Anticoagulants Flashcards
Which drug is a Natural anticoagulant produced by mast cells & basophils?
Unfractionated heparin
Unfractionated heparin MOA?
increases the activity of antithrombin III by 1000 folds → inhibits factor 2 ,10, 9
in a past exam it tries to trick u by putting “directly acts on Factor Xa” which is not true bc it inhibits it thru acting on Antithrombin III
why is Unfractionated heparin not absorbed orally?
bcuz of its big size and negative charge
methods of administrating Unfractionated heparin?
(2)
- IV
- Subcutaneously
Under which circumstance does UFH’s half-life prolong? and why?
UFH is metabolized in the liver into inactive products
liver damage → UFH doesn’t metabolized → longer half-life
such as liver cirrhosis
Uses of Unfractionated heparin?
Mostly used for short-term immediate anticoagulation.
In thromboembolic events:
1. Acute MI
2. DVT
3. Atrial fibrillation
4. PE
Preventing blood clotting during:
1. Open heart surgery
2. Kidney dialysis
3. Blood transfusion
You accidentally overdosed a p/x w/ Unfractionated heparin, how would u treat that?
i’d give them Protamine sulfate
Side effects of UFH?
(6)
- Bleeding
- hypersensitivity
- Thrombocytopenia
- Osteoporosis
- Abdominal and joint pain
- Headache
what is an example of Low molecular weight heparin?
Enoxaparin
How is Enoxaparin prepared?
(LMWH)
Prepared from UFH by chemical or enzymatic depolymerization
How is Enoxaparin (LMWH) better than Unfractionated heparin?
(6)
- less protein binding, better bioavailability
- reduced risk of osteoporosis and bone fracture
- predictable activity
- no need to monitor APTT
- lower risk of thrombocytopenia
- longer half life and duration of action
Enoxaparin MOA?
(LMWH)
Activates antithrombin III and inhibits activated factor Xa only
compared to UFH which inhibits IIa, IXa, Xa
Can u treat Enoxaparin (LMWH) overdose the same way you would treat UFH overdose?
(with Protamine sulfate)
Yes, however Protamine only partially neutralizes its activity
What kind of drug is Warfarin?
Vitamin k antagonist → inhibits the formation of active forms for factors (2,7,9,10)
How is warfarin given?
orally
Warfarin MOA?
Inhibits Vit. K epoxide reductase
(converts vit. k to its reduced form which is used for the formation of active forms)
Warfarin is metabolized where?
Liver
Uses of Warfarin?
(6)
- DVT
- PE
- MI
- Atrial fibrillation
- Recurrent stroke
- Cardiac valve replacement
you should NEVER give warfarin to who?
Pregnant Women
Side effects of Warfarin?
(2)
- Bleeding
- Teratogenesis (nasal hypoplasia, depressed nasal bridge)
bleeding is controlled by giving vit. K
Which anticoagulants require INR monitoring and which one of those dont?
Require INR monitoring:
- Warfarin
Don’t require INR monitoring:
- Dabigatran
- Rivaroxaban
Compare Dabigatran & Rivaroxaban to Warfarin?
(4 differences)
- Directly inactivate coagulation factors
- More potent and predictable
- Less bleeding
- Doesn’t need INR monitoring
Dabigatran & Rivaroxaban are both direct oral anticoagulants, compare their MOA?
-
Dabigatran:
Direct and reversible inhibition of thrombin (factor IIa) → inhibits thrombin-mediated platelet aggregation (Anti-platelet activity) -
Rivaroxaban:
Direct and selective inhibitor of factor Xa
Rivaroxaban inhibits xa
True or False?
“Rivaroxaban is fully metabolized in the liver then excreted by the kidneys”
False
60% is metabolized in the liver, the 40% left is excreted unchanged by the kidneys
Uses of Directs Oral Anticoagulants?
Dabigatran & Rivaroxaban
- DVT
- PE
- Non-valvular atrial fibrillation
Adverse effects of Dabigatran?
- bleeding
- 4 Ds → Dyspepsia, dizziness, diarrhea, dyspnea
- Headache and edema
How would u treat a Dabigatran overdose?
Antidote: Idarucizumab → monoclonal antibody that binds dabigatran and reduces its activity
Adverse effects of Rivaroxaban?
- Bleeding
- Breathing and swallowing difficulty
- Bowel or bladder dysfunction
- Leg weakness
How would u treat Rivaroxaban overdose?
Antidote:
Andexanet
What antidotes would u give patients overdosed on these anticoagulants?
- Heparin
- Dabigatran
- Rivaroxaban
- Heparin → Protamine Sulfate
- Dabigatran → Idarucizumab (monoclonal Ab)
- Rivaroxaban → Andexanet