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109 Cards in this Set

  • Front
  • Back
What are the 3 classes of Anticlotting Drugs?
- Anticoagulants
- Thrombolytics
- Antiplatelet Drugs
What are the 3 classes of Proclotting Drugs?
- Replacement Factors
- Vitamin K
- Antiplasmin Drugs
What are the 3 main types of Anticoagulants?
1.) Heparins
2.) Direct Thrombin Inhibitors
3.) Warfarin
What are the 2 Thrombolytic drugs?
1.) t-PA Derivatives
2.) Streptokinase
What are the 4 Antiplatelet drugs?
1.) Aspirin
2.) Glyocoprotein IIb/IIIa Inhibitors
3.) ADP inhibitors (clopidogrel)
4.) PDE/adenosine uptake inhibitors
What are the 3 classes of Anticlotting Drugs?
- Anticoagulants
- Thrombolytics
- Antiplatelet Drugs
What are the 3 classes of Proclotting Drugs?
- Replacement Factors
- Vitamin K
- Antiplasmin Drugs
What are the 3 main types of Anticoagulants?
1.) Heparins
2.) Direct Thrombin Inhibitors
3.) Warfarin
What are the 2 Thrombolytic drugs?
1.) t-PA Derivatives
2.) Streptokinase
What are the 4 Antiplatelet drugs?
1.) Aspirin
2.) Glyocoprotein IIb/IIIa Inhibitors
3.) ADP inhibitors (clopidogrel)
4.) PDE/adenosine uptake inhibitors
What can you use to neutralize the acidity of Heparin
Protamine
How is Heparin administered and why?
i.v. or s.c.

to avoid the risk of hematoma associated with intramuscular
What is Enoxaparin?
Low molecular weight fractions of heparin
Why are LMW Heparins better?
They have a greater biovailability + longer durations of action than unfractionated heparin

Can be given less frequently throughout the day, like 1-2 times daily.
What is Fondaparinux?
A small syntetic drug that is biologically active pentasaccharide present in unfractionated and LMW heparins.
MOA of Heparin
Binds to Antithrombin III, making it proteolyze Thrombin and Xa 1000-times faster
What is Antithrombin III?
An endogenous anticlotting protein that irreversibly inactivates thrombin and factor Xa. Its enxymatic action is markedly accelerated by Heparins
How long does it take for heparin to take effect?
Immediately
How do you monitor the actio nof Heparin?
aPTT

activated partial thromboplastin time
What is the difference in MOA between LMW heparins/fondaparinux and unfractionated heparin?
LMW's bind to ATIII, with the same effect on Xa, but do not affect thrombin.

Therefore, aPTT tests aren't as reliable in measuring their anticoagulant effect. Esp. in renal failure, b/c clearance is decreased.
Clinical Use of Heparins
- DVT's
- Pulmonary Embolism
- Acute MI
- w/ thrombolytics for revascularization
- w/ glycoprotein IIb/IIIa inhibitors during angioplasty and placing stents
What is Heparin the DOC for?
Pregnant ppl who need an anticoagant
SE of Heparin
- XS bleeding
- Hemorrhagic stroke
- Transient/severe thrombocytopenia (unfractionated; HIT)
- Osteoporosis (longterm use)
Describe the effect that Protamine has on the different kinds of heparin
Used on UNfractionated heparin the most

Only partially works on LMW Heparins

No effect on Fondaparinux
What are the 4 kinds of Direct Thrombin Inhibitors?
Lepirudin
Desirudin
Bivalirudin
Argatroban
Where are direct thrombin inhibitors extracted from?
proteins made by Hirudo medicinalis, the medicinal Leech.
What is the difference between Lepirudin and Desirudin & Bivalirudin?
Lepirudin is the recombinant form of the leech protein Hirudin

Desirudin&Bivalirudin are modified forms of hirudin.
MOA of Lepirudin, Desirudin, and Bivalrudin
Bind simultaneously to the active site of Thrombin and Thrombin substrates.
MOA of Argatroban
Binds solely to the active site of thrombin
How are Direct Thrombin Inhibitors different from Heparins
DTI's inhibit both the soluble thrombin and the thrombin enmeshed within developing clots
Which DTI also inhibits platelet activation?
Bivalrudin
Clinical use of DTI's
In pts with Heparin-induced thrombocytopenia, as an alternative to heparin
This drug is also used with aspirin during percutaneous coronary angioplasty
Bivalirudin
How do you monitor the used of DTI's?
aPTT
SE of DTI's
- Bleeding
- No reversal agent exists.
- Prolonged Lepirudin --> anaphylactic rxns
Describe the metabolism of Warfarin
Binds to plasma proteins > 99% and its eliminated by P450
MOA of Warfarin
Interferes with the posttranslational modification of clotting factors in the liver.

Takes much longer to take effect b/c the clotting factors have a t1/2 of 8-60 h, takes longer to get rid of them
Clinical Use of Warfarin
Chronic anticoag & everything heparin's uesd for
Warfarin is Contraindicated in
Pregnancy
SE of Warfarin
- Bleeding
- Hypercoagulability early in does, due to Protein C deficiency. Protein C has a shorter halfl-life
- Bone defects and hemorrhage in fetus
Drug interactions of Warfarin
P450 INDUCERS: carbamazepine, pheyntoin, rifampin, barbiturates
* Increase Warfarin's CLEARANCE *
* Reduce anticoag. effect *

P450 INHIBITORS: amiodarone, SSRI's, cimetidine
* Reduce Warfarin's Clearance *
* Increase the anticoag effect *
What are the 2 kinds of Thrombolytic drugs?
1.) forms of t-PA (alteplase, tenecteplase, reteplase)
2.) Streptokinase
What is plasmin?
A Fibrinolytic enzyme that degrades clots by splitting fibrin into fragments.
How do thrombolytic enzymes work?
Catalyze the conversion of Plasminogen to Plasmin
MOA of t-PA
- Directly converts plasminogen to plasmin

- Has selectivity for plasminogen already bound to fibrin (i.e. in a clot)
What is alteplase?
Normal human plasminogen activator
What is reteplase?
- a mutated form of human t-PA
- w/ similar effects but a slightly faster onset of action and longer duration of action
What is tenecteplase?
Another mutated form of t-PA wtih lonfer half life
MOA of Streptokinase
- Not an enzyme itself, but forms a complex w/ endogenous plasminogen.
- the Plasminogen in the complex changes conformation to convert free plasminogen to plasmin

- no selectivity for fibrin-bound plasminogen
Clinical Uses of Thrombolytics agents
- An alternative to percutaneous coronary angioplasty in emergency coronary artery thrombosis(w/in 6h)
- Very prompt use (w/in 3h) is good for ppl with ischemic stroke
- Pulmonary Emolism
What should you make sure before you adminster t-PA?
Cerebral hemorrhage should be ruled out
SE of thrombolytic agents, t-PA and streptokinase
- Bleeding
- Cerebral Hemorrhage (most serious)
- Severe Allergies in pts who had strepp infection and take streptokinase
Platelet aggregation is especialy important in which circulation
Arterial

Esp Coronary and cerebral
What are some triggers of platelet aggregation?
- Thromboxane
- ADP
- Thrombin
- Fibrin
What are some inhibitors of platelet aggregation?
Things that increased intracellular cAMP:
- prostacyclin
- adenosine
What are abciximab, tirofiban, adn eptifibatide
Glycoprotein IIb/IIIa receptor inhibitors
What are clopidogrel and ticlopidine?
Antagonists of ADP receptors
What are dipyridamole and cilostazol?
Inhibitors of phosphodiesterase 3
What is Thromboxane A2?
A potent STIMULATOR of Platelet aggregation
MOA of Aspirin
Irreversibly Inhibits COX, which is used to form Thromboxane, so inhibits platelet aggregation.

Lasts long, b/c platelets can't make their own proteins.
MOA of Abciximab
Monoclonal Antibody

Reversibly inhibits the Fibrin binding to Glycoprotein IIb/IIIa receptor on the platelet
What is the Glycoprotein IIb/IIIa receptor
A cell surface protein involved in platelet cross-linking
MOA of eptifibatide and tirofiban
Reversibly block the glycoprotein IIb/IIIa
MOA of Clopidogrel and Ticlopidine
Irreversibly inhibits Platelet ADP receptor

Thus prevents ADP-mediated platelet aggregation
MOA of Dipyridamole and Cilostazol
1.) Phosphediesterase 3 degrades cAMP. These drugs inhibit phosphodiesterase, thus increasing levels of cAMP which inhibits platelet aggregation.

2.) Inhibit the uptake of adenosine by endothelial cells adn RBCs, thus increasing plasma [adenosine]. Adenosine increases platelet cAMP via platelet adenosine A2 recetors
Clinical Use of Aspirin
- to Prevent further infarcts in pts wtih 1 or more MI's/prevent first MI
- to Prevent TIAs, ischemic stroke, and thrombotic events
Clinical Use of Glycoprotein IIb/IIIa receptors inhibitors
- Prevent restenosis after Coronary angioplasty
- Acute coronary syndomes: unstable angina & non-Q-wave Acute MI
Clinical Use of Clopidogrel and Ticlopidine
- Preventing TIA's and ischemic strokes (esp in pts intolerant of Aspirin)
- Clopidogrel usu used to prevent thrombosis after CA stent
Clinical use of Dipyridamole and Cilostazol
- Intermittent Claudication
SE of Aspirin
- GI and CNS effects
- Enhance the effects of other anticlotting agents
SE of Glycoprotein IIb/IIIa receptor inhibitors
- Bleeding
- Thrombocytopenia (chronic use)
SE of Ticlopidine
*Rarely used*
- Bleeding in 5% of pts.
- Neutropenia 1%
- Thrombotic thrombocytopenic purpura (TTP)
SE of Dipyradimole & Cilostazol
- Headaches
- Palpations
How do you treat thrombocytopenia
Administration of Platelets or Oprelvekin
What is Oprelvekin
The recombinant form of megakaryocyte growth factor IL-11
How do you treat Vitamin K deficiency?
Phytonadione (Vitamin K1)
Clinical uses of Phytonadione
(Vitamin K1)
- Vitamin K Deficiency
- All newborns
- To reverse the anticoag effect of XS warfarin
What agents do you use to treat Hemophilia?
- Fresh plasma
- Factor VIII (Hemophilia A)
- Factor IX (Hemophilia B)
What do you used to prepare pts w/ von Willebrand disease and Hemophilia A for eective surgery? Why?
Desmopressin acetate

Its a V2 agonist, and increases plasma conc. of vWF and VIII
What the three Antiplasmin agents?
- Aminocaproic acid
- Tranexamic acid
- Aprotinin
MOA of Aminocaproic acid and tranexamic acid
Inhibit plasminogen activation

So inhibits fibrinolysis
MOA of Aprotinin
Serine protease inhibitor

So inhibits fibrinolysis by plasmin and by the plasmin-streptokinase
Clinical Use of Aprotinin
Pts undergoing Coronary artery bypass grafting who are at risk of bleeding
SE of Aprotinin
Increased risk of MI, Stroke, Renal damage
* Vitamin K dependent anticoagulant
* Warfarin (PT)
* Warfarin is contraindicated in
* Pregnancy
* Anticoagulant of choice for Pregnancy
* Heparin
* Heparin (PTT) increases activity of
* Antithrombin 3
* Route of administration of warfarin
* Oral
* Routes of adminstration of heparin
* i.v. and i.m. (only LMW)
* SE of both warfarin and heparin
* Bleeding
* SE of Heparin
* Heparin Induced thrombocytopenia
* Alternative anticoagulant used if HIT develops
* Lepirudin
* Antidote to reverse actions of Warfarin
* Vitamin K or Fresh Frozen Plasma
* Antidote used to reverse actions of Heparin
* Protamine sulfate
* MOA of aspirin
* Irreversibly blocks COX
* Agent used to treat MI and to reduce incidence of subsequent MI
* Aspirin, Metoprolol
* SE of Aspirin
* GI Bleeding
* Antiplatelet drug reserved for pts allergic to Aspirin
* Ticlopidine
* SE of Ticlopidine
* Neutropenia and agranulocytosis
* Effective in preventing TIA's
* Clopidogrel and ticlopidine
* Prevents thrombosis in pts with artificial heart valve
* Dipyridamole
* Blocks glycoprotein IIb/IIIa involved in platelet cross linking
* Abciximab, tirofiban, eptifibatide
* MOA of thrombolytics
* Degradation of fibrin clots and are administered IV
* Thrombolytics are used for
* Pulmonary Embolism and DVT
* Thrombolytic that can cause an allergic reaction
* Streptokinase
* Thrombolytic used for acute MI and ischemic (non-hemorrhagic) CVA
* Tissue plasmin activator (t-PA)
* SE of t-PA
* Cerebral Hemorrhage
* Antidote for thrombolytics
* Aminocaproic acid