Cardio Lecture 1

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Which of the following is a type of antithrombotic drug?

All of the above

What is the function of heparin within the secretory granules of mast cells?

To store specific granule proteases

Which factor is required for an activated coagulation factor to cleave and activate the next coagulation factor?

Gamma carboxyglutamate

Which natural anticoagulant molecule enhances the activity of antithrombin by about 1000-fold?

Heparan sulfate proteoglycans

Which of the following is NOT one of the principal players of the clotting factor cascade?

Xa

What is the difference between the Intrinsic and Extrinsic pathways?

The Intrinsic pathway is activated by trauma to the blood vessel wall, while the Extrinsic pathway is activated by trauma to the surrounding tissue.

Which anticoagulant agent cannot be reversed with a reversal agent?

Direct oral anticoagulants (DOACs)

Which of the following is NOT a direct factor Xa inhibitor?

Betrixaban

Which of the following is a unique characteristic of Rivaroxaban?

It has limited aqueous solubility

What is the function of Andexanet alfa?

It acts as a decoy receptor to bind and sequester direct factor Xa inhibitors

Which of the following is a method used in the manufacturing process of low molecular weight heparins (LMWHs)?

Nitrous acid depolymerization

Which of the following is a major advantage of LMWHs over unfractionated heparin (UFH)?

Fixed dosage administration

Which of the following is true about the molecular weight (MW) of LMWHs and UFH?

LMWHs have a lower average MW than UFH

Which of the following can cause heparin-induced thrombocytopenia (HIT)?

Full length heparin (UFH)

Which of the following drugs blocks the gama-carboxylation of glutamate residues in prothrombin and factors II, VII, IX, X and the endogenous anticoagulant protein C?

Warfarin

What is the mechanism of action of warfarin?

Blocks the reduction of Vitamin K epoxide to its active hydroquinone form

Which of the following drugs can cause prolonged resistance to warfarin when taken in high doses?

Vitamin K1

Which of the following drugs directly inhibits thrombin?

Hirudin

Which of the following is true about heparin chains?

All of the above

What is the significance of the antithrombin-binding pentasaccharide in heparin?

All of the above

What is the main mechanism of action of low molecular weight heparin (LMWH)?

Activation of antithrombin

What is the average molecular weight of low molecular weight heparin (LMWH)?

5,000

Which of the following is a direct inhibitor of thrombin that binds both the catalytic site and the anion binding exosite of circulating and clot-bound thrombin?

Bivalirudin

Which of the following is a direct oral anticoagulant that is a factor Xa inhibitor?

Rivaroxaban

Which of the following is a unique formulation of Dabigatran?

Dabigatran Etexilate

Which drug is used as a reversal agent for Dabigatran to reverse/block its anticoagulant activity?

Idarucizumab

Which of the following is a direct oral anticoagulant that is a factor Xa inhibitor?

Rivaroxaban

What is the average molecular weight of low molecular weight heparin (LMWH)?

10000 Da

What is the main mechanism of action of warfarin?

Inhibition of vitamin K epoxide reductase

Which of the following is a major advantage of low molecular weight heparins (LMWHs) over unfractionated heparin (UFH)?

Fixed Dose administration

Which of the following is NOT a consequence of LMWH structural variability?

Inhibition of formed TF

What is the molecular weight range of unfractionated heparin (UFH)?

3000 - 5000 Da

What is the ratio of Anti-Xa to Anti-IIa (thrombin) activity for fondaparinux (synthetic pentasaccharide)?

Xa only

Which of the following is NOT a type of antithrombotic drug in clinical use?

Thrombolytic agents

What is the function of antithrombin in the coagulation cascade?

Inhibit coagulation enzymes

Which factor is required for an activated coagulation factor to cleave and activate the next coagulation factor?

Calcium

What is the mechanism of action of heparin within the secretory granules of mast cells?

Storage of specific granule proteases

Which of the following is a characteristic of low molecular weight heparin (LMWH)?

LMWH promotes anticoagulation primarily by inhibiting thrombin.

What is the average molecular weight of unfractionated heparin (UFH)?

12,000 to 14,000

Which of the following is a method used in the manufacturing process of low molecular weight heparins (LMWHs)?

Depolymerization

What is the main mechanism of action of unfractionated heparin (UFH)?

Binding to antithrombin and inhibiting thrombin

Which of the following is a direct inhibitor of thrombin that binds both the catalytic site and the anion binding exosite of circulating and clot-bound thrombin?

Bivalirudin

Which of the following is an orally active direct thrombin inhibitor?

Dabigatran

Which of the following is a unique formulation of Dabigatran?

Dabigatran etexilate mesylate

Which of the following is a major P-gp drug-drug interaction (DDI) with Dabigatran?

Amiodarone

Which of the following is a direct factor Xa inhibitor that competitively binds and blocks the active site of FXa, but does not inhibit thrombin and therefore has no direct effects on platelets?

Edoxaban

Which of the following is a reversal agent for direct FXa inhibitors, designed to bind and sequester the factor Xa inhibitors so that they can no longer bind and inhibit endogenous factor Xa?

Andexanet alfa

Which of the following direct FXa inhibitors has a unique absorption and PK profile, with a mandatory food requirement for higher doses due to its lipophilic structure and limited aqueous solubility?

Rivaroxaban (Xarelto)

Which of the following is true about the mechanism of action of Vitamin K antagonists such as warfarin?

They block the reduction of Vitamin K epoxide to its active hydroquinone form.

Which of the following drugs can promote bleeding by displacing warfarin from albumin?

Aspirin

Which of the following drugs can inhibit the degradation of warfarin and lead to an increase in its effect?

Rifampin

Which of the following drugs can decrease the synthesis of clotting factors and result in a decrease in warfarin's anticoagulant effect?

Oral contraceptives

Test your knowledge on the comparison between natural hirudin and recombinant hirudin (Lepirudin, Refludan) used clinically. Explore their linking domains, active-site binding/inhibiting domains, and their role as direct inhibitors of thrombin. Also, learn about Bivalirudin (Angiomax™), an approved alternative.

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