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21 Cards in this Set
- Front
- Back
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1. What are the platelet membrane proteins that bind to collagen and vWF causing adherence to the subendothelium?
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a. GPIa/IIa
b. GPIb |
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2. What are the steps to platelet aggregation?
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1. Collagen and vWF is exposed d/t tissue damage
2. Platelet receptors GPIa/IIa and GPIb bind to collagen and vWF 3. Thrombin activates Protease-activated receptors 1 and 4 4. Thrombin also activates P2Y1 and P2Y12 purinergic receptors for ADP (as in not ATP) 5. When these receptors are activated, they activate fibrinogen-binding protein GPIIb/IIIa and COX1 to promote platelet aggregation and secretion 6. Fibrinogen binding = cross linking of adjacent platelets 7. XA2 is major product of COX-1 and promotes aggregation 8. PGI2 is synthsized by COX-1 in endothelial cells and inhibit platelet activation |
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3. What is the MOA of aspirin and its antiplatelet activity?
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a. It irreversibly inhibits platelet cyclooxygenase 1 and 2
b. It acetylates serine residues near active site of the enzyme c. Blocks thromboxane formation in platelet |
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4. What are the two major adverse effects of aspirin?
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a. GI upset
b. GI bleeding |
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5. What are the therapeutic uses of aspirin?
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a. MI prophylaxis
b. Used in acute phase of ischemic stroke c. used in stroke prophylaxis d. Used in unstable angina e. Used in preeclampsia prophylaxis |
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6. What is the MOA for dipyridamole
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a. A phosphodiesterase inhibitor and/or blockade of uptake of adenosine
b. increases cAMP c. inhibits platelet aggregation |
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7. What are the three adverse effects of diphyridamole?
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a. headache
b. GI upset c. Dizziness |
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8. What is the therapeutic use of dipyridamole?
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a. prevention of thromboemboli (with warfarin) in pts with prosthetic heart valves
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9. What are the two anti-platelet drugs that involve P2Y1/P2Y12 receptors?
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a. Ticlopidine
b. Clopidogrel |
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10. What is the MOA for Ticlopidine and Clopidogrel?
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a. Blocks ADP binding to P2Y1/P2Y12 receptors (normally ADP binds to P2Y coupled to Gi and inhibits adenyl cycles...this decreases levels of cAMP)
b. Therefore, there is no activation that normally leads to an increase in COX2 activation of thombolytics |
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11. What the intended effects of ticlopidine/clopidogrel?
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a. prolonged bleeding time?
b. inhibit platelet aggregation, c. Delay clot traction |
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12. What CYP enzyme is clopidogrel metabolized by? How might this a problem in some people?
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a. CYP2C19
b. 3-20% of population have polymorph, making them poor metabolizers and decrease active [Rx] (remember that clopidogrel must be activated by CYP2C19 before it is functional) |
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13. What are the major adverse sfx of ticlopidine?
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a. Serious, sometimes fatal dyscrasias (cancer of plasma cells)
b. neutropenia |
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14. What is the important drug interaction to remember with clopidogrel and CYP2C19?
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a. If coadministered with omeprazole, both compete for CYP2C19 and clopidogrel will not be activated, and therefore no therapeutic effect
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15. What are the 7 therapeutic uses for Ticlopidine?
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a. Secondary prevention of cerebrovascular disease
b. myocardial infarction c. unstable angina d. coronary artery stenting e. peripheral vascular disease f. patients with transient ischemic attacks g. completed strokes |
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16. What are the two therapeutic uses of clopidogrel?
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a. Myocardial infarction prophylaxis
b. Stroke prophylaxis |
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17. What is the MOA of abciximab?
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a. It blocks glycoprotein IIB/IIIa receptor - the majore surface receptor involved in platelet aggregation
b. Therefore inhibits platelet aggregation |
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18. How is abciximab adminstered?
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a. IV bolus injection followed by continuous infusion for up to 72 hrs.
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19. What are the adverse effects of abciximab?
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a. Bleeding
b. Thrombocytopenia |
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20. What are the therapeutic uses of Abciximab?
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a. Adjunct percutaneous coronary intervention for prevention of cardiac ischemic complications
b. Pts with unstabel angina not responding to conventional medical therapy |
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21. Abciximab is intended for use with these two drugs:
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a. aspirin
b. heparin |
