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Pharmacology > Anticoagulants > Flashcards

Anticoagulants Flashcards

1
Q

Direct Thrombin Inhibitors (DTIs)

A

MOA: Directly inactivates Factor IIa, impeding the activation of Factor I to fibrin

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2
Q

Direct Thrombin Inhibitors

A

Hirudin
Lepirudin
Bivalirudin
Argatroban
Dabigatran

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3
Q

Used for the Mx of HIT (Heparin Induced Thrombocytopenia)

A

Hirudin - Derived from Hiruda medicinalis (medicinal leeches)
Lepirudin - Recombinant form of Hirudin; less associated with hypersensitivity reactions

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4
Q

Toxicity of Hirudin/Lepirudin

A

Bleeding (monitor with aPTT)
Anaphylactic reactions

Management: Idarucizumab + Activated Charcoal + Aminocaproic Acid

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5
Q

Used in the management of acute thrombosis post-angioplasty

A

Bivalirudin

Parenteral

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6
Q

Prophylaxis and treatment of thrombosis in patients with HIT

A

Argatroban

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7
Q

First oral direct thrombin inhibitor

A

Dabigatran

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8
Q

Alternative to Warfarin

A

Dabigatran
Alternative for
* Stroke prophlaxis, prevention in px with atrial fibrillation
* Management of vascular thromboembolic events
* Deep Vein Thrombosis (DVT)

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9
Q

Advantages of Dabigatran

A
  • No PT-INR monitoring required
  • No significant drug interaction (drug-food)
  • AE: Hemorrhage
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10
Q

Indirect Thrombin Inhibitors

A

Heparin
Unfractionated Heparin (UFH) / Regular Heparin
Low Molecular Weight Heparinm(LMWH)
Warfarin

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11
Q

Mixture of sulfated mucopolysaccharides

MW: 5,000 - 30,000

A

Heparin

ACIDIC, PARENTERAL

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12
Q

Clinical Uses of Heparin

A

Initiating anticoagulation therapy
Management of acute coronary syndrome
Management of Deep Vein Thrombosis, VTE (venous thromboembolism), pulmonary embolism

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13
Q

Anticoagulant for Pregnant women

A

Heparin

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14
Q

Monitoring needed for Heparin

A

Activated Partial Thromboplastin Clotting Time (aPTT)

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15
Q

Adverse Effects of Heparin

A

Bleeding/Hemorrhage (Tx: Protamine sulfate)
HIT (heparin-induced thrombocytopenia)
Alopecia
Osteoporosis with chronic use

CI: Active Bleeding, Thrombocytopenia

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16
Q

MOA of Unfractionated Heparin (UFH) / Regular Heparin

A

Forms an active complex with ATIII by 1000-fold; inactivation of IXa, Xa, XIa, XIIIa

17
Q

Routes of Admin for Unfractionated Heparin

A
  • IV bolus (80M/kgBW) or IV infusion (180 units/kgBW/hr)
    For the management of venous thromboembolism, DVT, embolism
  • IV Bolus (50M/kBW) or IV Infusion (12-15mg)
    Management of acute coronary syndome (MI)
  • Monitoring for IV infusion:
    aPPT: activated partial prothrombin time
    Goal: 60-85 sec delay!
    <40: underdose
    >40: overdose
18
Q

Low Molecular Weight Heparin (LMWH)

A

Enoxaparin
Dalteparin
Tinzaparin
Fondaparinux

19
Q

Dalteparin, Enoxaparin

A

MOA: Inactivates Xa
MW: 2,000 - 9,000
Less affinity to thrombin
Route: SQ
Monitoring: None required

20
Q

Fondaparinux

A

Selective inhibitor of Xa
Synthetic LMWH
No aPTT

21
Q

MOA of Warfarin

A
  • Inhibits vitamin K epoxide reductase (inactive from of Vitamin K)
  • Interferes with production of functional vitamin K-dependent clotting and anticlotting factors (II, VII, IX, X)
  • Inhibits Protein C & S (endogenous anticoagulants/anticlotting factors)
22
Q

Effects of Warfarin

A

Initial: Transient procoagulation Effect
Mx: Add LMW Heparin

Final: ANTICOAGULATION

23
Q

Doses of Warfarin

A

Dosing for Caucaseans: 5mg daily
Dosing for Asians: 1-2 mg daily
(lower dose because there is less
expression of VKERC)

24
Q

Clinical Use of Warfarin

A

For chronic anticoagulation
* Chronic atrial fibrillation
* Prosthetic heart valve
* Rheumatic heart disease (RHD)
* DVT, VTE

25
Q

Contraindications for Warfarin

A

Contraindicated to Pregnants
Fetal Warfarin syndrome

26
Q

Monitoring of Warfarin

A
  • PT-INR (prothrombin time - international normalized ratio)
  • Goal: 2-3 (most patients)
  • 2.4-3.5 : patients with prosthetic heart valve
  • > 2: underdose (thrombosis)
  • > 3.5: overdose (hemorrhage)
27
Q

Adverse Effects of Warfarin

A

Bleeding/Hemorrhage (tx: Vit K1, Fresh plasma, F IX)
Cutaneous Necrosis due to procoagulant effect
Purple Toe Syndrome

28
Q

Drug Interactions of Warfarin

A

Increased PT-INR (Hemorrhage)

Warfarin + Cimetidine = Decreased metabolism of
Warfarin + Antibiotics
Warfarin + Aspirin
Warfarin + Hyperthyroidism

Decreased PT-INR (Thrombosis)
Warfarin + Phenobarbital
Warfarin + Green Leafy Vegetables
Warfarin + Hypothyroidism

29
Q

Active Factor X Inhibitors

Newer Oral Anticoagulants (NOACs/NOVEL)

A

Rivaroxaban, Apixaban, Edoxaban
Antidote: r-Antidote

30
Q

Anti-Coagulants

A

Direct Thrombin Inhibitors
* Hirudin
* Lepirudin
* Bivalirudin
* Argatroban
* Dabigatran (Oral)

Indirect Thrombin Inhibitors
* Warfarin
* Heparin
* Unfractionated Heparin
* LMWH (Dalterparin, Enoxaparin, Tinzaparin) - SQ, IV
* Fondaparinux

Newer Oral Anticoagulants
* Apixaban
* Edoxaban
* Rivaroxaban

Pharmacology (26 decks)

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