Anticoagulants, Antithrombotics & Thrombolytic Drugs Flashcards
1
Q
Heparine Sulfate (UFH)
A
Anticoagulant
- Linear polysaccharide delivered parenterally. Bovine or porcine source.
- Catalyzes antithrombin activity by direct binding. Inhibits IIa, IXa, Xa.
- Used to treat acute DVT or PE, prophylaxis of venous thrombosis and DIC and arterial thrombosis
- Side Effects: bleeding, allergy, thrombosis, osteoporosis, HIT-heparin induced thrombocytopenia- systemic hypercoagulable state following > 7 day treatment of heparin. Never administer intramuscularly
- Monitor PTT
- Clearance by RES (saturatable) and kidney (non-saturatable)
2
Q
Rivaroxaban
A
Anticoagulant
- Orally admin once daily factor X inhibitor
- Maximal effect 4 h
- Liver, Renal and Fecal biliary clearance
- No monitoring, short half life, no reversal agent
3
Q
Warfarin
A
Antigoagulant
- Inhibits vitamin K metabolism which disrupts gamma carboxylation of several glutamate residues in factors II, VII, IX, X, C, S. C & S drops first, so does with heparin at first. No degradation of factors. Effect dependent on factor half life.
- Side Effects: bleeding, skin necrosis, teratogenesis
- INTERACTS WITH NUMEROUS OTHER DRUGS, DISEASES, DIETS!
- Liver and kidney clearance
- Monitor therapy with INR and PT
- Add Menadione (Vit K), FFP and factor VIIa to counteract
4
Q
Protamine
A
Heparin Antagonist
*Cationic protein binds to heparin to form stable ion pair.
5
Q
Menadione
A
Vitamin K, Warfarin Antidote
6
Q
Dalteparin
A
LMW Heparin
- Enhances antithrombin action on factor X
- Metabolized by kidney, so use caution in pts with renal disease
- Doesn’t require careful monitoring
- Protamine partially effective inhibitor
7
Q
Enoxaparin
A
LMW Heparin
- Enhances antithrombin action on factor X
- Metabolized by kidney, so use caution in pts with renal disease
- Doesn’t require careful monitoring
- Protamine partially effective inhibitor
8
Q
Fondaparinux
A
LMW Heparin
- Pentasaccharide with added methyl groups
- Enhances antithrombin action on factor X
- Metabolized/cleared by kidney, so use caution in pts with renal disease
- Doesn’t require careful monitoring
- Protamine INEFFECTIVE
9
Q
Argatroban
A
Direct Thrombin Inhibitor
- Small molecule administered IV due to short half life
- Hepatic clearance
- Selection based on clearance organ function
10
Q
Bivalirudin
A
Direct Thrombin Inhibitor
- 20 aa peptide, admin IV
- Hepatic and Renal (20%) clearance
- Selection based on clearance organ function
11
Q
Lepirudin
A
Direct Thrombin Inhibitor
- 65 aa peptide, admin IV
- Renal Clearance
- Selection based on clearance organ function
12
Q
Dabigatran
A
Direct Thrombin Inhibitor
- Oral, effect within 2-3 h
- 80% renal clearance
- No monitoring
- Short half life
- No good reversal agent
- Side Effect: GI Bleeding
13
Q
Tissue Plasminogen Activator (tPA)
A
Thrombolytic, human
- Shortest half life
- Used to treat MI, PE, or massive Venous thrombosis
- 1% Risk of intracranial hemorrhage
14
Q
Streptokinase
A
Thrombolytic, bacterial
- Longest half life
- Used to treat MI, PE, or massive Venous thrombosis
- 1% Risk of intracranial hemorrhage
15
Q
Urokinase
A
Thrombolytic, human
- Intermediate half life
- Used to treat MI, PE, or massive Venous thrombosis
- 1% Risk of intracranial hemorrhage
