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Pharmacology > Coagulation drugs > Flashcards

Coagulation drugs Flashcards

1
Q

drugs used to reduce clotting

A

platelet aggregation inhibitors; anticoagulants; thrombolytics

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2
Q

drugs used in bleeding disorders

A

plasminogen activation inhibitors; protamine sulfate; vitamin k; serine protease inhibitors; plasma fractions

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3
Q

platelet aggregation inhibitors

A

dec synth/chemical signals for platelet aggregation; aspirin/other cox inhibitors; ADP receptor blockers; phosphodiesterase inhibitors; GP IIb/IIIA receptor blockers on platelets

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4
Q

aspirin characteristics

A

prototype cox inhibitor -> inhibits thromboxane A2 synth

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5
Q

ADP receptor blockers

A

1st gen - ticlopidine; 2nd gen - clopidogrel; 3rd gen - prasugrel

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6
Q

ticlopidine, clopidogrel, prasugrel pk

A

prodrugs; slow onset; loading dose may be req’d

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7
Q

ticlopidine, clopidogrel, prasugrel pd

A

irreversible inhibitor of P2Y12 (ADP receptor on platelet surface)

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8
Q

ticlopidine, clopidogrel, prasugrel uses

A

pt’s intolerant to aspirin; combo w/aspirin; prevention

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9
Q

phosphodiesterase inhibitors - dipyridamole pd

A

inhibit phosphodiesterase -> inc cAMP; block adenosine uptake (acts at A2 receptors - activate platelet adenylyl cyclase)

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10
Q

dipyridamole uses

A

combo w/aspirin/warfarin - preventative (prosthetic heart valves); test coronary reserve; NOT anti-anginal (could provoke acute attack - coronary steal)

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11
Q

phosphodiesterase inhibitors - cilostazol characteristics

A

newer; promotes vasodilation, inhibition of platelet aggregation; treat intermittent claudication (window shopper disease)

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12
Q

blockers of GP IIb/IIIA receptors characteristics

A

for acute coronary syndromes

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13
Q

blockers of GP IIb/IIIA receptors

A

ABCIXIMAB; eptifibatide; tirofiban

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14
Q

ABCIXIMAB characteristics

A

monoclonal antibody against human GP IIb/IIIa

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15
Q

eptifibatide characteristics

A

cyclic peptide reversible antagonist of GP IIb/IIIa

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16
Q

tirofiban characteristics

A

nonpeptide reversible antagonist of GP IIb/IIIa

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17
Q

anticoagulants

A

unfractioned heparin (UFH) -> lead to low molecular weight heparins (LMWH) -> lead to selective factor Xa inhibitors; direct thrombin inhibitors (DTIs); coumarin anticoagulants

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18
Q

heparin characteristics

A

injectable; fast anticoag; used acutely to stop thrombi formation

19
Q

heparin pd

A

binds to antithrombin III to allow more rapid inhibition of thrombin EXCEPT those already bound to fibrin; inhibits ongoing coag, but can’t dissolve pre-existing thrombi; effect directly dose-dependent

20
Q

low molecular weight heparin characteristics

A

heterogeneous compounds from depolymerization of UFH; inhibit factor Xa, less effect on thrombin vs UFH; higher therapeutic index vs UFH -> no monitoring needed -> better

21
Q

heparin adverse effects

A

bleeding; HYPERSENSITIVITY rxns; thrombosis from longterm use -> dec ATIII (use low-dose heparin); heparin-induced thrombocytopenia type II

22
Q

heparin-induced thrombocytopenia (HIT) type II

A

antibodies recognize complexes of heparin, platelet protein (platelet factor 4) -> platelet aggregation, release of platelet contents -> life-threatening; treat: sub heparin w/direct thrombin inhibitor (DTI) or fondaprarinux

23
Q

reversal of heparin action

A

excessive anticoag from heparin - treat by stopping drug; if bleeding -> give protamine sulfate

24
Q

danaparoid characteristics

A

low molecular weight heparinoid from pig; similar to LMWH -> inhibit factor X; approved for prophylaxis of deep-vein thrombosis in hip replacement surgery; effective in treat of HIT

25
Q

selective factor Xa inhibitors - fondaparinux characteristics

A

synthetic pentasaccharide -> binds to ATIII -> conformational change to bind to factor Xa; negligible ATIII activity; for prevention/treat deep-vein thrombosis; daily subQ injection

26
Q

direct thrombin inhibitors

A

direct bind active site of thrombin; lepirudin, desirudin, bivalirudin, argatroban

27
Q

lepirudin characteristics

A

recombinant form of hirudin - powerful thrombin inhibitor from leeches; can reach/inactivate fibrin-bound thrombin in thrombi; parenterally; no antidote (blood transfusion only)

28
Q

desirudin characteristics

A

another recombinant form of hirudin

29
Q

bivalirudin characteristics

A

synthetic derivative of hirudin

30
Q

argatroban characteristics

A

small molecule thrombin inhibitor

31
Q

coumarin anticoagulants

A

warfarin, dicumarol

32
Q

warfarin, dicumarol pk

A

oral unlike heparin

33
Q

warfarin, dicumarol pd

A

inhibit vit K epoxide reductase -> production of inactive clotting factors (lack gamma-carboxyglutamyl side chains); overcome anticoag effects with vit K

34
Q

warfarin monitoring

A

narrow TI; many drug interactions; with prothrombin time (extrinsic, common pathways); warfarin dec fxn’l factor VII -> inc PT

35
Q

warfarin, dicumarol adverse effects

A

hemmorrhage; cutaneous necrosis w/dec protein C; crosses placenta -> hemorrhagic disorder in fetus

36
Q

warfarin, dicumarol contraindications

A

pregnancy

37
Q

thrombolytics (fibrinolytics)

A

lyse thrombi; streptokinase; urokinase; anistreplase; alteplase, reteplase, tenecteplase

38
Q

thrombolytics pd

A

lyse thrombi by catalyzing conversion of plasminogen to plasmin; dec acute MI mortality;

39
Q

thrombolytics uses

A

when angioplasty not readily available

40
Q

drugs used to treat bleeding

A

plasminogen activation inhibitors; protamine sulfate; vit k; serine protease inhibitors; plasma fractions

41
Q

plasminogen activation inhibitors

A

aminocaproic acid; tranexamic acid

42
Q

protamine sulfate pd

A

antagonizes heparin (from fish sperm/testes); high arginine (cationic) -> complex w/anionic heparin -> dec anticoag activity

43
Q

vitamin K characteristics

A

stop bleeding due to oral anticoags (warfarin)

44
Q

serine protease inhibitors - aprotinin pd

A

blocks plasmin; inc death risk (w/drawn)

Pharmacology (15 decks)

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