Flashcards in Anticoagulants Deck (48):
Vit K Dependent Coag Factors
Accelerates inactivation by Antithrombin 3 (reversible binding)
Can you use heparin in pregnancy?
How do you monitor heparin?
Activated partial thromboplastin (aPTT) -- monitors common and intrinsic pathway
Can you give heparin intramuscular?
NO. Contraindicated (painful hematoma)
Side effects of heparin
Bleeding -- thrombocytopenia
Osteoporosis (long term)
How do you treat excess hemorrhage (with heparin)
Whole blood with coag factors
PROTAMINE SULFATE (NOT with protamine allergy -- FISH; also no NPH insulin)
Low MW Heparin (3 types)
Benefits of low MW heparin
Higher specificity for Enhanced Antithrombin 3 inactivation of Xa
Longer intervals between dosing (ONCE A DAY!)
Does not require monitoring
Can you use low MW heparin in pregnant women?
When to use Low MW heparin
Prophylaxis and acute DVT
How do you administer low MW heparin?
How do you administer Heparin?
Fondaparinux (pentasaccharide) MOA
Binds to AT2 to accelerate ONLY factor Xa inactivation
How do you give Fondaparinux?
What is Fondaparinux used for?
Can you use Fondaparinux in pregnancy?
Inhibits hepatic synthesis of biologically active Vit K Dependent clotting factors, Protein C, and S
-- inhibits conversion of Vit K Epoxide to Hydroquinone
Warfarin is the DOC for what?
Warfarin is effective as an anticoag ONLY when what?
administered in vivo
How do you monitor warfarin?
INR - laboratory standardized quick-one stage prothrombin time
Monitor extrinsic pathway with prothrombin time
When prophylactic for heart valves: 2.5-3.0
Adverse Rxns are more likely to occur with Warfarin if:
Changes in warfarin or Vit K
Alteration of coag factors
Change in fibrin degradation
Change in platelet number or fxn
What genes cause the need to use LESS warfarin?
CYP2CP and VKORC1
Warfarin metabolism is mediated by what?
Drugs which INCREASE warfarin's response
Drugs which DECREASE warfarin response
Can you give Warfarin to a pregnant woman?
NO NO NO
-neonatal and fetal hemorrhage
Treatment of overdose of warfarin
VIT K1 - Phytonadione
Direct Thrombin Inhibitors
How do you administer Argatroban?
How do you give Dabigatran?
Use of Argatroban
Thrombosis with heparin induced thrombocytopenia (treat and prophy)
Use of Dabigatran
NOT a p450 substrate
Substrate for P-glycoprotein transport
Converted to 4 diff glucuronides
Clopidogrel, Ticlopidine, Cangelor
Inhibit platelet aggregation
Irreversible inhibitor of cycloox
Inhibits phosphodiesterase (inc platelet cAMP)
Little benefit alone
Given with warfarin
MOA for Ticlopidine and Clopidogrel
Block ADP binding at the P2Y12 Receptor
Impairs ADP action on platelets
BOTH ARE PRODRUGS
Reversible inhibitor or P2Y12 Receptor
Benefits of Clopidogrel
Better safety profile and shorter duration of action
Peak action takes 5 days and residual action lasts 72 hours after treatment
Can cause life threatening agranulocytosis
MOA for Abciximab and Eptifibatide
Platelet gyp 2b3a receptor antagonists
competitive reversible inhibitors
inhibit platelet cross linking with fibrinogen
CANNOT USE WITH WARFARIN
Ab = 24-48 hours
Ep = shorter
restricts clot expansion and degrades fibrin during wound healing
Complexes with Plasminogen
HIGH ANTIGENIC ACTIVITY
More specific binding to thrombi
activates fibrin bound plasminogen more selectively than circulating plasminogen
Lytic state less marked
Derivative of Alteplase
longer half life
greater fibrin specificity