Pharm Block 2 (Antithrombotic drugs)
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What are the Three main Classes of Anti-Thrombotic Drugs?
Where are they best used?
- 1. Anti-Coagulants-- Venous Side
- 2. Fibrinolytic-- Destoying Clots (MI)
- 3. Anti-Platlet-- Arterial Side
What are the General Functions of Anti-Thrombotic drugs?
-These are more for Prevention of Clots in the Venous thromboemboli, prevention of strokes in patients with AFib, and the prevention and treatment of acute coronary syndrome (ACS)
- This is used for disolution of pre-existing clots and play an important role in acute treatment of thrombosis.
What are the Three principle classes of anticoagulants??
- - Heparins
- - Vitamin K antagonists
- - Direct thrombin inhibitors
What is heparin and what is LMWH?
Heparin= Unfractionated Heparin. Meaning that it has its long polysaccharide tail AND its specific Pentasaccharide sequence that is responsible for its activity.
LMWH= Low molecular weight heparin meaning that it only has the short Pentasaccharide portion. Still has the same effect as Heparin, but is Specific for Factor X.
How does heparin work?
What about LMWH?
It Enhances the activity of Endogenous Anticoagulant Antithrombin III
by increasesing its affinity for Thrombin
- Antithrombin II also inhibits factors X,IX and XI
- LMWL does the same thing but is Specific for Factor X
What are the Pharmacokinetics of Heparin?
- -It is Highly ionized so it is not available orally, only via IV. Since it is Ionized it cannot cross the Placenta membrane and thus is a good treatment it Pregnent women.
- - It is dose dependent (Zero order), thus half life is dependent on dose.
What are some adverse effects of Heparin?
It can cause Thrombocytopenia and some bleeding
Facts about LMWH.
Give some examples of LMWH preparations.
- - it is selective for factor X
- - better bioavailability (80%)
- -longer acting
- - no lab monitoring required
- -LOW RISK for thrombocytopenia
Name a Heparin Antagonist.
- -Strongly basic
- - Less effective against LMWH
What is Fondaparinux?
It is a Direct factor X inhibitor ( a Synthetic form of LMWH)
-Has very very low rist for Thrombocytopenia
What are Direct Thrombin inhibitors?
When would you use it clinically?
-They are drugs that directly inhibit throbin with out involving Anti-thrombin drugs or vitamin K
- us it in patients with heparin induced thrombocytopenia (thus cannot used heparin to prevent clotting).
Name some Direct acting Throbin inhibitors
What is Danaparoid?
What is special about it?
When do we use it?
-It is a heparinoid consisting of heparin sulfate, dermatan sulfate and chondroitin sulfate
-has greater anti-factor X activity then LMWH
- used it in patients with heparin induced thrombocytopenia
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