Episode 6 - Anticoagulants, Thrombolytics (Fibrinolytics), Antiplatelet Agents and Antifibrinolytics Flashcards
What are anticoagulants?
Substances that prevent the synthesis of a fibrin network which inhibits coagulation and the formation of thrombi.
How fast do anticoagulants work and what does this mean with regards to how they should be used?
IV will work within minutes and orally will work within hours.Because immediate defect these should be used with great caution.sufficient therapy and hemorrhagic risk is narrow and varies considerably patient to patient.
Anticoagulants are divided into 4 groups:
1 indirect thrombin inhibitors (basically heparin)
2 Coumarin Anticoagulants (basically Warfarin)
3 Direct thrombin inhibitors4 Direct factor X inhibitors
Commercial Heparin is actually a mixture of Heparins. The two most common mixtures are what?
1 Unfractionated Heparin (UFH) - Heparin Sodium
2 Low-molecular-weight heparin (LMWH) - Fragmin, innohep, lovenox
How the crap does Heparin work?
Heparin stimulates antithrombin-3, which in turn neutralizes the activity of factor 10 (as well as other clotting factors. With no 10 no prothrombin to thrombin, and eventually no fibrinogen to fibrin (indirect thrombin inhibitor)*also stimulates heparin cofactor 2 which inhibits thrombin
What is unfractionated heparin (UFH)?
Effective parenteral anticoagulant. Binds to plasma proteins, which reduces its anticoagulation activity and causes large anticoagulatant response. Also binds to endothelial cells and macrophages
What test is used to monitor UFH and its clinical effectiveness?
Activated partial thromboplastin time (APTT)
Will typically prolong APTT to 2-2.5 time that of normal value
Why is Low Molecular Weight Heparins useful?
Can be given in hospital or out of hospital. Administered SC (sub-cutaneous) and doesn’t need laboratory monitoring.
What is the only major coumarin anticoagulant found in in the US of A? And whats the fun nugg related to warfarin?
warfarin (Coumadin)main active ingredient in many rodent poisons which will can lead to death by hemorrhage and internal bleeding
How does warfarin work?
interferes with hepatic synthesis of vit K dependent clotting factors (2, 7,9,10)
What is the target INR for most patients using warfarin?
should be adjusted to acheive INR=2.0-3.0
DDI (drug-drug interactions): what agents inhibit warfarin metabolism?
Cimetidine (Tagamet) Acetaminophen (Tylenol) High dose, acute alcohol Azithromycin (Zithromax) Ciprofloxacin Clarithromycin Erythromycin
DDI: which drugs stimulate warfarin metabolism?
Chronic alcohol usephenytoin (dilantin)oral contraceptives increase the synthesis of many clotting factors and can reduce the effect of warfarin
How can diet effect warfarin?
food rich in vit K result in effects in warfarin
What is the most common side effect of warfarin?
Bleeding that occurs most often in the mucous membranes of GI tract and GU tract. Warfarin is contraindicated during pregnancy because is crosses the placenta. Breast feeding should also be avoided
What was the first oral direct thrombin inhibitor? Why is it so snazzy?
Dabigatran (Pradaxa)orally administered, doesn’t require frequent blood tests for INR.
Daily DoubleThe only thing mentioned about Direct factor X inhibitors was: when was the first of its kind released?
Aug-11
What is the mechanism which thrombolytics work? (Fibrinolytics are mentioned here i’m assuming say type of mech used)
Thrombolytics rapidly lyse thrombi when administered intravenously by catalyzing the formation of plasmin from plasminogen
What are some example of Thrombolytics?
Streptokinase, urokinase, synthetic tPA
What are the three classes of anti-platelet agents?
Cyclooxygenase inhibitors (mainly aspirin) cox blockerThienopyridines (ADP inhibitors)GP IIa/IIIa inhibitors
What is the mechanism by which aspirin works?
Inhibits the synthesis of TXA2
What does thienopyridines (ADP Inhibitor) and what is the main drug that fits into this category?
Prevent ADP from binding to their receptors on platelets.Main Drug: clopidogrel (Plavix)
What does GP IIb/IIIa inhibitors do and what is an example of this drug?
Inhibit the activation of glycoprotein IIb/IIIa receptors on plateletsExample of drug: abciximab (ReoPro)
Take a break
Tooshie squeezes all around
What does antifibrinolytics do and a where is it used in denistry?
Tranexamic acid inhibits the activation of plasminogen to plasmin.Dental: tranexamic acid is used in the form of 5% mouth wash after extraction or surgery with prolonged bleeding.