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Pharm BMED 575
Anticoagulants
| Question | Answer |
|---|---|
| Name three drugs that inhibit thrombogenesis | Aspirin Clopidogrel (Plavix) Abciximab (ReoPro) |
| What is the MOA of aspirin? | inhibits thromboxane A2 synthesis |
| What patient group is aspirin used for? | Those at risk for embolism |
| What drug is used to treat unstable angina not responding to conventional therapy? | abciximab |
| Hemophiliacs are best treated with heparin | FALSE |
| Heparin should be used as an adjunct treatment for infective endocarditis? | FALSE |
| A threatened abortion is a contraindication for heparin | TRUE |
| What procedures are contraindicated for patients on aspirin? | Dental or surgical |
| What procedures are treated with abciximab? | Angioplasty, atherectomy, and stent placement |
| What side effect does clopidogrel have less than aspirin? | Less GI effect because clopidogrel does not effect prostaglandin |
| Can abciximab be used to treat AMI? | Yes |
| Heparin and what drug is used for patients undergoing percutaneous coronary intervention? | abciximab |
| What drug dosing needs to be adjusted with aspirin therapy? | Warfarin |
| What activated clotting factors does ATIII work on (with the enhancing effect of heparin) | XIIa, XIa, IXa, Xa and especially IIa (thrombin) |
| What is the recommended dose of aspirin therapy? | 325 mg per day for primary prevention of MI |
| Heparin should be used in patients that are actively bleeding. | FALSE |
| Thrombocytopenia purpura is a contraindication for using heparin. | TRUE |
| Why is abciximab given IV | Because it is a peptide |
| Heparin sodium (Liquaemin) and LMW Heparins such as enoxaprin (Lovenox) have what MOA? | enhance ATIII |
| Can clopidogrel be given during an acute MI? | Yes |
| Patients with active tuberculosis should not use heparin. | TRUE |
| What are the side effects of heparin? | Hemorrhage, osteoporosis, allergic reactions, decreased platelets (thrombocytopenia) |
| Heparin aids in the treatment of visceral carcinoma. | FALSE |
| Advanced renal or hepatic disease is a contraindication for using heparin | TRUE |
| Surgery of what body parts is the use of heparin contraindicated for? | During or after surgery of the brain, spinal cord, or eye. Lumbar puncture or regional anesthetic |
| What is eptifibatide | a cyclic peptide like abciximab |
| LMWH enoxaprin (Lovenox) can be used as an intraoperative anticoagulant | TRUE |
| Acetylsalicylic acid (Aspirin) MOA | Inhibits the synthesis of the thromboxane A2 |
| What are the effects of inhibiting thromboxane A2? | Irreversible platelet dysfunction lasting the lifespan of the platelet (7-10 days) |
| Heparin is good for patients with severe hypertension or intracranial hemorrhage. | FALSE |
| What is the MOA of abciximab (ReoPro)? | inhibits GPIIb/IIIa receptors |
| What inhibits binding of fibrinogen and von Willebrand factor? | abciximab |
| Why does tirofiban last longer than abciximab? | It is not a peptide, so it lasts longer in circulation. |
| What is the MOA for clopidogrel (Plavix)? | Inhibits platelets aggregation by blocking the ADP receptor |
| For patients allergic to aspirin what is an alternative treatment | Clopidogrel (Plavix) |
| What are the toxicities of abciximab? | Bleeding, thrombocytopenia |
| Enoxaprin can be used for thrombosis prophylaxis, catheters and bypass anticoagulation | TRUE |
| Heparin should not be used to anticoagulate collected blood | FALSE |
| Heparin is dangerous to use in pregnancy | FALSE |
| What effects will protamine sulfate have is given when not heparin is present? | Produces an anticoagulant effect on platelets and fibrinogen |
| What is the antagonist for heparin | Protamine sulfate |
| Enoxoprin (Lovenox) is an appropriate prophylactic antithrombotic | TRUE |
| Can enoxoprin (Lovenox) be used to keep catheters from clotting? | YES |
| While ACD is used to anti-coagulate homologous blood when collected, heparin and what else can be used for autologous intraoperative shed blood collection? | Enoxoprin (Lovenox) |
| If a patient has been treated with warfarin and becomes pregnant it is okay to switch to enoxoprin (Lovenox). | TRUE |
| What are the toxicity's of protamine sulfate? | Hypotension due to histamine release, pulmonary hypertension and anaphylactic allergic reaction |
| Lepirudin (Refludan) is made by recombinant amplification, what is original source genetics for lepirudin? | Leeches produce hirudin |
| What is the target of recombinant hirudin? | Lepirudin is a direct thrombin inhibitor (specifically inactivates IIa without ATIII) |
| Is it okay to give lepirudin orally? | No, it is an IV formulation like heparin |
| What is the MOA of ancrod (Viprinex)? | Ancrod (Viprinex) is a primary fibrinolytic. It is able to degrade fibrinogen into soluble fibrin fragments that cannot participate in clot formation |
| Name two clinical circumstances where ancrod (Viprinex) is used | HIT and stroke |
| What is a significant side effect of ancrod (Viprinex)? | intracranial bleeding |
| What is warfarin a structural analog of ? | Vitamin K |
| What factors does warfarin affect the synthesis of? | II, VII, IX and X (2,7,9, and 10) |
| Can warfarin achieve activity in stored blood? | No, since warfarin affects the synthesis of clotting factors 2, 7, 9, and 10 it can act only in vivo. |
| What is there a time lag in the effectiveness of warfarin? | The existing factors have to be depleted |
| What test is used to measure warfarin? | The PT or protime test |
| How is protime measured? | In seconds |
| What calculated value is derived from the protime? | INR, international normalizing ratio is a calculated value based on the PT in seconds |
| What is a target INR of patients on warfarin | An INR between 2 and 3 |
| If warfarin is taken and the patients is also taking aspirin what side effect can occur? | Bleeding |
| Why do we care about other drugs that affect liver function (such as cimetidine [Tagamet])? | Because clotting factors are produced in the liver, if a vitamin K antagonist such as warfarin is given, it will decrease the production of clotting factors significantly (could throw patient into bleeding instead of just prevently clotting) |
| What other activity affects liver function? | Chronic alcoholics will have a lower rate of clotting factor synthesis |
| Why are oral contraceptives a concern for some patients? | They cause clots to form in some patients |
| What is the concern with barbiturates and warfarin? | Barbiturates decrease the anticoagulant effect of warfarin |
| Is warfarin safe to use in pregnancy? | No it is embryotoxic |
| What two diseases increase the anticoagulant effect of warfarin? | Hyperthyroidism and hepatic disease |
| What it the main result of warfarin overdose and how is it treated? | hemorrhage, treat with a vitamin K antidote |
| Is warfarin effective against existing thromboembolism? | No, it is a preventative medication |
| What is the primary clotting problem warfarin is given to patients to prevent? | DVT |
| Is warfarin given just as needed or is it a long term medication? | Is is used long term (chronically) |
| What is the MOA of cilostazol (Pletal) | a phosphodiesterase inhibitor |
| Can cilostazol be taken orally? | yes |
| What are the effects of taking cilostazol (Pletal) | promotes vasodilation and inhibits platelet aggregation |
| A patient complains of muscle cramps and fatigue when walking, what medication can treat them? | cilostazol (Pletal) |
| What patient group is contraindicated for taking cilostazol (Pletal) | CHF |
| In addition to lepirudan (Refludan) what other drug is a direct inhibitor of thrombin? | bivalirudin (Angiomax) and argatroban (Novastan) |
| Bivalirudin (Angiomax) has two mechanisms for anticoagulation, what are they? | directly inhibits IIa and also in inhibit platelet activation (prevents them from releasing their granules) |
| How much bivalirudin is cleared renally? | 20% |
| How much bivalirudin is cleared by metabolic pathways? | 80% |
| What treatment is bivalirudin approved for? | Percutaneous coronary angioplasty |
| What is the MOA of argatroban (Novastan) | direct inhibitor of thrombin |
| What two drugs can be used for patients with HIT? | Argatroban (Novastan) and lepirudin (Refludan) |
| Where is agratroban cleared from? | the liver |
| Can argatroban (Novastan) be given to patients orally? | No, warfarin is the only oral anticoagulant |
| What is the experimental (now withdrawn) pro-drug that can also be given orally? | ximelagatran (Exanta) |
| melagatran acts on what to achieve anticoagulation? | it is a direct inhibitor of IIa (thrombin) |
| Why was ximelagatran (Exanta) an attractive alternative to warfarin? | unlike warfarin, ximelagatran (Exanta) has a predictable bioavailability and kinetics, also is has a rapid onset and offset, no p450 interactions to worry about |
| The extended length of time it takes for ximelagatran (Exanta) to work is why it was not approved for use | FALSE, it acts as a direct thrombin inhibitor, therefor a rapid onset and offset of action |
| As warfarin acts on synthesis of clotting enzymes, so does ximelagatran (Exanta) that is why liver function is important to consider | FALSE, only warfarin acts as an inhibitor of factor production, ximelagatran (Exanta) acts directly on IIa |