med chem test 3 antiplatelet

  1. what 6 things play a role in the "equilibrum" that normally prevents us from clotting up
    • cAMP
    • ADP
    • ATP
    • serotonin
    • prostaglandins
    • calcium
  2. what is the integrin receptor for antiplatelets
    glycoprotein IIb/IIIa
  3. inhibition by reversibly binding of P2Y12
    metabolized by CYP3A4 to an active metabolite
    bleeding risk - intrcranial hemorrhage
    alternate to thienopyridines
    platelet function recovers twice as fast
    brilinta (ticagrelor)
  4. glycoasaminoglycan
    ind - thrombosis/embolism, DIC, DVT, prophylactic clot formatin
    binds to antithrombin III which then inhibits factor Xa
    unfractionated heparin
  5. 2 most common clinical side effects of unfractionated heparin
    heparin induced thrombocytopenia
  6. a 50% drop in platelet count or less than 100,000 platelets per mL
  7. time to onset of heparin induced cytopenia is a function of exposre history - describe the 2
    • previous exposure - platelet count can dive in hours
    • first exposure - platelet count drops in 5-100 days
  8. is the risk of thrombocytopenia greater with unfractionated heparin or low-molecular weight heparin
  9. LMW heparin
    prophylaxis of cancer-associated venous thromboembolism
    dalteparin sodium - fragmin
  10. LMW heparin
    less thrombin activity with potent factor Xa inhibition
    enoxaparin sodium - lovenox
  11. Not a LMWH - synthetic
    binds to AT III then inhibits selectively only factor Xa
    2.5mg/day hip or knee replacement
    fondaparinux sodium - arixtra
  12. 4 advantages of LMWH over unfractionated heparins
    • can be self administered by the patient in an outpatient setting at home or by a home health care nurse
    • improved control of bioavailability
    • more selective for factor Xa
    • less probability of thrombocytpenia
  13. how do you reverse the anticoagulatory effect of heparin
    protamine sulfate
  14. poly-cation amine rich in arginine groups isolated from fish
    derived from SAM
    protamine sulfate
  15. reverses anticoagulatory effect of heparin without some of the side effects
    PEG-modified protamine
  16. irreversible thrombin inhibitor
    recombinant hirudin protein
    gender difference issue with drug exposure
    overdosage - whole blood replacement or thrombi
    lepirudin - refludan
  17. reversible thrombin inhibitor
    used for acute coronary syndrome, unstable angina undergoing PCTA
    bivalirudin - angiomax
  18. human derived thrombin used topically in surgery
  19. irreversible thrombin inhibitor
    used for DVT prophylaxis in elective hip replacement therapy
    IV - caution in patients receiving epidural or spinal anesthisia - hematomas possible
    desirudin - iprivask
  20. reversible thrombin inhibitor
    free and clot associated inhibitor
    IV anticoagulant for HIT
    argatroban - acova
  21. reversible thrombin inhibitor
    oral - in patients with non-valvular atrial fibrillation
    dispense and store in the original bottle only
    6- day shelf life once opened - moisture
    no known antidote
    dabigatran etexilate - pradaxa
  22. treats chronic idiopathic thrombocytopenia
    oral - acts at the bone marrow level
    may cause hepatotoxicity
    eltrombopag - promacta
  23. vitamin K reductase inhibitor
    prophylaxis for venous thrombosis, PE, Afib
    dosage must be individualized
    monitor INR
    do not switch brands
    protein displacement is a major cause of drug interactions 
    warfarin sodium - coumadin
  24. 5 times more potent form of warfarin
  25. which enatiomer of warfarin is metabolized by CYP3A4
    what is its T 1/2
    • R
    • 37-89 hours
  26. which enantiomer of warfarin is metabolized by CYP2C9
    what is its half life
    • S
    • 36-42 hours
  27. a single nucleotide polymorphism of what gene has been associated with lower dose requirements for warfarin
    • VKORC1
    • 30% variance alone
    • 40% variance with CYP2C9 genes
    • 55% variance with CYP2C9 genes, age,height,body weight, interactind drugs
  28. this causes an interaction with warfarin
    INR's can increae by up to 50
    flavinoids inhibit CYP2C9
    cranberry juice
  29. this interacts with warfarin by inducing CYP2C9
    american ginseng
  30. vitamin K reductase inhibitor reserved for patients that can not tolerate coumarin type drugs
    anisindione - miradon
  31. factor Xa inhibitor
    pure S enantiomer
    substrate for CYP3A4/3A5
    possible spinal and epidural hematoma
    rivaroxaban - xarelto
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med chem test 3 antiplatelet