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PHRM 5001 > 12. Antithrombotics and Thrombolytics > Flashcards

12. Antithrombotics and Thrombolytics Flashcards

1
Q
  1. The body normally maintains an equilibrium between which 2 mechanisms in relation to hemostasis?
  2. Why is the blood clotting mechanism essential? (2)
  3. Hemostasis involves which 3 important factors?
A
  1. Clot formation (thrombosis) and Clot breakdown (fibrinolysis)
  2. Prevents blood loss and Repairs damaged vessels
  3. platelet membrane phospholipids, calcium , and activation of protein coagulation factors
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2
Q
  1. Complex biochemical reactions leading to clotting are initiated via which 2 cascade pathways?
  2. Extrinsic pathway is the ____ factor pathway. Therefore, factors are located where?
  3. What does this pathway initiate?
A
  1. Extrinsic and Intrinsic
  2. tissue –> located outside the plasma
  3. coagulation during hemostasis
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3
Q
  1. The Intrinsic pathway of clotting involves factors that are located where?
  2. This pathway is called the ______ ________ pathway.
  3. How is this pathway activated?
A
  1. present within the plasma
  2. contact activation pathway
  3. by trauma or infection
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4
Q
  1. What happens to the Intrinsic and Extrinsic pathways prior to forming a blood clot?
  2. What 2 factors act as a catalyst for prothrombin –> thrombin?
  3. What does thrombin catalyze? What does this end up activating?
  4. What is the end product of this whole cascade pathway?
A
  1. they will merge into a final common pathway
  2. activated factor X (Xa) + calcium
  3. fibrinogen’s conversion to fibrin activating fibrin stabilizing factor
  4. stable fibrin clot
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5
Q
  1. With maintaining hemostasis, there is eventual activation of the fibrinolytic system, how?
  2. From the previous question, plasminogen –> plasmin, what does this lead to?
  3. What are antithrombotic agents?
  4. How are the different class of antithrombotic agents classified?
A
  1. by tissue plasminogen activator (t-PAs)
  2. Dissolves fibrin and fibrinogen to dissolve clot
  3. agents that prevent or break up blood clots
  4. according to MOA
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6
Q
  1. What are the 3 classes of antithrombotic agents?
  2. What 2 things do anticoagulants prevent?
  3. What do antiplatelets do?
  4. What do thrombolytics do?
  5. Out of the above medications, which is the only one capable of breaking up a clot already formed?
A
  1. Anticoagulants, Antiplatelets, and Thrombolytics
  2. prevent the formation of fibrin clots and further clot formation in pre-existing thrombi
  3. inhibit platelet action at the onset of clotting
  4. break up thrombi through fibrin degradation
  5. thrombolytics! - others are for prophylaxis
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7
Q
  1. What type of drug is Heparin?
  2. This native substance is found where? What can this drug be extracted from? (2)
  3. What is the name of natural heparin? What does this mean? What does this lead to?
A
  1. anticoagulant
  2. in mast cells, can be extracted from bovine lung or porcine intestines
  3. unfractionated heparin (UFH) meaning it varies in length and molecular size leading to less predictable treatment
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8
Q
  1. What are the 4 traditional indications to using Heparin?
  2. What are the 3 novel indications for using this drug?
  3. What are 3 contraindications?
  4. What are 2 adverse effects?
A
  1. Prevention and treatment of VTE (DVT), PE & peripheral arterial embolism, Treatment of Afib with embolization (blood can become stagnant), Treatment of DIC, and Prevention of clot formation in invasive lines
  2. ARDS, inhalational injuries, and allergic responses
  3. Pre-existing bleeding disorders, Recent surgery, Active bleeding sites
  4. osteoporosis and heparin induced thrombocytopenia (HIT)
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9
Q
  1. What drug is known as the heparin antidote?
  2. MOA? (2)
  3. Where in the hospital is this drug often used? why?
A
  1. Protamine (reversal agent)
  2. Combines with free heparin forming inactive salt and Also dissociates heparin-antithrombin III complexes
  3. OR’s to maintain hemostasis and decrease bleeding during surgery
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10
Q
  1. What is the dose when using Protamine? What is the maximum amount that can be given?
  2. A slow IV infusion over 1-3 minutes is recommended to prevent what 3 effects?
  3. This drug poses a risk of allergic anaphylactic reaction in which patients? (3)
A
  1. 1 mg for every 100 U of heparin, up to 50 mg
  2. hypotension, bradycardia, and dyspnea
  3. Patients receiving insulin that contains protamine, Vasectomy patients, and Patients with fish sensitivity*
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11
Q
  1. What is the other drug name for Enoxaparin? For Dalteparin?
  2. What type of drug class are these?
  3. These drugs are considered ____ _______ _______ heparin. These drugs consist of what type of molecular chains?
  4. When are these drugs typically prescribed?
A
  1. Lovenox and Fragmin
  2. Anticoagulant agents
  3. low molecular weight heparin (LMWH) consisting of polysaccharide chains (uniform in length/size)
  4. mostly out-patient therapy (becoming the standard of care)
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12
Q
  1. What are 4 additional advantages of LMWH such as Enoxaparin and Dalteparin?
  2. What are the 7 indications? (same as heparin)
  3. What are the 2 contraindications?
A
  1. OD dosing, ↑ half-life and bioavailability, SC administration, ↓ risk of osteoporosis and HIT
  2. Prevention and treatment of VTE (DVT), PE & peripheral arterial embolism, Treatment of Afib with embolization, Treatment of DIC, Prevention of clot formation in invasive lines, ARDS, Inhalational injuries, and Allergic responses
  3. Pre-existing bleeding disorders, and End-stage renal disease
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13
Q
  1. What is the other drug name for Fondaparinux?
  2. What type of drug is this?
  3. This drug is a synthetic derivative of?
  4. What does this drug inhibit? And causes indirect suppression via?
A
  1. Arixtra
  2. anticoagulant
  3. heparin
  4. factor Xa inhibitor, and causes indirect suppression via ATIII
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14
Q
  1. Regarding Fondaparinux, a daily SC injection is used to treat? (2)
  2. Fondaparinux has a better safety profile then which 2 types of heparin?
  3. What are the 3 adverse reactions of this drug?
A
  1. Deep vein thrombosis (DVT) and pulmonary embolism
  2. UFH and LMWH
  3. bleeding, low risk of osteoporosis and HIT
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15
Q
  1. What is the other drug name for Rivaroxaban?
  2. What type of drug is this?
  3. Is a direct inhibitor of? Interferes with?
A
  1. Xarelto
  2. anticoagulant
  3. factor Xa and interferes with final common pathway
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16
Q
  1. How is this drug taken? why?
  2. Rivaroxaban is partially cleared by the ______.
  3. This drug was approved for prevention of?
A
  1. by mouth - orally active
  2. kidneys
  3. VTE following hip/knee replacement surgery
17
Q
  1. Direct thrombin inhibitors (anticoagulant drugs) will inhibit?
  2. less likely to cause?
  3. What are 2 indications for using this class of drugs?
  4. This class of anticoagulants are called ____ group of drugs. Polypeptide found where? Example?
A
  1. prothrombin enzyme (factor IIa)
  2. bleeding complications
  3. HIT and acute coronary syndrome
  4. Hirudin –> found in salivary glands of leeches
    ex. / dabigatran (pradaxa) used in ortho patients
18
Q
  1. What is the other drug name for Warfarin?
  2. What type of drug is this?
  3. MOA?
  4. suppresses which 4 key coagulation factors?
A
  1. Coumadin
  2. Anticoagulant
  3. synthetic vitamin K antagonist –> inhibits enzyme that activates vit K
  4. VII, IX, X, and prothrombin?
19
Q
  1. Where is Warfarin active? Where is it rapidly absorbed in the body?
  2. This drug has a delayed? how long? how long till therapeutic effect is reached?
  3. What are 2 indications?
A
  1. orally active, rapidly absorbed by the gut
  2. onset of action (1-3 mins) –> 1 week for full therapeutic effect
  3. Prevention and treatment of DVT, and Superwarfarins used as rat poisons (make the rat bleed out)
20
Q
  1. What are the 3 contraindications for using Warfarin? (same as heparin)
  2. What are the 3 precautions?
  3. What drugs increase the effects of warfarin? (6)
A
  1. Pre-existing bleeding disorders, Recent surgery, and Active bleeding
  2. Bleeding, Unpredictable pharmacodynamics, and Significant drug and food interactions
  3. Antibiotics, NSAIDs, Loop diuretics, GERD agents, Statins, and Antifungal agents
21
Q
  1. What drugs decrease the effects of warfarin? (6)

2. What foods decrease the effects of warfarin? (7)

A
  1. Oral contraceptives, Rifampin, Barbiturates, Spironolactone, Thiazide diuretics, and vitamin K
  2. Liver, Broccoli, Brussel sprouts, Leafy green veggies, Cranberry and grapefruit juice, Mango, and Soy products
22
Q
  1. Platelet aggregation is important for?
  2. Normally, which cell surface is anticoagulated?
  3. What happens when the above cell surface is disrupted? (3)
A
  1. controlling ruptured vessels
  2. endothelial surface
  3. procoagulant subendothelium exposed, chemotactic factors released–> promoting platelet aggregation
23
Q
  1. What are the 4 categories of antiplatelet drugs?
  2. What is the other drug name for Acetylsalicylic acid?
  3. What type of drug is this?
A
  1. COX inhibitors, ADP receptor antagonists, Prostaglandin analogues, and Glycoprotein IIb/IIa inhibitors
  2. Aspirin
  3. antiplatelet drug
24
Q
  1. What pathway does Aspirin act on? What does this inhibit?
  2. What are the 3 indications to using this drug?
  3. What is the other drug name for Clopidogrel?
A
  1. arachidonic acid pathway –> inhibits COX-1 enzyme
  2. Thromboprophylaxis, Low dose therapy (81 mg) daily for cardiac pts, and Useful in areas with high shear rates (vessel stenosis and atherosclerotic plaques)
  3. Plavix
25
Q
  1. What type of drug is Clopidogrel?
  2. What type of inhibitor is this drug?
  3. What does this drug decrease?
  4. When is this drug indicated?
  5. Useful for patients who?
A
  1. antiplatelet drug
  2. ADP receptor inhibitor
  3. platelet aggregation
  4. for CVA (stroke)
  5. can’t tolerate ASA
26
Q
  1. What do thrombolytic drugs induce? Which 3 locations in the body especially?
  2. What do this class of drugs help to convert? Therefore these drugs are also called?
  3. MOA?
  4. These drugs have an effect in reducing?
A
  1. fibrinolysis of life threatening clots - especially pulmonary, coronary and cerebral
  2. Plasminogen –> plasmin and also called plasminogen activators
  3. degrade fibrin without releasing thromboemboli
  4. infarct size
27
Q
  1. What is sensitive about thrombolytic agents? Typically given within?
  2. When are thrombolytics preferred over PCI? (2)
  3. Thrombolytics decrease the incidence/severity of? (2)
A
  1. administration is time sensitive –> given within 12-24 hours of symptoms
  2. if STEMI patient presents to hospital within 3 hours of symptom onset and door to primary PCI time > 90 mins
  3. CVA’s and MI’s
28
Q

Thrombolytic agents have 9 contraindications, can you list a few?

A
  • History/evidence of ICH (intracranial hemorrhage)
  • SAH (subarachnoid hemorrhage)
  • Known AV malformation: arteries and veins do not connect normally, increasing pressure and chances of bleeding
  • SBP > 185 mmHg or DBP > 110 mmHg
  • Seizure with postictal neurological impairment
  • Platelet < 100,000/mm3
  • INR > 1.7
  • Active internal bleeding/trauma
  • Head trauma/stroke within 3 months
29
Q
  1. What is the other drug name for Streptokinase?
  2. What type of drug is this?
  3. This drug was derived from?
A
  1. Streptase
  2. thrombolytic agent
  3. Streptococcal virulence factor
30
Q
  1. What are the 4 precautions to using Streptokinase?
  2. What are the 2 adverse effects?
  3. This is the preferred thrombolytic for patients how old? why?
A
  1. ↑ risk of bleeding with antithrombotic therapy, Streptococcal infections, Allergic reactions, and Lacks fibrin specificity
  2. bleeding during surgery and cerebral hemorrhage
  3. > 75 years old –> increased risk of hemorrhagic stroke with other agents
31
Q
  1. What is the other drug name for Urokinase?
  2. What type of drug is this?
  3. This drug is an enzyme found in?
  4. This drug is bioengineered from?
  5. Causes direct conversion of?
  6. Adverse side effects and precautions are similar to?
A
  1. Abbokinase
  2. thrombolytic drugs
  3. human urine
  4. kidney cells cultures
  5. Plasminogen to plasmin
  6. Streptokinase
32
Q
  1. What is the other drug name for Alteplase? (2)
  2. What type of drug is this?
  3. MOA? (3)
A
  1. activase, rt-PA
  2. thrombolytic agent
  3. endothelial cells of vessel walls release rt-PA, splits plasminogen to release active plasmin, then dissolves fibrin mesh in clots
33
Q
  1. Alteplase (rt-PA) is only active for how long? Therefore, causes less?
  2. What does this drug degrade?
  3. Indicated for the acute treatment of? (2)
A
  1. 10 mins therefore, less bleeding than other thrombolytics
  2. circulating fibrinogen (can increase risk of hemorrhage)
  3. massive PE and acute ischemic stroke
34
Q
  1. What is the other drug name for Tenecteplase? (2)
  2. Recombinant version of?
  3. MOA?
A
  1. TNkase, TNK-tPA
  2. hamster cells
  3. tissue plasminogen activator –> splits plasminogen
35
Q
  1. Tenecteplase is commonly used to treat?
  2. This drug has high fibrin specificity causing?
  3. There is a moderate risk of what when taking this drug?
A
  1. STEMI
  2. low risk of systemic bleeding
  3. intracranial hemorrhage

PHRM 5001 (12 decks)

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