Drugs for disorders of Hemostasis Flashcards
1
Q
Heparin
A
- A GAG similiar structure of sugars. Binds to Antithrombin and inreases its activity of blockade of both thrombin and factor 10.
- First line therapy for acute clot (DVT) and immediate post hospitalization anticoagulation.
- SE- Heparin Induced Thrombocytopenia type 2: hapten forms with PF4 and Heparin, causes platelet aggregation and clotting. Clots are seen as platelets in large vessels.
- Administered IV. Protamine is antidote. Levels of AT are not accurate while on heparin therapy. Function is monitored with elevations in PT.
2
Q
Low Molecular Weight Heparin (LMWH)
A
- Catalyzes function of AT, but does not effect thrombin. Blocks Factor 10 function.
- Used as anticoagulation post DVT, etc.
- SE: Improved when compared with heparin.
- Administered SubQ daily.
3
Q
Fondiparinux
A
- Catalyzes Antithrombin activity. Only blocks factor 10.
- Used for DVT post therapy anticoaguation, smiliar to LMWH
- SE are minimal in comparison to heparin (hypotension and bleeding)
- Admnistered subQ
4
Q
Rivaroxiban
A
- Binds directly to factor 10 and inhibits function.
- Used to treate hypercagulation and DVT post therapy/AFib
- SE are minimal
- Metabolized by cyp3A4, pharmacokinetics will change. Administered orally, advantage over other drugs in class.
5
Q
Hirudian
A
- Taken from leeches is direct thrombin inhbitor
- Generally reserved for patients who have shown heparin induced thrombocytopenia
- Administered IV
6
Q
Dabigatran
A
-Non-hirudin direct inhibitor of thrombin.
-Used in patients who have shown HIT and A fib prophylaxis
-
7
Q
Aratroban
A
Argenine analog inhibits thrombin.
8
Q
Warfarin
A
- Competiive inhibitor of epoxide reductase in liver and prevents the synthesis of vitamin K dependent factors. Does this by preventing gamma carboxylation and removes binding site for calcium. (2,7,9,10, c)
- NEVER TO BE USED ALONE IN ACUTE THERAPY FOR DVT OR EMBOLISM. Must co administer with heparin or similiar to prevent necrosis or worsening. Given for long term anticoagulation therapy.
- SE: Warfarin induced skin necrosis. Factor C is vit K dependent and has short half life. Goes down fast and leads to hypercoagulability and thrombi in microvasculature and skin necrosis.
- Contraindicated in pregnancy (fetal bone development)
- Oral drug with high bioavailability. Adherence is important. Diet must be minitored for consumption of vitamin K containing foods. Efficacy measured with PT/INR. Effect is not immediate, generally takes 2-3 days. Tests for any vitamin K dependent factor will be inaccurate on warfarin therapy.
9
Q
Reteleplase, Ateleplase
A
- tPA analogs lead to acitvation of Plasmin from plasminiogen leading to clot dissolution. Given for MI and Ischemic attacks of brain, etc.
- SE: Intracranial hemorrhage
- Contraindicate in any type of trauma, surgery, or HTN.
10
Q
Steptokinase
A
-Complexes with active plasmin and increases activity. May cause hypotension and hemorrhage.
11
Q
Delta Amniocaproic Acid
Tranexamic acid
A
- Can be used to block the effects of plasmin.
- Antidote to reteleplase, ateleplase, and streptokinase. Cause hypercoagulabale state.
12
Q
Clopidrogel
A
- Irreversible inhbitor ADP receptor on platelets and prevents their activation and function (expression of gp2b3a mostly). Must be metabolized in liver to active metabolite by CYPs.
- Indicated in CABG etc. and those allergic to aspirin.
- SE: TTP
13
Q
Aspirin (ASA)
A
- COX irreversible inhibitor prevents the synthesis of TXA2 which prevents platelet activation.
- Commonly used as prophylaxis against many clotting events (Stroke, MI, DVT, etc)
- SE: Reye’s (flu),
- Contraindicated in pregancy and CHF.
14
Q
Abciximab
Eptifibitide
Tirofiban
A
- Inhibitors of gp2b3a. Abciximab is a chimeric monoclonal antibody. Eptifiitide is a peptide. Tirofiban is a small moleucle.
- Short duration of action and given IV.
15
Q
Dipyrimadole
A
-Antiplatelet Phosphodiesterase inhibitor and blocks reuptake of ADP.
16
Q
Cilostazol
A
-Phosphodiestrase inhibitor causes vasodilation.
