Pharmacology of Anticoagulation Therapy Flashcards

1
Q

Anti-thrombotic drugs either ________, ________, or ________.

A

prevent formation of thrombi; lyse formed thrombi; inhibit formation of platelet products

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2
Q

Thrombi often form on ___________.

A

damaged endothelium, frequently from atheroslcerotic plaques; valves in the legs; or in the heart secondary to atrial fibrilation

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3
Q

There are three kinds of heparin: __________.

A

unfractionated heparin (made from pig intestine), low molecular weight heparin (depolymerized form), and fondaparinux (a synthetic pentasaccharide that corresponds to the smallest component of heparin that is an anti-coagulant)

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4
Q

Heparin works by ______________.

A

binding to anti-thrombin, which is an enzyme that deactivates the activated forms of serine proteases in the coagulation cascade; thus, heparin prevents thrombin formation

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5
Q

Unfractionated heparin must be given __________; however, it has the advantage of __________.

A

IV, because it has a poor bioavailability (it is a highly charged molecule); not crossing the placenta

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6
Q

Low molecular weight heparin and fondaparinux can _________.

A

be given subcutaneously and in outpatient settings

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7
Q

Heparin is used in ___________.

A

venous thrombosis, pulmonary embolism, abdominal surgery, management of unstable angina, acute myocardial infarction, surgery that requires cardiopulmonary bypass

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8
Q

Heparin can be negated with _________.

A

protamine sulfate; heparin is negatively charged (because of the sulfate groups) and protamine sulfate is positively charged

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9
Q

Heparin can also cause ____________.

A

thrombocytopenia, because antibodies can be made in response to platelets bound to heparin; this can be reversed with argatroban and lepirudin

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10
Q

The name Warfarin comes from __________.

A

Wisconsin alumni research foundation

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11
Q

Warfarin was originally used as rat poison, but it was discovered to be anti-thrombotic when _______________.

A

an army recruit tried to commit suicide by ingesting lots of rat poison

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12
Q

Warfarin is an ________________.

A

analog of vitamin K that competes with vitamin K for the enzyme vitamin K epoxide reductase; without vitamin K, the serine proteases cannot be carboxylated and thence cannot bind calcium

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13
Q

Pharmacologically, Warfarin has the advantages of ___________, and the disadvantages of ___________.

A

being rapidly absorbed, having a long half-life, and having high bioavailability; being teratogenic, causing hemorrhage, having drug interactions, being slow to take effect, and being genetically polymorphic

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14
Q

Warfarin is used to __________.

A

deep vein thromboses, strokes, and embolism in patients with atrial fibrilation

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15
Q

List the three fibrinolytic agents.

A

Tissue plasminogen activator, urokinase (from renal cells), and streptokinase (from Streptococcus bacteria)

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16
Q

Fibrinolytic drugs are used in ___________.

A

emergency treatment for acute myocardial infarctions, ischemic stroke, DVTs, and pulmonary emboli

17
Q

Aspirin inhibits clot formation by ___________.

A

irreversibly inhibiting cyclooxygenase 1, which limits the production of thromboxane A2 by platelets; TXA2 activates platelets, so without it platelets will not be activated

18
Q

Aspirin is used to treat _______.

A

thrombotic stroke and after acute myocardial infarctions

19
Q

Why do the coagulation serine proteases require gamma-carboxylation?

A

Because they use that carboxyl group to bind calcium

20
Q

In terms of interactions, what drugs increase the action of warfarin?

A

Aspirin (which inhibits platelet activation); antibiotics (that kill intestinal flora that help deconjugate vitamin K and recirculate vitamin K back to the body); phenytoin and clofibrate (which displace warfarin from proteins and thus increases the free concentration); drugs that decrease its liver metabolism (cimetidine, amiodorone, and phenylbutazone)

21
Q

Which drugs decrease the action of warfarin?

A

Rifampin and barbiturates (which stimulate CYP450s); cholestyramine (which decreases absorption from the GI tract)

22
Q

The newer anti-coagulants are have the advantages of __________.

A

being faster; not needing monitoring; and no known food/drug interactions

23
Q

Clopidogrel and ticlodipine are _________.

A

ADP receptor antagonists

24
Q

Dabigatran is __________.

A

a thrombin inhibitor

25
Q

Abixaban and Rivaroxaban are _________.

A

Xa inhibitors

26
Q

Abciximab is _________.

A

a GPIIb/IIIa inhibitor