Drugs Used For PAD and DVT Flashcards
What type of clots are seen during deep venous thrombosis?
What is it rich in?
1) Red clot
2) Fibrin
What does cilostazol inhibit?
What does this cause?
1) Phosphodiesterase (Type 3 inhibitor)
2) Prolongs life of cAMP in platelets and cells
What effects does cilostazol have?
1) Inhibits platelet aggregation
2) Vasodilation
What is the clinical application of cilostazol?
Intermittent claudication
What toxicities are notable with cilostazol?
1) Headaches
2) Peripheral edema
What is the black box warning for cilostazol?
Contraindicated in patients with HF
What is a pharmacologic risk factor of DVT?
Oral contraceptive or hormone replacement therapy (estrogen)
What is the active region of unfractionated heparin?
What does this region bind to?
What does this cause?
1) Pentasaccharide sequence
2) Antithrombin III
3) Inhibits factor Xa and blocks the generation of thrombin
Unfractionated heparin is used whenever there is a need or rapid onset anticoagulation such as?
1) PE
2) Stroke
3) DVT
4) Acute MI
Can unfractionated heparin be used in pregnancy?
Why/why not?
Yes, because it doesn’t cross the placenta
Why must unfractionated heparin be given parenterally (IV or SC)?
What happens if given IM?
1) It has a large molecular weight
2) Hematoma
Unfractionated heparin is contraindicated for patients with?
Thrombocytopenia and uncontrollable bleeding
What is enoxaparin?
What effect does it have?
1) A low molecular weight heparin
2) Selectively blocks factor Xa
What is the clinical application of enoxaparin?
Can it be used during pregnancy?
1) Prevention/treatment of DVT
2) Yes
Why is enoxaparin easier to use than unfractionated heparin?
It doesn’t have the issue of nonselective binding that unfractionated heparin making dosing as use at home without regular monitoring safer
Which is the first choice for Tx/prevention of DVT?
Enoxaparin
What drug is a synthetic pentasaccharide identical to the antithrombin binding structure of heparin?
Fondaparinux
What does fondaparinux selectively inhibit without affecting thrombin?
What effect does this have?
1) Factor Xa
2) Prevents prothrombin to thrombin
What is the clinical application of fondaparinux?
In conjunction with?
1) Prevent/treat DVT
2) Warfarin
How does fondaparinux compare to enoxaparin?
More effective but has higher chance of bleed
What is the antidote for unfractionated heparin and enoxaparin?
Does it work for fondaparinux as well?
1) Protamine
2) No
Which injectable anticoagulant inhibits both factor Xa and thrombin?
Which just binds/activates antithrombin and is not reversed by protamine?
Which only blocks factor Xa?
1) Heparin
2) Fondaparinux
3) LMW heparin (enoxaparin)
What is a synthetic 20 aa peptide similar to hirudin (anticoagulant of leeches)?
What is its effect?
It can it be given in combination with what other drug to patients undergoing coronary angioplasty?
1) Bivalirudin
2) Reversibly inhibits thrombin
3) Aspirin
Bivalirudin must be given via what route?
How does it compare to heparin?
1) IV
2) As effective, doesn’t require antithrombin, and causes less bleeding
Argatroban is a small molecular weight thrombin inhibitor that directly bind to?
Catalytic site of thrombin
What is the clinical application of argatroban?
Prophylaxis and treatment of thrombin in patients with heparin-induced thrombocytopenia
Warfarin is an antagonist to?
This leads to the decrease production of what clotting factors and regulatory factors?
1) Vitamin K
2) II, VII, IX, X, and proteins C and S
Why is warfarin the most widely used long-term prophylaxis of thrombosis?
In what setting is it not effective?
1) Orally active (100% bioavailability)
2) Emergencies since effects are delayed
How is warfarin induced bleeding treated?
Administering vitamin K
Can warfarin be used in pregnancy?
Why/why not?
No, because it crosses the placenta
Why is it important to cautiously transition a patient from heparin like anticoagulant to warfarin?
To avoid cutaneous necrosis
Rivaroxaban is an oral anticoagulant that is a direct inhibitor of?
This has what effect?
1) Factor Xa
2) Inhibits thrombin production
What is the clinical application of rivaroxaban?
1) Prevention of DVT and PE
2) Prevention of stroke in patients with nonvalvular Afib
How does rivaroxaban compare to warfarin?
Safer and has faster onset
Dabigatran is an oral anticoagulant that is a direct inhibitor of?
What is it indicated for?
What contraindication does it have?
1) Thrombin
2) Prevention of stroke in patients with nonvalvular Afib
3) Those with mechanical heart valves
