12-06 L3 Blood Clotting Antiplatelets Anticoagulation Flashcards
unfractionated heprin
MOA
acts via enhancement of antithrombin
(irreversibly inactivates Xa and IIa)
antithrombin III
is a serine protease inhibitor, clotting factor attacks antithrombin III
What is the drug of choice in anticoagulation for pregnancy?
Unfractionated heparin
What do you use to treat sever bleeding caused by heparin?
- Protamin sulfate (basic)
how does heparin cause thrombocytopenia
heprain binds to platelet factor 4 complex
immune recognizes it as foregin
LMWH
MOA
inhibition of Xa
LMWH
drug of choice for what?
- Prophylaxix
- treatment of DVT/PE
- Management of acute coronary syndrome
Wafarin is adminstered how?
orally
Warfarin
MOA
interferes with the normal posttranslational modification of clotting factors in the liver
(a process that depends on vit. K)
How do you monitor heprin and warfarin?
- heprin: aPTT
- Warfarin: PT
What is a major countra-indication of warfarin
- Do not use in pregnancy
- aborption, severe birh defect,
- UFH or LMWH are alternatives
Warfarin drug interactions
- responsible for more adverse drug interactions than any other drugs (goes to war with all the other drugs)
- P450 inhibitors: increase activity, e.g ASA
- P450 activators: decreases activity e.g. barbiturates
Dabigatran
Indication
MOA
- Indication: 1st alternative oral anticoagulant
- MOA: direct thrombin inhibitor
Fondaparinux (arixtra)
admin
MOA
- Parenteral (subcutaneous) shot
- selective FXa inhibitor
Streptokinase
MOA
- binds plasminogen
- exposes active site
- promotes conversion of additional plasminogen to plasmin
t-PA
MOA
serine protease, naturally occuring regulator of thrombolysis
converts plasminogen to plasmin
Tenecteplase
(t-PA modified)
- increases activity (K)-H-R-R
- Increases 1/2 life: T and N mutation
What doe you use to manage bleeding caused by t-PA?
what is the MOA of this drug
Aminocaproic acid
(binds to plasminogen and plasmin, blocks access of fibrin)
Aspirin
MOA
irreversible inhibition of COX-1 and AA–> TXA2
Clopidogrel
MOA
Pharmacokinetics
- MOA: a pro drug, irreversible inhibition of P2Y12 ADP receptor
- Pharm: rapid absorptoin, aggregation returns to normal at 5 days post-DC
ABCIXIMAB
- MOA
- Indication
- Toxicities
- MOA: monoclonal antibody that reversibly inhibits the binding of fibrin and other ligands to the GP2b/3a receptor
- Indications: typically used during PCI such as stent placement
- Toxicities: Bleeding, thrombocytopenia