?

A

1 mg of protamine neutralized 100 units of heparin

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14
Q

Low Molecular Weight Heparins (LMWH) (SQ)

A

Enoxaparin
Dalteparin

Mech: binds to factor Xa and factor IIa (thrombin) to neutralize their activity

Indications: Prevention of DVT, treatment of venous thromboembolism (VTE), treatment of MI

Adverse Effects: hemorrhage, spinal/epidural hematoma, heparin-induced thrombocytopenia

Excretion: renally excreted, reduced doses required for pts. with renal impairment

** No lab monitoring needed

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15
Q

What is the primary difference between unfractionated heparin and LMWH heparin?

A

smaller chain length with LMWH’s, so less binding to factor IIa (thrombin)

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16
Q

What is required for the inactivation of factor IIa

A

binding of heparin to BOTH antithrombin II and factor IIa molecule

17
Q

Fondaparinux

A

Mech: binds to antithrombin and causes conformational change, but ONLY binds to factor Xa and not factor IIa

Indications: prophylaxis of DVT and treatment of VTE

Adverse Effects: hemorrhage, spinal/epidural hematoma

** NO lab monitoring needed and NO risk for heparin-induced thrombocytopenia (HIT)

18
Q

Which heparin derivative drug requires lab monitoring?

A

Unfractionated Heparin

(aPTT and anti-factor assay)

(Assay is a test to determine the presence of something )

19
Q

Which heparin derivative drugs carry a risk for heparin-induced thrombocytopenia?

A

Unfractionated heparin and low molecular weight heparins (NOT Fondaparinux)

20
Q

What type of drug is warfarin?

A

Vitamin K antagonist

vitamin K helps us to clot

21
Q

Warfarin

A

Mech: decreased production of clotting factors 7, 9, 10, 2 (SNTT)

Indications: treatment and prevention of VTE, prevention of thromboembolism in patients with mechanical heart valves, prevention of thromboembolism in patients with atrial fibrillation

Pharmako: full effects seen in 3-5 days

Monitoring: International Normalized Ratio (INR)/prothtrombin time

Adverse Effects: hemorrhage, fetal hemorrhage during pregnancy (Category X)

DDI’s: other anticoagulants, drugs that decrease anticoagulant effects (phenytoin/vitamin K)

22
Q

What clotting factors does the acronym SNTT represent?

A

7, 9, 10 and 2

23
Q

Which category is warfarin for pregnancy?

A

Category X

24
Q

Which foods should patients taking warfarin avoid and why?

A

mayonnaise, green leafy vegetables, soybean oil

These are high in vitamin k, so may counteract with warfarin’s anticoagulant capability

25
Q

Warfarin Reversal

A

Vitamin K (phytonadione) and fresh frozen plasma (FFP) in life-threatening bleeds

26
Q

Direct Thrombin Inhibitors (DTI)

A

Dabigatran (PO)
Bivalirudin (IV)
Argatroban (IV)

Mech: bind to and inhibit factor IIa (thrombin)

Adverse Effects: dyspesia

** NO need for lab monitoring with oral formulations (dabigatran)

27
Q

Factor Xa Inhibitors (PO)

A

Rivaroxaban (PO)
Apixaban (PO)

Indications: prevention and treatment of VTE, prevention of thromboembolism in atrial fibrillation

** NO laboratory monitoring needed

28
Q

What is the primary difference between Fondaparinux and Factor Xa Inibitors?

A

Fondaparinux binds to antithrombin III FIRST then binds to factor Xa, Factor Xa inhibitors bind directly

29
Q

What drug is used for reversal of direct thrombin inhibitors?

A

Idarucizumab (Praxbind)

30
Q

What drug is used for the reversal of Factor Xa inhibitors?

A

Adexanet-alfa

31
Q

Aspirin

A

Mech: Irreversible inhibitor of COX-1 and COX-2,
Prevents production of thromboxane A2 (TXA2),
TXA2 can promote platelet aggregation

Indications: ischemic stroke, transient ischemic attack (TIA), acute coronary syndrome

Adverse Effects: GI bleeding and ulcers

32
Q

P2Y12 Adenosine Diphosphate Receptor Antagonists

A

Clopidogrel (irreversible inhibitor)
Prasugrel (irreversible inhibitor)
Ticagrelor (reversible inhibiitor)

Mech: block P2Y12ADP on platelet surface, prevents ADP stimulated platelet aggregation

Indications: prevention of thrombosis of coronary stents after PCI, secondary prevention of stroke, MI and peripheral vascular disease

Adverse EffectsL Dyspnea with Ticagrelor, bleeding with any of these meds

DDI’s: omeprazole because omeprazole inhibits CYP2C19

33
Q

Which P2Y12 Adenosine Diphosphate Receptor Antagonist is actually reversible?

A

Ticagrelor

34
Q

Glycoprotein IIb/IIIa Receptor Anatagonists

A

Tirofiban
Eptifibatide
Abciximab

Mech: Reversible blockade of GIIb/IIIa receptors

Indications: prevention of ischemic events in patients with acute coronary syndromes (ACS) and undergoing PCI
*Typically only used in the cath lab

Adverse Effects: bleeding

**Used in combination with heparin during PCI

35
Q

Thrombolytic (Fibrinolytic) Drugs

A

Alteplase
Tenecteplase

Indications: ischemic sroke, myocardial infarction, pulmonary embolism

**HIGH. risk of bleeding associated with these medications

36
Q

Alteplase (IV)

** Bolus followed by infusion

A

Also know as tissue plasminogen activator (tPA)

Indications: acute ischemic stroke, acute myocardial infarction, acute pulmonary embolism

Adverse Effects: bleeding, angioedema (hive-like reaction in deep layers of the skin)

Contraindications: Prior intracranial hemorrhage,
Ischemic stroke or MI in last 3 months, Active bleeding, Suspected aortic dissection

37
Q

Avoiding bleeding from alteplase administration

A

Avoid SQ or MI injections during administration, minimize invasive procedures, minimize concurrent use of anticoagulants or antiplatelet drugs

Pharmacology (5 decks)

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